【摘 要】
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Podophyllotoxin(PPT)has cathartic,antiviral and antimitotic activity.1,2 As part of our ongoing efforts towards the development of new podophyllotoxin-based compounds with potent activities3,we synthe
【机 构】
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School of Pharmacy,Lanzhou University,Lanzhou 730000,P.R.China
【出 处】
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全国药物化学学术会议暨第四届中英药物化学学术会议
论文部分内容阅读
Podophyllotoxin(PPT)has cathartic,antiviral and antimitotic activity.1,2 As part of our ongoing efforts towards the development of new podophyllotoxin-based compounds with potent activities3,we synthesized and found the N-(1-oxyl-4′-demethyl-4-deoxypodophyllic)-D-methine amide(DPMA)(Scheme 1),exhibited anti-proliferative activity and induced apoptosis in A549 cells in a dose-and time-dependant manner.Furthermore,DPMA induced expression of Bax,cleaved caspase-3,p53 and ROS,and inhibited Bcl-2 expression(Fig.1).DPMA also affected cyclinB1,cdc2 and p-cdc2 expression,inducing cell cycle arrest(Fig.2).In addition,DPMA also inhibited tube formation of VEGF-induced human umbilical vein endothelial cells(Fig.2).These studies demonstrate that DPMA inhibits p53/cdc2/Bax signaling,thereby inhibiting cell growth/angiogenesis and inducing apoptosis.
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