Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein

作者：Fang Wenlong; Liu Songtao; Nie Yingkun^*

来源：Molecules, 2011, 16(8): 6243-6254.

DOI：10.3390/molecules16086243

• chamaejasmine
• anti-cancer activity
• PC-3 cells
• tubulin
• docking

In this work, the anticancer activity of chamaejasmine was studied by evaluating its in vitro cytotoxicity against several human cancer cell lines (MCF-7, A549, SGC-7901, HCT-8, HO-4980, Hela, HepG2, PC-3, LNCap, Vero and MDCK) using the MTT assay. Results indicated chamaejasmine showed more notable anticancer activity than taxol against PC-3 cells, with IC(50) values of 2.28 and 3.98 mu M, respectively. Furthermore, Western blot analysis showed that chamaejasmine was able to increase the expression of beta-tubulin, but not alpha-tubulin. In silico simulations indicated that chamaejasmine specifically interacts with the active site which is located at the top of beta-tubulin, thanks to the presence of strong hydrophobic effects between the core templates and the hydrophobic surface of the TB active site. The binding energy (E(inter)) was calculated to be -164.77 kcal.mol(-1). Results presented here suggest that chamaejasmine possesses anti-cancer properties relating to beta-tubulin depolymerization inhibition, and therefore is a potential source of anticancer leads for the pharmaceutical industry.

• 出版日期2011-8
• 单位哈尔滨医科大学