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Cytotoxic and apoptosis-inducing activity of C21 steroids from the roots of Cynanchum atratum.

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机构: [1]Laboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, PR China [2]Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, PR China [3]Department of Natural Medicinal Chemistry & State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, PR China [4]Institute of Traditional Chinese Medicine and Natural Products & Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, Jinan University, Guangzhou, PR China [5]Institute of Chinese Medical Sciences (ICMS), University of Macau, PR China
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关键词: Cynanchum atratum C21 steroids Cytotoxic activity Apoptosis Mitochondrial pathway

摘要:
Two new (1-2) and two known C21 steroids (3-4) were isolated from the roots of Cynanchum atratum. Their structures were elucidated by detailed 1D and 2D spectroscopic. The MTT assay showed that compounds 1-4 displayed obvious cytotoxic activities against HepG2 cells with IC50 values ranging from 10.19μM to 76.12μM. Compounds 1-3 also exhibited cytotoxic effects in A549 cells with IC50 values of 30.87-95.39μM. Compound 3 showed the antiproliferative activity via G0/G1 cell cycle arrest and proapoptosis in HepG2 cells by Flowcytometry analysis. Western blotting analysis revealed that compound 3 could induce HepG2 cell apoptosis via the mitochondrial pathway by downregulating Bcl-2 expression, upregulating Bax protein expression, and activating caspase-9 and caspase-3. Copyright © 2017 Elsevier Inc. All rights reserved.

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出版当年[2016]版:
大类 | 3 区 医学
小类 | 4 区 生化与分子生物学 4 区 内分泌学与代谢
最新[2025]版:
大类 | 4 区 医学
小类 | 4 区 生化与分子生物学 4 区 内分泌学与代谢
第一作者:
第一作者机构: [1]Laboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, PR China [2]Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, PR China
通讯作者:
通讯机构: [3]Department of Natural Medicinal Chemistry & State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, PR China [*1]Department of Natural Medicinal Chemistry & State Key Laboratory of Natural Medicines, China Pharmaceutical University, No. 24, Tongjiaxiang, Gulou District, Nanjing 210009, Jiangsu Province, China.
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