来自隔山消的具有细胞毒活性的C21甾体苷类化合物。
C21 steroidal glycosides with cytotoxic activities from Cynanchum otophyllum.
作者信息
Dong Jinrun, Peng Xingrong, Li Lei, Lu Shuangyang, Zhou Lin, Qiu Minghua
机构信息
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, China; University of the Chinese Academy of Sciences, Beijing, China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
出版信息
Bioorg Med Chem Lett. 2018 May 15;28(9):1520-1524. doi: 10.1016/j.bmcl.2018.03.078. Epub 2018 Mar 29.
Eight new C21 steroidal glycosides, namely cynanotins A-H (1-8), together with fifteen known analogues, were isolated from the roots of Cynanchum otophyllum. Their structures were elucidated by spectroscopic analysis and chemical methods. In this study, all of isolates were tested for their vitro inhibitory activities against five human tumor cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480). Compounds 3-15 showed moderate cytotoxic activities against HL-60 cell lines with IC values ranging from 11.4 to 37.9 µM. Compounds 5, 9, and 10 showed marked or moderate cytotoxic activities against five human tumor cell lines with IC values ranging from 11.4 to 36.7 µM. Compound 11 displayed moderate cytotoxic activities against HL-60, SMMC-7721, MCF-7 and SW480 cell lines with IC values of 12.2-30.8 µM. Compared to the positive control (IC: 35.0 µM), compounds 5, 9-11 exhibited more potential inhibitory activity against MCF-7 cells (IC: 16.1-25.6 µM).
从耳叶牛皮消的根部分离得到8个新的C21甾体糖苷，即蓝耳草苷A - H（1 - 8），以及15个已知类似物。通过光谱分析和化学方法阐明了它们的结构。在本研究中，对所有分离物进行了体外对5种人类肿瘤细胞系（HL - 60、SMMC - 7721、A - 549、MCF - 7和SW480）的抑制活性测试。化合物3 - 15对HL - 60细胞系表现出中等细胞毒活性，IC值范围为11.4至37.9 μM。化合物5、9和10对5种人类肿瘤细胞系表现出显著或中等细胞毒活性，IC值范围为11.4至36.7 μM。化合物11对HL - 60、SMMC - 7721、MCF - 7和SW480细胞系表现出中等细胞毒活性，IC值为12.2 - 30.8 μM。与阳性对照（IC：35.0 μM）相比，化合物5、9 - 11对MCF - 7细胞表现出更强的潜在抑制活性（IC：16.1 - 25.6 μM）。
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