Journal
CHEMICO-BIOLOGICAL INTERACTIONS
Volume 224, Issue -, Pages 100-107Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.cbi.2014.09.022
Keywords
Podophyllum hexandrum; Cytotoxicity; Chk2; G2/M arrest; Breast cancer
Funding
- Council of Scientific and Industrial Research, Govt. of India
- CSIR [P-81101]
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We investigated the root of Podophyllum hexandrum as a potential source of lead bioactive metabolites with anticancer activity. The present study led to the isolation of six known aryltetralin-type lignans designated as 4'-demethyl-deoxypodophyllotoxin (1), podophyllotoxin (2), 4'-demethyl-podophyllotoxin (3), podophyllotoxin-4-O-beta-D-glucopyranoside (4), 4'-demethyl-deoxypodophyllotoxin-4-O-beta-D-glucopyranoside (5), 4'-demethyl-podophyllotoxin-4-O-beta-D-glucopyranoside (6), along with three known flavones Kaempferol (7), Quercetin (8), Astragalin (9) from the root of P. hexandrum. Compounds (1-9) exhibited the remarkable cytotoxic potential in diverse cancer cell lines. 5 therapeutic potential was extensively studied first time which exhibiting antiproliferative and ROS generating activity than its non-glycoside analogue 1. Furthermore, 5 augmented the apoptotic cascades in MCF-7 breast cancer cells, viz, nuclear condensation, membrane blebbing, probably by destabilizing the micro-tubular protein tubulin. Strikingly, our docking study and in vitro assays demonstrate that 5 binds to and modulate checkpoint kinase-2, a key cell cycle regulatory protein in normal and cancer cells. (C) 2014 Elsevier Ireland Ltd. All rights reserved.
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