Vanillin analog - vanillyl mandelic acid, a novel specific inhibitor of snake venom 5'-nucleotidase

Arun, R. and Arafat, A. S. S. Y. and D'Souza, C. J. M. and Sivaramakrishnan, V. and Dhananjaya, B. L. (2014) Vanillin analog - vanillyl mandelic acid, a novel specific inhibitor of snake venom 5'-nucleotidase. Archiv der Pharmazie, 347 (9). pp. 616-623. ISSN 1521-4184

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Snake venom 5�-nucleotidase (5�NUC) plays a very important role in envenomation strategies; however, apart from its modulation of hemostatic functions, its other pharmacological effects are not yet well characterized. Several studies have used specific inhibitors of enzyme toxins as a biochemical or pharmacological tool to characterize or establish its mechanism of action. We report here for the first time vanillin mandelic acid (VMA), an analog of vanillin, to potentially, selectively, and specifically inhibit venom 5�NUC activity among other enzymes present in venoms. VMA is much more potent in inhibiting 5�NUC activity than vanillyl acid (VA). The experimental results obtained are in good agreement with the in silico molecular docking interaction data. Both VA and VMA are competitive inhibitors as evident by the inhibition-relieving effect upon increasing the substrate concentration. VMA also dose-dependently inhibited the anticoagulant effect in Naja naja venom. In this study, we report novel non-nucleoside specific inhibitors of snake venom 5�NUC and experimentally demonstrate their involvement in the anticoagulant activity of N. naja venom. Hence, we hypothesize that VMA can be used as a molecular tool to evaluate the role of 5�NUC in snake envenomation and to develop prototypes and lead compounds with potential therapeutic applications against snake bites.

Item Type: Article
Uncontrolled Keywords: Anticoagulant, 5�-Nucleotidase, Purines, Snake venoms, Vanillyl mandelic acid
Subjects: C Chemical Science > Biochemistry
Divisions: Department of > Biochemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 05 Sep 2019 10:11
Last Modified: 05 Sep 2019 10:11

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