Analysis of the molecular interactions and complexation of chloroquine with bovine serum albumin
-
Mahmoud Kandeel
and
Yukio Kitade
Abstract
Background: Pharmacokinetic parameters, drug bioavailability, and biological activities depend on the mechanisms of interaction with serum albumin. In this study, the binding properties as well as mechanisms of interaction of chloroquine with bovine serum albumin (BSA) were investigated.
Methods: The binding of chloroquine with BSA was carried out using a microcalorimetric approach. The mechanism of binding, the number of binding molecules as well as changes of BSA upon complexation with chloroquine were investigated.
Results: The binding isotherms indicated a variable number of binding sites of chloroquine on one molecule of BSA. At lower temperatures, larger numbers of binding sites were available for chloroquine, these decrease by increasing the temperature. The binding constant of chloroquine with BSA varied from 9.4×103 M–1 at 25°C to 5.7×103 M–1 at 40°C. Chloroquine showed temperature-dependent binding affinity, with stronger affinity at lower temperature. By increasing the temperature, from 25°C to 40°C, the binding affinity was decreased by approximately 60% of its value.
Conclusions: Chloroquine showed weak binding affinity with BSA. The weak binding affinity of chloroquine with BSA is important in determining the drug-drug interactions at the binding sites of BSA. The presence of stronger binding ligands, e.g., chloramphenicol, tetracyclines or diclofenac, can compete with chloroquine for its binding sites, and therefore lowers its serum albumin binding. This study will be helpful in understanding the binding properties of mechanisms of interaction of chloroquine with BSA.
©2012 by Walter de Gruyter Berlin Boston
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Articles in the same Issue
- Editorial
- Cytochrome P450 enzymes
- Reviews
- The aryl hydrocarbon receptor system
- Herb-drug interactions with Danshen (Salvia miltiorrhiza): a review on the role of cytochrome P450 enzymes
- Pharmacokinetic interactions of selective serotonin reuptake inhibitors with other commonly prescribed drugs in the era of pharmacogenomics
- Original Articles
- Effects of CYP2D6*10, CYP3A5*3, CYP1A2*1F, and ABCB1 C3435T polymorphisms on the pharmacokinetics of flecainide in healthy Chinese subjects
- Analysis of the molecular interactions and complexation of chloroquine with bovine serum albumin
- The microstructure of DNA-egg yolk phosphatidylcholine-gemini surfactants complexes: effect of the spacer length
- Meeting Reports
- Report from the European Society of Pharmacogenomics and Theranostics (ESPT) Inaugural Symposium 2011 in Bled
- Pharmacogenetics in Latin American populations: regulatory aspects, application to herbal medicine, cardiovascular and psychiatric disorders
- Masthead
- Masthead
