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Nitric oxide-donating derivatives of hederacolchiside A1: Synthesis and biological evaluation in vitro and in vivo as potential anticancer agents
Authors:Yuanying Fang  Rikang Wang  Mingzhen He  Hesong Huang  Qi Wang  Zunhua Yang  Yan Li  Shilin Yang  Yi Jin
Affiliation:1. National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China;2. College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, 818 Xingwan Road, Nanchang 330004, China
Abstract:A series of nitric oxide (NO) donating derivatives of hederacolchiside A1 bearing triterpenoid saponin motif were designed, synthesized and evaluated for their anticancer activity. All of the tested furoxan-based NO releasing compounds showed significant proliferation inhibitory activities. Especially compound 6a exhibited strong cytotoxicity (IC50 = 1.6–6.5 μM) against four human tumor cell lines (SMMC-7721, NCI-H460, U251, HCT-116) in vitro and the highest level of NO releasing. Furthermore, compound 6a was revealed low acute toxicity to mice and weak haemolytic activity with potent tumor growth inhibition against mice H22 hepatocellular cells in vivo (51.5%).
Keywords:Nitric oxide  Furoxan  Triterpenoid saponin  Anticancer activity
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