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Molecules 2011, 16(8), 6243-6254; doi:10.3390/molecules16086243
Article

Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein

1,†
,
2,†
 and
1,*
1 Department of Rheumatology, The Second Hospital Affiliated Harbin Medical University, Harbin 150086, China 2 Hei longjiang Disabled Federation for Human Care Clinic, Harbin 150020, China These two authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 28 June 2011 / Revised: 15 July 2011 / Accepted: 18 July 2011 / Published: 25 July 2011
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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.
Keywords: chamaejasmine; anti-cancer activity; PC-3 cells; tubulin; docking chamaejasmine; anti-cancer activity; PC-3 cells; tubulin; docking
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Fang, W.; Liu, S.; Nie, Y. Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein. Molecules 2011, 16, 6243-6254.

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