目的探讨替莫唑胺酯在体外抑制脑胶质瘤LN229细胞生长并诱导凋亡的作用及可能的机制,同时检测替莫唑胺酯是否能够克服替莫唑胺耐药。方法用四甲基偶氮唑蓝比色法比较相同浓度梯度(62.5,125,250,500,1000μmol·L-1)的替莫唑胺和替莫唑胺酯对LN229细胞增殖的影响。用流式细胞仪检测细胞凋亡率及细胞周期。用Western blot法检测替莫唑胺和替莫唑胺酯对凋亡蛋白Bax和Bcl-2的影响。构建过表达MGMT耐药细胞系LN229/MGMT,用四甲基偶氮唑蓝法检测替莫唑胺酯对耐药细胞系的增殖抑制作用。结果替莫唑胺酯较替莫唑胺明显抑制LN229细胞的生长,呈浓度和时间依赖性。替莫唑胺酯诱导LN229细胞发生凋亡率高于替莫唑胺。替莫唑胺酯能够导致LN229细胞发生S和G2期阻滞。替莫唑胺酯能够增加Bax/Bcl-2的比值,诱导发生凋亡。替莫唑胺酯能够克服替莫唑胺MGMT阳性的耐药。结论替莫唑胺酯对脑胶质瘤LN229细胞的增殖抑制及诱导凋亡的作用优于替莫唑胺,且能够克服替莫唑胺耐药。 Objective To investigate the effect and possible mechanism of temozolomide inhibiting growth and inducing apoptosis of glioma LN229 cells in vitro and to determine whether temozolomide can overcome the resistance of temozolomide. Methods The effects of temozolomide and temozolomide with the same concentration gradient (62.5,125,250,500,1000μmol·L-1) on the proliferation of LN229 cells were compared by MTT assay. Flow cytometry was used to detect apoptosis rate and cell cycle. The effect of temozolomide and temozolomide on apoptosis proteins Bax and Bcl-2 was detected by Western blot. MGMT overexpressing cell line LN229 / MGMT was constructed and the inhibitory effect of temozolomide on the proliferation of drug-resistant cell lines was detected by MTT assay. Results Compared with temozolomide, temozolomide significantly inhibited the growth of LN229 cells in a concentration- and time-dependent manner. Temozolomide induced apoptosis in LN229 cells was higher than that of temozolomide. Temozolomide can cause S phase and G2 phase arrest in LN229 cells. Temozolomide can increase the ratio of Bax / Bcl-2 and induce apoptosis. Temozolomide can overcome temozolomide MGMT-positive resistance. Conclusion The effect of temozolomide on proliferation and apoptosis of glioma LN229 cells is better than that of temozolomide and can overcome the resistance of temozolomide.