Bi Chong-Wen, Zhang Cai-Xia, Li Yang-Biao, Zhao Wu-Li, Shao Rong-Guang, Mei Lin, Song Dan-Qing
Yao Xue Xue Bao. 2013 Dec;48(12):1800-6.
A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.
设计、合成了一系列环小檗碱衍生物，并对其体外抗癌活性进行了评估。在这些类似物中，化合物6c、6e和6g对人肝癌HepG2细胞表现出强烈的抑制作用。它们对多柔比星耐药的MCF-7乳腺癌细胞也有显著效果。初步机制表明，通过流式细胞术检测，用6g处理的HepG2细胞的细胞周期在G2/M期被阻断。在浓度为0.1 mg/mL时，它能显著抑制DNA拓扑异构酶I的活性。我们的结果为开发这类新型抗癌药物提供了依据。
