Jingjing Wang, Zhuang Yang, Jiaolin Wen, Feng Ma, Fang Wang, Kun Yu, Minghai Tang, Wenshuang Wu, Yinfeng Dong, Xia Cheng, Chunlai Nie, Lijuan Chen
SKLB-M8, a derivative of millepachine, showed significant anti-proliferative effects in melanoma cell lines. In this study, we investigated the anti-melanoma and anti-angiogenic activity of SKLB-M8 on three melanoma cell lines (A2058, CHL-1, and B16F10) and human umbilical vein endothelial cells (HUVECs). In vitro, SKLB-M8 showed anti-proliferative activity with IC50 values of 0.07, 0.25, and 0.88 μM in A2058, CHL-1, and B16F10 cell lines, respectively. Flow cytometory analysis showed that SKLB-M8 induced G2/M arrest in three melanoma cell lines, and western blotting demonstrated that SKLB-M8 down-regulated the expression of cdc2, up-regulated p53 in A2058 and CHL-1 cells, and triggered cell apoptosis through down-regulating AKT and phosphorylated mTOR (p-mTOR)...
2014: Journal of Pharmacological Sciences