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Título : Design, synthesis, and docking of highly hypolipidemic agents:Schizosaccharomyces pombe as a new model for evaluating a-asarone-based HMG-CoA reductase inhibitors
Autor : Jiménez Montejo, Fabiola Eloísa
Palabras clave : Alpha-asarone
HMG-CoA reductase
Fecha de publicación : 26-feb-2013
Resumen : A series of a-asarone-based analogues was designed by conducting docking experiments with published crystal structures of human HMG-CoA reductase. Indeed, synthesis and evaluation of this series showed a highly hypocholesterolemic in vivo activity in a murine model, as predicted by previous docking studies. In agreement with this model, the polar groups attached to the benzene ring could play a key role in the enzyme binding and probably also in its biological activity, mimicking the HMG-moiety of the natural substrate. The hypolipidemic action mechanism of these compounds was investigated by developing a simple, efficient, and novel model for determining HMG-CoA reductase inhibition. The partial purification of the enzyme from Schizosaccharomyces pombe allowed for testing of a-asarone- and fibrate-based analogues, resulting in positive and significant inhibitory activity. 2010 Elsevier Ltd. All rights reserved.
Descripción : Article
URI : http://www.repositoriodigital.ipn.mx/handle/123456789/13813
Aparece en las colecciones: Congresos

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4. Bioorganic & Medicinal Chemistry 2010, 18 4238 – 4248.pdf94.14 kBAdobe PDFVisualizar/Abrir

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