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题名: Study of interaction between drug enantiomers and serum albumin by capillary electrophoresis
作者: Ding, YS;  Zhu, XF;  Lin, BC
关键词: capillary electrophoresis ;  interaction ;  binding constant ;  enantiomer ;  chiral separation ;  stereoselectivity ;  competition ;  synergism
刊名: ELECTROPHORESIS
发表日期: 1999-07-01
卷: 20, 期:9, 页:1890-1894
收录类别: ISTP ;  SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine ;  Physical Sciences
类目[WOS]: Biochemical Research Methods ;  Chemistry, Analytical
研究领域[WOS]: Biochemistry & Molecular Biology ;  Chemistry
英文摘要: The interaction between drugs and human serum albumin (HSA) was investigated by capillary electrophoresis (CE). It involves stereoselectivity, drug displacement and synergism effects. Under protein-drug binding equilibrium, the unbound concentrations of drug enantiomers were measured by frontal analysis (FA). The stereoselectivity of verapamil (VER) binding to HSA was proved by the different free fractions of two enantiomers. In physiological pH (7.4, ionic strength 0.17 phosphate buffer) when 300 mu M (+/-) VER were equilibrated with 500 mu M HSA, the concentration of unbound S-VER was about 1.7 times its antipode. The binding constants of two enantiomers, KR-VER and KS-VER, were 2670 and 850 M-1, respectively. However, no obvious stereoselective binding of propranolol (PRO) to HSA was observed. Trimethyl-beta-cyclodextrin (45 mM) was used as a chiral selector in pH 2.5 phosphate buffer. Several drug systems were studied by the method. When ibuprofen (IBU) was added into VER-HSA solution. R-VER was partially displaced while S-VER was not displaced at all. A binding synergism effect between bupivacaine (BUP) and verapamil was observed and further study suggested that verapamil and bupivacaine occupy different binding site of HSA (site II and site III, respectively).
关键词[WOS]: PROTEIN-BINDING ;  ALPHA-1-ACID GLYCOPROTEIN ;  FRONTAL ANALYSIS ;  BASIC DRUG ;  CONSTANTS ;  IBUPROFEN ;  SITES
语种: 英语
原文出处: 查看原文
WOS记录号: WOS:000081688800013
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/86215
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China

Recommended Citation:
Ding, YS,Zhu, XF,Lin, BC. Study of interaction between drug enantiomers and serum albumin by capillary electrophoresis[J]. ELECTROPHORESIS,1999,20(9):1890-1894.
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