Sarkate A, Dhaneshwar SS. Investigation of mitigating effect of colon-specific prodrugs of boswellic acid on 2,4,6-trinitrobenzene sulfonic acid-induced colitis in Wistar rats: Design, kinetics and biological evaluation. World J Gastroenterol 2017; 23(7): 1147-1162 [PMID: 28275295 DOI: 10.3748/wjg.v23.i7.1147]
Corresponding Author of This Article
Suneela S Dhaneshwar, PhD, Professor, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth University, Erandwane, Pune, Maharashtra 411038, India. suneeladhaneshwar@rediffmail.com
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Chemistry, Medicinal
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Basic Study
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Sarkate A, Dhaneshwar SS. Investigation of mitigating effect of colon-specific prodrugs of boswellic acid on 2,4,6-trinitrobenzene sulfonic acid-induced colitis in Wistar rats: Design, kinetics and biological evaluation. World J Gastroenterol 2017; 23(7): 1147-1162 [PMID: 28275295 DOI: 10.3748/wjg.v23.i7.1147]
World J Gastroenterol. Feb 21, 2017; 23(7): 1147-1162 Published online Feb 21, 2017. doi: 10.3748/wjg.v23.i7.1147
Investigation of mitigating effect of colon-specific prodrugs of boswellic acid on 2,4,6-trinitrobenzene sulfonic acid-induced colitis in Wistar rats: Design, kinetics and biological evaluation
Ajinkya Sarkate, Suneela S Dhaneshwar
Ajinkya Sarkate, Suneela S Dhaneshwar, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth University, Maharashtra 411038, India
Author contributions: Sarkate A and Dhaneshwar SS substantially contributed to the conception and design of the study, acquisition, analysis and interpretation of data; both authors drafted the article and made critical revisions related to the intellectual content of the manuscript, and approved the final version of the article to be published.
Institutional review board statement: No human subjects were used in this study.
Institutional animal care and use committee statement: All animal experimentation was approved by the Institutional Animal Ethics Committee (IAEC-approval number: CPCSEA/PCH/10/2014-15) of Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune- 411038, India.
Conflict-of-interest statement: The authors declare no conflicts of interest.
Data sharing statement: There are no additional data available in relation to this manuscript.
Correspondence to: Suneela S Dhaneshwar, PhD, Professor, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth University, Erandwane, Pune, Maharashtra 411038, India. suneeladhaneshwar@rediffmail.com
Telephone: +91-20-25437237 Fax: +91-20-25439382
Received: October 14, 2016 Peer-review started: October 14, 2016 First decision: December 1, 2016 Revised: December 16, 2016 Accepted: January 4, 2017 Article in press: January 4, 2017 Published online: February 21, 2017 Processing time: 129 Days and 17.1 Hours
Core Tip
Core tip: Boswellic acids (BAs) are traditionally used in the treatment of inflammatory diseases and are effective in the treatment of inflammatory bowel disease (IBD) in particular, but they undergo extensive metabolism that results in low oral bioavailability. Colon-targeted delivery of BA was achieved by designing prodrugs that deliver BA site-specifically. The synthesized prodrugs were designed by semi-synthetic approach, wherein β-boswellic acid (BBA) was derivatized into a bioreversible delivery system by incorporation of amino acids as promoities for targeted delivery to inflamed colon in IBD. Prodrug of BBA with L-tryptophan (BT) was 1.7-times more effective than sulfasalazine (SLZ) in 2,4,6-trinitrobenzene sulfonic acid-induced colitis in Wistar rats. In vivo behavior of prodrug BT was very interesting and similar to SLZ, which is known to treat local inflammation in IBD as well as in rheumatoid arthritis (RA). The outcome of this study strongly suggests that these prodrugs might have dual applicability to IBD and chronotherapy of RA.
