硫辛酸修饰胰岛素与胰岛素受体的结合能力

The binding potency of lipoic acid modified insulin with insulin receptor

目的考察硫辛酸修饰胰岛素与胰岛素受体的结合能力。方法通过与125I-胰岛素对大鼠肝细胞膜胰岛素受体的竞争结合,比较硫辛酰胰岛素(B29LA-ins)和天然猪胰岛素的受体结合能力。结果B29LA-ins与胰岛素受体的结合能力为天然猪胰岛素的4.8倍。结论硫辛酸对LysB29的修饰提高了胰岛素的受体结合能力,这可能是促使其体内作用时间延长的因素之一。

Purpose To investigate the binding potency of lipoic acid modified insulin with insulin receptor.Methods Competitive insulin receptor binding assay with ^125 I-insulin to rat hepatic membranes was conducted for lipoyl-insulin （B29LA-ins） and the native porcine insulin. Results B29LA-ins showed about 4.8- fold recptor binding potency compared with the native porcine insulin. Conclusion The covalent modification of insulin at LysB29 with lipoic acid enhanced the receptor- binding potency and this may be one of the factors which contributed to the protraction of the in vivo action of B29LA-ins.