Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein

Molecules

Wenlong Fang¹  Songtao Liu¹ 

[1] ¹Department of Rheumatology, The Second Hospital Affiliated Harbin Medical University, Harbin 150086, China ²Hei longjiang Disabled Federation for Human Care Clinic, Harbin 150020, China ^†These two authors contributed equally to this work.

关键词: chamaejasmine;    anti-cancer activity;    PC-3 cells;    tubulin;    docking;   

DOI  :  10.3390/molecules16086243

来源: mdpi

【 摘 要 】

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 (E_inter) 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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.