delta-Lactam derivative from thermophilic soil fungus exhibits in vitro anti-allergic activity
Contribuinte(s) |
UNIVERSIDADE DE SÃO PAULO |
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Data(s) |
05/11/2013
05/11/2013
2012
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Resumo |
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. CAPES CAPES CNPq CNPq FAPESP [04/07935-6] FAPESP |
Identificador |
NATURAL PRODUCT RESEARCH, ABINGDON, v. 26, n. 23, supl. 4, Part 1-2, pp. 2168-2175, MAY, 2012 1478-6419 http://www.producao.usp.br/handle/BDPI/41667 10.1080/14786419.2011.647020 |
Idioma(s) |
eng |
Publicador |
TAYLOR & FRANCIS LTD ABINGDON |
Relação |
NATURAL PRODUCT RESEARCH |
Direitos |
closedAccess Copyright TAYLOR & FRANCIS LTD |
Palavras-Chave | #HUMICOLA GRISEA VAR THERMOIDEA #THERMOPHYLIC FUNGUS #DELTA-LACTAM DERIVATIVE #IN SILICO #ANTI-ALLERGIC ACTIVITY #MAST-CELLS #HISTAMINE #RELEASE #CHEMISTRY, APPLIED #CHEMISTRY, MEDICINAL |
Tipo |
article original article publishedVersion |