摘要
Podophyllotoxone(1) was isolated from the roots of Dysosma versipellis. The structure was determined by spectroscopic analysis in combination with single-crystal X-ray analysis. The absolute configuration of compound 1 was assigned based on the Flack parameter. It showed significant inhibitory activities against human prostate cancer cells PC3 and DU145 with IC50 values being 14.7 and 20.6 μmol·L-1, respectively. It also arrested the cells at G2/M phase. Tubulin polymerization assay showed that it inhibited the tubulin polymerization in a dose-dependent manner, and molecular docking analysis revealed a different binding mode with tubulin as compared with those known tubulin inhibitors.
Podophyllotoxone （1） was isolated from the roots of Dysosma versipellis. The structure was determined by spectro- scopic analysis in combination with single-crystal X-ray analysis. The absolute configuration of compound 1 was assigned based on the Flack parameter. It showed significant inhibitory activities against human prostate cancer cells PC3 and DU145 with IC50 values being 14.7 and 20.6 μmol.L^-1, respectively. It also arrested the cells at G2/M phase. Tubulin polymerization assay showed that it inhib- ited the tubulin polymerization in a dose-dependent manner, and molecular docking analysis revealed a different binding mode with tubulin as compared with those known tubulin inhibitors.
基金
supported by the Fund of Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization(Nos.FPRU2013-4,and ZRJJ2013-4)
the National Natural Science Foundation of China(No.21072078)
the Fundamental Research Funds for the Central Universities(No.11609202)
the Guangdong High Level Talent Scheme to R.W.J
