Evaluation of in vitro toxicity of peptide N-acetyl-Leu-Gly-Leu-COOH-substituted-β-cyclodextrin derivative, a novel drug carrier, in PC-12 cellsReportar como inadecuado




Evaluation of in vitro toxicity of peptide N-acetyl-Leu-Gly-Leu-COOH-substituted-β-cyclodextrin derivative, a novel drug carrier, in PC-12 cells - Descarga este documento en PDF. Documentación en PDF para descargar gratis. Disponible también para leer online.

DARU Journal of Pharmaceutical Sciences

, 21:75

First Online: 20 December 2013Received: 21 July 2013Accepted: 02 September 2013

Abstract

BackgroundCyclodextrins CDs have been shown to improve physicochemical and biopharmaceutical properties of drugs when low solubility and low safety limit their use in the pharmaceutical field. Recently, a new amphiphilic peptide-substituted-β-CD, hepta-N-acetyl-Leu-Gly-Leu-β-CD hepta-N-acetyl-LGL-β-CD, is developed which exhibited good solubility, strong inclusion ability and an appropriate average molecular weight. However, there is limited information available about its toxic effects. This study was designed to evaluate cytotoxic effects of the hepta-N-acetyl-LGL-β-CD 50, 200, 400, and 800 μg-ml on rat pheochromocytoma PC-12 cells.

ResultsA significant reduction of cell viability with IC50 values of 1115.0 μg-ml, 762.4 μg-ml, and 464.9 μg-ml at 6, 12, and 24 h post-treatment, respectively, as well as increased lipid peroxide levels and DNA damage were observed.

ConclusionsIn conclusion, hepta-N-acetyl-Leu-Gly-Leu-β-CD exhibit significant toxic properties at high concentrations, probably through induction of oxidative stress and genotoxicity.

KeywordsHepta-N-acetyl-Leu-Gly-Leu-β-CD Lipid peroxidation DNA damage Oxidative stress PC-12 cells Electronic supplementary materialThe online version of this article doi:10.1186-2008-2231-21-75 contains supplementary material, which is available to authorized users.

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Autor: Hamid Reza Sadeghnia - Faezeh Vahdati Hassani - Hamid Sadeghian - Maryam Miandehi - Farzin Hadizadeh - Gholamreza Karimi

Fuente: https://link.springer.com/







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