蜂毒多肽空间稳定免疫脂质体的制备及体外对肿瘤细胞的选择性  

Preparation and in vitro tumor cells selectivity of sterically stabilized immunoliposomal peptides in bee venom

作　　者：胡海洋[1] 陈大为[1] 刘彦仿[2] 乔明曦[1] 赵秀丽[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]第四军医大学基础医学院病理教研室,陕西西安710032

出　　处：《药学学报》2007年第11期1201-1205,共5页Acta Pharmaceutica Sinica

摘　　要：蜂毒多肽在肿瘤治疗中的应用引起研究者的极大兴趣。本研究使用大豆磷脂、胆固醇、羧酸化PEG-胆固醇制备了蜂毒多肽空间稳定脂质体,并将二硫键稳定抗人肝癌单链抗体联结PEG-胆固醇末端。使用酶联免疫法考察了蜂毒多肽空间稳定免疫脂质体的活性。蜂毒多肽空间稳定免疫脂质体有较高的肿瘤细胞选择性。体外实验证明,其对SMMC-7721细胞的杀伤能力远强于蜂毒多肽空间脂质体,而对Hela细胞的杀伤能力与蜂毒多肽空间脂质体无区别。蜂毒多肽空间稳定免疫脂质体对肿瘤细胞的选择性,可使其成为一种有效的靶向制剂。Recently the use of peptides in bee venom （PBV） for cancer therapy has attracted considerable attention. In this study, the sterically stabilized liposomal PBV （PBV-SL） was prepared using soybean phosphatidylcholine, cholesterol, and cholesterol-PEG-COOH. The humanized anti- hepatoma disulfide-stabilized Fv （hdscFv25） was coupled to sterically stabilized liposomes using the N-hydroxysuccinimide ester method. The hdscFv25-immunoliposomes （ SIL[ hdscFv25 ]） were immunoreactive as determined by ELISA assay. SIL[ hdscFv25 ] showed higher tumor cells selectivity. PBV-SIL[ hdscFv25 ] can kill SMMC-7721 cells in vitro with higher efficiency than non-targeted liposomes. Whereas cytotoxicties were compared for Hela cells, no significant differences was observed between PBV-SIL[ hdscFv25 ] and PBV-SL. Sterically stabilized immunoliposomal peptides in bee venom could be one drug targeting delivery system.

关 键 词：蜂毒多肽 空间稳定免疫脂质体 肿瘤细胞选择性 体外细胞毒作用 

分 类 号：R943.4[医药卫生—药剂学]