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目的研究~(11)C-4-(3-溴苯氨基)-6,7-双甲氧喹唑啉(PD153035)摄取与表皮生长因子受体(EGFR)表达水平之间的关系。方法在体外测定人乳腺癌细胞 MDA-MB-468、MDA-MB-231和人肺腺癌细胞 A549的 EGFR 表达水平以及对~(11)C-PD153035的摄取。分别建立裸鼠种植瘤模型,通过尾静脉注射~(11)C-PD153035后即刻行 PET 显像,用感兴趣区(ROI)法在注射后即刻及10,20,30,40,50和60 min 测定病灶/健侧前肢正常组织放射性计数(T/NT)比值。显像结束后立即处死动物,切除肿瘤,测量肿瘤内摄取的放射性。结果在体外肿瘤细胞对~(11)C-PD153035的摄取与肿瘤细胞 EGFR 表达水平明显相关(r~2=0.78,P=0.001)。在动物体内,T/NT 与肿瘤细胞的 EGFR 表达水平明显相关(r~2=0.65,P=0.004)。离体肿瘤组织对~(11)C-PD153035的摄取与肿瘤细胞的 EGFR 表达水平明显相关(r~2=0.64,P=0.005)。结论 ~(11)C-PD153035的摄取与肿瘤细胞的 EGFR 表达水平明显相关,EGFR 的~(11)C-PD153035 PET 显像有可能为肿瘤的诊断与治疗提供依据。
Objective To study the relationship between the uptake of epidermal growth factor receptor (EGFR) and the uptake of ~ (11) C-4- (3-bromophenylamino) -6,7-bismethoxyquinazoline (PD153035) Methods The EGFR expression of human breast cancer cells MDA-MB-468, MDA-MB-231 and human lung adenocarcinoma A549 cells were measured in vitro and the uptake of ~ (11) C-PD153035 was measured. The nude mice model of implanted tumor was established. PET imaging was performed immediately after injection of ~ (11) C-PD153035 through the caudal vein. Immediately after the injection and with ROI (10-, 30, 40, 50 and 60 min determination of lesion / contralateral forelimb normal tissue radioactivity count (T / NT) ratio. The animals were sacrificed immediately after the imaging, the tumors were resected, and the radioactivity in the tumors was measured. Results The in vitro uptake of ~ (11) C-PD153035 by tumor cells was significantly correlated with the expression of EGFR in tumor cells (r ~ 2 = 0.78, P = 0.001). In animals, T / NT was significantly correlated with tumor cell EGFR expression (r = 2 = 0.65, P = 0.004). The in vitro tumor tissue uptake of ~ (11) C-PD153035 was significantly correlated with the level of EGFR in tumor cells (r ~ 2 = 0.64, P = 0.005). Conclusion The uptake of (11) C-PD153035 is significantly correlated with the expression of EGFR in tumor cells. The ~ (11) C-PD153035 PET imaging of EGFR may provide the basis for the diagnosis and treatment of tumors.