A quantitative circular dichroic investigation of the binding of the enantiomers of ibuprofen and naproxen to human serum albumin

被引:33
作者
Cheruvallath, VK
Riley, CM
Narayanan, SR
Lindenbaum, S
Perrin, JH
机构
[1] UNIV FLORIDA,DEPT MED CHEM,GAINESVILLE,FL 32610
[2] HOECHST MARION ROUSSEL,KANSAS CITY,MO 64134
[3] DUPONT MERCK PHARMACEUT CO,WILMINGTON,DE 19880
[4] DURA PHARMACEUT,SAN DIEGO,CA 92121
关键词
enantiomers; racemate; ibuprofen; naproxen; extrinsic cotton effects; binding constants; diazepam;
D O I
10.1016/S0731-7085(96)01956-5
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
The binding constants for racemic, R and S naproxen and ibuprofen to human serum albumin have been determined by a circular dichroic technique. The ibuprofens and naproxens show no measurable extrinsic optical activity on interaction with the protein, and so the extrinsic Cotton effect shown following the diazepam-albumin interaction is used as a probe. The presence of the drugs reduce the amount of diazepam bound as shown by the reduced size of the induced ellipticity. The calculated primary binding constants show that the S form of both drugs bind to the albumin more tightly than the R form and that the racemic forms bind less tightly than either enantiomer. (C) 1997 Elsevier Science B.V.
引用
收藏
页码:1719 / 1724
页数:6
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