粉防己碱
细胞凋亡
癌细胞
细胞培养
白血病
细胞生长
细胞毒性
化学
细胞周期检查点
癌症
氨基酸
生物化学
细胞周期
体外
药理学
生物
免疫学
遗传学
作者
Shengcao Hu,Jin Yang,Chao Chen,Jiahui Song,Weidong Pan
出处
期刊:Molecules
[MDPI AG]
日期:2020-04-09
卷期号:25 (7): 1738-1738
被引量:5
标识
DOI:10.3390/molecules25071738
摘要
Tetrandrine, a dibenzyltetrahydroisoquinoline alkaloid isolated from the root of the traditional Chinese medicinal plant Stephania tetrandra S. Moore, a member of the Menispermaceae, showed anti-cancer activity by inhibiting cell proliferation, preventing cell cycle progress and induction of cell death and autophagy. In this study, twelve tetrandrine-l-amino acid derivatives and twelve tetrandrine-14-l-amino acid-urea derivatives were designed and synthesized, using C14-aminotetrandrine as raw material. Then the preliminary in vitro anti-cancer activities of these derivatives against human breast cancer cell line MDA-MB-231, human leukemia cell lines HEL and K562 were evaluated. The in vitro cytotoxicity results showed that these derivatives exhibited potent inhibitory effects on cancer cell growth, and the primary structure-activity relationships were evaluated. Notably, compound 3f exhibited satisfactory anticancer activity against all three cancer cell lines, especially the HEL cell line, with the IC50 value of 0.23 µM. Further research showed that 3f could induce G1/S cycle arrest and apoptosis in a dose- and time- dependent manner on the leukemia cell line HEL. The results suggested that 3f may be used as a potential anti-cancer agent for human leukemia.
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