化学
赫拉
人血清白蛋白
白花丹
细胞毒性
癌细胞
细胞周期蛋白依赖激酶1
活性氧
体外
生物化学
细胞凋亡
立体化学
细胞周期
癌症
生物
医学
内科学
遗传学
作者
Yi Gou,Zhan Zhang,Jinxu Qi,Shichu Liang,Zuping Zhou,Feng Yang,Hong Liang
标识
DOI:10.1016/j.jinorgbio.2015.09.004
摘要
The folate (FA)-functionalized human serum albumin (HSA) carrier (FA-HSA) is promising for improving the target and efficiency of anticancer drugs. To develop FA-HSA carrier for metal anticancer drugs, we investigated anticancer properties and mechanism of FA-HSA carrier for Cu(II) complexes derived from plumbagin. The fluorescence spectroscopy and molecular docking revealed that Cu(II) complexes bind to IIA subdomain of HSA. Compared with Cu(II) complex alone, FA-HSA-metallodrug complex enhances cytotoxicity to FA-positive cancer cells (HeLa) but do not raise cytotoxicity levels in normal cells in vitro through selectively accumulating in cancer cells to some extent; FA-HSA-metallodrug complex has a stronger capacity for cell cycle arrest in the G2/M phase of HeLa cells, and down-regulating the expression of cyclin-dependent kinase 1 (CDK1) and cyclin B1. Moreover, FA-HSA-metallodrug complex promotes HeLa cells apoptosis through intrinsic reactive oxygen species (ROS) mediated mitochondrial pathway, accompanied by the regulation of Bcl-2 family proteins.
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