| Interaction of antithyroid drugs with bovine serum albumin: electrophoretic and fluorimetric study. | |
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MedLine Citation:
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PMID: 19774650 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The pre-equilibrium capillary zone electrophoretic (pre-eq CZE) method to determine association constants of active anionic forms of antithyroid drugs: 6-n-propyl-2-thiouracil (PTU), 6-methyl-2-thiouracil (MTU), 2-thiouracil (TU) with bovine serum albumin (BSA) under physiological pH 7.4 has been developed for the first time. Using the decrease of the selective electrochromatographic peak area of a drug anionic form due to binding with BSA the association constants K of the binary BSA complexes were calculated. It has been found that the binding constants (log K) of BSA with TU, MTU, and PTU are equal to 2.99, 1.85, and 2.11, respectively. The interaction of PTU, MTU, TU, 2-mercapto-1-methylimidazole (MMI), and ethyl-3-methyl-2-thionoimidazoline-1-carboxylate (Carb), which is considered to be a prodrug for MMI, with BSA has been investigated under physiological conditions by means of fluorescence spectroscopy. Fluorescence emission spectra of BSA in the presence of thioamides recorded at 295 nm excitation wavelength clearly show that the studied drugs act as quenchers, except MMI, which acts as quencher when being excited at 280 nm. The 295 nm light excites tryptophan residues, while the 280 nm light excites both tryptophan and tyrosine residues. The binding constants (log K) of BSA with PTU, MTU, TU, MMI, and Carb have been found to be 4.51, 4.30, 4.30, 2.64, and 4.32, respectively. |
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Authors:
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Margarita S Chernov'yants; Andrey O Dolinkin; Anatoly V Chernyshev; Evgeniy V Khohlov; Elizaveta G Golovanova |
Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: Journal of pharmaceutical sciences Volume: 99 ISSN: 1520-6017 ISO Abbreviation: J Pharm Sci Publication Date: 2010 Mar |
Date Detail:
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Created Date: 2010-01-19 Completed Date: 2010-04-02 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 2985195R Medline TA: J Pharm Sci Country: United States |
Other Details:
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Languages: eng Pagination: 1567-73 Citation Subset: IM |
Copyright Information:
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2009 Wiley-Liss, Inc. and the American Pharmacists Association |
Affiliation:
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Department of Analytical Chemistry, Southern Federal University, Rostov-on-Don 344090, Russia. chernov@rsu.ru |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antithyroid Agents
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pharmacokinetics* Electrophoresis, Capillary / methods* Fluorometry / methods* Methylthiouracil / pharmacokinetics Propylthiouracil / pharmacokinetics Protein Binding Serum Albumin, Bovine / metabolism* Thiouracil / pharmacokinetics |
| Chemical | |
Reg. No./Substance:
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0/Antithyroid Agents; 0/Serum Albumin, Bovine; 141-90-2/Thiouracil; 51-52-5/Propylthiouracil; 56-04-2/Methylthiouracil |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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