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A comparative study of the interaction of Tamiflu and Oseltamivir carboxylate with bovine serum albumin

Paper ID Volume ID Publish Year Pages File Format Full-Text
29461 44409 2013 6 PDF Available
Title
A comparative study of the interaction of Tamiflu and Oseltamivir carboxylate with bovine serum albumin
Abstract

Oseltamivir phosphate (Tamiflu) is a pro-drug that is metabolized to its active form (Oseltamivir carboxylate), after oral administration. OC inhibits influenza A and B neuraminidases in vitro and OP inhibits influenza virus infection and replication in vitro. Serum albumin is the most abundant of the proteins in the circulatory system of a wide variety of organisms and plays an important role in the transport and deposition of many drugs. The aim of this study was to examine the interaction of BSA with Tamiflu and Oseltamivir carboxylate in aqueous solution at physiological conditions, using a constant protein concentration and various drug contents. FTIR, UV–Vis spectroscopic methods were used to determine the drugs binding mode, the binding constant and the effects of drug complexation on protein secondary structure.Structural analysis showed that OP and OC bind BSA with overall binding constants of KOP–BSA = 1.88 (±0.16) × 104 M−1 and KOC–BSA = 5.7 (±0.09) × 102 M−1. Drug complexation alters protein conformation by major reduction of α-helix and random coil and increase of β-sheet and turn structures that indicate a partial protein destabilization. The results suggest that BSA might act as carrier proteins for OP in delivering it to target molecules.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► The binding affinity of Oseltamivir phosphate and Oseltamivir carboxylate to BSA was determined. ► The stronger binding was observed for Oseltamivir phosphate than Oseltamivir carboxylate. ► At high drug concentrations protein destabilization was observed. ► BSA might act as carrier proteins for OP in delivering it to target molecules.

Keywords
Bovine serum albumin; Oseltamivir phosphate; Oseltamivir carboxylate; FT-IR; UV–Vis spectroscopy
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A comparative study of the interaction of Tamiflu and Oseltamivir carboxylate with bovine serum albumin
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Publisher
Database: Elsevier - ScienceDirect
Journal: Journal of Photochemistry and Photobiology B: Biology - Volume 119, 5 February 2013, Pages 65–70
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us