Guangxi Key Laboratory of Natural Polymer Chemistry and Physics, Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, School of Chemistry and Material, Nanning Normal University, Nanning 530001, PR China.
Guangxi Key Laboratory of Natural Polymer Chemistry and Physics, Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, School of Chemistry and Material, Nanning Normal University, Nanning 530001, PR China.
Steroids. 2021 May;169:108822. doi: 10.1016/j.steroids.2021.108822. Epub 2021 Mar 12.
In this work, a series of Biotin-substituted B-nor-cholesteryl benzimidazole compounds were synthesized. The antiproliferativeactivities of these compounds were evaluated in vitro using a series of human cancer cell lines, including HeLa (cervical cancer), SKOV3 (ovarian cancer), T-47D (thymus gland cancer), MCF-7 (human breast cancer) and HEK293T (normal renal epithelial) cells. These compounds displayed distinct antiproliferative activities against the currently tested cancer cells. The apoptotic properties induced by compound 6d were further investigated. Our results showed that compound 6d could induce the apoptosis of SKOV3 cells, blocking the cell growth in S-phase. Western blotting analyses revealed that compound 6d can induce cell apoptosis via the mitochondria-dependent pathway.
在这项工作中，合成了一系列生物素取代的 B-降胆甾基苯并咪唑化合物。这些化合物的抗增殖活性通过一系列人癌细胞系进行了体外评估，包括 HeLa（宫颈癌）、SKOV3（卵巢癌）、T-47D（胸腺腺癌）、MCF-7（人乳腺癌）和 HEK293T（正常肾上皮）细胞。这些化合物对目前测试的癌细胞表现出明显的抗增殖活性。进一步研究了化合物 6d 诱导的凋亡特性。我们的结果表明，化合物 6d 可以诱导 SKOV3 细胞凋亡，阻止细胞在 S 期生长。Western blot 分析显示，化合物 6d 可以通过线粒体依赖性途径诱导细胞凋亡。
