| Full text | |
| Author(s): Show less - |
Andrioli, W. J.
[1]
;
Santos, M. S.
[2, 3]
;
Silva, V. B.
[1]
;
Oliveira, R. B.
[1]
;
Chagas-Paula, D. A.
[1]
;
Jorge, J. A.
[4]
;
Furtado, N. A. J. C.
[1]
;
Pupo, M. T.
[1]
;
Silva, C. H. T. P.
[1]
;
Naal, R. M. Z. G.
[2, 3]
;
Bastos, J. K.
[1]
Total Authors: 11
|
| Affiliation: | [1] Univ Sao Paulo, Dept Ciencias Farmaceut, BR-14040903 Sao Paulo - Brazil
[2] Univ Sao Paulo, Dept Quim & Fis, Fac Ciencias Farmaceut Ribeirao Preto, BR-14040903 Sao Paulo - Brazil
[3] Univ Estadual Campinas, Inst Nacl Ciencia & Tecnol Bioanalit, Sao Paulo - Brazil
[4] Univ Sao Paulo, Dept Biol, Fac Filosofia Ciencias & Letras Ribeirao Preto, BR-14040903 Sao Paulo - Brazil
Total Affiliations: 4
|
| Document type: | Journal article |
| Source: | NATURAL PRODUCT RESEARCH; v. 26, n. 23, p. 2168-2175, 2012. |
| Web of Science Citations: | 1 |
| 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. (AU) | |
| FAPESP's process: | 04/07935-6 - Bioprospection in fungi: the search of lead compounds for drug design and enzymes for pharmaceutical and industrial applications |
| Grantee: | Jairo Kenupp Bastos |
| Support Opportunities: | BIOTA-FAPESP Program - Thematic Grants |