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作者报道胃癌单克隆抗体MG11-丝裂霉素C(MMC)结合物的制备及其对肿瘤细胞的杀伤作用。首先用戊二酐处理MMC,于MMC上引入羧基,MMC衍生物与N羟基琥珀酰亚胺及2,2′-二环已基碳二亚胺反应,得到MMC活性酯,后者与抗体反应将MMC引入抗体中。经测定,每克分子抗体中引入约6~7克分子药物,结合物对人胃癌细胞KATⅢ具有较强的选择性杀伤作用,在0.56μg/ml水平(药物浓度)对肿瘤细胞杀伤牢达60%,优于游离药物(51%)及无关抗体结合物(9.3%),提示选用的胃癌单抗对MMC具有较好的导向作用。
The authors reported the preparation of gastric cancer monoclonal antibody MG11-mitomycin C (MMC) conjugates and their killing effect on tumor cells. The MMC is first treated with glutaric anhydride, and the carboxyl group is introduced on the MMC. The MMC derivative is reacted with N-hydroxysuccinimide and 2,2′-dicyclohexylcarbodiimide to obtain the MMC active ester, which reacts with the antibody. MMC was introduced into the antibody. It has been determined that about 6 to 7 moles of drug are introduced per gram of antibody, and the conjugate has a strong selective killing effect on human gastric cancer cell KATIII, and the tumor cell killing rate is up to 60 at a level of 0.56 μg/ml (drug concentration). %, better than free drug (51%) and irrelevant antibody conjugate (9.3%), suggesting that the selected gastric cancer monoclonal antibody has a better guiding effect on MMC.