任杰副教授在Cell Biology International杂志上发表相关科研论文

发布时间:2014-04-16浏览次数:513

DMPPQA, a novel angiogenesis inhibitor, induces apoptosis in humancolon cancer HCT-116 cells and HUVECs

Jie Ren, Hefei Jiang, Juan Zhao, WenqunXin, YuanyuanXu, Xin Chen and Kun Hu*

Cell Biology International2014, 38(3), 343-54.

 

A series of new 4β-(1,3,4-oxadiazole-2-amino)-podophyllotoxin derivatives were designed and synthesized. Their cytotoxicity in vitro against six tumor cell lines (DU-145, SGC-7901, A549, SH-SY5Y, HepG2 and Hela) were evaluated by standard MTT assay. The pharmacological results showed that most of the newly synthesized podophyllotoxin derivatives displayed potent cytotoxicity against at least one of the tested tumor cells; and among the new derivatives, 11b was more potent than podophyllotoxin against HepG2 and Hela cell lines. Furthermore, 11b exhibited much better selectivity toward the normal cell lines L929 and Vero than etoposide, 5-Fu and podophyllotoxin. The possible antitumor mechanism of 11b is to inhibit the activity of DNA topoisomerase II, result in the S-phase arrest, and then cause apoptotic cell death.