Determining binding sites of drugs on human serum albumin using FIA-QCM
Zhang, Qundan; Huang, Yanyan; Zhao, Rui; Liu, Guoquan; Chen, Yi
AbstractA simple and effective method was developed for determining binding sites of drugs on human serum albumin (HSA) by independent binding or competitive displacement of bilirubin using flow injection analysis-quartz crystal microbalance (FIA-QCM) system. Both independent and competitive bindings were entirely monitored in real time. Bilirubin as a site I-bincling ligand was pre-bound to HSA sensor so as to occupy the drug-binding site I. When the model site II-binding drugs (ibuprofen, ketoprofen and flurbiprofen) were injected into the bilirubin pre-bound HSA system, the frequency continuously decreased by 6 Hz, 4 Hz and 5 Hz, respectively, which was the same as that of their individual binding to HSA sensor. It indicated that the drug binding to site II was independent and did not interfere with bilirubin binding. However, when the model site I-bincling drugs (iodipamide and magnesium salicylate) were introduced into the system, the frequency remained unchanged in the initial several minutes and then rapidly decreased by 4 Hz for iodipamide and increased by 4 Hz for magnesium salicylate. This phenomenon revealed site I-binding drugs competitively bound to HSA against bilirubin and displaced the pre-bound bilirubin. The results demonstrate FIA-QCM can be a valid approach for monitoring the dynamic interaction between drugs and HSA in real time further identifying drug-binding sites without the need of labels. (C) 2008 Elsevier B.V. All rights reserved.
KeywordHuman Serum Albumin Drugs Binding Sites Fia-qcm Bilirubin
Indexed BySCI
WOS IDWOS:000259425300007
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Cited Times:35[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Corresponding AuthorZhao, Rui
AffiliationChinese Acad Sci, Inst Chem, Lab Analyt Chem Life Sci, Beijing Natl Lab Mol Sci, Beijing 100080, Peoples R China
Recommended Citation
GB/T 7714
Zhang, Qundan,Huang, Yanyan,Zhao, Rui,et al. Determining binding sites of drugs on human serum albumin using FIA-QCM[J]. BIOSENSORS & BIOELECTRONICS,2008,24(1):48-54.
APA Zhang, Qundan,Huang, Yanyan,Zhao, Rui,Liu, Guoquan,&Chen, Yi.(2008).Determining binding sites of drugs on human serum albumin using FIA-QCM.BIOSENSORS & BIOELECTRONICS,24(1),48-54.
MLA Zhang, Qundan,et al."Determining binding sites of drugs on human serum albumin using FIA-QCM".BIOSENSORS & BIOELECTRONICS 24.1(2008):48-54.
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