DU145型
穿心莲内酯
化学
细胞凋亡
癌症
癌细胞
细胞周期
细胞周期检查点
体外
细胞培养
细胞生长
流式细胞术
IC50型
癌症研究
药理学
生物化学
分子生物学
生物
内科学
LNCaP公司
医学
遗传学
作者
Yaping Song,Zhengyuan Xin,Yumeng Wan,Jiabin Li,Boping Ye,Xiang Xue
标识
DOI:10.1016/j.ejmech.2014.12.017
摘要
A series of novel indolo[3,2-b]andrographolide derivatives were designed, synthesized and screened in vitro against three human cancer cell lines MCF7 (human breast cancer), HCT116 (human colon cancer), and DU145 (human prostate cancer). Fourteen compounds 6b, 6e, 6i, 6j, 6l, 6m, 6n, 12a, 12b, 13a, 13b, 15a, 17a, and 17b exhibited better anti-cancer activities than andrographolide for all three human cancer lines, with compound 6l displaying best activity with IC50 values of 1.85, 1.22 and 1.24 μM against MCF7, HCT116 and DU145 respectively. Preliminary anti-cancer mechanistic investigation was performed in terms of the cell cycle arrest and cell apoptosis assays of compound 6l against HCT116 using flow cytometry, and the results suggested that compound 6l inhibited tumor proliferation through inducing early and late cellular apoptosis in a concentration-dependent manner and causing cell cycle arrest in the S-phase.
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