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	Enantiospecific binding of Rotigotine and its antipode to serum albumins: Investigation of binding constants and binding sites by partial-filling ACE
	Chu, Bao-Lin ; Lin, Jin-Ming ; Wang, Zhihua ; Guo, Baoyuan
	2010-10-12 ; 2010-10-12
关键词	ACE Binding constant Chiral separation Rotigotine Serum albumin AFFINITY ELECTROKINETIC CHROMATOGRAPHY CAPILLARY-ELECTROPHORESIS DRUG-BINDING CHIRAL SELECTOR ALPHA(1)-ACID GLYCOPROTEIN INCLUSION COMPLEXES CIRCULAR-DICHROISM PROTEIN-BINDING MIGRATION TIME CYCLODEXTRIN Biochemical Research Methods Chemistry, Analytical
中文摘要	Enantiospecific binding of antiparkinsonian medication Rotigotine (S-enantiomer) and its antipode to HSA or BSA was demonstrated employing partial-filling ACE (PF-ACE) under near-physiological conditions (50 mM phosphate, pH 7.4, 37 degrees C). The enantioseparation of the enantiomers was achieved by PF-ACE. Subsequently, the binding characteristics of the enantiomers to the serum albumins were investigated. Based on the PF-ACE data, the following binding constants were obtained: K-b,K-HSA,K-S = 8884 +/- 255 M-1, K-b,K-HSA,K-R=17648 +/- 587M(-1), K-b,K-BSA,K-S=7348 +/- 237 M-1, K-b,K-BSA,K-R=9353 +/- 352 M-1. It revealed that Rotigotine had weaker affinity for the two serum albumins, and both enantiomers showed stronger affinity for HSA than BSA. The presence of either site marker (warfarin or ketoprofen) had adverse effect on the enantioseparation due to the competitive binding, or even eliminated the enantioselective binding of the enantiomers to the albumin when the molar ratio of the site marker to the albumin was at certain level. Although there might be a synergistic binding between the drug and the albumin, it was suggested that site II and I were the preferential binding site of the drug on HSA and BSA, respectively.
语种	英语 ; 英语
出版者	WILEY-V C H VERLAG GMBH ; WEINHEIM ; PO BOX 10 11 61, D-69451 WEINHEIM, GERMANY
内容类型	期刊论文
源URL	[http://hdl.handle.net/123456789/80790]
专题	清华大学
推荐引用方式 GB/T 7714	Chu, Bao-Lin,Lin, Jin-Ming,Wang, Zhihua,et al. Enantiospecific binding of Rotigotine and its antipode to serum albumins: Investigation of binding constants and binding sites by partial-filling ACE[J],2010, 2010.
APA	Chu, Bao-Lin,Lin, Jin-Ming,Wang, Zhihua,&Guo, Baoyuan.(2010).Enantiospecific binding of Rotigotine and its antipode to serum albumins: Investigation of binding constants and binding sites by partial-filling ACE..
MLA	Chu, Bao-Lin,et al."Enantiospecific binding of Rotigotine and its antipode to serum albumins: Investigation of binding constants and binding sites by partial-filling ACE".(2010).

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