College of TCM, Guangdong Pharmaceutical University, No. 280 Outside Loop East Road of Higher Education Mega Center, Panyu District, Guangzhou 510006, China.
College of Pharmacy, Harbin Medical University-Daqing, Daqing 163319, China.
Molecules. 2017 Nov 30;22(12):2101. doi: 10.3390/molecules22122101.
As a TCM, Willd. has been using to treat malignant tumors, and many studies also showed that the extracts from Willd. possessed evident antitumor activities. Therefore, we carried out chemical study on Willd. and investigated the cytotoxicity of the obtained compounds on a panel of eight tumor cell lines. As a result, four new compounds were isolated from Willd., including three iridoid glycosides of Shecaoiridoidside A-C (-) and a cerebroside of shecaocerenoside A (). Also, six known iridoid compounds (-) were also obtained. The cytotoxicity of all compounds against human tumor cell lines of HL-60, HeLa, HCT15, A459, HepG2, PC-3, CNE-2, and BCG-823 were also evaluated in vitro. New compound exhibited evident cytotoxicity to all tumor cell lines except the Hela, and the IC values are from 9.6 µM to 62.2 µM, while new compound showed moderate cytotoxicity to all the cell lines, and the IC values are from 33.6 µM to 89.3 µM. By contrast, new compound and known compound showed moderate cytotoxicity to HCT15, A459, and HepG2 selectively. Known compound also exhibited moderate cytotoxicity to HCT15 and A459 selectively.
作为一种中药，威灵仙已被用于治疗恶性肿瘤，许多研究也表明威灵仙的提取物具有明显的抗肿瘤活性。因此，我们对威灵仙进行了化学研究，并考察了所得到的化合物对一组八种肿瘤细胞系的细胞毒性。结果，从威灵仙中分离得到了四个新化合物，包括三个裂环烯醚萜糖苷（Shecaoiridoidside A-C）和一个神经酰胺（shecaocerenoside A）。此外，还得到了六个已知的裂环烯醚萜化合物。所有化合物对人肿瘤细胞系 HL-60、HeLa、HCT15、A459、HepG2、PC-3、CNE-2 和 BCG-823 的体外细胞毒性也进行了评估。新化合物 对除 HeLa 以外的所有肿瘤细胞系均表现出明显的细胞毒性，IC 值为 9.6 µM 至 62.2 µM，而新化合物 对所有细胞系均表现出中等细胞毒性，IC 值为 33.6 µM 至 89.3 µM。相比之下，新化合物 和已知化合物 对 HCT15、A459 和 HepG2 选择性地表现出中等细胞毒性。已知化合物 对 HCT15 和 A459 也表现出中等细胞毒性。
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