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Kilibarda S, Jović MD, Milinčić DD, Vuković S, Trifković JĐ, Pešić MB, Kostić AŽ. Phytochemical Profile and Biological Activities of Rtanj's Hypericum perforatum Infusion Tea and Methanolic Extracts: Insights from LC-MS/MS and HPTLC-Bioautography. PLANTS (BASEL, SWITZERLAND) 2025; 14:1377. [PMID: 40364406 PMCID: PMC12073223 DOI: 10.3390/plants14091377] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Received: 03/26/2025] [Revised: 04/29/2025] [Accepted: 04/29/2025] [Indexed: 05/15/2025]
Abstract
This study aimed to examine wild-growing Hypericum perforatum L. tea (Hyperici herba) collected from Rtanj Mountain (Serbia). This research includes the following approaches: phytochemical and antioxidant characterization of H. perforatum infusion tea to determine its realistic composition (What do we consume when drinking the tea?), as well as a detailed examination of methanol(ic) extracts as the optimal extraction system. Due to the broad spectrum of both polar and nonpolar metabolites, 80% methanolic and pure methanol extracts were prepared for ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC Q-ToF) characterization through untargeted metabolomics analysis. Given the high diversity of compounds identified, the 80% methanolic extract was selected for further antioxidant examination and bioautographic characterization, including an antimicrobial activity assessment. UHPLC Q-ToF analysis identified 35 phenolics in the methanolic extract, compared to 25 metabolites in the infusion tea. The main differences were observed in flavonol/flavan-3-ol aglycones, xantones, and coumestans, which are more nonpolar compounds found only in the methanol(ic) system. Notably, specific H. perforatum metabolites were entirely absent in the infusion tea. Specifically, pseudohypericin, pseudoprotohypricin, and adhyperfirin were detected in the pure methanol extract, whereas hyperfirin was present in both methanol(ic) extracts. Additionally, eight furano-polycyclic polyprenylated acilphloroglucinols (FPPAPs) were identified in the methanol(ic) extracts as possible products of the thermal degradation and/or oxidation of hypericin/hyperforin. Both the infusion tea and methanolic extracts exhibited excellent antioxidant properties, with variations depending on the applied assay. High-performance thin-layer chromatography (HPTLC) analysis also confirmed the presence of a wide spectrum of phytochemical classes. Bioautography confirmed a promising activity of methanolic extracts against both Staphylococcus aureus and Klebsiella pneumoniae.
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Affiliation(s)
- Sofija Kilibarda
- Department for Crop and Vegetable Production, Faculty of Agriculture, University of Belgrade, Nemanjina 6, 11080 Belgrade, Serbia; (S.K.); (S.V.)
| | - Marko D. Jović
- Innovation Center, Faculty of Chemistry, University of Belgrade, Studentski Trg 12-16, 11000 Belgrade, Serbia;
| | - Danijel D. Milinčić
- Department for Chemistry and Biochemistry, Faculty of Agriculture, University of Belgrade, Nemanjina 6, 11080 Belgrade, Serbia; (D.D.M.); (M.B.P.)
| | - Sandra Vuković
- Department for Crop and Vegetable Production, Faculty of Agriculture, University of Belgrade, Nemanjina 6, 11080 Belgrade, Serbia; (S.K.); (S.V.)
| | - Jelena Đ. Trifković
- Faculty of Chemistry, University of Belgrade, Studentski Trg 12-16, 11158 Belgrade, Serbia;
| | - Mirjana B. Pešić
- Department for Chemistry and Biochemistry, Faculty of Agriculture, University of Belgrade, Nemanjina 6, 11080 Belgrade, Serbia; (D.D.M.); (M.B.P.)
| | - Aleksandar Ž. Kostić
- Department for Chemistry and Biochemistry, Faculty of Agriculture, University of Belgrade, Nemanjina 6, 11080 Belgrade, Serbia; (D.D.M.); (M.B.P.)
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Sotirova Y, Ivanova N, Ermenlieva N, Vilhelmova-Ilieva N, Simeonova L, Metodiev M, Gugleva V, Andonova V. Antimicrobial and Antiherpetic Properties of Nanoencapsulated Hypericum perforatum Extract. Pharmaceuticals (Basel) 2025; 18:366. [PMID: 40143142 PMCID: PMC11944447 DOI: 10.3390/ph18030366] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/06/2025] [Revised: 02/27/2025] [Accepted: 03/01/2025] [Indexed: 03/28/2025] Open
Abstract
Background/Objectives: This study aims to gain insights into the antimicrobial and antiherpetic activity of hyperforin-rich Hypericum perforatum L. (HP) extract using nanostructured lipid carriers (NLCs) as delivery platforms. Methods: Two established NLC specimens, comprising glyceryl behenate and almond oil or borage oil, and their extract-loaded counterparts (HP-NLCs) were utilized. Their minimal bactericidal/fungicidal concentrations (MBC; MFC) were investigated against Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 10145, Klebsiella pneumoniae ATCC 10031, and Candida albicans ATCC 10231. The anti-herpesvirus (HSV-1) potential was evaluated concerning antiviral and virucidal activity and impact on viral adsorption. Results: The borage oil-based extract-loaded nanodispersion (HP-NLC2) exhibited pronounced microbicidal activity against S. aureus (MBC 6.3 mg/mL), K. pneumoniae (MBC 97.7 µg/mL), and C. albicans (MFC < 48.8 µg/mL), unlike the almond oil-containing sample (HP-NLC1), which showed only weak inhibition of the fungal growth. HP-NLC2 was found to be less cytotoxic and to suppress HSV-1 replication slightly more than HP-NLC1, but generally, the effects were weak. Neither the empty lipid nanoparticles nor the HP extract-loaded carriers expressed activity against E. coli, P. aeruginosa, the HSV-1 extracellular virions, or viral adhesion. Conclusions: It could be concluded that both HP-NLC samples revealed only minor antiherpetic potential of the hyperforin-rich extract, but HP-NLC2 demonstrated significant antibacterial and antimycotic activity. Therefore, the latter was featured as a more convenient HP-carrier system for nano-designed dermal pharmaceutical formulations. Such a thorough investigation of hyperforin-determined anti-HSV-1 effects and antibacterial and antimycotic properties, being the first of its kind, contributes to the fundamental knowledge of HP and reveals new perspectives for the utilization, limitations, and therapeutic designation of its non-polar components.
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Affiliation(s)
- Yoana Sotirova
- Department of Pharmaceutical Technologies, Faculty of Pharmacy, Medical University of Varna, 9000 Varna, Bulgaria; (Y.S.); (V.G.); (V.A.)
| | - Nadezhda Ivanova
- Department of Pharmaceutical Technologies, Faculty of Pharmacy, Medical University of Varna, 9000 Varna, Bulgaria; (Y.S.); (V.G.); (V.A.)
| | - Neli Ermenlieva
- Department of Microbiology and Virology, Faculty of Medicine, Medical University of Varna, 9000 Varna, Bulgaria;
| | - Neli Vilhelmova-Ilieva
- Department of Virology, Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 26 G. Bonchev Str., 1113 Sofia, Bulgaria; (N.V.-I.); (L.S.); (M.M.)
| | - Lora Simeonova
- Department of Virology, Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 26 G. Bonchev Str., 1113 Sofia, Bulgaria; (N.V.-I.); (L.S.); (M.M.)
| | - Miroslav Metodiev
- Department of Virology, Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 26 G. Bonchev Str., 1113 Sofia, Bulgaria; (N.V.-I.); (L.S.); (M.M.)
| | - Viliana Gugleva
- Department of Pharmaceutical Technologies, Faculty of Pharmacy, Medical University of Varna, 9000 Varna, Bulgaria; (Y.S.); (V.G.); (V.A.)
| | - Velichka Andonova
- Department of Pharmaceutical Technologies, Faculty of Pharmacy, Medical University of Varna, 9000 Varna, Bulgaria; (Y.S.); (V.G.); (V.A.)
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Farasati Far B, Gouranmohit G, Naimi-Jamal MR, Neysani E, El-Nashar HAS, El-Shazly M, Khoshnevisan K. The potential role of Hypericum perforatum in wound healing: A literature review on the phytochemicals, pharmacological approaches, and mechanistic perspectives. Phytother Res 2024; 38:3271-3295. [PMID: 38600756 DOI: 10.1002/ptr.8204] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/03/2023] [Revised: 03/18/2024] [Accepted: 03/21/2024] [Indexed: 04/12/2024]
Abstract
St. John's Wort, commonly known as Hypericum perforatum L., is a flowering plant in the Clusiaceae family that traditionally been employed for treating anxiety, depression, wounds, burns, sunburn, irritation, and stomach ailments. This review provides a synopsis of H. perforatum L. phytoconstituents and their biological effects, highlighting its beneficial therapeutic properties for dermatological indications, as well as its antioxidant, antimicrobial, anti-inflammatory, and anti-angiogenic activity in various applications including wound healing and skin conditions such as eczema, sun burn and minor burns also spastic paralysis, stiff neck and mood disorders as anti-depressant and nerve pains such as neuralgia. The data were collected from several databases as Web of Science PubMed, ScienceDirect, Scopus and Google Scholar using the terms: "H. perforatum L.", "H. perforatum L. /phytochemistry," and "H. perforatum extracts/wound healing" collected from 1994 to 2023. The findings suggest H. perforatum L. acts through various mechanisms and plays a role in each phase of the wound healing process, including re-epithelialization, angiogenesis, wound contraction, and connective tissue regeneration. H. perforatum L. enhances collagen deposition, decreases inflammation, inhibits fibroblast migration, and promotes epithelialization by increasing the number of fibroblasts with polygonal shape and the number of collagen fibers within fibroblasts. H. Perforatum L. extracts modulate the immune response and reduce inflammation were found to accelerate the wound healing process via inhibition of inflammatory mediators' production like interleukin-6, tumor necrosis factor-α, cyclooxygenase-2 gene expression, and inducible nitric oxide synthase. Thus, H. perforatum L. represents a potential remedy for a wide range of dermatological problems, owing to its constituents with beneficial therapeutic properties. H. perforatum L. could be utilized in the development of novel wound healing therapies.
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Affiliation(s)
- Bahareh Farasati Far
- Research Laboratory of Green Organic Synthesis and Polymers, Department of Chemistry, Iran University of Science and Technology, Tehran, Iran
| | - Ghazaleh Gouranmohit
- Faculty of Pharmaceutical Chemistry, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran
| | - Mohammad Reza Naimi-Jamal
- Research Laboratory of Green Organic Synthesis and Polymers, Department of Chemistry, Iran University of Science and Technology, Tehran, Iran
| | - Erfan Neysani
- Pharmaceutical Sciences Research Center, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran
| | - Heba A S El-Nashar
- Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
| | - Mohamed El-Shazly
- Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
| | - Kamyar Khoshnevisan
- Medical Nanotechnology and Tissue Engineering Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran
- Department of Tissue Engineering and Applied Cell Sciences, School of Advanced Technologies in Medicine, Shahid Beheshti University of Medical Sciences, Tehran, Iran
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Peng Z, Lu J, Liu K, Xie L, Wang Y, Cai C, Yang D, Xi J, Yan C, Li X, Shi M. Hypericin as a promising natural bioactive naphthodianthrone: A review of its pharmacology, pharmacokinetics, toxicity, and safety. Phytother Res 2023; 37:5639-5656. [PMID: 37690821 DOI: 10.1002/ptr.8011] [Citation(s) in RCA: 6] [Impact Index Per Article: 3.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/24/2023] [Revised: 08/28/2023] [Accepted: 08/29/2023] [Indexed: 09/12/2023]
Abstract
Hypericin can be derived from St. John's wort, which is widely spread around the world. As a natural product, it has been put into clinical practice such as wound healing and depression for a long time. In this article, we review the pharmacology, pharmacokinetics, and safety of hypericin, aiming to introduce the research advances and provide a full evaluation of it. Turns out hypericin, as a natural photosensitizer, exhibits an excellent capacity for anticancer, neuroprotection, and elimination of microorganisms, especially when activated by light, potent anticancer and antimicrobial effects are obtained after photodynamic therapy. The mechanisms of its therapeutic effects involve the induction of cell death, inhibition of cell cycle progression, inhibition of the reuptake of amines, and inhibition of virus replication. The pharmacokinetics properties indicate that hypericin has poor water solubility and bioavailability. The distribution and excretion are fast, and it is metabolized in bile. The toxicity of hypericin is rarely reported and the conventional use of it rarely causes adverse effects except for photosensitization. Therefore, we may conclude that hypericin can be used safely and effectively against a variety of diseases. We hope to provide researchers with detailed guidance and enlighten the development of it.
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Affiliation(s)
- Zhaolei Peng
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Jing Lu
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Kai Liu
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Long Xie
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Yulin Wang
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Chunyan Cai
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Dejun Yang
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Jingjing Xi
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Chunmei Yan
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Xiaofang Li
- State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China
| | - Mingyi Shi
- School of Intelligent Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China
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Different Types of Hypericum perforatum cvs. (Elixir, Helos, Topas) In Vitro Cultures: A Rich Source of Bioactive Metabolites and Biological Activities of Biomass Extracts. Molecules 2023; 28:molecules28052376. [PMID: 36903619 PMCID: PMC10005045 DOI: 10.3390/molecules28052376] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/26/2022] [Revised: 02/18/2023] [Accepted: 02/28/2023] [Indexed: 03/08/2023] Open
Abstract
Microshoot agitated and bioreactor cultures (PlantForm bioreactors) of three Hypericum perforatum cultivars (Elixir, Helos, Topas) were maintained in four variants of Murashige and Skoog medium (MS) supplemented with 6-benzylaminopurine (BAP) and 1-naphthaleneacetic acid (NAA) (in the range of 0.1-3.0 mg/L). In both types of in vitro cultures, the accumulation dynamics of phenolic acids, flavonoids, and catechins were investigated during 5- and 4-week growth cycles, respectively. The contents of metabolites in methanolic extracts from biomasses collected in 1-week intervals were estimated by HPLC. The highest total contents of phenolic acids, flavonoids, and catechins were 505, 2386, and 712 mg/100 g DW, respectively (agitated cultures of cv. Helos). The extracts from biomass grown under the best in vitro culture conditions were examined for antioxidant and antimicrobial activities. The extracts showed high or moderate antioxidant activity (DPPH, reducing power, and chelating activity assays), high activity against Gram-positive bacteria, and strong antifungal activity. Additionally, experiments with phenylalanine feeding (1 g/L) in agitated cultures were performed reaching the highest enhancement of the total contents of flavonoids, phenolic acids, and catechins on day 7 after the addition of the biogenetic precursor (2.33-, 1.73- and 1.33-fold, respectively). After feeding, the highest accumulation of polyphenols was detected in the agitated culture of cv. Elixir (4.48 g/100 g DW). The high contents of metabolites and the promising biological properties of the biomass extracts are interesting from a practical point of view.
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Yontar AK, Çevik S. Effects of Plant Extracts and Green-Synthesized Silver Nanoparticles on the Polyvinyl Alcohol (PVA) Nanocomposite Films. ARABIAN JOURNAL FOR SCIENCE AND ENGINEERING 2023. [DOI: 10.1007/s13369-023-07643-w] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 02/12/2023]
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Ilieva Y, Marinov T, Trayanov I, Kaleva M, Zaharieva MM, Yocheva L, Kokanova-Nedialkova Z, Najdenski H, Nedialkov P. Outstanding Antibacterial Activity of Hypericum rochelii-Comparison of the Antimicrobial Effects of Extracts and Fractions from Four Hypericum Species Growing in Bulgaria with a Focus on Prenylated Phloroglucinols. Life (Basel) 2023; 13:life13020274. [PMID: 36836632 PMCID: PMC9959064 DOI: 10.3390/life13020274] [Citation(s) in RCA: 7] [Impact Index Per Article: 3.5] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/08/2022] [Revised: 01/14/2023] [Accepted: 01/16/2023] [Indexed: 01/20/2023] Open
Abstract
Microbial infections are by no means a health problem from a past era due to the increasing antimicrobial resistance of infectious strains. Medicine is in constant need of new drugs and, recently, plant products have had a deserved renaissance and garnered scientific recognition. The aim of this work was to assess the antimicrobial activity of ten active ingredients from four Hypericum species growing in Bulgaria, as well as to obtain preliminary data on the phytochemical composition of the most promising samples. Extracts and fractions from H. rochelii Griseb. ex Schenk, H. hirsutum L., H. barbatum Jacq. and H. rumeliacum Boiss. obtained with conventional or supercritical CO2 extraction were tested on a panel of pathogenic microorganisms using broth microdilution, agar plates, dehydrogenase activity and biofilm assays. The panel of samples showed from weak to extraordinary antibacterial effects. Three of them (from H. rochelii and H. hirsutum) had minimum inhibitory concentrations as low as 0.625-78 mg/L and minimum bactericidal concentrations of 19.5-625 mg/L against Staphylococcus aureus and other Gram-positive bacteria. These values placed these samples among the best antibacterial extracts from the Hypericum genus. Some of the agents also demonstrated very high antibiofilm activity against methicillin-resistant S. aureus. Ultra-high-performance liquid chromatography-high-resolution mass spectrometry revealed the three most potent samples as rich sources of biologically active phloroglucinols. They were shown to be good drug or nutraceutical candidates, presumably without some of the side effects of conventional antibiotics.
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Affiliation(s)
- Yana Ilieva
- Department of Infectious Microbiology, The Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
| | - Teodor Marinov
- Pharmacognosy Department, Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria
| | - Iliyan Trayanov
- Department of Chemical Engineering, Faculty of Chemical and System Engineering, University of Chemical Technology and Metallurgy, 1756 Sofia, Bulgaria
- Institute of Chemical Engineering, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
| | - Mila Kaleva
- Department of Infectious Microbiology, The Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
| | - Maya Margaritova Zaharieva
- Department of Infectious Microbiology, The Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
| | - Lyubomira Yocheva
- Department of Biology, Medical Genetics and Microbiology, Faculty of Medicine, Sofia University “St. Kliment Ohridski”, 1407 Sofia, Bulgaria
| | | | - Hristo Najdenski
- Department of Infectious Microbiology, The Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
- Correspondence: or (H.N.); (P.N.)
| | - Paraskev Nedialkov
- Pharmacognosy Department, Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria
- Correspondence: or (H.N.); (P.N.)
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Synergistic Action of Cinnamomum verum Essential Oil with Sertraline. Antibiotics (Basel) 2022; 11:antibiotics11111617. [PMID: 36421261 PMCID: PMC9686778 DOI: 10.3390/antibiotics11111617] [Citation(s) in RCA: 10] [Impact Index Per Article: 3.3] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/29/2022] [Revised: 11/09/2022] [Accepted: 11/09/2022] [Indexed: 11/16/2022] Open
Abstract
Cinnamomum verum L. essential oil (CEO), commonly known as Ceylon cinnamon or cinnamon tree, is regarded as one of the most employed essential oils in the field of aromatherapy. It is usually applied externally as astringent, antipruritic, rubefacient, and anti-septic agent. Furthermore, both in vitro and in vivo research have demonstrated its numerous pharmacological effects, including the potentiality for treating neuralgia, myalgia, headache, and migraine. Several pieces of research also corroborated its significant antiviral and antimicrobial properties. Cinnamaldehyde, eugenol, caryophyllene, cinnamyl acetate, and cinnamic acid are the most representative compounds that are generally found in greater quantities in CEO and play a pivotal role in determining its pharmacological activities. Due to the global antibiotic resistance scenario and the dwindling amount of funding dedicated to developing new antibiotics, in recent years research has concentrated on exploring specific economic approaches against microbial infections. In this context, the purpose of this study was the investigation of the synergistic antibacterial activities of commercially available and chemically characterized CEO in combination with sertraline, a selective serotonin reuptake inhibitor (SSRI), whose repositioning as a non-antibiotic drug has been explored over the years with encouraging results. In vitro effects of the titled combination were assessed toward a wide panel of both Gram-positive and Gram-negative bacteria. The antimicrobial efficacy was investigated by using the checkerboard microdilution method. The interesting preliminary results obtained suggested a synergistic effect (fractional inhibitory index, FICI < 0.5) of sertraline in combination with CEO, leading to severe growth inhibition for all bacterial species under investigation.
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LIU S, YU B, DAI J, CHEN R. Targeting the biological activity and biosynthesis of hyperforin: a mini-review. Chin J Nat Med 2022; 20:721-728. [DOI: 10.1016/s1875-5364(22)60189-4] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/20/2022] [Indexed: 11/03/2022]
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Zimmerman T, Ibrahim SA. Quercetin Is a Novel Inhibitor of the Choline Kinase of Streptococcus pneumoniae. Antibiotics (Basel) 2022; 11:antibiotics11091272. [PMID: 36140052 PMCID: PMC9495829 DOI: 10.3390/antibiotics11091272] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/12/2022] [Revised: 09/09/2022] [Accepted: 09/14/2022] [Indexed: 12/05/2022] Open
Abstract
The effectiveness of current antimicrobial methods for addressing for food-borne Gram-positive pathogens has dropped with the emergence of resistant strains. Consequently, new methods for addressing Gram-positive strains have to be developed continuously. This includes establishing novel targets for antimicrobial discovery efforts. Eukaryotic choline kinases have been highly developed as drug targets for the treatment of cancer, rheumatoid arthritis, malaria and many other conditions and diseases. Recently, choline kinase (ChoK) has been proposed as a drug target for Gram-positive species generally. The aim of this work was to discover novel, natural sources of inhibitors for bacterial ChoK from tea extracts. We report the first natural bacterial ChoK inhibitor with antimicrobial activity against Streptococcus pneumoniae: quercetin.
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Bulgarian Medicinal Extracts as Natural Inhibitors with Antiviral and Antibacterial Activity. PLANTS 2022; 11:plants11131666. [PMID: 35807618 PMCID: PMC9268788 DOI: 10.3390/plants11131666] [Citation(s) in RCA: 6] [Impact Index Per Article: 2.0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Received: 05/30/2022] [Revised: 06/16/2022] [Accepted: 06/21/2022] [Indexed: 11/17/2022]
Abstract
Background: Bulgaria is a country with a wide range of medicinal plants, with uses in traditional medicine dating back for centuries. Methods: Disc diffusion assay was used to evaluate the antimicrobial activity of the plant extracts. A cytopathic effect inhibition test was used for the assessment of the antiviral activity of the extracts. The virucidal activity of the extracts, their influence on the stage of viral adsorption, and their protective effect on uninfected cells were reported using the end-point dilution method, and Δlgs was determined as compared to the untreated controls. Results: The results of the study reveal that the antibacterial potential of G. glabra and H. perforatum extracts in Gram-positive bacteria is more effective than in Gram-negative bacteria. When applied during the replication of HSV-1 and HCov-OC-43, only some of the extracts showed weak activity, with SI between 2 to 8.5. Almost all tested extracts inhibited the extracellular virions of the studied enveloped viruses (HSV-1 and HCov-OC-43) to a greater extent than of the non-enveloped viruses (PV-1 and HAdV-5). They inhibited the stage of viral adsorption (HSV-1) in the host cell (MDBK) to varying degrees and showed a protective effect on healthy cells (MDBK) before they were subjected to viral invasion (HSV-1). Conclusion: The antipathogenic potential of extracts of H. perforatum and G. glabra suggests their effectiveness as antimicrobial agents. All 13 extracts of the Bulgarian medicinal plants studied can be used to reduce viral yield in a wide range of viral infections.
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Delcanale P, Abbruzzetti S, Viappiani C. Photodynamic treatment of pathogens. LA RIVISTA DEL NUOVO CIMENTO 2022; 45:407-459. [PMCID: PMC8921710 DOI: 10.1007/s40766-022-00031-4] [Citation(s) in RCA: 7] [Impact Index Per Article: 2.3] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Subscribe] [Scholar Register] [Received: 10/10/2021] [Accepted: 01/10/2022] [Indexed: 06/01/2023]
Abstract
The current viral pandemic has highlighted the compelling need for effective and versatile treatments, that can be quickly tuned to tackle new threats, and are robust against mutations. Development of such treatments is made even more urgent in view of the decreasing effectiveness of current antibiotics, that makes microbial infections the next emerging global threat. Photodynamic effect is one such method. It relies on physical processes proceeding from excited states of particular organic molecules, called photosensitizers, generated upon absorption of visible or near infrared light. The excited states of these molecules, tailored to undergo efficient intersystem crossing, interact with molecular oxygen and generate short lived reactive oxygen species (ROS), mostly singlet oxygen. These species are highly cytotoxic through non-specific oxidation reactions and constitute the basis of the treatment. In spite of the apparent simplicity of the principle, the method still has to face important challenges. For instance, the short lifetime of ROS means that the photosensitizer must reach the target within a few tens nanometers, which requires proper molecular engineering at the nanoscale level. Photoactive nanostructures thus engineered should ideally comprise a functionality that turns the system into a theranostic means, for instance, through introduction of fluorophores suitable for nanoscopy. We discuss the principles of the method and the current molecular strategies that have been and still are being explored in antimicrobial and antiviral photodynamic treatment.
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Affiliation(s)
- Pietro Delcanale
- Dipartimento di Scienze Matematiche, Fisiche e Informatiche, Università degli Studi di Parma, Parco Area delle Scienze 7A, 43124 Parma, Italy
| | - Stefania Abbruzzetti
- Dipartimento di Scienze Matematiche, Fisiche e Informatiche, Università degli Studi di Parma, Parco Area delle Scienze 7A, 43124 Parma, Italy
| | - Cristiano Viappiani
- Dipartimento di Scienze Matematiche, Fisiche e Informatiche, Università degli Studi di Parma, Parco Area delle Scienze 7A, 43124 Parma, Italy
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Bittner Fialová S, Rendeková K, Mučaji P, Nagy M, Slobodníková L. Antibacterial Activity of Medicinal Plants and Their Constituents in the Context of Skin and Wound Infections, Considering European Legislation and Folk Medicine-A Review. Int J Mol Sci 2021; 22:ijms221910746. [PMID: 34639087 PMCID: PMC8509446 DOI: 10.3390/ijms221910746] [Citation(s) in RCA: 18] [Impact Index Per Article: 4.5] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/23/2021] [Revised: 09/26/2021] [Accepted: 10/01/2021] [Indexed: 12/24/2022] Open
Abstract
Bacterial infections of skin and wounds may seriously decrease the quality of life and even cause death in some patients. One of the largest concerns in their treatment is the growing antimicrobial resistance of bacterial infectious agents and the spread of resistant strains not only in the hospitals but also in the community. This trend encourages researchers to seek for new effective and safe therapeutical agents. The pharmaceutical industry, focusing mainly on libraries of synthetic compounds as a drug discovery source, is often failing in the battle with bacteria. In contrast, many of the natural compounds, and/or the whole and complex plants extracts, are effective in this field, inactivating the resistant bacterial strains or decreasing their virulence. Natural products act comprehensively; many of them have not only antibacterial, but also anti-inflammatory effects and may support tissue regeneration and wound healing. The European legislative is in the field of natural products medicinal use formed by European Medicines Agency (EMA), based on the scientific work of its Committee on Herbal Medicinal Products (HMPC). HMPC establishes EU monographs covering the therapeutic uses and safe conditions for herbal substances and preparations, mostly based on folk medicine, but including data from scientific research. In this review, the medicinal plants and their active constituents recommended by EMA for skin disorders are discussed in terms of their antibacterial effect. The source of information about these plant products in the review is represented by research articles listed in scientific databases (Science Direct, PubMed, Scopus, Web of Science, etc.) published in recent years.
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Affiliation(s)
- Silvia Bittner Fialová
- Department of Pharmacognosy and Botany, Faculty of Pharmacy, Comenius University in Bratislava, Odbojárov 10, 832 32 Bratislava, Slovakia; (K.R.); (P.M.); (M.N.)
- Correspondence: ; Tel.: +421-250-117-206
| | - Katarína Rendeková
- Department of Pharmacognosy and Botany, Faculty of Pharmacy, Comenius University in Bratislava, Odbojárov 10, 832 32 Bratislava, Slovakia; (K.R.); (P.M.); (M.N.)
| | - Pavel Mučaji
- Department of Pharmacognosy and Botany, Faculty of Pharmacy, Comenius University in Bratislava, Odbojárov 10, 832 32 Bratislava, Slovakia; (K.R.); (P.M.); (M.N.)
| | - Milan Nagy
- Department of Pharmacognosy and Botany, Faculty of Pharmacy, Comenius University in Bratislava, Odbojárov 10, 832 32 Bratislava, Slovakia; (K.R.); (P.M.); (M.N.)
| | - Lívia Slobodníková
- Institute of Microbiology, Faculty of Medicine and the University Hospital in Bratislava, Comenius University in Bratislava, Sasinkova 4, 811 08 Bratislava, Slovakia;
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14
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Yazarlu O, Iranshahi M, Kashani HRK, Reshadat S, Habtemariam S, Iranshahy M, Hasanpour M. Perspective on the application of medicinal plants and natural products in wound healing: A mechanistic review. Pharmacol Res 2021; 174:105841. [PMID: 34419563 DOI: 10.1016/j.phrs.2021.105841] [Citation(s) in RCA: 88] [Impact Index Per Article: 22.0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 06/08/2021] [Revised: 08/14/2021] [Accepted: 08/17/2021] [Indexed: 12/14/2022]
Abstract
Wound is defined as any injury to the body such as damage to the epidermis of the skin and disturbance to its normal anatomy and function. Since ancient times, the importance of wound healing has been recognized, and many efforts have been made to develop novel wound dressings made of the best material for rapid and effective wound healing. Medicinal plants play a great role in the wound healing process. In recent decades, many studies have focused on the development of novel wound dressings that incorporate medicinal plant extracts or their purified active compounds, which are potential alternatives to conventional wound dressings. Several studies have also investigated the mechanism of action of various herbal medicines in wound healing process. This paper attempts to highlight and review the mechanistic perspective of wound healing mediated by plant-based natural products. The findings showed that herbal medicines act through multiple mechanisms and are involved in various stages of wound healing. Some herbal medicines increase the expression of vascular endothelial growth factor (VEGF) and transforming growth factor-β (TGF-β) which play important role in stimulation of re-epithelialization, angiogenesis, formation of granulation tissue, and collagen fiber deposition. Some other wound dressing containing herbal medicines act as inhibitor of tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β) and inducible nitric oxide synthase (iNOS) protein expression thereby inducing antioxidant and anti-inflammatory properties in various phases of the wound healing process. Besides the growing public interest in traditional and alternative medicine, the use of herbal medicine and natural products for wound healing has many advantages over conventional medicines, including greater effectiveness due to diverse mechanisms of action, antibacterial activity, and safety in long-term wound dressing usage.
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Affiliation(s)
- Omid Yazarlu
- Mashhad University of Medical Sciences, Department of General Surgery, Mashhad, Iran
| | - Mehrdad Iranshahi
- Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran
| | | | - Sara Reshadat
- Department of Internal Medicine, Semnan University of Medical Sciences, Semnan, Iran
| | - Solomon Habtemariam
- Pharmacognosy Research Laboratories and Herbal Analysis Services UK, University of Greenwich, Central Avenue, Chatham-Maritime, Kent ME4 4TB, UK
| | - Milad Iranshahy
- Department of Pharmacognosy, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
| | - Maede Hasanpour
- Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
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15
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Jakubczyk A, Kiersnowska K, Ömeroğlu B, Gawlik-Dziki U, Tutaj K, Rybczyńska-Tkaczyk K, Szydłowska-Tutaj M, Złotek U, Baraniak B. The Influence of Hypericum perforatum L. Addition to Wheat Cookies on Their Antioxidant, Anti-Metabolic Syndrome, and Antimicrobial Properties. Foods 2021; 10:1379. [PMID: 34203621 PMCID: PMC8232325 DOI: 10.3390/foods10061379] [Citation(s) in RCA: 2] [Impact Index Per Article: 0.5] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/25/2021] [Accepted: 06/08/2021] [Indexed: 12/17/2022] Open
Abstract
The aim of this study was to characterize wheat cookies enriched with 0.5% and 1.0% of Hypericum perforatum L. (St. John's wort, SJW) and determine their pro-health properties in vitro after hydrolysis in simulated gastrointestinal conditions. The results indicated that 1.0 SJW was characterized by the highest content of polyphenols, flavonoids, and phenolic acids (2.32 mg mL-1, 4.93 µg mL-1, and 12.35 µg mL-1, respectively). The enriching cookies had no effect on water absorption capacity (WAC) and oil absorption capacity (OAC). After in vitro hydrolysis, the highest peptide content was noted in 1.0 SJW (0.52 mg mL-1), and the bioactive compounds were characterized by high potential bioaccessibility (PAC), but poor bioavailability (PAV). The addition of SJW increased the ACE, α-amylase, and LOX inhibitory effect, but reduced the inhibition of pancreatic lipase. The highest antioxidant activity was noted for 1.0 SJW. The results showed that only 0.5 SJW and 1.0 SJW had slight antimicrobial activity against E. coli ATCC 25922 and B. cereus ATCC 14579 with MIC = 12.5 mg mL-1. Fractions with molecular mass <3.0 kDa were characterized with the highest p-coumaric acid content. The results show that SJW cookies had a higher content of bioactive compounds and more potent anti-metabolic syndrome effects.
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Affiliation(s)
- Anna Jakubczyk
- Department of Biochemistry and Food Chemistry, University of Life Sciences in Lublin, Skromna 8, 20-704 Lublin, Poland; (A.J.); (U.G.-D.); (M.S.-T.); (B.B.)
| | - Kaja Kiersnowska
- Scientific Students Group of Food Biochemistry and Nutrition, Department of Biochemistry and Food Chemistry, University of Life Sciences in Lublin, 20-704 Lublin, Poland;
| | - Begümhan Ömeroğlu
- Department of Nutrition and Dietetics, Marmara Üniversitesi Göztepe Yerleşkesi, Kadıköy/İstanbul 34722, Turkey;
| | - Urszula Gawlik-Dziki
- Department of Biochemistry and Food Chemistry, University of Life Sciences in Lublin, Skromna 8, 20-704 Lublin, Poland; (A.J.); (U.G.-D.); (M.S.-T.); (B.B.)
| | - Krzysztof Tutaj
- Department of Biochemistry and Toxicology, Faculty of Animal Sciences and Bioeconomy, University of Life Sciences in Lublin, Akademicka 13, 20-950 Lublin, Poland;
| | - Kamila Rybczyńska-Tkaczyk
- Department of Environmental Microbiology, University of Life Sciences in Lublin, St. Leszczyńskiego 7, 20-069 Lublin, Poland;
| | - Magdalena Szydłowska-Tutaj
- Department of Biochemistry and Food Chemistry, University of Life Sciences in Lublin, Skromna 8, 20-704 Lublin, Poland; (A.J.); (U.G.-D.); (M.S.-T.); (B.B.)
| | - Urszula Złotek
- Department of Biochemistry and Food Chemistry, University of Life Sciences in Lublin, Skromna 8, 20-704 Lublin, Poland; (A.J.); (U.G.-D.); (M.S.-T.); (B.B.)
| | - Barbara Baraniak
- Department of Biochemistry and Food Chemistry, University of Life Sciences in Lublin, Skromna 8, 20-704 Lublin, Poland; (A.J.); (U.G.-D.); (M.S.-T.); (B.B.)
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Jarzębski M, Smułek W, Baranowska HM, Masewicz Ł, Kobus-Cisowska J, Ligaj M, Kaczorek E. Characterization of St. John's wort (Hypericum perforatum L.) and the impact of filtration process on bioactive extracts incorporated into carbohydrate-based hydrogels. Food Hydrocoll 2020. [DOI: 10.1016/j.foodhyd.2020.105748] [Citation(s) in RCA: 17] [Impact Index Per Article: 3.4] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/31/2023]
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17
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Akşit NN, Gürdap S, İşoğlu SD, İşoğlu İA. Preparation of antibacterial electrospun poly(D, L-lactide-co-glycolide)/gelatin blend membranes containing Hypericum capitatum var. capitatum. INT J POLYM MATER PO 2020. [DOI: 10.1080/00914037.2020.1765354] [Citation(s) in RCA: 6] [Impact Index Per Article: 1.2] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/20/2022]
Affiliation(s)
- Nazende Nur Akşit
- Bioengineering Department, Faculty of Life and Natural Sciences, Abdullah Gül University, Kayseri, Turkey
| | - Seda Gürdap
- Bioengineering Department, Faculty of Life and Natural Sciences, Abdullah Gül University, Kayseri, Turkey
| | - Sevil Dinçer İşoğlu
- Bioengineering Department, Faculty of Life and Natural Sciences, Abdullah Gül University, Kayseri, Turkey
| | - İsmail Alper İşoğlu
- Bioengineering Department, Faculty of Life and Natural Sciences, Abdullah Gül University, Kayseri, Turkey
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18
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The antibacterial and antivirulent potential of Hypericum lydium against Staphylococcus aureus: Inhibition of growth, biofilm formation, and hemolytic activity. Eur J Integr Med 2020. [DOI: 10.1016/j.eujim.2020.101061] [Citation(s) in RCA: 8] [Impact Index Per Article: 1.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/06/2023]
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Tresch M, Mevissen M, Ayrle H, Melzig M, Roosje P, Walkenhorst M. Medicinal plants as therapeutic options for topical treatment in canine dermatology? A systematic review. BMC Vet Res 2019; 15:174. [PMID: 31133058 PMCID: PMC6537371 DOI: 10.1186/s12917-019-1854-4] [Citation(s) in RCA: 20] [Impact Index Per Article: 3.3] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/04/2018] [Accepted: 03/27/2019] [Indexed: 12/14/2022] Open
Abstract
Background Medicinal plants have been used traditionally since centuries for wound care and treatment of skin diseases both in human and animals. Skin diseases are one of the most common reasons for owners to take their dog to the veterinarian. The demands for treatment and prophylaxis of these diseases are broad. A wide range of bacteria including antibiotic-resistant bacteria can be involved, making the treatment challenging and bear an anthropo-zoonotic potential. The aim of this review is to systematically evaluate based on recent scientific literature, the potential of four medicinal plants to enrich the therapeutic options in pyoderma, canine atopic dermatitis, otitis externa, wounds and dermatophytosis in dogs. Results Based on four books and a survey among veterinarians specialized in phytotherapy, four medicinal plants were chosen as the subject of this systematic review: Calendula officinalis L. (Marigold), Hypericum perforatum L. agg. (St. John’s Wort), Matricaria chamomilla L. (syn. Matricaria recutita L., Chamomile) and Salvia officinalis L. (Sage). According to the PRISMA statement through literature research on two online databases a total of 8295 publications was screened and narrowed down to a final 138 publications for which full-text documents were analyzed for its content resulting in a total of 145 references (21 clinical, 24 in vivo and 100 in vitro references). Conclusions All four plants were proven to have antibacterial and antifungal effects of a rather broad spectrum including antibiotic-resistant bacteria. This makes them an interesting new option for the treatment of pyoderma, otitis externa, infected wounds and dermatophytosis. Marigold, St. John’s Wort and Chamomile showed wound-healing properties and are thus promising candidates in line to fill the therapeutic gap in canine wound-healing agents. St. John’s Wort and Chamomile also showed anti-inflammatory and other beneficial effects on healthy skin. Due to the wide range of beneficial effects of these medicinal plants, they should be taken into account for the treatment of dermatologic diseases in dogs at least in future clinical research. Electronic supplementary material The online version of this article (10.1186/s12917-019-1854-4) contains supplementary material, which is available to authorized users.
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Affiliation(s)
- Milena Tresch
- Division Veterinary Pharmacology & Toxicology, Department Clinical Research and Veterinary Public Health, Vetsuisse Faculty, University of Bern, Laenggassstrasse 124, 3012, Bern, Switzerland
| | - Meike Mevissen
- Division Veterinary Pharmacology & Toxicology, Department Clinical Research and Veterinary Public Health, Vetsuisse Faculty, University of Bern, Laenggassstrasse 124, 3012, Bern, Switzerland
| | - Hannah Ayrle
- Department of Livestock Sciences, Research Institute of Organic Agriculture (FiBL), Ackerstrasse 113, Postbox 219, 5070, Frick, Switzerland
| | - Matthias Melzig
- Dahlem Centre of Plant Sciences, Institute of Pharmacy, Freie Universität Berlin, Koenigin-Luise-Strasse 2+4, 14195, Berlin, Germany
| | - Petra Roosje
- Division of Clinical Dermatology, Department of Clinical Veterinary Medicine, Vetsuisse Faculty, University of Bern, Laenggassstrasse 124, 3012, Bern, Switzerland
| | - Michael Walkenhorst
- Department of Livestock Sciences, Research Institute of Organic Agriculture (FiBL), Ackerstrasse 113, Postbox 219, 5070, Frick, Switzerland.
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20
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Doğan Ş, Gökalsın B, Şenkardeş İ, Doğan A, Sesal NC. Anti-quorum sensing and anti-biofilm activities of Hypericum perforatum extracts against Pseudomonas aeruginosa. JOURNAL OF ETHNOPHARMACOLOGY 2019; 235:293-300. [PMID: 30763694 DOI: 10.1016/j.jep.2019.02.020] [Citation(s) in RCA: 24] [Impact Index Per Article: 4.0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 12/22/2018] [Revised: 01/30/2019] [Accepted: 02/11/2019] [Indexed: 06/09/2023]
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE Hypericum perforatum L. (Hypericaceae) has been used as a traditional therapeutic for skin wounds, burns, cuts and stomach ailments including stomach ache, ulcers for a long time in many societies. Although many studies about its antibacterial properties can be found, there is a lack of studies about its quorum sensing inhibition properties, which effects bacterial vulnerability directly, on Pseudomonas aeruginosa. AIM OF THE STUDY Evaluation of anti-quorum sensing (anti-QS) and anti-biofilm activity of ethanol, methanol, acetone and ultra-sonicated extracts of Hypericum perforatum L. (HP) which is a well-known wound healer, against P. aeruginosa. MATERIALS AND METHODS Aerial parts of HP were extracted with ethanol, methanol and acetone. In addition, separate extractions with ultrasonication were carried out with same solvents. Anti-QS activity tests with different doses of HP extracts were performed by employing biomonitor strains, of which the promoter of QS regulating and green fluorescent protein (GFP) genes were fusioned. For anti-biofilm activity, HP extracts were applied to wild type PAO1 strains and biofilm inhibition was quantified via crystal violet staining method. RESULTS HP's ethanol, methanol and acetone extracts (250 µg/ml doses) inhibited LasIR signalling pathway up to 65.43%, 59.60%, 55.95% and same solvent extracts obtained with ultrasonication inhibited 71.33%, 64.47%, 57.35% respectively. Moreover, inhibition rates of RhlIR pathway were 28.80%, 50.83%, 45.84% for ethanol, methanol, acetone extracts (250 µg/ml doses) and 51.43%, 57.41%, 50.02% for ultrasonication extracts (250 µg/ml doses), compared to untreated controls. In the experiments, ethanol, methanol, acetone and ultra-sonicated extracts of HP did not inhibit biofilm formation. CONCLUSIONS This study shows that HP plant is capable for blocking of las and rhl QS systems of P. aeruginosa. However, it was observed that ethanol, methanol and acetone extract of the plant samples did not show anti-biofilm activity against P. aeruginosa. This led us to thinking that biofilm formation was caused via another pathway such as IQS or PQS. Further studies with isolated active compounds of HP might give a better understanding of the effects on biofilm formation of P. aeruginosa.
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Affiliation(s)
- Şule Doğan
- Department of Pharmaceutical Botany, Institute of Health Sciences, Marmara University, 34854 Istanbul, Turkey
| | - Barış Gökalsın
- Department of Biology, Institute of Pure and Applied Sciences, Marmara University, 34730 Istanbul, Turkey
| | - İsmail Şenkardeş
- Department of Pharmaceutical Botany, Faculty of Pharmacy, Marmara University, 34668 Istanbul, Turkey
| | - Ahmet Doğan
- Department of Pharmaceutical Botany, Faculty of Pharmacy, Marmara University, 34668 Istanbul, Turkey
| | - N Cenk Sesal
- Department of Biology, Faculty of Arts and Sciences, Marmara University, 34730 Istanbul, Turkey.
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21
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Milevskaya V, Prasad S, Temerdashev Z. Extraction and chromatographic determination of phenolic compounds from medicinal herbs in the Lamiaceae and Hypericaceae families: A review. Microchem J 2019. [DOI: 10.1016/j.microc.2018.11.041] [Citation(s) in RCA: 27] [Impact Index Per Article: 4.5] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/13/2022]
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22
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Agapouda A, Booker A, Kiss T, Hohmann J, Heinrich M, Csupor D. Quality control of Hypericum perforatum L. analytical challenges and recent progress. J Pharm Pharmacol 2019; 71:15-37. [PMID: 28266019 DOI: 10.1111/jphp.12711] [Citation(s) in RCA: 29] [Impact Index Per Article: 4.8] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/08/2016] [Accepted: 01/26/2017] [Indexed: 11/29/2022]
Abstract
OBJECTIVES The most widely applied qualitative and quantitative analytical methods in the quality control of Hypericum perforatum extracts will be reviewed, including routine analytical tools and most modern approaches. KEY FINDINGS Biologically active components of H. perforatum are chemically diverse; therefore, different chromatographic and detection methods are required for the comprehensive analysis of St. John's wort extracts. Naphthodianthrones, phloroglucinols and flavonoids are the most widely analysed metabolites of this plant. For routine quality control, detection of major compounds belonging to these groups seems to be sufficient; however, closer characterization requires the detection of minor compounds as well. CONCLUSIONS TLC and HPTLC are basic methods in the routine analysis, whereas HPLC-DAD is the most widely applied method for quantitative analysis due to its versatility. LC-MS is gaining importance in pharmacokinetic studies due to its sensitivity. Modern approaches, such as DNA barcoding, NIRS and NMR metabolomics, may offer new possibilities for the more detailed characterization of secondary metabolite profile of H. perforatum extracts.
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Affiliation(s)
- Anastasia Agapouda
- Research Cluster "Biodiversity and Medicines" , Research Group "Pharmacognosy and Phytotherapy" , UCL School of Pharmacy , University of London, London, UK
| | - Anthony Booker
- Research Cluster "Biodiversity and Medicines" , Research Group "Pharmacognosy and Phytotherapy" , UCL School of Pharmacy , University of London, London, UK
- Division of Herbal and East Asian Medicine, Department of Life Sciences, University of Westminster, London, UK
| | - Tivadar Kiss
- Department of Pharmacognosy, University of Szeged, Szeged, Hungary
- Interdisciplinary Centre of Natural Products, University of Szeged, Szeged, Hungary
| | - Judit Hohmann
- Department of Pharmacognosy, University of Szeged, Szeged, Hungary
- Interdisciplinary Centre of Natural Products, University of Szeged, Szeged, Hungary
| | - Michael Heinrich
- Research Cluster "Biodiversity and Medicines" , Research Group "Pharmacognosy and Phytotherapy" , UCL School of Pharmacy , University of London, London, UK
| | - Dezső Csupor
- Department of Pharmacognosy, University of Szeged, Szeged, Hungary
- Interdisciplinary Centre of Natural Products, University of Szeged, Szeged, Hungary
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23
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Nazlı O, Baygar T, Demirci Dönmez ÇE, Dere Ö, Uysal Aİ, Aksözek A, Işık C, Aktürk S. Antimicrobial and antibiofilm activity of polyurethane/Hypericum perforatum extract (PHPE) composite. Bioorg Chem 2018; 82:224-228. [PMID: 30342304 DOI: 10.1016/j.bioorg.2018.08.017] [Citation(s) in RCA: 20] [Impact Index Per Article: 2.9] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/25/2018] [Revised: 08/08/2018] [Accepted: 08/09/2018] [Indexed: 12/01/2022]
Abstract
Microbial accumulation in materials used in sectors such as medical, textile and food can lead to serious diseases, infections and uncontrollable problems. Many of the materials used in the above-mentioned industries have highly sensitive surfaces for microorganisms and cause colonization and biofilm formation. Colonization and biofilm formation threaten human health and they cause many diseases that result in death every year. Antimicrobial materials have an important role in combating pathogens. This article is about a new material with antibiofilm and antimicrobial properties combining polyurethane and Hypericum perforatum extract (PHPE) together. Antimicrobial effect of H. perforatum extract was determined against three clinical pathogens; C. albicans, E. coli and S. aureus. The highest antimicrobial activity of H. perforatum extract was found against S. aureus strain. Antibiofilm analysis results revealed that H. perforatum was also inhibited by the biofilm formation of S. aureus by 56.85%. The combination of polyurethane material and H. perforatum extract (PHPE) resulted in 92.85% decrease in S. aureus biofilm compared to control group. The reduction of S. aureus after H. perforatum incorporation was revealed by Scanning Electron Microscopy (SEM) study. The results show that the polyurethane material combined with H. perforatum extract inhibits the formation of S. aureus biofilm.
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Affiliation(s)
- Okay Nazlı
- Department of General Surgery, Muğla Sıtkı Koçman University, 48000 Muğla, Turkey
| | - Tuba Baygar
- Research and Application Center for Research Laboratories, Muğla Sıtkı Koçman University, 48000 Muğla, Turkey
| | | | - Özcan Dere
- Department of General Surgery, Muğla Sıtkı Koçman University, 48000 Muğla, Turkey
| | - Ali İhsan Uysal
- Department of Anesthesia and Reanimation, Muğla Sıtkı Koçman University Training and Research Hospital, 48000 Muğla, Turkey
| | - Alper Aksözek
- Department of Medical Microbiology, Muğla Sıtkı Koçman University, 48000 Muğla, Turkey
| | - Ceyhun Işık
- Department of Chemistry, Muğla Sıtkı Koçman University, 48000 Muğla, Turkey
| | - Selçuk Aktürk
- Department of Physics, Muğla Sıtkı Koçman University, 48000 Muğla, Turkey.
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24
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Rosato A, Carocci A, Catalano A, Clodoveo ML, Franchini C, Corbo F, Carbonara GG, Carrieri A, Fracchiolla G. Elucidation of the synergistic action of Mentha Piperita essential oil with common antimicrobials. PLoS One 2018; 13:e0200902. [PMID: 30067803 PMCID: PMC6070247 DOI: 10.1371/journal.pone.0200902] [Citation(s) in RCA: 55] [Impact Index Per Article: 7.9] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/23/2017] [Accepted: 07/05/2018] [Indexed: 11/26/2022] Open
Abstract
Mentha piperita L. essential oil (EO) is employed for external use as antipruritic, astringent, rubefacient and antiseptic. Several studies demonstrated its significant antiviral, antifungal and antibacterial properties. The aim of this work is the study of the synergistic effects of M. piperita EO with antibacterials and antifungals that are widely available and currently prescribed in therapies against infections. The observed strong synergy may constitute a potential new approach to counter the increasing phenomenon of multidrug resistant bacteria and fungi. In vitro efficacy of the association M. piperita EO/drugs was evaluated against a large panel of Gram-positive and Gram-negative bacteria and yeast strains. The antimicrobial effects were studied by checkerboard microdilution method. The synergistic effect of M. piperita EO with gentamicin resulted in a strong growth inhibition for all the bacterial species under study. The synergistic effect observed for M. piperita EO and antifungals was less pronounced.
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Affiliation(s)
- Antonio Rosato
- Department of Pharmacy–Drug Sciences, University of Bari “A. Moro”, Bari, Italy
| | - Alessia Carocci
- Department of Pharmacy–Drug Sciences, University of Bari “A. Moro”, Bari, Italy
| | - Alessia Catalano
- Department of Pharmacy–Drug Sciences, University of Bari “A. Moro”, Bari, Italy
| | - Maria Lisa Clodoveo
- Department of Agro-Environmental and Territorial Sciences, University of Bari “A. Moro”, Bari, Italy
| | - Carlo Franchini
- Department of Pharmacy–Drug Sciences, University of Bari “A. Moro”, Bari, Italy
| | - Filomena Corbo
- Department of Pharmacy–Drug Sciences, University of Bari “A. Moro”, Bari, Italy
| | | | - Antonio Carrieri
- Department of Pharmacy–Drug Sciences, University of Bari “A. Moro”, Bari, Italy
| | - Giuseppe Fracchiolla
- Department of Pharmacy–Drug Sciences, University of Bari “A. Moro”, Bari, Italy
- * E-mail:
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25
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Béjaoui A, Ben Salem I, Rokbeni N, M’rabet Y, Boussaid M, Boulila A. Bioactive compounds from Hypericum humifusum and Hypericum perfoliatum: inhibition potential of polyphenols with acetylcholinesterase and key enzymes linked to type-2 diabetes. PHARMACEUTICAL BIOLOGY 2017; 55:906-911. [PMID: 28147885 PMCID: PMC6130493 DOI: 10.1080/13880209.2016.1270973] [Citation(s) in RCA: 21] [Impact Index Per Article: 2.6] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 08/03/2016] [Revised: 10/12/2016] [Accepted: 12/07/2016] [Indexed: 05/28/2023]
Abstract
CONTEXT Natural products are reported to have a wide spectrum of pharmacological properties such as antimicrobial, anti-inflammatory and anti-cholinesterase. The genus Hypericum (Hypericaceae) is a source of a variety of molecules with different biological activities, notably hypericin and various phenolics. OBJECTIVES The goals of the present work were the determination of total phenolic and flavonoid content, hypericin and hyperforin concentration as well as the evaluation of biological of Hypericum humifusum L. (Hhu) and Hypericum perfoliatum L. (Hper). MATERIALS AND METHODS The various extracts of aerial parts were powdered, and then extracted with methanol. Antibacterial activity was performed according to minimum inhibitory concentration (MIC) and minimum bactericidal (MBC) methods against four Gram-positive bacteria, four Gram-negative bacteria and yeast. RESULTS The results revealed that H. humifusum, bear the highest total phenolic and flavonoid content (48-113 mg GAE/g and 8-41 mg RE/g, respectively) as well as hypericin (60-90 mg/g) and hyperforin (8-30 mg/g) concentration. Both species showed significant antioxidant activity as revealed by DPPH, FRAP, ABTS, and metal chelating assays. H. humifusum exhibited a strong acetylcholinesterase (3.86-4.57 mg GALAEs/g), α-glucosidase (0.73-2.55 mmol ACEs/g) and α-amylase (3-8 mmol ACEs/g) inhibitory activity. The extract of H. humifusum exhibited strong antibacterial activity mainly against Staphylococcus epidermidis, Staphylococus aureus, and Enterococcus faecium (MIC values ranging from 200 to 250 μg/mL). The highest antifungal activity was showed for H. perfoliatum extract (MIC value = 250 μg/mL). CONCLUSION The data suggest that H. humifusum could be used as valuable new natural agents with functional properties for pharmacology industries.
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Affiliation(s)
- Afef Béjaoui
- Laboratory of Plant Biotechnology, National Institute of Applied Sciences and Technology, Tunis, Tunisia
| | - Issam Ben Salem
- National Centre for Nuclear Science and Technology (CNSTN), Ariana, Tunisia
| | - Nesrine Rokbeni
- Laboratory of Natural Substances, National Institute of Research and Physico-chemical Analysis, Ariana, Tunisia
| | - Yassine M’rabet
- Laboratory of Natural Substances, National Institute of Research and Physico-chemical Analysis, Ariana, Tunisia
| | - Mohamed Boussaid
- Laboratory of Plant Biotechnology, National Institute of Applied Sciences and Technology, Tunis, Tunisia
| | - Abdennacer Boulila
- Laboratory of Natural Substances, National Institute of Research and Physico-chemical Analysis, Ariana, Tunisia
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Srisuwan S, Voravuthikunchai SP. Rhodomyrtus tomentosa Leaf Extract Inhibits Methicillin-Resistant Staphylococcus aureus Adhesion, Invasion, and Intracellular Survival in Human HaCaT Keratinocytes. Microb Drug Resist 2017; 23:1002-1012. [PMID: 28475464 DOI: 10.1089/mdr.2016.0284] [Citation(s) in RCA: 14] [Impact Index Per Article: 1.8] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/23/2023] Open
Abstract
Methicillin-resistant Staphylococcus aureus (MRSA) has an ability to invade nonprofessional phagocytic cells, resulting in persistent infections and most likely host cell death. Series of our studies have claimed pronounced antibacterial efficacy of Rhodomyrtus tomentosa leaf extract. This study was to further investigate potency of the extract in intracellular killing of human HaCaT keratinocytes. Pretreatment of MRSA with the extract resulted in a remarkable reduction in the bacterial adhesion to HaCaT keratinocytes, compared with untreated control (p < 0.001). In addition, at least 60% inhibition of the bacterial invasion into HaCaT cells was observed. Intracellular killing assay demonstrated that the extract exhibited strong antibacterial activity against intracellular MRSA at nontoxic concentrations (128 mg/L), which may have resulted from the increase in bactericidal activity under phagolysosomal pH. Transmission electron microscopy displayed the effects of the extract on alterations in the bacterial cell morphology with cell lysis. Fluorescence microscopy revealed that the extract decreased MRSA-induced apoptosis in HaCaT cells. In addition, cytotoxicity of HaCaT cells caused by MRSA supernatant was reduced at least 50% by the extract. The potential activities of R. tomentosa extract may be useful in an alternative treatment of MRSA infections in slight acidic compartments, particularly skin infections.
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Affiliation(s)
- Sutthirat Srisuwan
- Excellence Research Laboratory on Natural Products and Department of Microbiology, Faculty of Science and Natural Products Research Center of Excellence, Prince of Songkla University , Songkhla, Thailand
| | - Supayang Piyawan Voravuthikunchai
- Excellence Research Laboratory on Natural Products and Department of Microbiology, Faculty of Science and Natural Products Research Center of Excellence, Prince of Songkla University , Songkhla, Thailand
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Biotechnological production of hyperforin for pharmaceutical formulation. Eur J Pharm Biopharm 2017; 126:10-26. [PMID: 28377273 DOI: 10.1016/j.ejpb.2017.03.024] [Citation(s) in RCA: 19] [Impact Index Per Article: 2.4] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/18/2017] [Revised: 03/28/2017] [Accepted: 03/29/2017] [Indexed: 01/09/2023]
Abstract
Hyperforin is a major active constituent of Hypericum perforatum (St. John's wort). It has amazing pharmacological activities, such as antidepressant properties, but it is labile and difficult to synthesize. Its sensitivity and lipophilicity are challenges for processing and formulation. Its chemical complexity provokes approaches of biotechnological production and modification. Dedifferentiated H. perforatum cell cultures lack appropriate storage sites and hence appreciable hyperforin levels. Shoot cultures are capable of forming hyperforin but less suitable for biomass up-scaling in bioreactors. Roots commonly lack hyperforin but a recently established adventitious root line has been demonstrated to produce hyperforin and derivatives at promising levels. The roots also contained lupulones, the typical constituents of hop (Humulus lupulus). Although shear-sensitive, these root cultures provide a potential production platform for both individual compounds and extracts with novel combinations of constituents and pharmacological activities. Besides in vitro cultivation techniques, the reconstruction of hyperforin biosynthesis in microorganisms is a promising alternative for biotechnological production. The biosynthetic pathway is under study, with omics-technologies being increasingly implemented. These biotechnological approaches may not only yield hyperforin at reasonable productivity but also allow for modifications of its chemical structure and pharmacological profile.
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Marčetić MD, Milenković MT, Lakušić DV, Lakušić BS. Chemical Composition and Antimicrobial Activity of the Essential Oil and Methanol Extract of Hypericum aegypticum subsp. webbii (Spach) N. Robson. Chem Biodivers 2017; 13:427-36. [PMID: 26923468 DOI: 10.1002/cbdv.201500119] [Citation(s) in RCA: 8] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/06/2015] [Accepted: 07/03/2015] [Indexed: 11/09/2022]
Abstract
Hypericum aegypticum subsp. webbii is an evergreen shrub spread in Mediterranean part of central and southeastern Europe. The chemical composition and antimicrobial activity of the essential oil and MeOH extract of H. aegypticum subsp. webbii were investigated. The monoterpenes α-pinene (63.4 - 68.5%) and β-pinene (16.9 - 17.0%) were main compounds in the volatile oil from aerial parts. In the cluster analysis, the essential oil of H. aegypticum subsp. webbii was separated and chemically different from the oil of other subspecies of H. aegypticum as well as other Hypericum species from Greece. SIMPER analysis revealed that α-pinene (24.79%) was the component that contributed the most to differences between all oils. Also, there was extremely high overall dissimilarity between three subspecies of H. aegypticum. MeOH extract of aerial parts of H. aegypticum subsp. webbii contained flavonoids rutin (56.4 ± 0.9 mg/g), hyperoside and quercetin, and phenolic acids chlorogenic and caffeic acid, while naphthodianthrones were not detected. The antimicrobial activity of essential oil was moderate (MIC from 100 to >200 μg/ml), while MeOH extract inhibited the growth of Gram-positive bacteria Bacillus subtilis, Enterococcus faecalis, Staphylococcus epidermidis, and Micrococcus luteus (MIC 50 - 100 μg/ml), more pronounced than the extract of H. perforatum (MIC 200 - >200 μg/ml).
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Affiliation(s)
- Mirjana D Marčetić
- Department of Pharmacognosy, Faculty of Pharmacy, University of Belgrade, V. Stepe 450, RS-11221, Belgrade
| | - Marina T Milenković
- Department of Microbiology and Immunology, Faculty of Pharmacy, University of Belgrade, V. Stepe 450, RS-11221, Belgrade
| | - Dmitar V Lakušić
- Institute of Botany and Botanical Garden 'Jevremovac', Faculty of Biology, University of Belgrade, Takovska 43, RS-11000, Belgrade
| | - Branislava S Lakušić
- Department of Botany, Faculty of Pharmacy, University of Belgrade, V. Stepe 450, RS-11221, Belgrade
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Sytar O, Švedienė J, Ložienė K, Paškevičius A, Kosyan A, Taran N. Antifungal properties of hypericin, hypericin tetrasulphonic acid and fagopyrin on pathogenic fungi and spoilage yeasts. PHARMACEUTICAL BIOLOGY 2016; 54:3121-3125. [PMID: 27564138 DOI: 10.1080/13880209.2016.1211716] [Citation(s) in RCA: 31] [Impact Index Per Article: 3.4] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 04/11/2016] [Accepted: 07/06/2016] [Indexed: 06/06/2023]
Abstract
CONTEXT The role of hypericin-mediated photodynamic antimicrobial properties on pathogenic fungi and photodynamic therapy for human cancer cells is known. Antifungal properties of Hypericum perforatum L. (Hypericaceae) and Fagopyrum esculentum Moench. (Polygonaceae) extracts were also studied. The different polarities of solvents can cause complication in the identification of antifungal effects of separate biologically active compounds. In recent experimental work, we compared antifungal properties of purified hypericin, hypericin tetrasulphonic acid (hypericin + S) and fagopyrin, which is analogue of hypericin. OBJECTIVE The antifungal properties of aromatic polyketide derivatives such as hypericin, hypericin + S and fagopyrin on the selected pathogenic fungi and spoilage yeasts have been studied. MATERIALS AND METHODS The antifungal properties of hypericin, hypericin + S and fagopyrin were determined using the broth microdilution method against a set of pathogenic fungi and spoilage yeasts including: Microsporum canis, Trichophyton rubrum, Fusarium oxysporum, Exophiala dermatitidis, Candida albicans, Kluyveromyces marxianus, Pichia fermentans and Saccharomyces cerevisiae. The tested concentrations of hypericin, hypericin + S and fagopyrin ranged from 750 to 0.011 μg/mL and MIC values were evaluated after 48 h incubation at 30 °C. RESULTS The results confirm different antifungal properties of hypericin, hypericin + S and fagopyrin on the selected pathogenic fungi and spoilage yeasts. For pathogenic fungi, the minimum inhibitory concentrations of hypericin ranged 0.18-46.9 μg/mL, hypericin + S 0.18-750 μg/mL and fagopyrin 11.7-46.9 μg/mL. For spoilage yeasts, the MICs of hypericin and hypericin + S ranged 0.18-46.9 and 0.011-0.73 μg/mL, respectively. DISCUSSION AND CONCLUSION The results obtained herein indicate that various chemical structures of hypericin, hypericin + S and fagopyrin can develop different antifungal properties.
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Affiliation(s)
- Oksana Sytar
- a Department of Plant Physiology , Institute of Biology, Kiev National University of Taras Shevchenko , Kiev , Ukraine
| | - Jurgita Švedienė
- b Nature Research Centre, Institute of Botany , Vilnius , Lithuania
| | - Kristina Ložienė
- b Nature Research Centre, Institute of Botany , Vilnius , Lithuania
| | - Algimantas Paškevičius
- b Nature Research Centre, Institute of Botany , Vilnius , Lithuania
- c Laboratory of Microbiology, Centre of Laboratory Medicine , Vilnius University Hospital Santariškių klinikos , Vilnius , Lithuania
| | - Anatolij Kosyan
- a Department of Plant Physiology , Institute of Biology, Kiev National University of Taras Shevchenko , Kiev , Ukraine
| | - Natalija Taran
- a Department of Plant Physiology , Institute of Biology, Kiev National University of Taras Shevchenko , Kiev , Ukraine
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Milevskaya VV, Statkus MA, Temerdashev ZA, Kiseleva NV, Butyl’skaya TS, Shil’ko EA. Extraction and determination of biologically active components of St. John’s wort and its pharmaceutical preparations. JOURNAL OF ANALYTICAL CHEMISTRY 2016. [DOI: 10.1134/s1061934816070133] [Citation(s) in RCA: 16] [Impact Index Per Article: 1.8] [Reference Citation Analysis] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 11/23/2022]
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Süntar I, Oyardı O, Akkol EK, Ozçelik B. Antimicrobial effect of the extracts from Hypericum perforatum against oral bacteria and biofilm formation. PHARMACEUTICAL BIOLOGY 2015; 54:1065-70. [PMID: 26510970 PMCID: PMC11133939 DOI: 10.3109/13880209.2015.1102948] [Citation(s) in RCA: 39] [Impact Index Per Article: 3.9] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 06/10/2015] [Revised: 07/30/2015] [Accepted: 09/28/2015] [Indexed: 06/05/2023]
Abstract
CONTEXT One traditional medicines, Hypericum perforatum L. (Hypericaceae), possesses several beneficial effects against depression, ulcers, dyspepsia, abdominal pains, burns, bacterial infections, migraine headaches, and sciatica. OBJECTIVE The present study investigates the antimicrobial activity of the ethanol extract (HP-EtOH) of H. perforatum and its sub-extracts, namely n-hexane (HP-hexane), chloroform (HP-CHCl3), ethyl acetate (HP-EtOAc), n-butanol (HP-n-BuOH), and water (HP-H2O) extracts, against Streptococcus mutans, S. sobrinus, Lactobacillus plantarum, and Enterococcus faecalis. MATERIALS AND METHODS For the evaluation of the antimicrobial activity, flowering aerial parts of H. perforatum were extracted with EtOH and then this extract was fractionated to obtain five sub-extracts in different polarities. Antimicrobial activities of HP-EtOH and its sub-extracts against Streptococcus mutans, S. sobrinus, L. plantarum, and E. faecalis were assessed by using colorimetric micro-well dilution at concentration ranges of 64-0.5 μg/ml as well as resazurin microplate and modified microtiter-plate assays between the ranges of 100 and 0.78125 μg/ml. RESULTS According to the results of the present study, HP-H2O sub-extract displayed strong antibacterial activity (MIC values 8 μg/mL) against S. sobrinus and L. plantarum, and exerted moderate activity against S. mutans and E. faecalis at 32 and 16 μg/mL concentrations, respectively. Other sub-extracts also demonstrated antimicrobial activity against S. sobrinus at a concentration of 16 μg/mL. HP-EtOAc and HP-n-BuOH showed antimicrobial activity against L. plantarum and HP-EtOAc and HP-H2O were also active against E. faecalis at the same concentrations (16 μg/mL). CONCLUSION According to the results, we suggest that H. perforatum could be employed as a natural antibacterial agent in oral care products.
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Affiliation(s)
| | - Ozlem Oyardı
- Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Gazi University, Ankara, Turkey
| | | | - Berrin Ozçelik
- Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Gazi University, Ankara, Turkey
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Ahmad A, Khan A, Samber N, Manzoor N. Antimicrobial activity of Mentha piperita essential oil in combination with silver ions. ACTA ACUST UNITED AC 2014. [DOI: 10.1016/j.synres.2014.11.001] [Citation(s) in RCA: 2] [Impact Index Per Article: 0.2] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 10/24/2022]
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Comparative study of iodine-123-labeled hypericin and (99m)Tc-labeled hexakis [2-methoxy isobutyl isonitrile] in a rabbit model of myocardial infarction. J Cardiovasc Pharmacol 2014; 62:304-11. [PMID: 23714775 DOI: 10.1097/fjc.0b013e31829b2c6b] [Citation(s) in RCA: 14] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Indexed: 12/20/2022]
Abstract
Identification of myocardial infarction (MI) by imaging is critical for clinical management of ischemic heart disease. Iodine-123-labeled hypericin (¹²³I-Hyp) is a new potent infarct avid agent. We sought to compare target selectivity and organ distribution between ¹²³I-Hyp and the myocardial perfusion agent, technetium-99m-labeled hexakis [2-methoxy isobutyl isonitrile] ((99m)Tc-Sestamibi) in rabbits with acute MI. Hypericin was radiolabeled with I using iodogen as oxidant, and (99m)Tc-Sestamibi was prepared from a commercial kit and radioactive sodium pertechnetate. Rabbits (n = 6) with 24-hour-old MI received ¹²³I-Hyp intravenously and received (99m)Tc-Sestamibi 9 hours later. They were studied by dual-isotope simultaneous acquisition micro single photon emission computed tomography/computed tomography (DISA-μSPECT/CT), tissue gamma counting (TGC), autoradiography, and histology. After purification, ¹²³I-Hyp was obtained with radiochemical purity around 99%. DISA-μSPECT/CT images showed ¹²³I-Hyp retention in infarcted but not in normal myocardium. By TGC, accumulation values reached 1.175 ± 0.096 percentage of injected dose per gram (%ID/g) and 0.028 ± 0.007%ID/g in infarcted myocardium and normal myocardium with high tracer concentration in liver, intestines, and gallbladder. (99m)Tc-Sestamibi was prepared with radiochemical purity over 95%. DISA-μSPECT/CT showed no accumulation in MI and high initial radioactivity levels in normal myocardium that were rapidly cleared as confirmed by TGC (0.011 ± 0.003%ID/g). Liver and intestines were clearly visualized. By TGC, gallbladder and kidneys show moderate (99m)Tc-Sestamibi uptake. The selectivity of ¹²³I-Hyp for infarcted myocardium and (99m)Tc-Sestamibi for normal myocardium was confirmed. ¹²³I-Hyp distribution in rabbits is characterized by hepatobiliary excretion. (99m)Tc-Sestamibi undergoes hepatorenal elimination.
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Cona MM, Feng Y, Zhang J, Li Y, Verbruggen A, Oyen R, Ni Y. Sodium cholate, a solubilizing agent for the necrosis avid radioiodinated hypericin in rabbits with acute myocardial infarction. Drug Deliv 2014; 22:427-35. [DOI: 10.3109/10717544.2013.873838] [Citation(s) in RCA: 12] [Impact Index Per Article: 1.1] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/19/2022] Open
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An overview of translational (radio)pharmaceutical research related to certain oncological and non-oncological applications. World J Methodol 2013; 3:45-64. [PMID: 25237623 PMCID: PMC4145570 DOI: 10.5662/wjm.v3.i4.45] [Citation(s) in RCA: 10] [Impact Index Per Article: 0.8] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 09/04/2013] [Revised: 10/03/2013] [Accepted: 10/18/2013] [Indexed: 02/06/2023] Open
Abstract
Translational medicine pursues the conversion of scientific discovery into human health improvement. It aims to establish strategies for diagnosis and treatment of diseases. Cancer treatment is difficult. Radio-pharmaceutical research has played an important role in multiple disciplines, particularly in translational oncology. Based on the natural phenomenon of necrosis avidity, OncoCiDia has emerged as a novel generic approach for treating solid malignancies. Under this systemic dual targeting strategy, a vascular disrupting agent first selectively causes massive tumor necrosis that is followed by iodine-131 labeled-hypericin (123I-Hyp), a necrosis-avid compound that kills the residual cancer cells by crossfire effect of beta radiation. In this review, by emphasizing the potential clinical applicability of OncoCiDia, we summarize our research activities including optimization of radioiodinated hypericin Hyp preparations and recent studies on the biodistribution, dosimetry, pharmacokinetic and, chemical and radiochemical toxicities of the preparations. Myocardial infarction is a global health problem. Although cardiac scintigraphy using radioactive perfusion tracers is used in the assessment of myocardial viability, searching for diagnostic imaging agents with authentic necrosis avidity is pursued. Therefore, a comparative study on the biological profiles of the necrosis avid 123I-Hyp and the commercially available 99mTc-Sestamibi was conducted and the results are demonstrated. Cholelithiasis or gallstone disease may cause gallbladder inflammation, infection and other severe complications. While studying the mechanisms underlying the necrosis avidity of Hyp and derivatives, their naturally occurring fluorophore property was exploited for targeting cholesterol as a main component of gallstones. The usefulness of Hyp as an optical imaging agent for cholelithiasis was studied and the results are presented. Multiple uses of automatic contrast injectors may reduce costs and save resources. However, cross-contaminations with blood-borne pathogens of infectious diseases may occur. We developed a radioactive method for safety evaluation of a new replaceable patient-delivery system. By mimicking pathogens with a radiotracer, we assessed the feasibility of using the system repeatedly without septic risks. This overview is deemed to be interesting to those involved in the related fields for translational research.
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Richard JA. Chemistry and Biology of the Polycyclic Polyprenylated Acylphloroglucinol Hyperforin. European J Org Chem 2013. [DOI: 10.1002/ejoc.201300815] [Citation(s) in RCA: 32] [Impact Index Per Article: 2.7] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/20/2022]
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Cona MM, Alpizar YA, Li J, Bauwens M, Feng Y, Sun Z, Zhang J, Chen F, Talavera K, de Witte P, Verbruggen A, Oyen R, Ni Y. Radioiodinated hypericin: its biodistribution, necrosis avidity and therapeutic efficacy are influenced by formulation. Pharm Res 2013; 31:278-90. [PMID: 23934256 DOI: 10.1007/s11095-013-1159-4] [Citation(s) in RCA: 17] [Impact Index Per Article: 1.4] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/03/2013] [Accepted: 07/22/2013] [Indexed: 12/22/2022]
Abstract
PURPOSE To study whether formulation influences biodistribution, necrosis avidity and tumoricidal effects of the radioiodinated hypericin, a necrosis avid agent for a dual-targeting anticancer radiotherapy. METHODS Iodine-123- and 131-labeled hypericin ((123)I-Hyp and (131)I-Hyp) were prepared with Iodogen as oxidant, and formulated in dimethyl sulfoxide (DMSO)/PEG400 (polyethylene glycol 400)/water (25/60/15, v/v/v) or DMSO/saline (20:80, v/v). The formulations with excessive Hyp were optically characterized. Biodistribution, necrosis avidity and tumoricidal effects were studied in rats (n = 42) without and with reperfused liver infarction and implanted rhabdomyosarcomas (R1). To induce tumor necrosis, R1-rats were pre-treated with a vascular disrupting agent. Magnetic resonance imaging, tissue-gamma counting, autoradiography and histology were used. RESULTS The two formulations differed significantly in fluorescence and precipitation. (123)I-Hyp/Hyp in DMSO/PEG400/water exhibited high uptake in necrosis but lower concentration in the lung, spleen and liver (p < 0.01). Tumor volumes of 0.9 ± 0.3 cm(3) with high radioactivity (3.1 ± 0.3% ID/g) were detected 6 days post-treatment. By contrast, (131)I-Hyp/Hypin DMSO/saline showed low uptake in necrosis but high retention in the spleen and liver (p < 0.01). Tumor volumes reached 2.6 ± 0.7 cm(3) with low tracer accumulation (0.1 ± 0.04%ID/g). CONCLUSIONS The formulation of radioiodinated hypericin/hypericin appears crucial for its physical property, biodistribution, necrosis avidity and tumoricidal effects.
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Affiliation(s)
- Marlein Miranda Cona
- Department of Imaging & Pathology, Faculty of Medicine Biomedical Sciences Group, KU Leuven, Herestraat 49, Leuven, Belgium
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Crispin MC, Hur M, Park T, Kim YH, Wurtele ES. Identification and biosynthesis of acylphloroglucinols in Hypericum gentianoides. PHYSIOLOGIA PLANTARUM 2013; 148:354-70. [PMID: 23600727 PMCID: PMC3687794 DOI: 10.1111/ppl.12063] [Citation(s) in RCA: 14] [Impact Index Per Article: 1.2] [Reference Citation Analysis] [Abstract] [MESH Headings] [Grants] [Track Full Text] [Subscribe] [Scholar Register] [Received: 02/01/2013] [Revised: 04/05/2013] [Accepted: 04/10/2013] [Indexed: 05/18/2023]
Abstract
Species of the genus Hypericum contain a rich array of unusual polyketides, however, only a small proportion of the over 450 Hypericum species, other than the popular medicinal supplement St. John's Wort (Hypericum perforatum), have even been chemically characterized. Hypericum gentianoides, a small annual used medicinally by Cherokee Americans, contains bioactive acylphloroglucinols. Here, we identify acylphloroglucinol constituents of H. gentianoides and determine a potential pathway to their synthesis. Liquid chromatography/electrospray ionization-mass spectrometry (LC/ESI-MS) and HPLC-UV indicate that the level of accumulation and profile of acylphloroglucinols in H. gentianoides vary little seasonally when grown in a greenhouse, but do vary with development and are highly dependent on the accession, highlighting the importance of the selection of plant material for study. We identify the chemical structures of the nine prevalent polyketides, based on LC/ESI-MS and hybrid quadrupole orthogonal time-of-flight (Q-TOF) mass spectrometry; these metabolites include one monomeric phlorisobutyrophenone (PIB) derivative and eight dimeric acylphloroglucinols. Q-TOF spectrometry was used to identify eight additional PIB derivatives that were not detected by LC/ESI-MS. These data lead us to propose that diacylphloroglucinols are synthesized via modification of PIB to yield diverse phloroglucinol and filicinic acids moieties, followed by dimerization of a phloroglucinol and a filicinic acid monomer to yield the observed complement of diacylphloroglucinols. The metabolomics data from H. gentianoides are accessible in plant metabolomics resource (PMR) (http://www.metnetdb.org/pmr), a public metabolomics database with analysis software for plants and microbial organisms.
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Affiliation(s)
- Matthew C. Crispin
- Department of Genetics, Developmental, and Cell Biology, Iowa State University USA
| | - Manhoi Hur
- Department of Genetics, Developmental, and Cell Biology, Iowa State University USA
| | - Taeseong Park
- Division of Mass Spectrometry Research, Korea Basic Science Institute, Ochang 863-883, Korea
| | - Young Hwan Kim
- Division of Mass Spectrometry Research, Korea Basic Science Institute, Ochang 863-883, Korea
- Graduate School of Analytical Science and Technology, Chungnam National University, Daejeon 305-764, Korea
| | - Eve Syrkin Wurtele
- Department of Genetics, Developmental, and Cell Biology, Iowa State University USA
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Mortensen T, Shen S, Shen F, Walsh MK, Sims RC, Miller CD. Investigating the effectiveness of St John's wort herb as an antimicrobial agent against mycobacteria. Phytother Res 2012; 26:1327-33. [PMID: 22294548 DOI: 10.1002/ptr.3716] [Citation(s) in RCA: 7] [Impact Index Per Article: 0.5] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/31/2011] [Revised: 10/27/2011] [Accepted: 11/02/2011] [Indexed: 01/16/2023]
Abstract
A persistent need exists for effective treatment agents for mycobacterial infections. This research investigated the effectiveness of the Hypericum perforatum herb (commonly known as St John's wort; SJW) in its growth inhibition of mycobacteria. A SJW extract was effective at inhibiting five nonpathogenic Mycobacterium isolates and Bacillus subtilis, but not Escherichia coli. Quantitative studies of concentration sensitivity to the SJW extract were performed with minimal bactericidal concentrations (MBC) ranging from 0.33 to 2.66 mg extract/mL. The SJW compounds hyperforin (Hfn), hypericin (Hpn), and pseudohypericin (Phn) were quantified in the extract using HPLC. The SJW extract solution of 133 mg extract/mL used in this study contained 2.3 mg Hfn/mL, 0.8 mg Hpn/mL, and 2.1 mg Phn/mL. Purified Hfn, Hpn, and Phn were tested for inhibitory activity against Mycobacterium JLS (M. JLS) at similar concentrations used in the crude extract. While Hfn was inhibitory at 46 µg/mL, none of the purified SJW constituents were bactericidal at concentrations corresponding to SJW treatments. Scanning electron microscopy (SEM) analysis of SJW-treated M. JLS cells showed changes in cell surface morphology.
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Affiliation(s)
- Trent Mortensen
- Department of Biological Engineering, Utah State University, 4105 Old Main Hill, Logan, UT 84322-4105, USA
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Arsić I, Žugić A, Tadić V, Tasić-Kostov M, Mišić D, Primorac M, Runjaić-Antić D. Estimation of dermatological application of creams with St. John's Wort oil extracts. Molecules 2011; 17:275-94. [PMID: 22205093 PMCID: PMC6268942 DOI: 10.3390/molecules17010275] [Citation(s) in RCA: 18] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/04/2011] [Revised: 11/30/2011] [Accepted: 12/16/2011] [Indexed: 11/16/2022] Open
Abstract
Oleum Hyperici, the oil extract of St. John’s Wort (SJW), is one of the oldest folk remedies, traditionally used in the topical treatment of wounds, bruises, ulcers, cuts, burns, hemorrhoids and also as an antiseptic. Considering the advantageous characteristics of emulsion applications, in the present study we have formulated three O/W creams containing 15% (w/v) of SJW oil extract as an active ingredient. The aim was to estimate dermatological application of the prepared creams for the abovementioned indications. The extracts were prepared according to the prescriptions from traditional medicine, however with different vegetable oils used as an extractant, namely: Olive, palm and sunflower oil. The investigated O/W creams demonstrated significant antiinflammatory effects in an in vivo double-blind randomized study, using a sodium lauryl sulphate test. Both skin parameters assessed in the study (electrical capacitance and erythema index), were restored to the baseline value after a seven-day treatment with the tested creams. Almost all investigated SJW oil extracts and corresponding creams displayed the same antimicrobial activity against the most of the investigated microorganisms with obtained minimal inhibitory concentrations values of 1,280 µg/mL, 2,560 µg/mL or >2,560 µg/mL.
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Affiliation(s)
- Ivana Arsić
- Department of Pharmaceutical Research and Development, Institute for Medicinal Plant Research "Dr Josif Pančić", Tadeuša Košćuška 1, 11 000 Belgrade, Serbia; (A.Ž.); (V.T.); (D.R.-A.)
- Author to whom correspondence should be addressed; ; Tel.: +381-11-303-1658; Fax: +381-11-303-1649
| | - Ana Žugić
- Department of Pharmaceutical Research and Development, Institute for Medicinal Plant Research "Dr Josif Pančić", Tadeuša Košćuška 1, 11 000 Belgrade, Serbia; (A.Ž.); (V.T.); (D.R.-A.)
| | - Vanja Tadić
- Department of Pharmaceutical Research and Development, Institute for Medicinal Plant Research "Dr Josif Pančić", Tadeuša Košćuška 1, 11 000 Belgrade, Serbia; (A.Ž.); (V.T.); (D.R.-A.)
| | - Marija Tasić-Kostov
- Department of Pharmacy, Faculty of Medicine, University of Niš, Dr Zoran Đinđić Boulevard 81, Niš, Serbia;
| | - Dušan Mišić
- Department of Microbiology and Immunology, Faculty of Veterinary Medicine, University of Belgade, Bulevar oslobođenja 18, 11 000 Belgrade, Serbia;
| | - Marija Primorac
- Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, Vojvode Stepe 450, 11 000 Belgrade, Serbia;
| | - Dušanka Runjaić-Antić
- Department of Pharmaceutical Research and Development, Institute for Medicinal Plant Research "Dr Josif Pančić", Tadeuša Košćuška 1, 11 000 Belgrade, Serbia; (A.Ž.); (V.T.); (D.R.-A.)
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Sun F, Liu JY, He F, Liu Z, Wang R, Wang DM, Wang YF, Yang DP. In-vitro antitumor activity evaluation of hyperforin derivatives. JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH 2011; 13:688-699. [PMID: 21751836 DOI: 10.1080/10286020.2011.584532] [Citation(s) in RCA: 8] [Impact Index Per Article: 0.6] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 05/31/2023]
Abstract
The derivatives of hyperforin, namely hyperforin acetate (2), 17,18,22,23,27,28,32,33-octahydrohyperforin acetate (3), and N,N-dicyclohexylamine salt of hyperforin (4), have been investigated for their antitumor properties. In-vitro studies demonstrated that 2 and 4 were active against HeLa (human cervical cancer), A375 (human malignant melanoma), HepG2 (human hepatocellular carcinoma), MCF-7 (human breast cancer), A549 (human nonsmall cell lung cancer), K562 (human chronic myeloid leukemia), and K562/ADR (human adriamycin-resistant K562) cell lines with IC(50) values in the range of 3.2-64.1 μM. The energy differences between highest occupied molecular orbital and lowest unoccupied molecular orbital of 2-4 were calculated to be 0.39778, 0.43106, and 0.30900 a.u., respectively, using the Gaussian 03 software package and ab initio method with the HF/6-311 G* basis set. The result indicated that the biological activity of 4 might be the strongest and that of 3 might be the weakest, which was in accordance with their corresponding antiproliferative effects against the tested tumor cell lines. Compound 4 caused cell cycle arrest at G2/M phase in flow cytometry experiment and induced apoptosis by 4',6-diamidino-2-phenylindole staining and Annexin V-FITC/PI (propidium iodide) double-labeled staining in HepG2 cells. The results indicated a potential for N,N-dicyclohexylamine salt of hyperforin as a new antitumor drug.
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Affiliation(s)
- Feng Sun
- School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China
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Biesaga M. Influence of extraction methods on stability of flavonoids. J Chromatogr A 2011; 1218:2505-12. [DOI: 10.1016/j.chroma.2011.02.059] [Citation(s) in RCA: 148] [Impact Index Per Article: 10.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/30/2010] [Revised: 01/24/2011] [Accepted: 02/23/2011] [Indexed: 02/08/2023]
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Liu JY, Liu Z, Wang DM, Li MM, Wang SX, Wang R, Chen JP, Wang YF, Yang DP. Induction of apoptosis in K562 cells by dicyclohexylammonium salt of hyperforin through a mitochondrial-related pathway. Chem Biol Interact 2011; 190:91-101. [DOI: 10.1016/j.cbi.2011.02.026] [Citation(s) in RCA: 25] [Impact Index Per Article: 1.8] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/21/2010] [Revised: 02/22/2011] [Accepted: 02/23/2011] [Indexed: 12/19/2022]
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Saddiqe Z, Naeem I, Maimoona A. A review of the antibacterial activity of Hypericum perforatum L. JOURNAL OF ETHNOPHARMACOLOGY 2010; 131:511-21. [PMID: 20659547 DOI: 10.1016/j.jep.2010.07.034] [Citation(s) in RCA: 175] [Impact Index Per Article: 11.7] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 12/18/2009] [Revised: 07/16/2010] [Accepted: 07/16/2010] [Indexed: 05/19/2023]
Abstract
Hypericum perforatum L. (Hypericaceae) is a perennial herb that is commonly known as St. John's Wort. The plant has been valued for its important biological and chemical perspectives and its use in the treatment of infectious diseases has been documented in ethnobotanical reports. Most recent interest in H. perforatum has focused on its antidepressant effects, and only recently has its antimicrobial activity been evaluated against a number of bacterial and fungal strains. The present review gives a comprehensive summary of the ethnobotanical uses, chemical constituents and biological effects (antibacterial and antifungal) of this species. A comprehensive account of the chemical constituents including anthraquinone derivatives (naphthodianthrones), flavonoids, prenylated phloroglucinols, tannins and volatile oils is also included. Various types of preparations, ointments, creams and extracts prepared with and compounds isolated from this species have been found to possess a broad spectrum of biological and pharmacological effects such as antidepressant effects, wound-healing, antiviral and antimicrobial activity. The antibacterial activity of crude extracts can be related to the use of the herb as a wound healer in ancient times. The sole antibacterial principle isolated to date is a tetraketone, hyperforin, also thought to be responsible for the antidepressant activity of the herb. The available literature indicates that it has a higher antibacterial activity against Gram-positive than Gram-negative bacteria, and alcoholic extracts (methanolic/ethanolic) were shown to possess more pronounced activity than aqueous extracts. Based on the chemical and pharmacological characteristics of H. perforatum, we concluded that this species has beneficial therapeutic properties and has the potential for use as an effective adaptogenic herbal remedy.
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Affiliation(s)
- Zeb Saddiqe
- Department of Chemistry, Lahore College for Women University, Jail Road, Lahore 54600, Pakistan. zeb
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Cui H, Gabriel AA, Nakano H. Antimicrobial efficacies of plant extracts and sodium nitrite against Clostridium botulinum. Food Control 2010. [DOI: 10.1016/j.foodcont.2009.12.023] [Citation(s) in RCA: 24] [Impact Index Per Article: 1.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 02/08/2023]
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Neagoe I, Macri BM, Flonta ML. Hyperici herba extract interaction with artificial lipid bilayers. J Pharm Pharmacol 2010; 56:1283-9. [PMID: 15482643 DOI: 10.1211/0022357044292] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 10/31/2022]
Abstract
Abstract
Hyperici herba (Hyp) is the aerial part collected during the flowering period from the well-known herb, Hypericum perforatum. Black lipid membrane experiments were performed to investigate the effect of the ethanolic Hyp extract on the electrical properties (capacitance and conductance) of artificial lipid bilayers. Hyp extract (1–10 μg mL−1) induced a concentration-dependent increase of both specific transmembrane capacitance and conductance in phosphatidylcholine (PC) membranes. The effect on conductance was enhanced when the Hyp extract (3 μg mL−1) was present on both sides of the membrane (Gm = 77.89 ± 8.81 nS cm−2, n = 5) compared with single-sided application (Gm = 36.48 ± 2.41 nS cm−2, n = 5). In bilayers containing PC and phosphatidylserine (PS), PC:PS, the Hyp extract effect was greater than on pure PC bilayers, although the surface charge was not the determining factor of this enhanced activity. Adding cholesterol to the PC:PS mixture reverted the conductance increase induced by the Hyp extract in a dose-dependent manner. The specific pattern of the Hyp extract interaction with lipid bilayers has possible consequences concerning its absorption and bioavailability, as well as its pharmacodynamic effects on neuronal excitability.
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Affiliation(s)
- Ioana Neagoe
- Department of Animal Physiology and Biophysics, University of Bucharest, Faculty of Biology, Splaiul Independentei 91-95, Bucharest R-050095, Romania
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Engelhardt V, Krammer B, Plaetzer K. Antibacterial photodynamic therapy using water-soluble formulations of hypericin or mTHPC is effective in inactivation of Staphylococcus aureus. Photochem Photobiol Sci 2010; 9:365-9. [DOI: 10.1039/b9pp00144a] [Citation(s) in RCA: 61] [Impact Index Per Article: 4.1] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/21/2022]
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Lüthi M, Besic Gyenge E, Engstrüm M, Bredell M, Grätz K, Walt H, Gmür R, Maake C. Hypericin- and mTHPC-mediated photodynamic therapy for the treatment of cariogenic bacteria. ACTA ACUST UNITED AC 2009. [DOI: 10.1016/j.mla.2009.07.004] [Citation(s) in RCA: 19] [Impact Index Per Article: 1.2] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 10/20/2022]
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Rosato A, Vitali C, Piarulli M, Mazzotta M, Argentieri MP, Mallamaci R. In vitro synergic efficacy of the combination of Nystatin with the essential oils of Origanum vulgare and Pelargonium graveolens against some Candida species. PHYTOMEDICINE : INTERNATIONAL JOURNAL OF PHYTOTHERAPY AND PHYTOPHARMACOLOGY 2009; 16:972-975. [PMID: 19616925 DOI: 10.1016/j.phymed.2009.02.011] [Citation(s) in RCA: 42] [Impact Index Per Article: 2.6] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 05/28/2023]
Abstract
In this study we investigated a synergistic effect between the essential oils Origanum vulgare, Pelargonium graveolens and Melaleuca alternifolia and the antifungal compound Nystatin. Nystatin is considered a drug of choice in the treatment of fungal infections, but it can cause some considerable problems through its side effects, such as renal damage. Finding a new product that can reduce the Nystatin dose via combination is very important. Our findings showed an experimental occurrence of a synergistic interaction between two of these essential oils and Nystatin. The essential oil O. vulgare appeared to be the most effective, inhibiting all the Candida species evaluated in this study. Some combinations of Nystatin and P. graveolens essential oil did not have any synergistic interactions for some of the strains considered. Associations of Nystatin with M. alternifolia essential oil had only an additive effect.
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Affiliation(s)
- Antonio Rosato
- Department of Pharmaceutical Chemistry, Section of Microbiology University of Bari, Via E. Orabona n.4, 70125 Bari, Italy.
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Rosato A, Vitali C, Gallo D, Balenzano L, Mallamaci R. The inhibition of Candida species by selected essential oils and their synergism with amphotericin B. PHYTOMEDICINE : INTERNATIONAL JOURNAL OF PHYTOTHERAPY AND PHYTOPHARMACOLOGY 2008; 15:635-638. [PMID: 18579358 DOI: 10.1016/j.phymed.2008.05.001] [Citation(s) in RCA: 51] [Impact Index Per Article: 3.0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 05/26/2023]
Abstract
In this work we highlight a possible synergistic anti-Candida effect between Melaleuca alternifolia, Origanum vulgare and Pelargonium graveolens essential oils and the antifungal compound Amphotericin B. The antifungal activity was assessed using the agar dilution method in eleven Candida strains. The results obtained indicate the occurrence of a synergistic interaction between the essential oils under study and Amphotericin B. P. graveolens essential oil appeared to be the most effective, inhibiting all the Candida species evaluated by this study.
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Affiliation(s)
- Antonio Rosato
- Department of Pharmaceutical Chemistry, Section of Microbiology, University of Bari, Via E. Orabona n. 4, 70125 Bari, Italy.
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