The effects of alpha-lipoic acid (ALA) supplementation on cardiovascular-related factors have been evaluated in a number of randomized clinical trials, with different results. Thus, in this meta-analysis, the effects of ALA on blood levels of inflammatory, lipid, and hematological markers as well as anthropometric indices in patients with chronic kidney disease (CKD) were evaluated.

Five electronic databases were used to conduct a comprehensive search through October 2023. Risk of bias assessment and data extraction were carried out separately by 2 reviewers on the included papers. The data were analyzed using the random-effects model in meta-analyses. The data were analyzed using the random-effects model in meta-analyses. We assessed inter-study heterogeneity with I2 and Cochran's Q test.

Nine of the 421 potential reports were included. Using random-effects models, no significant changes were observed in weight loss, body mass index, hemoglobin, and iron following ALA supplementation (600 mg/day). Results exhibited that ALA significantly reduced high-sensitivity C-reactive protein levels in individuals with CKD (weighted mean difference (WMD) = -2.91 mg/L, 95% CI: -4.65, -1.17, I2 = 50.5%, P = .09); however, there were no significant variations in levels of interleukin-6 (IL-6) or malondialdehyde. Regarding lipid profiles, findings revealed that ALA administration had no significant impact on high-density lipoprotein cholesterol and triglycerides levels among patients with CKD. However, compared to the control group, total cholestrol levels were considerably lower in CKD patients (WMD = -5.48 mg/dL, 95% CI: -10.55, -0.41, I2 = 0.0%, P = .50). Moreover, the sensitivity analyses showed that pooled WMDs for low-density lipoprotein cholesterol levels were significantly changed (-6.88 mg/dL, 95% CI, -12.78, -0.98).

These findings revealed that ALA supplementation slightly but significantly reduced blood levels of high-sensitivity C-reactive protein, total cholestrol, and low-density lipoprotein cholesterol, but did not affect IL-6, malondialdehyde, high-density lipoprotein cholesterol, weight, body mass index, iron, and hemoglobin in patients with CKD.

Quercetin is known for its ability to inhibit mast cell degranulation and reduce the release of inflammatory mediators. However, it has also been reported to sensitize mast cells, potentially leading to hyperresponsiveness. This necessitates careful optimization of its use in the treatment of chronic inflammatory diseases. To fully harness quercetin's therapeutic potential, this study investigated the effects of quercetin on rat basophilic leukemia (RBL-2H3) cells responsiveness over varying durations of exposure. We employed comprehensive transcriptome analysis and subsequent functional validation of key signaling pathways. Our findings revealed that quercetin initially reduced cell activity with short-term treatment. However, with prolonged exposure, quercetin transiently enhanced both IgE cross-linkage-mediated and non-IgE-mediated responses. Specifically, prolonged quercetin treatment downregulated IgE-mediated degranulation and FcεRI expression, while potentially sensitizing RBL-2H3 cells to other non-IgE secretagogues through enhanced PKC activity. Given quercetin's multifaceted effects on intracellular signaling pathways, it is crucial to further investigate its efficacy and potential risk of adverse effects. Future studies should focus on a deeper understanding of these mechanisms to optimize quercetin's therapeutic applications while mitigating any possible negative outcomes.

Quercetin (QUE) is a natural flavonoid with well-known anticancer capabilities, although its effect on viral-induced cancers is less studied. Kaposi's sarcoma (KS) is a viral cancer caused by the human herpesvirus-8, which, during its lytic phase, expresses a constitutively activated viral G protein-coupled receptor (vGPCR) able to induce oncogenic modifications that lead to tumor development. The aim of this work was to investigate the potential effect of QUE on in vitro and in vivo models of Kaposi's sarcoma, developed by transforming endothelial cells with the vGPCR of Kaposi's sarcoma-associated herpesvirus. Initially, the antiproliferative effect of QUE was determined in endothelial cells stably expressing the vGPCR (vGPCR cells), with an IC50 of 30 μM. Additionally, QUE provoked a decrease in vGPCR cell viability, interfered with the cell cycle progression, and induced apoptosis, as revealed by annexin V/PI analysis and caspase-3 activity. The presence of apoptotic bodies and disorganized actin filaments was observed by SEM and phalloidin staining. Furthermore, tumors from vGPCR cells were induced in nude mice, which were treated with QUE (50 or 100 mg/kg/d) resulting in retarded tumor progression and reduced tumor weight. Notably, neither kidney nor liver damage was observed, as indicated by biochemical parameters in serum. In conclusion, this study suggests for the first time that QUE exhibits antineoplastic activity in both in vitro and in vivo models of KS, marking a starting point for further investigations and protocols for therapeutic purpose.

Quercetin, a flavonoid found in vegetables and fruits, has been extensively studied for its health benefits and disease management. Its role in the prevention of various pathogenesis has been well-documented, primarily through its ability to inhibit oxidative stress, inflammation, and enhance the endogenous antioxidant defense mechanisms. Electronic databases such as Google Scholar, Scopus, PubMed, Medline, and Web of Science were searched for information regarding quercetin and its role in various pathogeneses. The included literature comprised experimental studies, randomized controlled trials, and epidemiological studies related to quercetin, while editorials, case analyses, theses, and letters were excluded. It has been reported to have a wide range of health benefits including hepatoprotective, antidiabetic, anti-obesity, neuroprotective, cardioprotective, wound healing, antimicrobial, and immunomodulatory effects, achieved through the modulation of various biological activities. Additionally, numerous in vitro and in vivo studies have shown that quercetin's efficacies in cancer management involve inhibiting cell signaling pathways, such as inflammation, cell cycle, and angiogenesis, activating cell signaling pathways including tumor suppressor genes, and inducing apoptosis. This review aims to provide a comprehensive understanding of the health benefits of quercetin in various pathogeneses. Additionally, this review outlines the sources of quercetin, nanoformulations, and its applications in health management, along with key findings from important clinical trial studies. Limited clinical data regarding quercetin's safety and mechanism of action are available. It is important to conduct more clinical trials to gain a deeper understanding of the disease-preventive potential, mechanisms of action, safety, and optimal therapeutic dosages. Furthermore, more research based on nanoformulations should be performed to minimize/overcome the hindrance associated with bioavailability, rapid degradation, and toxicity.

Gastric cancer remains a significant global health challenge, driving the need for innovative therapeutic approaches. Natural polyphenolic compounds such as resveratrol, piceatannol, curcumin, and quercetin currently show promising results in the prevention and treatment of various cancers, due to their diverse biological activities. This review presents the effects of natural compounds on important processes related to cancer, such as apoptosis, proliferation, migration, invasion, angiogenesis, and autophagy. Resveratrol, naturally found in red grapes, has been shown to induce apoptosis and inhibit the proliferation, migration, and invasion of gastric cancer cells. Piceatannol, a metabolite of resveratrol, shares similar anticancer properties, particularly in modulating autophagy. Curcumin, derived from turmeric, is known for its anti-inflammatory and antioxidant properties, and its ability to inhibit tumor growth and metastasis. Quercetin, a flavonoid found in various fruits and vegetables, induces cell cycle arrest and apoptosis while enhancing the efficacy of conventional therapies. Despite their potential, challenges such as low bioavailability limit their clinical application, necessitating further research into novel delivery systems. Collectively, these compounds represent a promising avenue for enhancing gastric cancer treatment and improving patient outcomes through their multifaceted biological effects.

Macrotyloma uniflorum is known for being a rich source of protein, fat, fiber, carbohydrates, vitamins, and micronutrients. Since ancient times, it has been used as a pulse and traditional remedy in the Himalayan Mountains for curing kidney and bladder stones, bronchitis, asthma, piles, leukoderma, and heart diseases. Horse gram contains bioactive compounds such as phenolic acids, flavonoids, and tannins, which contribute to its health advantages. These bioactive compounds demonstrated antioxidant, antidiabetic, anti-inflammatory, anticarcinogenic, antimicrobial, antidiarrheal, and neuroprotective effects. These horse gram products are now considered superfoods and are widely utilized in worldwide cuisines. Horse gram and its crude extracts or fractions have been shown to exhibit a wide range of in vivo and in vitro pharmacological and nutraceutical properties. However, there is currently a scarcity of structure-activity investigations of isolated compounds and mechanistic research on this species. This review demonstrates that horse gram, despite its traditional usage by diverse cultures, has a profusion of bioactive chemicals with a wide range of biological effects that might be employed as biopharmaceuticals and adopted by nutraceutical industries. This study focuses on the thorough phytochemistry, folk medicinal applications, and pharmacological properties of this versatile legume plant. Furthermore, we discussed the value of plants as a source of functional foods and nutraceuticals.

Glehnia littoralis is a medicinal plant, but the scientific basis is still unclear. This study thoroughly investigated phenols from Glehnia littoralis extract (GLE) to determine their potential as anti-inflammatory and antioxidant agents.

High-performance liquid chromatography (HPLC) and mass spectrometry (MS) were used to analyze the compounds in GLE. In addition, we performed GLE in vitro in macrophages after lipopolysaccharide (LPS)-induced inflammation.

The extract contained eight peaks representing phenolic compounds and one peak representing riboflavin, with the corresponding mass spectrometry data documented. These biologically active compounds were purified by ultrafiltration using LC to determine their ability to target cyclooxygenase-2 (COX-2) and 2,2-diphenyl-1-picrylhydrazyl (DPPH). The results showed that significant compounds were identified, demonstrating a binding affinity for both COX-2 and DPPH. This suggests that the compounds showing excellent binding affinity for COX-2 and DPPH may be the main active ingredients. Vital inflammatory cytokines, including COX-2, inducible nitric oxide synthase (iNOS), mitogen-activated protein kinase (MAPK), and nuclear factor kappa B (NF-κB), were found to be down-regulated during the treatment. In addition, we revealed that the selected drugs exhibited potent binding capacity to inflammatory factors through molecular docking studies. In addition, we confirmed the presence of phenolic components in GLE extract and verified their possible anti-inflammatory and antioxidant properties.

This study provided evidence for an efficient strategy to identify critical active ingredients from various medicinal plants. These data may serve as a baseline for further investigations of applying GLE in the pharmaceutical industry.

Oligonol, a low-molecular-weight polyphenol derived from lychee fruit, is well recognized for its antioxidant properties, blood glucose regulation, and fat mass reduction capability. However, its effect on the central nervous system remains unclear. Here, we investigated the effects of oligonol on brain in a high-fat diet (HFD) fed mouse model, and SH-SY5Y neuronal cells and primary cultured cortical neuron under insulin resistance conditions. HFD mice were orally administered oligonol (20 mg/kg) daily, and SH-SY5Y cells and primary cortical neurons were pretreated with 500 ng/mL oligonol under in vitro insulin resistance conditions. Our findings revealed that oligonol administration reduced blood glucose levels and improved spatial memory function in HFD mice. In vitro data demonstrated that oligonol protected neuronal cells and enhanced neural structure against insulin resistance. We confirmed RNA sequencing in the oligonol-pretreated insulin-resistant SH-SY5Y neuronal cells. Our RNA-sequencing data indicated that oligonol contributes to metabolic signaling and neurite outgrowth. In conclusion, our study provides insights into therapeutic potential of oligonol with respect to preventing neuronal cell damage and improving neural structure and cognitive function in HFD mice.

Inhibition of pancreatic lipase (PL) is a strategy to prevent obesity. The inhibitory effects of Flos Sophorae Immaturus (FSI) extract and its main flavonoid components, rutin and quercetin, on PL were investigated. The contents of rutin and quercetin in FSI extract were 44.10 ± 1.33 % and 6.07 ± 1.62 %, respectively. The IC50 values of FSI extract, rutin and quercetin on PL were 322, 258 and 71 μg/mL, respectively. Rutin and quercetin inhibited PL in a reversible and noncompetitive manner. The combination of rutin and quercetin exhibited synergistic inhibitory effects at low concentration. The binding of rutin/quercetin with PL caused the fluorescence quenching of protein. Fluorescence titration showed the binding affinity of quercetin with PL protein was stronger than that of rutin. Circular dichroism analysis showed the binding changed the secondary structure of PL with an increase in random coil and a decrease in α-Helix and β-Sheet. Molecular docking revealed that rutin and quercetin could interact with the amino acid residues around the catalytic site through multiple secondary interactions. In vivo studies showed that FSI extract can reduce fat absorption and promote fecal fat excretion through inhibition of PL activity, and the effects were mainly due to rutin and quercetin.

Nonalcoholic fatty liver disease (NAFLD) has become a growing public health problem worldwide. However, there is still lack of effective treatment strategies except lifestyle intervention.

To evaluate whether quercetin improves intrahepatic lipid content in patients with NAFLD.

In this randomized, double-blind, placebo-controlled crossover trial, 41 patients with NAFLD were randomly assigned to receive the quercetin (500 mg) or placebo capsules for 12 wk, then switched interventions for another 12 wk after a 4-wk washout period. The primary outcome was intrahepatic lipid content evaluated by magnetic resonance imaging estimated proton density fat fraction. The secondary outcomes were liver function measurements, etc. Safety outcomes included blood routine.

A total of 36 patients completed the trial. In intention-to-treat analyses, the quercetin intervention moderately decreased the intrahepatic lipid contents from 11.5% ± 6.4% to 9.6% ± 5.8%, compared with the placebo intervention (decreased by 0.1% ± 2.6%, P = 0.013 and adjusted P value is 0.028). Body weight and body mass index were mildly reduced by 1.5 ± 2.6 kg and 0.5 ± 0.9 kg/m2 after the quercetin intervention (P < 0.05 and both adjusted P values are 0.038), whereas the reductions were only 0.2 ± 1.8 kg and 0.1 ± 0.7 kg/m2 after the placebo intervention. The intrahepatic lipid content reductions were noticeably positively associated with the body weight losses after the quercetin and placebo interventions (r = 0.557 and 0.412, P < 0.001 and P = 0.007, respectively). Subgroup analyses found that the reduction of intrahepatic lipid contents in females (3.0% ± 3.7%) was about twice as large as that in males (1.4% ± 2.5%) with a trend of statistical significance (P = 0.113 and adjusted P value is 0.061). There were no significant differences in other secondary and safety outcomes. No adverse events associated with study intervention were found.

Twelve weeks treatment of quercetin could reduce intrahepatic lipid contents in patients with NAFLD, possibly explained by a slightly larger body weight loss in the quercetin group.

The trial is registered at www.chictr.org.cn as ChiCTR2100047904.

Numerous cellular, humoral, and molecular processes are involved in the intricate process of wound healing.

Numerous bioactive substances, such as ß-sitosterol, tannic acid, gallic acid, protocatechuic acid, quercetin, ellagic acid, and pyrogallol, along with their pharmacokinetics and bioavailability, have been reviewed. These phytochemicals work together to promote angiogenesis, granulation, collagen synthesis, oxidative balance, extracellular matrix (ECM) formation, cell migration, proliferation, differentiation, and re-epithelialization during wound healing.

To improve wound contraction, this review delves into how the application of each bioactive molecule mediates with the inflammatory, proliferative, and remodeling phases of wound healing to speed up the process. This review also reveals the underlying mechanisms of the phytochemicals against different stages of wound healing along with the differentiation of the in vitro evidence from the in vivo evidence There is growing interest in phytochemicals, or plant-derived compounds, due their potential health benefits. This calls for more scientific analysis and mechanistic research. The various pathways that these phytochemicals control/modulate to improve skin regeneration and wound healing are also briefly reviewed. The current review also elaborates the immunomodulatory modes of action of different phytochemicals during wound repair.

This study aimed to investigate the antioxidant and anti-inflammatory properties of quercetin on the cellular components of the Enteric Nervous System in the ileum of rats with arthritis. Rats were distributed into five groups: control (C), arthritic (AIA), arthritic treated with ibuprofen (AI), arthritic treated with quercetin (AQ) and arthritic treated with both ibuprofen and quercetin (AIQ). The ileum was processed for immunohistochemical techniques for HuC/D, calcitonin gene-related peptide, and vasoactive intestinal polypeptide. Measurements in histological sections, chemiluminescence assays, and total antioxidant capacity were also performed. Rheumatoid arthritis resulted in a decrease in neuronal density, yet neuroplasticity mechanisms were evident through observed changes in varicosities size and neuronal area compared to the control group. Reduced paw edema and neuroprotective effects were predominantly noted in both plexuses, as evidenced by the increased density preservation of HuC/D-IR neurons in the AIQ group. The increase of lipoperoxidation levels and paw edema volume in the AQ group was observed compared to the arthritic, whereas the AIQ group mainly showed similar results to those observed in the control. The enteropathy associated with arthritis proved to be significant in the field of gastroenterology, and the combination of quercetin and ibuprofen demonstrated promising anti-inflammatory and neuroprotective effects.

Colorectal cancer is a serious threat to people's life due to its high incidence and high mortality. Quercetin can effectively treat colorectal carcinoma (CRC), but its exact mechanism of action is still unclear. Then quercetin-related target genes were obtained from Swiss Target Prediction database and Similarity Ensemble Approach (SEA) database, and CRC-related target genes were obtained from GeneCards database, respectively. Common target genes were obtained by FunRich software. String software was used to construct a protein-protein interaction (PPI) network. R package was used for gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analysis. Molecular docking, molecular dynamics (MD) simulation and post-dynamics simulation were used to explore the binding stability of quercetin to key targets. In total, 103 and 141 target information of quercetin were obtained from the Swiss Target Prediction database and SEA database, respectively. 1,649 CRC-related genes were obtained from GeneCards database. FunRich software was used to draw venny map and obtain 36 intersection targets of quercetin and CRC. String software was used to construct the PPI network. The core genes were AKT1, EGFR, MMP9, KDR, MET and PTK2. There were 532 items related to biological processes, 14 items related to cellular components, and 43 items related to molecular functions among the key target GO enrichment items. KEGG enrichment pathways of key targets involved cancer pathways, PI3K-Akt signal pathway, etc. The results of molecular docking, MD simulation and post-dynamics simulation showed they had a good affinity and formed a stable effect. So quercetin may play an important role in the treatment of CRC by acting on AKT1, EGFR, MMP9, KDR, MET and PTK2 to affect the development of CRC.Communicated by Ramaswamy H. Sarma.

Dietary intervention, including polyphenol consumption, is recognized as an effective strategy to prevent obesity. Although fermented jujube juice (FJJ) with lactic acid bacteria has been shown to be rich in polyphenols and have strong antioxidant properties, little is known about its anti-obesity properties.

Untargeted metabolomics was employed to identify and analyze the differential metabolites between FJJ and raw jujube juice. A total of 431 metabolites belonging to diverse classes and with various functional active ingredients were quantitatively identified. The animal experiments results showed that FJJ administration for 13 weeks significantly inhibited high-fat-diet-induced body and epididymal adipose weight gain, and improved the serum lipid parameters in obese mice. Additionally, DNA-sequencing results revealed that FJJ treatment increased Akkermansia abundance in the gut and changed the composition of fecal microbiota by decreasing the Firmicutes/Bacteroidota ratio and Helicobacter pylori abundance.

These findings suggest that FJJ contributes to regulating lipid accumulation and gut microbiota composition in high-fat-diet-induced obese mice, which helps to prevent obesity. Hence, FJJ has the potential to be a beneficial beverage for controlling obesity. © 2024 Society of Chemical Industry.

Fruits and vegetables (like apples, citrus, grapes, onions, parsley, etc.) are the primary dietary sources of quercetin. In addition, isolated quercetin is also available on the market as a dietary supplement with a daily dose of up to 1000 mg/d. The objective of the present study is to explore the therapeutic potential and clinical efficacy of quercetin as a dietary supplement. The present paper highlights the safety parameters and clinical trial studies with several targets reviewed from the data available on PubMed, Science Direct, ClinicalTrails. gov, and from many reputed foundations. The results of the studies prove the unique position of quercetin in the treatment of various disorders and the possibility of using phytochemicals such as quercetin for an efficient cure. As evidenced by the numerous published reports on human interventions, it has been concluded that quercetin intake significantly improves disease conditions with minimal adverse effects.

Obesity is a complex medical condition mainly caused by eating habits, genetics, lifestyle, and medicine. The present study deals with traditional diets like the Mediterranean diet, Nordic diet, African Heritage diet, Asian diet, and DASH, as these are considered to be sustainable diets for curing obesity. However, the bioavailability of phytonutrients consumed in the diet may vary, depending on several factors such as digestion and absorption of phytonutrients, interaction with other substances, cooking processes, and individual differences. Hence, several phytochemicals, like polyphenols, alkaloids, saponins, terpenoids, etc., have been investigated to assess their efficiencies and safety in the prevention and treatment of obesity. These phytochemicals have anti-obesity effects, mediated via modulation of many pathways, such as decreased lipogenesis, lipid absorption, accelerated lipolysis, energy intake, expenditure, and preadipocyte differentiation and proliferation. Owing to these anti-obesity effects, new food formulations incorporating these phytonutrients were introduced that can be beneficial in reducing the prevalence of obesity and promoting public health.

A new sample preparation method based on microextraction in packed syringe was developed for preconcentration of quercetin prior to its spectrophotometric determination. Molecularly imprinted polymers as packing material was used for higher extraction efficiency. First, glass powder as support material because of low cost and available substrate was modified, and then molecularly imprinted polymers were synthesized by the sol-gel method using 3-aminopropyltriethoxysilane as a functional monomer and tetraethyl orthosilicate as cross-linker agent. The combination of a molecularly imprinted polymers and microextraction in packed syringe increased the selectivity and sensitivity. The surface morphology and functionality of the prepared molecularly imprinted polymers was characterized using Fourier-transform infrared spectroscopy, Field emission scanning electron microscopy, energy dispersive X-ray spectroscopy, and thermogravimetric analysis. Different influencing parameters on extraction efficiency such as effect of the number of sample sorption/desorption cycles, type and volume of desorption solvent, pH of the sample solution, and molecularly imprinted polymers amounts were optimized. Under the optimum condition, the proposed method displayed a linear range from 0.01 to 5 µg mL-1 and limit of detection 3.68 ng mL-1 . Relative standard deviation for three replicate determination of 1 µg mL-1 quercetin was 2.1 %. The proposed method was applied successfully for the selective extraction of quercetin from tea and coffee samples.

In this study, the ability of zein nanospheres (NS) and zein nanocapsules containing wheat germ oil (NC) to enhance the bioavailability and efficacy of quercetin was evaluated. Both types of nanocarriers had similar physico-chemical properties, including size (between 230 and 250 nm), spherical shape, negative zeta potential, and surface hydrophobicity. However, NS displayed a higher ability than NC to interact with the intestinal epithelium, as evidenced by an oral biodistribution study in rats. Moreover, both types of nanocarriers offered similar loading efficiencies and release profiles in simulated fluids. In C. elegans, the encapsulation of quercetin in nanospheres (Q-NS) was found to be two twice more effective than the free form of quercetin in reducing lipid accumulation. For nanocapsules, the presence of wheat germ oil significantly increased the storage of lipids in C. elegans; although the incorporation of quercetin (Q-NC) significantly counteracted the presence of the oil. Finally, nanoparticles improved the oral absorption of quercetin in Wistar rats, offering a relative oral bioavailability of 26% and 57% for Q-NS and Q-NC, respectively, compared to a 5% for the control formulation. Overall, the study suggests that zein nanocarriers, particularly nanospheres, could be useful in improving the bioavailability and efficacy of quercetin.

Quercetin, a flavonoid found in fruits and vegetables, has been a part of human diets for centuries. Its numerous health benefits, including antioxidant, antimicrobial, anti-inflammatory, antiviral, and anticancer properties, have been extensively studied. Its strong antioxidant properties enable it to scavenge free radicals, reduce oxidative stress, and protect against cellular damage. Quercetin's anti-inflammatory properties involve inhibiting the production of inflammatory cytokines and enzymes, making it a potential therapeutic agent for various inflammatory conditions. It also exhibits anticancer effects by inhibiting cancer cell proliferation and inducing apoptosis. Finally, quercetin has cardiovascular benefits such as lowering blood pressure, reducing cholesterol levels, and improving endothelial function, making it a promising candidate for preventing and treating cardiovascular diseases. This review provides an overview of the chemical structure, biological activities, and bioavailability of quercetin, as well as the different delivery systems available for quercetin. Incorporating quercetin-rich foods into the diet or taking quercetin supplements may be beneficial for maintaining good health and preventing chronic diseases. As research progresses, the future perspectives of quercetin appear promising, with potential applications in nutraceuticals, pharmaceuticals, and functional foods to promote overall well-being and disease prevention. However, further studies are needed to elucidate its mechanisms of action, optimize its bioavailability, and assess its long-term safety for widespread utilization.

Polyphenols have attracted great interest as potent antioxidant compounds and nutraceuticals; however, their antioxidant properties represent a multifaceted phenomenon, including pro-oxidant effects under particular conditions and complex behavior when multiple polyphenols are simultaneously present. Moreover, their intracellular behavior cannot always be predicted from their ability to counteract the production of ROS in acellular assays. The present work aimed to study the direct intracellular redox activity of two polyphenols, resveratrol and quercetin, singly and in mixture in a cellular short-term bioassay under both basal and pro-oxidant conditions. The study was carried out by spectrofluorimetric assessment of the intracellular fluorescence of CM-H₂DCFDA-charged HeLa cells under either basal conditions, due to the reactive species associated with the normal cellular oxidative metabolism, or pro-oxidant conditions induced by H₂O₂ exposure. Under basal conditions, the obtained results showed a significant antioxidant effect of quercetin and a weaker antioxidant effect of resveratrol when used singly, while antagonism of their effect was detected in their equimolar mixtures at all the concentrations used. Under exposure of the cells to H₂O₂, quercetin exhibited a dose-dependent intracellular antioxidant activity whereas resveratrol manifested a pro-oxidant intracellular activity, while their equimolar mixtures showed an intracellular interaction between the 2 polyphenols, with additive effects at 5 µM and synergic at 25 µM and 50 µM. Thus, the results clarified the direct intracellular antioxidant/pro-oxidant activity of quercetin and resveratrol alone and in their equimolar mixtures in the cell model HeLa cells and highlighted that the antioxidant properties of polyphenols in mixtures at the cellular level depend not only on the nature of the compounds themselves but also on the type of interactions in the cellular system, which in turn are influenced by the concentration and the oxidative status of the cell.

Obesity is characterized by the excessive accumulation of fat, which triggers a low-grade chronic inflammatory process. Currently, the search for compounds with anti-obesogenic effects that help reduce body weight, as well as associated comorbidities, continues. Among this group of compounds are plant extracts and flavonoids with a great diversity of action mechanisms associated with their beneficial effects, such as anti-inflammatory effects and/or as signaling molecules. In the bark of Tabebuia rosea tree, there are different classes of metabolites with anti-inflammatory properties, such as quercetin. Therefore, the present work studied the effect of the ethanolic extract of T. rosea and quercetin on the mRNA of inflammation markers in obesity compared to the drugs currently used. Total RNA was extracted from epididymal adipose tissue of high-fat diet-induced obese Wistar rats treated with orlistat, phentermine, T. rosea extract, and quercetin. The rats treated with T. rosea and quercetin showed 36 and 31% reductions in body weight compared to the obese control, and they likewise inhibited pro-inflammatory molecules: Il6, Il1b, Il18, Lep, Hif1a, and Nfkb1 without modifying the expression of Socs1 and Socs3. Additionally, only T. rosea overexpressed Lipe. Both T. rosea and quercetin led to a reduction in the expression of pro-inflammatory genes, modifying signaling pathways, which led to the regulation of the obesity-inflammation state.

Java plum is widely recognized as a plant with valuable medicinal properties, originating from Indonesia and India and distributed globally in the tropic and sub-tropic regions of the world. The plant is rich in alkaloids, flavonoids, phenyl propanoids, terpenes, tannins, and lipids. The phytoconstituents of the plant seeds possess various vital pharmacological activities and clinical effects including their antidiabetic potential. The bioactive phytoconstituents of Java plum seeds include jambosine, gallic acid, quercetin, β-sitosterol, ferulic acid, guaiacol, resorcinol, p-coumaric acid, corilagin, ellagic acid, catechin, epicatechin, tannic acid, 4,6 hexahydroxydiphenoyl glucose, 3,6-hexahydroxy diphenoylglucose, 1-galloylglucose, and 3-galloylglucose. Considering all the potential beneficial effects of the major bioactive compounds present in the Jamun seeds, in the current investigation, the specific clinical effects and the mechanism of action for the major bioactive compounds along with the extraction procedures are discussed.

Neurodegenerative diseases, such as Alzheimer's disease or Parkinson's disease, significantly reduce the quality of life of patients and eventually result in complete maladjustment. Disruption of the synapses leads to a deterioration in the communication of nerve cells and decreased plasticity, which is associated with a loss of cognitive functions and neurodegeneration. Maintaining proper synaptic activity depends on the qualitative composition of mitochondria, because synaptic processes require sufficient energy supply and fine calcium regulation. The maintenance of the qualitative composition of mitochondria occurs due to mitophagy. The regulation of mitophagy is usually based on several internal mechanisms, as well as on signals and substances coming from outside the cell. These substances may directly or indirectly enhance or weaken mitophagy. In this review, we have considered the role of some compounds in process of mitophagy and neurodegeneration. Some of them have a beneficial effect on the functions of mitochondria and enhance mitophagy, showing promise as novel drugs for the treatment of neurodegenerative pathologies, while others contribute to a decrease in mitophagy.

The inclusion of beans in the diet has been recommended for obesity control. However, its beneficial effect varies depending on agroclimatic factors acting during plant development. The antiobesogenic capacity of Dalia bean (DB) seeds obtained by water restriction (WR) during the vegetative or reproductive stage of plant growth (50/100 and 100/50% of soil moisture in vegetative/reproductive stage, respectively), during the whole cycle (50/50), and well-watered plants (100/100) was researched. After phytochemical characterization, harvested beans from each experimental unit were pooled among treatments, based on a multivariate canonical discriminant analysis considering concentration of non-digestible carbohydrates (total, soluble and insoluble dietary fiber and resistant starch), phenolic compounds (total phenols, flavonoids, anthocyanins and condensed tannins) and total saponins, which showed no differences among replicas of each treatment. Obesity was induced in rats (UAZ-2015-36851) with a high fat diet (HFD) for four months. Afterwards, rats were fed with the HFD supplemented with 20% of cooked DB for three months. During treatment, 100/50 beans, improved blood triglycerides, cholesterol, and glucose, and alleviated early insulin resistance (IR) related to inhibition of lipase, α-amylase and -glucosidase activity. After sacrifice, a hypolipidemic capacity and atherogenic risk reduction was observed, especially from the 100/50 treatment, suggesting that intake of DB obtained from WR may prevent IR and dyslipidemia.

Food bioactive compounds (FBC) comprise a vast class of substances, including polyphenols, with different chemical structures, and they exert physiological effects on individuals who consume them, such as antioxidant and anti-inflammatory action. The primary food sources of the compounds are fruits, vegetables, wines, teas, seasonings, and spices, and there are still no daily recommendations for their intake. Depending on the intensity and volume, physical exercise can stimulate oxidative stress and muscle inflammation to generate muscle recovery. However, little is known about the role that polyphenols may have in the process of injury, inflammation, and muscle regeneration. This review aimed to relate the effects of supplementation with mentation with some polyphenols in oxidative stress and post-exercise inflammatory markers. The consulted papers suggest that supplementation with 74 to 900 mg of cocoa, 250 to 1000 mg of green tea extract for around 4 weeks, and 90 mg for up to 5 days of curcumin can attenuate cell damage and inflammation of stress markers of oxidative stress during and after exercise. However, regarding anthocyanins, quercetins, and resveratrol, the results are conflicting. Based on these findings, the new reflection that was made is the possible impact of supplementation associating several FBCs simultaneously. Finally, the benefits discussed here do not consider the existing divergences in the literature. Some contradictions are inherent in the few studies carried out so far. Methodological limitations, such as supplementation time, doses used, forms of supplementation, different exercise protocols, and collection times, create barriers to knowledge consolidation and must be overcome.

Quercetin, a flavonol present in many vegetables and fruits, has been identified as a chemoprevention agent in several cancer models. However, the molecular mechanism of quercetin's anticancer activity is not entirely understood. MicroRNAs (miRNAs), small noncoding RNAs, have been reported to play key roles in various biological processes by regulating their target genes. We hypothesized that quercetin can exert an anticancer effect through the regulation of miRNAs. To test this hypothesis, we investigated the effects of quercetin on the expression of tumor-suppressive miRNAs in cervical cancer. Quercetin up-regulated the in vivo and in vitro expression of tumor-suppressive miRNAs miR-26b, miR-126, and miR-320a. Quercetin suppressed the level of β-catenin, encoded by catenin beta 1 (CTNNB1), by up-regulating miR-320a in HeLa cells. Moreover, quercetin increased the expression of mir-26b, mir-126, and mir-320a precursors in HeLa cells. The results from this study show that quercetin has the potential to prevent cervical cancer by regulating the expression of tumor-suppressive miRNAs.

Obesity represents the most frequent chronic disease among children worldwide, with a significant global burden on society. Metabolically unhealthy obesity (MUO) can affect children since their first years of life, and novel therapeutic strategies to tackle metabolic complications are under investigation. This review focuses on bioactive compounds and their possible beneficial effects on obesity, particularly omega-3, docosahexaenoic acid, vitamin D, biotics, polysaccharide macromolecules, polyphenols, inositols, alpha lipoic acid, and bromelaine. Our aim is to summarize current evidence about bioactive compounds in the treatment of obesity, highlighting recent findings on their use in children and adolescents. Most studied molecules are omega-3 and vitamin D, despite the heterogeneity between the studies. Moreover, given the emerging interest in the gut-brain axis in the link between metabolic health and microbiota, various studies on prebiotics, probiotics, synbiotics, postbiotics and polysaccharide macromolecules have been considered. Some preclinical studies seem to highlight a possible role of the polyphenols, even if their clinical evidence is still discussed. Lastly, we describe possible effects of inositols and alpha-lipoic acid. Despite some dietary supplements seem to be promising in overweight subjects, only in a few of them a dose/response efficacy has been found in the pediatric age. Innovative, well-designed and targeted clinical trials are then needed to prove the beneficial effects of these compounds that could support the standard behavioral therapy for obesity.

Chemotherapy has opened a new window in cancer therapy. However, the resistance of cancer cells has dramatically reduced the efficacy of chemotherapy. Cisplatin is a chemotherapeutic agent and its potential in cancer therapy has been restricted by resistance of cancer cells. As a consequence, the scientists have attempted to find new strategies in elevating chemotherapy efficacy. Due to great anti-tumour activity, naturally occurring compounds are of interest in polychemotherapy. Quercetin is a flavonoid with high anti-tumour activity against different cancers that can be used with cisplatin to enhance its efficacy and also are seen to sensitise cancer cells into chemotherapy. Furthermore, cisplatin has side effects such as nephrotoxicity and ototoxicity. Administration of quercetin is advantageous in reducing the adverse effects of cisplatin without compromising its anti-tumour activity. In this review, we investigate the dual role of quercetin in enhancing anti-tumour activity of cisplatin and simultaneous reduction in its adverse effects.

Natural products have offered a number of exciting approaches in cancer treatment over the years. In this study, we investigated the prophylactic and therapeutic effects of the polyphenol-enriched fraction extracted from Myrtus communis (PEMC) on acute and chronic leukemia. According to the UHPLC-MSⁿ, the fraction is rich in flavonoids. Protective activity of the PEMC was assessed by evaluating the antioxidant, anti-inflammatory, wound healing, and hemolysis potential in a series of in vivo and in vitro assays, while the therapeutic approach consisted of the evaluation of cytotoxic activity of the PEMC against HL60 and K562 leukemia cell lines. Safety of the fraction was also evaluated on a non-cancerous Vero cell line and by an acute toxicity test performed in mice. The PEMC demonstrated a significant anti-inflammatory and healing potential. The activities found at the dose of 100 mg/kg were better than those observed using a reference drug. The PEMC demonstrated a significant antioxidant effect and a specific cytotoxicity towards HL60 (IC₅₀ = 19.87 µM) and K562 (IC₅₀ = 29.64 µM) cell lines being non-toxic to the Vero cell line. No hemolytic activity was observed in vitro and no toxicity effect was found in mice. Thus, the PEMC has a pharmacological potential as both preventive and therapeutic agent. However, further research is necessary to propose its mechanism of action.

The importance of the circadian clock in maintaining human health is now widely acknowledged. Dysregulated and dampened clocks may be a common cause of age-related diseases and metabolic syndrome Thus, circadian clocks should be considered as therapeutic targets to mitigate disease symptoms. This review highlights a number of dietary compounds that positively affect the maintenance of the circadian clock. Notably the polymethoxyflavone nobiletin has shown some encouraging results in pre-clinical experiments. Although many more experiments are needed to fully elucidate its exact mechanism of action, it is a promising candidate with potential as a chronotherapeutic agent.

The simultaneous improvement of quercetin (QUE) processing stability and bioavailability has always presented a technical challenge during food processing. This study constructed a water-soluble carrier consisting of oleic acid (OA) and sodium caseinate (NaCas) in an ultrasonic field and investigated the effect of its encapsulation on improving the thermal stability and bioaccessibility of QUE. The results showed that the OA and NaCas generated uniform, stable water-soluble particles with a poly dispersity index (PDI) below 0.3 and an absolute value of Zeta potential above 30 mV in optimized conditions (a protein concentration of 4 mg/mL, ultrasonic power of 300 W, and ultrasonic time of 5 min). OA-NaCas mass ratio of 1:40, 1:15, 1:8, and 1:4 was selected for QUE loading to compare its encapsulation effect at different mass ratios. Compared with the NaCas without OA, the QUE embedding rate reached 95 % at OA-NaCas mass ratios of 1:15 and 1:8. In addition, the transmission electron microscopy (TEM) images confirmed that QUE was embedded in OA-NaCas particles, forming regular, spherical OA-NaCas-QUE particles at mass ratios or 1:15 and 1:8. Next, when heated at 80 °C for 120 min, the OA-NaCas (OA:NaCas, 1:15, 1:8, and W/W) particles significantly improved the QUE retention rate. The simulated in vitro gastrointestinal digestion experiments showed that the QUE bioaccessibility increased from 25 % to more than 60 % when it was encapsulated in OA-NaCas (OA:NaCas, 1:15, 1:8, and W/W) particles. These results indicated that the OA-NaCas complex was suitable as a hydrophilic delivery carrier of fat-soluble polyphenols.

Musa (ABB group) “Kluai Namwa” bananas (Musa sp.) are widely grown throughout Thailand. Mali Ong is the most popular Kluai Namwa variety used as raw material for sun-dried banana production, especially in the Bangkratum District, Phitsanulok, Thailand. The sun-dried banana product made from Nanwa Mali Ong is well recognized as the best dried banana product of the country, with optimal taste compared to one made from other Kluai Namwa varieties. However, the production of Mali Ong has fluctuated substantially in recent years, leading to shortages. Consequently, farmers have turned to using other Kluai Namwa varieties including Nuanchan. This study investigated the nutraceutical contents of two popular Namwa varieties, Mali Ong and Nuanchan, at different ripening stages. Nutraceuticals in the dried banana products made from these two Kluai Namwa varieties and four commercial dried banana products were compared. Results indicated that the content of moisture, total sugar, and total soluble solids (TSS) (°Brix) increased, while total solids and texture values decreased during the ripening stage for both Kluai Namwa varieties. Rutin was the major flavonoid found in both Namwa Mali Ong and Nuanchan varieties ranging 136.00−204.89 mg/kg and 129.15−260.38 mg/kg, respectively. Rutin, naringenin, quercetin and catechin were abundant in both Namwa varieties. All flavonoids increased with ripening except for rutin, gallocatechin and gallocatechin gallate. There were no significant differences (p < 0.05) in flavonoid contents between both varieties. Tannic acid, ellagic acid, gallic acid, chlorogenic acid and ferulic acid were the main phenolic acids found in Mali Ong and Nuanchan varieties, ranging from 274.61−339.56 mg/kg and 293.13−372.66 mg/kg, respectively. Phenolic contents of both varieties decreased, increased and then decreased again during the development stage. Dopamine contents increased from 79.26 to 111.77 mg/kg and 60.38 to 125.07 mg/kg for Mali Ong and Nuanchan, respectively, but the amounts were not significantly different (p < 0.5) between the two Namwa varieties at each ripening stage. Inulin as fructooligosaccharide (FOS) increased with ripening steps. Production stages of sun-dried banana products showed no statistically significant differences (p < 0.05) between the two Namwa varieties. Therefore, when one variety is scarce, the other could be used as a replacement in terms of total flavonoids, phenolic acid, dopamine and FOS. In both Namwa varieties, sugar contents decreased after the drying process. Sugar contents of the dried products were 48.47 and 47.21 g/100 g. The drying process caused a reduction in total flavonoid contents and phenolic acid at 63−66% and 64−70%, respectively. No significant differences (p < 0.05) were found for total flavonoid and phenolic contents between the dried banana products made from the two Namwa varieties (178.21 vs. 182.53 mg/kg and 96.06 vs. 102.19 mg/kg, respectively). Products made from Nuanchan varieties (24.52 mg/kg) contained significantly higher dopamine than that from Mali Ong (38.52 mg/kg). The data also suggest that the banana maturity stage for production of the sun dried products was also optimum in terms of high nutraceutical level.

This study was designed to screen the phytochemical composition and investigate the biological activities of Hedysarum candidissimum extracts and also support the results with molecular docking studies. LC/MS/MS analysis revealed the presence of 22 phytochemical constituents (mainly phenolic acids, flavonoids, and flavonoid glycosides) in the plant structure. The methanol extract exhibited the strongest antioxidant activity among all the extracts with its strong DPPH radical scavenging and iron reducing capacity, as well as high phenolic and flavonoid contents. Additionally, it was found to be the most promising acetylcholinesterase (AChE: IC₅₀ : 93.26 μg/mL) and α-glycosidase (AG: IC₅₀ : 28.57 μg/mL) inhibitory activities, supported by the major phenolics of the species through in silico studies. Ethyl acetate extract had the strongest cytotoxic effect on HT-29 (IC₅₀ : 63.03 μg/mL) and MDA-MB-453 (IC₅₀ : 95.36 μg/mL) cancer cell lines. Both extracts exhibited considerable apoptotic and anti-migrative effects on HT-29 cells. The investigations provide phyto-analytical and bio-pharmacological results which can be extended by in vivo studies in the future.

Quercetin is the most abundant polyphenolic flavonoid (flavonol subclass) in vegetal foods and medicinal plants. This dietary chemopreventive agent has drawn significant interest for its multiple beneficial health effects ("polypharmacology") largely associated with the well-documented antioxidant properties. However, controversies exist in the literature due to its dual anti-/pro-oxidant character, poor stability/bioavailability but multifaceted bioactivities, leaving much confusion as to its exact roles in vivo. Increasing evidence indicates that a prior oxidation of quercetin to generate an array of chemical diverse products with redox-active/electrophilic moieties is emerging as a new linkage to its versatile actions. The present review aims to provide a comprehensive overview of the oxidative conversion of quercetin by systematically analyzing the current quercetin-related knowledge, with a particular focus on the complete spectrum of metabolite products, the enzymes involved in the catabolism and the underlying molecular mechanisms. Herein we review and compare the oxidation pathways, protein structures and catalytic patterns of the related metalloenzymes (phenol oxidases, heme enzymes and specially quercetinases), aiming for a deeper mechanistic understanding of the unusual biotransformation behaviors of quercetin and its seemingly controversial biological functions.

Bambara groundnut (BGN) is an underexploited crop with a rich nutrient content and is used in traditional medicine, but limited information is available on the quantitative characterization of its flavonoids and phenolic acids. We investigated the phenolic profile of whole seeds and cotyledons of five BGN varieties consumed in South Africa using UPLC-qTOF-MS and GC-MS. Twenty-six phenolic compounds were detected/quantified in whole seeds and twenty-four in cotyledon, with six unidentified compounds. Flavonoids include flavan-3-ol (catechin, catechin hexoside-A, catechin hexoside-B), flavonol (quercetin, quercetin-3-O-glucoside, rutin, myricetin, kaempherol), hydroxybenzoic acid (4-Hydroxybenzoic, 2,6 Dimethoxybenzoic, protocatechuic, vanillic, syringic, syringaldehyde, gallic acids), hydroxycinnamic acid (trans-cinnamic, p-coumaric, caffeic, ferulic acids) and lignan (medioresinol). The predominant flavonoids were catechin/derivatives, with the highest content (78.56 mg/g) found in brown BGN. Trans-cinnamic and ferulic acids were dominant phenolic acid. Cotyledons of brown and brown-eyed BGN (317.71 and 378.59 µg/g) had the highest trans-cinnamic acid content, while red seeds had the highest ferulic acid (314.76 µg/g) content. Colored BGN had a significantly (p < 0.05) higher content of these components. Whole BGN contained significantly (p < 0.05) higher amount of flavonoids and phenolic acids, except for the trans-cinnamic acid. The rich flavonoid and phenolic acid content of BGN seeds highlights the fact that it is a good source of dietary phenolics with potential health-promoting properties.

Quercetin belongs to the broader category of polyphenols. It is found, in particular, among the flavonols, and along with kaempferol, myricetin and isorhamnetin, it is recognized as a foreign substance after ingestion in contrast to vitamins. Quercetin occurs mainly linked to sugars with the most common compounds being quercetin-3-O-glucoside or as an aglycone, especially in the plant population. The aim of this review is to present a recent bibliography on the mechanisms of quercetin absorption and metabolism, bioavailability, and antioxidant and the clinical effects in diabetes and cancer. The literature reports a positive effect of quercetin on oxidative stress, cancer, and the regulation of blood sugar levels. Moreover, research-administered drug dosages of up to 2000 mg per day showed mild to no symptoms of overdose. It should be noted that quercetin is no longer considered a carcinogenic substance. The daily intake of quercetin in the diet ranges 10 mg-500 mg, depending on the type of products consumed. This review highlights that quercetin is a valuable dietary antioxidant, although a specific daily recommended intake for this substance has not yet been determined and further studies are required to decide a beneficial concentration threshold.

Obesity is a metabolic disorder that has become critically prevalent throughout the world. Obesity has been linked to other chronic diseases such as diabetes mellitus, cardiovascular diseases and cancer. Natural products such as honey have been investigated for their potential effect on obesity. Hence, this study systematically reviewed the recent literature concerning the effects of honey on obesity in obese animal models and in people with obesity. The Ovid MEDLINE, PubMed, Scopus, Web of Science and Google Scholar electronic databases were searched for relevant articles. A total of 130 relevant articles were obtained from the initial search. Following a thorough screening, nine articles were selected for data extraction, including six animal studies and three clinical trials. In most of the animal studies, honey demonstrated an anti-obesity effect by reducing body weight, body fat composition and adipocyte size, among others. However, supplementation of honey in clinical trials showed conflicting results. Even though honey supplementation did not demonstrate any weight-reducing effect in some of the clinical trials, none of the trials showed that honey increases body weight. However, the results should be interpreted with caution as most of the studies involved animal models and there is a limited number of high quality, randomized, controlled clinical trials.

https://inplasy.com/inplasy-2022-6-0038/ PROSPERO, identifier 10.37766/inplasy2022.6.0038.