Zhivkova Z D, Russeva V N
Department of Chemistry, Faculty of Pharmacy, Medical University, Sofia, Bulgaria.
J Chromatogr B Biomed Sci Appl. 1998 Sep 4;714(2):277-83. doi: 10.1016/s0378-4347(98)00211-4.
A chiral stationary phase based on immobilized human serum albumin (HSA) was used to study the stereoselective binding of ketoprofen enantiomers by means of high-performance liquid affinity chromatography. The technique of zonal elution was applied together with a novel mathematical approach describing attachment to more than one type of binding site. Phenylbutazon (PBZ) and diazepam (DAZ) were used as markers for the major believed binding regions on HSA. Both R- and S-ketoprofen (KTR and KTS) display high affinity to the primary PBZ- and DAZ-binding sites and low-affinity to the secondary DAZ sites. The binding to high-affinity regions is accepted to be a stepwise process initiated by the binding to the primary DAZ sites and followed by the attachment to the primary PBZ sites. The chiral recognition is attributed to the high-affinity PBZ-binding sites and to the low-affinity DAZ-binding sites.
基于固定化人血清白蛋白（HSA）的手性固定相，通过高效液相亲和色谱法研究了酮洛芬对映体的立体选择性结合。采用了区域洗脱技术，并结合一种描述与多种结合位点结合的新型数学方法。苯丁酮（PBZ）和地西泮（DAZ）用作HSA上主要的假定结合区域的标记物。R-和S-酮洛芬（KTR和KTS）对主要的PBZ和DAZ结合位点均显示出高亲和力，而对次要的DAZ位点显示出低亲和力。与高亲和力区域的结合被认为是一个逐步过程，首先是与主要的DAZ位点结合，然后是与主要的PBZ位点结合。手性识别归因于高亲和力的PBZ结合位点和低亲和力的DAZ结合位点。
