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Type: Artigo de periódico
Title: delta-Lactam derivative from thermophilic soil fungus exhibits in vitro anti-allergic activity
Author: Andrioli, W. J.
Santos, M. S.
Silva, V. B.
Oliveira, R. B.
Chagas-Paula, D. A.
Jorge, J. A.
Furtado, N. A. J. C.
Pupo, M. T.
Silva, C. H. T. P.
Naal, R. M. Z. G.
Bastos, J. K.
Abstract: From cultures of thermophilic soil fungus Humicola grisea var thermoidea, a delta-lactam derivative (3-(2-(4-hydroxyphenyl)-2-oxoethyl)-5,6-dihydropyridin-2( 1H)-one) that displayed anti-allergic activity was isolated, which was predicted by in silico computational chemistry approaches. The in vitro anti-allergic activity was investigated by beta-hexosaminidase release assay in rat basophilic leukaemia RBL-2H3 cells. The delta-lactam derivative exhibited similar anti-allergic activity (IC50 = 18.7 +/- 6.7 mu M) in comparison with ketotifen fumarate (IC50 = 15.0 +/- 1.3 mu M) and stronger anti-allergic activity than azelastine (IC50 = 32.0 mu M). Also, the MTT cytotoxicity assay with RBL-2H3 cells showed that delta-lactam does not display cytotoxicity at concentrations lower than 50 mu M. This study suggests that the delta-lactam derivative has the potential to be used as a lead compound in the development of anti-allergic drugs for clinical use in humans.
Subject: Humicola grisea var thermoidea
thermophylic fungus
delta-lactam derivative
in silico
anti-allergic activity
Editor: Taylor & Francis
Citation: Natural Product Research. Taylor & Francis, v.26, n.23, p.2168-2175, 2012
Rights: fechado
Identifier DOI: 10.1080/14786419.2011.647020
Date Issue: 2012
Appears in Collections:IQ - Artigos e Outros Documentos

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