Department of Rheumatology, The Second Hospital Affiliated Harbin Medical University, Harbin 150086, China.
Molecules. 2011 Jul 25;16(8):6243-54. doi: 10.3390/molecules16086243.
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.
在这项工作中，通过评估 chamaejasmine 对几种人癌细胞系（MCF-7、A549、SGC-7901、HCT-8、HO-4980、Hela、HepG2、PC-3、LNCap、Vero 和 MDCK）的体外细胞毒性，研究了 chamaejasmine 的抗癌活性，使用 MTT 法进行评估。结果表明，chamaejasmine 对 PC-3 细胞的抗癌活性比紫杉醇更显著，IC₅₀ 值分别为 2.28 和 3.98 μM。此外，Western blot 分析表明，chamaejasmine 能够增加 β-微管蛋白的表达，但不能增加 α-微管蛋白的表达。计算结果表明，chamaejasmine 与位于 β-微管蛋白顶部的活性位点特异性相互作用，这得益于核心模板与 TB 活性位点的疏水表面之间存在强烈的疏水相互作用。结合能（E(inter)）计算为-164.77 kcal·mol⁻¹。结果表明，chamaejasmine 具有与β-微管蛋白解聚抑制相关的抗癌特性，因此是制药行业潜在的抗癌先导化合物来源。
