Tamarixetin 3‑O‑β‑D‑Glucopyranoside from Azadirachta indica Leaves: Gastroprotective Role through Inhibition of Matrix Metalloproteinase‑9 Activity in Mice

Yadav, Dharmendra K and Bharitkar, Yogesh P and Hazra, Abhijit and Pal, Uttam and Verma, Sugreev and Jana, Sayantan and Singh, Umesh Prasad and Maiti, Nakul Chandra and Mondal, Nirup B and Swarnakar, Snehasikta (2017) Tamarixetin 3‑O‑β‑D‑Glucopyranoside from Azadirachta indica Leaves: Gastroprotective Role through Inhibition of Matrix Metalloproteinase‑9 Activity in Mice. Journal of Natural Products, 80 (5). pp. 1347-1357.

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    Abstract

    Neem (Azadirachta indica) is a well-known medicinal and insecticidal plant. Although previous studies have reported the antiulcer activity of neem leaf extract, the lead compound is still unidentified. The present study reports tamarixetin 3-O-β-D-glucopyranoside (1) from a methanol extract of neem leaves and its gastroprotective activity in an animal model. Compound 1 showed significant protection against indomethacin-induced gastric ulceration in mice in a dose-dependent manner. Moreover, ex vivo and circular dichroism studies confirmed that 1 inhibited the enzyme matrix metalloproteinase-9 (MMP-9) activity with an IC50 value of ca. 50 μM. Molecular docking and dynamics showed the binding of 1 into the pocket of the active site of MMP-9, forming a coordination complex with the catalytic zinc, thus leading to inhibition of MMP-9 activity.

    Item Type: Article
    URI: http://www.eprints.iicb.res.in/id/eprint/2708
    Subjects: Cancer Biology and Inflammatory Disorder Division
    Chemistry
    Structural Biology & Bioinformatics
    Divisions: Indian Institute of Chemical Biology
    Depositing User: Ms Sutapa Ganguly
    Date Deposited: 03 Aug 2017 12:09
    Last Modified: 11 Oct 2017 17:03
    Official URL: http://dx.doi.org/10.1021/acs.jnatprod.6b00957
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