新型抗癌甘草次酸和齐墩果酸的设计与合成
Design and Synthesis of New Anticancer Glycyrrhetinic Acids and Oleanolic Acids.
作者信息
Wang Rui, Zheng Qing-Xuan, Wang Wei, Feng Ling, Li Hui-Jing, Huai Qi-Yong
机构信息
Marine College, Shandong University.
Department of Biology and Chemistry, City University of Hong Kong.
出版信息
Biol Pharm Bull. 2017;40(5):703-710. doi: 10.1248/bpb.b17-00016.
A series of new glycyrrhetinic acids and oleanolic acids has been designed and synthesized based on the principles of combinatorial chemical synthesis. Their anticancer activities were further studied by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method with hepatocellular carcinoma (Hep-G2), breast cancer (MCF-7) cell lines and a normal hepatic cell (LO2). Cytotoxicity tests (in vitro) indicated that compound 6a showed the highest cytotoxicity with the lowest IC values of 23.34 µM on Hep-G2 cells, 12.23 µM on MCF-7 cells, and 44.47 µM on LO2, which would widen the structural diversity of these anticancer targets and confirm the perspectives of further investigations.
基于组合化学合成原理，设计并合成了一系列新的甘草次酸和齐墩果酸。采用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法，以肝癌（Hep-G2）、乳腺癌（MCF-7）细胞系和正常肝细胞（LO2）进一步研究了它们的抗癌活性。细胞毒性试验（体外）表明，化合物6a表现出最高的细胞毒性，对Hep-G2细胞的最低半数抑制浓度（IC）值为23.34 µM，对MCF-7细胞为12.23 µM，对LO2细胞为44.47 µM，这将拓宽这些抗癌靶点的结构多样性，并证实进一步研究的前景。
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