【摘要】 在合成了7种拟糖蛋白的基础上,用活性酯中间物法和水溶性碳二亚胺(ECDI)法将抗癌药甲氨喋呤(MTX)与拟糖蛋白及牛血清白蛋白(BSA)偶联。结果表明,两种方法都能使 MTX与拟糖蛋白及 BSA 偶联。活性酯中间物法的偶联率(8.52±2.52%)高于 ECDI 法(5.01±0.65%)。MTX 与蛋白质的偶联率及摩尔比与反应液中 MTX、ECDI 含量密切相关。这些 MTX-拟糖蛋白复合物对肝癌细胞有明显的抑制生长作用。更多还原

【Abstract】 On the basis of synthesizing seven neogly-coproteins,an anti-cancer drug,methotrexate(MTX),was coupled to neoglycoproteins andbovine serum albumin(BSA)by active ester in-termediate and water-soluble carbodiimide(EC-DI).The results showed that MTX could be effi-ciently coupled to both neoglycoproteins and BSAby the two methods.The coupling rate of MTXby active ester intermediate method(8.52±2.52%)was higher than that by ECDI method(5.01±0.65%).The coupling rate and the ra-tio of MTX to the proteins in conjugates wereclosely related to the concentrations of MTX,ECDI and other coupling reagents in reaction so-lutions.MTX-neoglycoprotein conjugates had in-hibitory effects on the growth of hepatoma cells.更多还原