【摘要】 目的研究叶酸偶联的青霉素G酰化酶(F-PGA)对叶酸受体阳性肿瘤细胞的靶向作用。方法用激光共聚焦显微镜观察宫颈癌HeLa、卵巢癌SKOV3和肺癌A549细胞对F-PGA以及游离叶酸(F-A)的摄取,并进一步用同位素示踪法加以验证和定量检测。结果F-PGA与F-A相似,均能被叶酸受体阳性的HeLa和SKOV3肿瘤细胞选择性摄取,且有饱和性、可逆性、温度依赖性和高亲和性的特点,但不能被叶酸受体阴性的A549细胞摄取。结论F-PGA与F-A都是通过叶酸受体介导,从而特异性地靶向于叶酸受体阳性肿瘤细胞的。更多还原

【Abstract】 Objective To explore the targeting effects of folate-conjugated penicillin G amidase(F-PGA)on folate receptor positive tumor cells.Methods The uptake of F-PGA and free folic acid(F-A)by HeLa,SKOV3 and A549 cells was observed using laser confocal microscopy,and was further confirmed and quantified by isotope trace method.Results F-PGA like F-A could be selectively absorbed by folate receptor positive tumor cells such as HeLa and SKOV3,with the characteristics of saturability,reversibility,temperature-dependent and high affinity,but not by folate receptor negative A549 cells.Conclusion Both F-PGA and F-A may specially target to folate receptor positive tumor cells,which is mediated by folate receptor.更多还原