摘要
目的研究苯磺酸氨氯地平及苯磺酸左旋氨氯地平与人血清白蛋白(HSA)间的相互作用。方法采用荧光分光光度法,研究苯磺酸氨氯地平及苯磺酸左旋氨氯地平对人血清白蛋白的猝灭。结果根据Stern-Volmer方程确定了苯磺酸氨氯地平对人血清白蛋白的猝灭类型为静态猝灭。通过计算求得生理条件下(pH7.4)苯磺酸氨氯地平及苯磺酸左旋氨氯地平与HSA的结合常数分别为5.40×104和6.82×104L.mol-1,结合位点数分别为1.15和1.18。实验考察了pH及微量金属离子对药物与HSA相互作用的影响。最后根据热力学方法确定了该药物与人血清白蛋白之间的作用力类型为静电作用力。结论本法简便、快速,实验结果有助于阐明手性药物不同对映体的药效差异。
OBJECTIVE To study the interaction between the chiral drug of amlodipine besylate and human serum albumin （HSA）, METHODS The fluorescent quenching of HSA by the chiral drug of amlodipine besylate was studied using fluorescence spectrophotometry. RESULTS The Stern-Volmer equation was employed to calculate the association constant and binding site number of the drug with HSA, The association constant was 5.40 ×10^4 for amlodipine besylate and 6.82×10^4 for L-amlodipine besylate, and the binding site number was 1.15 for amlodipine besylate and 1.18 for L- amlodipine besylate. The quenching type of HSA by the chiral drug of amlodipine besylate was considered as static quenching, The effect of pH and two mental cations on the association constant and the binding site number of L-amlodipine besylate with HSA was examined, At last the results suggested that the binding type was mainly electrostatic action, CONCLUSION This method is simple and rapid, The results are useful for clarifying the different curative effect of two enantiomers
出处
《中国药学杂志》
CAS
CSCD
北大核心
2008年第4期311-314,共4页
Chinese Pharmaceutical Journal
关键词
苯磺酸氨氯地平
立体选择性
人血清白蛋白
荧光光谱法
amlodipine besylate
enantioselection
human serum albumin
fluorescence spectrophotometry
