摘要
基于荧光光谱分析技术,通过体外模拟生理环境实验和动物体内实验探索了地西泮与乙醇的协同作用机制.研究结果表明,在地西泮体内代谢初期,血液中乙醇的存在可以降低地西泮-人血清白蛋白(HSA)络合物的结合平衡常数,致使血液中地西泮游离分子的浓度相对增大,可加速地西泮分子的代谢速率,降低药物的半衰期,从而增强地西泮在体内的药效,产生协同作用.
The synergistic mechanism of diazepam and ethanol was investigated based on fluorescence spectroscopic method by simulating the physiological environment in vitro and the in vivo experiments in mice.The experimental results revealed that the presence of ethanol in the blood can reduce the equilibrium binding constant of diazepam-HSA complex in the early metabolism of diazepam,which resulted in the increase of the free diazepam proportion,accelerating the metabolic rate of diazepam,and shorten the half-life and storage time of diazepam in the blood,thereby enhancing its bioactive efficacy.
作者
崔胜峰
万敬伟
周成合
CUI Shengfeng;WAN Jingwei;ZHOU Chenghe(Center for Physical and Chemical Evidence Examination, Department of Public Security Technology, Railway Police College, Zhengzhou 450053, China;Institute of Bioorganic ＆ Medicinal Chemistry, School of Chemistry and Chemical Engineering Southwest University, Chongqing 400715, China)
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2018年第6期1178-1184,共7页
Chemical Journal of Chinese Universities
基金
河南省科技攻关计划项目(批准号:172102310603
172102210112)
河南省高等学校重点科研项目计划(批准号:16A350009
16A150041)
中央高校基本科研业务经费项目(批准号:2016TJJBKY025)资助~~
关键词
地西泮
酒精依赖
荧光光谱
人血清白蛋白
光谱分析
Diazepam
Alcohol dependence
Fluorescence
Human serum albumin
Spectral analysis
