抗IV型胶原酶单抗3G11与力达霉素偶联物的抗肿瘤作用  

Antitumor effects of the immunoconjugate composed of lidamycin and monoclonal antibody 3G11

作　　者：王风强[1] 尚伯杨[1] 甄永苏[1] 

机构地区：[1]中国医学科学院,中国协和医科大学医药生物技术研究所,北京100050

出　　处：《药学学报》2003年第7期515-519,共5页Acta Pharmaceutica Sinica

基　　金：国家重点基础性研究 973项目基金 (G19980 5 12 12 )

摘　　要：目的　观察抗IV型胶原酶单抗 3G11与力达霉素 (LDM)偶联物的抗肿瘤作用。方法　用MTT法测定其对肿瘤细胞的增殖抑制作用 ;用小鼠移植性肝癌H2 2观察体内抗肿瘤作用。结果　 3G11 LDM偶联物保留了单抗3G11与IV型胶原酶和靶细胞H2 2细胞的结合能力 ,体外试验H2 2细胞显示比游离LDM更强的细胞增殖抑制作用。体内 3G11 LDM偶联物 0 0 5和 0 10mg·kg- 1 对小鼠移植性肝癌H2 2的抑瘤率分别为 87 8%和 97 2 % ,而游离LDM0 0 5mg·kg- 1 的抑瘤率为 6 7 1% ,且 3G11 LDM偶联物组小鼠的中位生存时间比LDM组明显延长。结论　 3G11 LDM偶联物对小鼠移植性肝癌H2 2的抑瘤作用比LDM强 ,可能成为抗肿瘤靶向药物。Aim To study the antitumor effects of an immunoconjugate composed of lidamycin (LDM) and monoclonal antibody 3G11 (3G11-LDM conjugate). Methods 3G11-LDM conjugate was prepared by using 2-iminothiolane (2-IT) and m -maleimidobenzoyl- N -hydroxy-succimide ester (MBS) as crosslinkers. The molecular weight of the conjugate was measured on non-reduced SDS-PAGE gel. Immunoreactivity of 3G11-LDM conjugate to type IV collagenase or to hepatoma 22 cells was determined by ELISA. The cytotoxicity of the immunoconjug...

关 键 词：IV型胶原酶 单克隆抗体 力达霉素 免疫偶联物 

分 类 号：R73-36[医药卫生—肿瘤]