PHLOROGLUCINOL DERIVATIVES AS POTENTIAL ANTIULCER COMPOUND THAT INHIBITS MATRIX METALLOPROTEINASE-9
Journal Title: International Journal of Pharmaceutical Applications - Year 2011, Vol 2, Issue 4
Abstract
Three phloroglucinol based polyphenolic compounds have been synthesized and their potential efficacy against gastric ulceration in mice was investigated. Polyphenol (I, II, III) were synthesized through Vilsmeier-Haack formylation, Schiff-base condensation of diformyl- phloroglucinol with 4-amino salicylic acid and Duff formylation reactions respectively. We administered indomethacin, a non-steroidal anti inflammatory drug (NSAID), to induce gastric ulceration in Balb/c mice and tested antiulcer efficacy of synthesized phloroglucinol derivatives. The pathogenesis of NSAID-induced ulceration is known to be associated to upregulation of matrix metalloproteinase (MMP)-9. All derivatives of phloroglucinol were found to prevent gastric ulceration in mice through depletion of oxidative stress in gastric tissue. Phloroglucinol derivatives also possessed antioxidant activity and they suppressed antioxidant enzymes in gastric tissues to almost normalcy during gastroprotection. Compound III was found to be most efficient anti-ulcer agent among others that inhibited the MMP-9 activity near to control value during prevention of NSAID-induced gastric ulceration. Thus, new polyphenolic compounds derived from phloroglucinol have antioxidant as well as anti-ulcer activity. We conclude that phloroglucinol derivatives as potent antiulcer compound in prevention of indomethacin induced gastric ulceration via attenuation of MMP-9 activity.
Authors and Affiliations
Susri Ray Chaudhuri(Guha) , Arindam Modak , Asim Bhaumik , Snehasikta Swarnakar
Keywords
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