Zhao Chunhui, Zhao Peizhe, Feng Bin, Hou Xiyan, Zhao Longxuan
School of Life Sciences, Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery, Liaoning Normal University.
Chem Pharm Bull (Tokyo). 2017 Mar 1;65(3):276-283. doi: 10.1248/cpb.c16-00836. Epub 2017 Jan 13.
A series of deoxycholic acid (DCA) derivatives bearing amino acid moiety has been synthesized and investigated for their potential antiproliferative activities. DCA derivative compounds were synthesized by a two or three step synthetic approach. Their bioactivities were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and Western blotting analysis on three tumor cell lines A549 (human lung cancer cell line), MCF-7 (human breast cancer cell line) and HeLa (human cervical carcinoma cell). The novel derivatives DCA3d, DCA5a, DCA5b, DCA5c, and DCA5d were found to be promising antiproliferative agents. Furthermore, DCA5b showed the greatest cytotoxic activity by induction of apoptosis. These compounds show potentiality for further optimization as antitumor drugs.
一系列带有氨基酸部分的脱氧胆酸（DCA）衍生物已被合成，并对其潜在的抗增殖活性进行了研究。DCA衍生物化合物通过两步或三步合成方法制备。使用3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐（MTT）法和蛋白质免疫印迹分析，在三种肿瘤细胞系A549（人肺癌细胞系）、MCF-7（人乳腺癌细胞系）和HeLa（人宫颈癌细胞）上评估了它们的生物活性。发现新型衍生物DCA3d、DCA5a、DCA5b、DCA5c和DCA5d是有前景的抗增殖剂。此外，DCA5b通过诱导凋亡表现出最大的细胞毒性活性。这些化合物显示出作为抗肿瘤药物进一步优化的潜力。
