论文部分内容阅读
运用毛细管电泳(CE)技术,在对碱性药物Verapamil(VER)手性拆分的基础上对Verapamil与人血清白蛋白(HSA)平行体系进行了相互作用研究。通过定量HSA-VER体系中VER对映体的浓度,建立对映体对结合位点竞争的理论方程,获得了R和S型药物对映体与HSA的结合常数,其值分别为K(R)-VER=2.7×103×(±4.4×102)和K(S)-VER=8.5×102(±1.0×102)。实验证实,HSA具有手性选择性,与(R)-VER的结合强于与(S)-VER的结合,结合比随着HSA与(±)VER的浓度比而变化。
The interaction between Verapamil and human serum albumin (HSA) system was studied by capillary electrophoresis (CE) based on the chiral resolution of verapamil (VER). By quantifying the concentration of VER enantiomers in HSA-VER system, the theoretical equation of enantioselectivity for binding sites was established, and the binding constants of enantiomers of R and S enantiomers to HSA were obtained. The values were K (R ) -VER = 2.7 × 103 × (± 4.4 × 102) and K (S) -VER = 8.5 × 102 (± 1.0 × 102). Experiments confirmed that HSA has chiral selectivity, binding to (R) -VER is stronger than binding to (S) -VER, and the binding ratio changes with the concentration ratio of HSA to (±) VER.