白薇根中C甾体的细胞毒性和诱导凋亡活性。
Cytotoxic and apoptosis-inducing activity of C steroids from the roots of Cynanchum atratum.
作者信息
Zhang Jian, Ma Lin, Wu Zheng-Feng, Yu Shu-Le, Wang Lei, Ye Wen-Cai, Zhang Qing-Wen, Yin Zhi-Qi
机构信息
Laboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, PR China; Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, PR China.
Laboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, PR China; Department of Natural Medicinal Chemistry & State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, PR China.
出版信息
Steroids. 2017 Jun;122:1-8. doi: 10.1016/j.steroids.2017.03.004. Epub 2017 Mar 19.
Two new (1-2) and two known C 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 IC values ranging from 10.19μM to 76.12μM. Compounds 1-3 also exhibited cytotoxic effects in A549 cells with IC 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.
从白薇的根部分离出两种新的（1 - 2）和两种已知的C甾体（3 - 4）。通过详细的一维和二维光谱对其结构进行了阐明。MTT分析表明，化合物1 - 4对HepG2细胞显示出明显的细胞毒活性，IC值范围为10.19μM至76.12μM。化合物1 - 3对A549细胞也表现出细胞毒作用，IC值为30.87 - 95.39μM。通过流式细胞术分析，化合物3在HepG2细胞中通过G0/G1细胞周期阻滞和促凋亡表现出抗增殖活性。蛋白质免疫印迹分析表明，化合物3可通过下调Bcl - 2表达、上调Bax蛋白表达以及激活caspase - 9和caspase - 3，经由线粒体途径诱导HepG2细胞凋亡。
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