Conference Proceeding

Genotoxicity and Anticancer Drug Discovery of Phenolic Leads from Indian Traditional Plants: A Laboraotrory Based High Throughput Screening Targeting Human Isomerism Topo I & II

Dr. Vedpal Parihar

The American Cancer Society’s estimate for that the cervical cancer in the United States for 2016 is about 12,990 new cases. Cervical cancer is one of the most common causes of death for American women (Atlanta GA et al. 2016). Hence the current research is focus on the discovery of human topo poisons I& II targeting the cervical cancer. Methods: A collaborative research programme was initiated in 2014 at JSS College of pharmacy, Ooty, India and Department of Plant and soil Sciences, University of Pretoria, South Africa, a total number of 16 traditional plants was selected for the current research after a through ethnomedicinal survey with traditional practitioners. Based on the cytotoxic values five plants was selected (Curculigo orchioides (Amaryllidaceae), Trichosanthes palmate (Cucurbitaceace), Centella asiatica (Apiaceae), Woodfordia fruticosa (Lythraceae) and Myristica fragrans (Myristicaceae). A total of five phenolics were discovered from curculigo orchiodes (Amaryllidaceae), using high throughput technique like Flash Chromatography technique. All this compounds were subjected to In vitro cytotoxic studies using MTT assay against HeLa Cell lines. As compared to standard quercetin the isolated molecules have been docked in to the crystalline targets into the crystal structre of topoisomerase I (1K4T ) topoisomerase II (1ZXN ) and the docking results proved that the isolated phenolics was a good dual Topo Poison in compare to standard quercetin. Result and Discussion: In-silico tools like Schrödinger suite, 2014-3. Out of total 16 traditional medicinal plants five plants extracts (Curculigo orchioides (Amaryllidaceae), Trichosanthes palmate (Cucurbitaceace), Centella asiatica (Apiaceae), Woodfordia fruticosa (Lythraceae) and Myristica fragrans (Myristicaceae) showing high cytotoxicity on HeLa cell lines were selected for in-depth research. Using flash chromatography, a total no of 05 secondary metabolites were separated and identified from (Curculigo orchioides (Amaryllidaceae), namely C1-(1Propanone, 1 (2-furanyl)). C2 (9, 12 Octadecadienoic acid (z, z) -, methyl ester.F1 (3-Methly-2-furoic acid). F2 (Phthalic acid, di (6methylhept2yl) ester]-and S1 (2-Hexanol, 2-methyl-). All the isolated molecules have been docked in to the crystalline targets into the crystal structre of topoisomerase I (1K4T ) and topoisomerase II (1ZXN ) and the docking results proved that the isolated phenolics were good dual topo poisons in compare to standard Quercetin and Camptothecin. The Topoisomerae assays proved that these novel compounds are acting as good human Topopoisons I & II at 200 and (<100 μg/ml). Hence the current research given a platform for the discovery of novel topo poison leads and further in depth molecular studies were in progress.

Published: 08 November 2017

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Copyright: © 2017 Dr. Vedpal Parihar. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.