Anticancer activity of chamaejasmine: effect on tubulin protein.

ABSTRACT: 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?? values of 2.28 and 3.98 µM, respectively. Furthermore, Western blot analysis showed that chamaejasmine was able to increase the expression of ?-tubulin, but not ?-tubulin. In silico simulations indicated that chamaejasmine specifically interacts with the active site which is located at the top of ?-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 ?-tubulin depolymerization inhibition, and therefore is a potential source of anticancer leads for the pharmaceutical industry.

SUBMITTER: Fang W 

PROVIDER: S-EPMC6264762 | biostudies-literature | 2011 Jul

REPOSITORIES: biostudies-literature