Artículos de revistas
delta-Lactam derivative from thermophilic soil fungus exhibits in vitro anti-allergic activity
Fecha
2012Registro en:
NATURAL PRODUCT RESEARCH, ABINGDON, v. 26, n. 23, supl. 4, Part 1-2, pp. 2168-2175, MAY, 2012
1478-6419
10.1080/14786419.2011.647020
Autor
Andrioli, Willian Jonis
Santos, M. S.
Silva, V. B.
Oliveira, R. B.
Chagas-Paula, D. A.
Jorge, J. A.
Furtado, Niege Araçari Jacometti Cardoso
Pupo, Monica Tallarico
Silva, Carlos Henrique Tomich de Paula da
Naal, Rose Mary Zumstein Georgetto
Bastos, Jairo Kenupp
Institución
Resumen
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.