叶酸偶联的青霉素G酰化酶对叶酸受体阳性肿瘤细胞的靶向作用  

The targeting effects of folate-conjugated penicillin G amidase on folate receptor positive tumor cells

作　　者：杨科亚[1] 张友九[2] 张奇[3] 许玉杰[2] 朱然[2] 胡明江[2] 王道锦[2] 项光亚[3] 范我[2] 

机构地区：[1]上海交通大学附属第六人民医院肿瘤放疗科,200233 [2]苏州大学放射医学与公共卫生学院 [3]湖北武汉华中科技大学

出　　处：《江苏医药》2007年第10期1018-1020,F0002,共4页Jiangsu Medical Journal

基　　金：国家自然科学基金(30300430)

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。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.

关 键 词：叶酸偶联的青霉素G酰化酶 叶酸受体 靶向作用 

分 类 号：R730.5[医药卫生—肿瘤]