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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.

Abstract

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.

摘要

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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