DICP OpenIR
Study of interaction between drug enantiomers and serum albumin by capillary electrophoresis
Ding, YS; Zhu, XF; Lin, BC
KeywordCapillary Electrophoresis Interaction Binding Constant Enantiomer Chiral Separation Stereoselectivity Competition Synergism
Source PublicationELECTROPHORESIS
1999-07-01
Volume20Issue:9Pages:1890-1894
Indexed ByISTP ; SCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences
WOS SubjectBiochemical Research Methods ; Chemistry, Analytical
WOS Research AreaBiochemistry & Molecular Biology ; Chemistry
WOS KeywordPROTEIN-BINDING ; ALPHA-1-ACID GLYCOPROTEIN ; FRONTAL ANALYSIS ; BASIC DRUG ; CONSTANTS ; IBUPROFEN ; SITES
AbstractThe 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).
Language英语
URL查看原文
WOS IDWOS:000081688800013
Citation statistics
Cited Times:36[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/86215
Collection中国科学院大连化学物理研究所
AffiliationChinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
Recommended Citation
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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