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Cytotoxic Steroids from Sonchus arvensis
Chemistry of Natural Compounds ( IF 0.8 ) Pub Date : 2020-11-01 , DOI: 10.1007/s10600-020-03234-5
Zhengxiang Xia , Lihua Lu , Lin Li

A new steroid, 22Z,24R-5α,6α-epoxyergosta-8(14),22-(Z)-diene-3β,7α-diol (1), and seven known steroids were isolated from Sonchus arvensis L. The structures were elucidated by spectroscopic data. All these known compounds except compounds (6 and 7) were isolated from the title plant for the first time. All compounds were evaluated for cytotoxic activities. The results indicated that 1 and 8 showed moderate cytotoxic activity against two endometrial carcinoma cell lines (ECC-1 and Ishikawa) with IC50 values of 11.2 and 9.1 μM and 5.4 and 8.6 μM, respectively. The pharmacological mechanisms of action were explained via virtual docking of compounds to the main sites in the human estrogen receptor α crystal structure, and western blot analysis showed 8 had stronger inhibitory effects than 1 on the expression of ER α.

中文翻译:

来自山茱萸的细胞毒性类固醇

从 Sonchus arvensis L 中分离出一种新的类固醇 22Z,24R-5α,6α-epoxyergosta-8(14),22-(Z)-diene-3β,7α-diol (1) 和七种已知的类固醇。由光谱数据阐明。除化合物(6和7)外,所有这些已知化合物均为首次从标题植物中分离得到。评估所有化合物的细胞毒性活性。结果表明,1 和 8 对两种子宫内膜癌细胞系(ECC-1 和 Ishikawa)显示出中等的细胞毒活性,IC50 值分别为 11.2 和 9.1 μM 以及 5.4 和 8.6 μM。通过化合物与人雌激素受体α晶体结构中的主要位点的虚拟对接来解释其药理作用机制,蛋白质印迹分析显示8种对ERα表达的抑制作用强于1种。
更新日期:2020-11-01
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