Nitric oxide-donating derivatives of hederacolchiside A1: Synthesis and biological evaluation in vitro and in vivo as potential anticancer agents |
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Authors: | Yuanying Fang Rikang Wang Mingzhen He Hesong Huang Qi Wang Zunhua Yang Yan Li Shilin Yang Yi Jin |
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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 |
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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%). |
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Keywords: | Nitric oxide Furoxan Triterpenoid saponin Anticancer activity |
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