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Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein

By Yingkun Nie, Wenlong Fang and Songtao Liu

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 IC50 values of 2.28 and 3.98 µM, respectively. Furthermore, Western blot analysis showed that chamaejasmine was able to increase the expression of β-tubulin, but not α-tubulin. In silico simulations indicated that chamaejasmine specifically interacts with the active site which is located at the top of β-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 (Einter) was calculated to be −164.77 kcal·mol−1. Results presented here suggest that chamaejasmine possesses anti-cancer properties relating to β-tubulin depolymerization inhibition, and therefore is a potential source of anticancer leads for the pharmaceutical industry

Topics: chamaejasmine, anti-cancer activity, PC-3 cells, tubulin, docking, LCC:Organic chemistry, LCC:QD241-441, LCC:Chemistry, LCC:QD1-999, LCC:Science, LCC:Q, DOAJ:Organic Chemistry, DOAJ:Chemistry
Publisher: Molecular Diversity Preservation International
Year: 2011
DOI identifier: 10.3390/molecules16086243
OAI identifier: oai:doaj.org/article:187ddb06567943db8120628ae84f38ae
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