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本文报道胃癌单抗MGb_2—牛血清白蛋白(BSA)—氨甲喋呤(MTX)结合物的制备及其对肿瘤靶细胞的杀伤作用。MTX与二环已基碳二亚胺及N—羟基琥珀酰亚胺作用得到MTX活性酯,MTX活性酯与暴露自身游离巯基的BSA作用将MTX引入BSA—SH。然后,BSA—SH与引入碘乙酰基团的单抗反应得到MGb_2—BSA—MTX结合物。结合物中MGb_2:BSA:MTX克分子比为1:1.5:30。该结合物对靶细胞具有较强的选择性杀伤作用,在1.8×10~(-9)M水平对胃癌细胞杀伤率为62％,而对非靶细胞作用很弱。提示选择的胃癌单抗对MTX具有较好的导向作用。
This paper reports the preparation of gastric cancer monoclonal antibody MGb_2-BSA-MTX conjugate and its killing effect on tumor target cells. MTX is reacted with bicyclohexylcarbodiimide and N-hydroxysuccinimide to obtain an MTX active ester. MTX active ester and BSA exposed to its free thiol group act to introduce MTX into BSA-SH. Then, BSA-SH was reacted with the iodoacetyl group-introduced monoclonal antibody to obtain MGb_2-BSA-MTX conjugate. The molar ratio of MGb_2:BSA:MTX in the conjugate was 1:1.5:30. The conjugate has a strong selective killing effect on the target cells, and the killing rate of the gastric cancer cells at a level of 1.8×10 -9 M is 62%, but the effect on the non-target cells is very weak. It is suggested that the selected gastric cancer monoclonal antibody has a good guiding effect on MTX.