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Study of interaction between drug enantiomers and serum albumin by capillary electrophoresis
Ding, YS; Zhu, XF; Lin, BC
关键词Capillary Electrophoresis Interaction Binding Constant Enantiomer Chiral Separation Stereoselectivity Competition Synergism
刊名ELECTROPHORESIS
1999-07-01
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
关键词[WOS]PROTEIN-BINDING ; ALPHA-1-ACID GLYCOPROTEIN ; FRONTAL ANALYSIS ; BASIC DRUG ; CONSTANTS ; IBUPROFEN ; SITES
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).
语种英语
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WOS记录号WOS:000081688800013
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被引频次:36[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/86215
专题中国科学院大连化学物理研究所
作者单位Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
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GB/T 7714
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.
APA Ding, YS,Zhu, XF,&Lin, BC.(1999).Study of interaction between drug enantiomers and serum albumin by capillary electrophoresis.ELECTROPHORESIS,20(9),1890-1894.
MLA Ding, YS,et al."Study of interaction between drug enantiomers and serum albumin by capillary electrophoresis".ELECTROPHORESIS 20.9(1999):1890-1894.
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