目的 探讨Src酪氨酸激酶抑制剂逆转人胃癌顺铂耐药细胞SGC7901/DDP的作用及机制.方法 以Src酪氨酸激酶抑制剂逆转前后的人胃癌顺铂耐药细胞SGC7901/DDP为研究对象,应用Western blot观察细胞内p-Src表达的变化,MTS法检测细胞的药物敏感性,流式细胞仪检测细胞Rh123外排及P-gp表达的水平.结果 Src酪氨酸激酶抑制剂可下调SGc7901/DDP细胞中p-Src表达,在5μmol/L及10μnol/L Src酪氨酸激酶抑制剂作用下,SGC7901/DDP细胞对顺铂的药物敏感性分别提高了1.52倍和3.96倍,细胞中Rh123含量分别提高了1.24倍和2.64倍,P-gp表达水平分别降低了65.8％和47.4％.结论 Src酪氨酸激酶抑制剂可逆转SGC7901/DDP细胞多药耐药性,其耐药表型的逆转可能与降低细胞Rh123外排及P-gp表达水平有关.%Objective To explore the effect of Src tyrosine kinase inhibitor on cisplatin-resistant human stomach cancer cell SGC7901/ DDP and its mechanism. Methods The 4-anilinoquirazoline was used to inhibit Src tyrosine kinase in human stomach cancer SGC7901/DDP cell line. Western blot assay was used to examine the expression of p-Src. MTS assay was used to examine the anti-tumor drug sensitivity. Flow cytometry was used to examine Rhl23 excretion and P-glycoprotein (P-gp) expression in SGC7901/DDP. Results Src tyrosine kinase inhibitor 4-anilinoquirazoline obviously decreased the expression of p-Src. The anti-rumor drug sensitivity increased 1. 52-fold and 3.96-fold,the Rh123 intra-ceuular concentration increased 1.24-fold and 2.64-fold,P-gp expression decreased 65.8% and47.4% in SGC7901/DDP after cultured with 5 μmol/L and 10 μmol/L 4-anilinoquirazoline, respectively. Conclusion Src tyrosine kinase inhibitor 4-anilinoquirazoline could reverse the multidrug resistance of SGC7901/DDP,which may be caused by the reduction of Rhl23 excretion and P-gp expression.
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