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1.
Molecules ; 21(8)2016 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-27517895

RESUMO

Two ergostanes, 5α,8α-epidioxy-22E-ergosta-6,22-dien-3ß-ol (1) and 5α-ergost-7,22-dien-3ß-ol (2), and a lanostane, 3ß-hydroxylanostan-8,24-diene-21-oic acid (trametenolic acid) (3), were isolated from an n-hexane extract prepared from the fruiting body of Trametes versicolor (Bres. Rivarden). The activity of the isolated sterols was evaluated against promastigotes and amastigotes of Leishmania amazonensis Lainson and Shaw, 1972. The lanostane, compound (3), showed the best inhibitory response (IC50 promastigotes 2.9 ± 0.1 µM and IC50 amastigotes 1.6 ± 0.1 µM). This effect was 25-fold higher compared with its cytotoxic effect on peritoneal macrophages from BALB/c mice. Therefore, trametenolic acid could be regarded as a promising lead for the synthesis of compounds with antileishmanial activity.


Assuntos
Esteróis/farmacologia , Trametes/química , Tripanossomicidas/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Carpóforos/química , Leishmania/efeitos dos fármacos , Macrófagos Peritoneais/efeitos dos fármacos , Camundongos , Estrutura Molecular , Esteróis/química , Esteróis/isolamento & purificação , Tripanossomicidas/química , Tripanossomicidas/isolamento & purificação
2.
Int J Med Mushrooms ; 17(5): 463-9, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26082985

RESUMO

In vitro anti-inflammatory activity of 4 extracts with different polarity from the basidiomycete Navisporus floccosus was evaluated by determination of the inhibition of prostaglandin E2 formation catalyzed by purified cyclooxygenase (COX)-1 and COX-2 enzymes, and of the inhibition of leukotriene (LT) B4 formation in human polymorphonuclear leukocytes. The n-hexane extract showed the highest activity in all 3 assays. Through analysis by gas chromatography coupled with mass spectrometry (GC-MS), 9 fatty acids and fatty acid esters were identified as the major constituents of this extract. As several of them also showed inhibitory activity in the COX and LTB4 formation assays, it can be assumed that the unsaturated as well as the saturated fatty acids, and maybe also the fatty acid esters, present in the extract synergistically contribute to its in vitro anti-inflammatory activity.


Assuntos
Anti-Inflamatórios/farmacologia , Ácidos Araquidônicos/metabolismo , Basidiomycota/química , Ácidos Graxos/isolamento & purificação , Anti-Inflamatórios/análise , Anti-Inflamatórios/isolamento & purificação , Ácidos Araquidônicos/antagonistas & inibidores , Ciclo-Oxigenase 1/efeitos dos fármacos , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/antagonistas & inibidores , Dinoprostona/metabolismo , Ácidos Graxos/química , Cromatografia Gasosa-Espectrometria de Massas , Hexanos , Humanos , Leucotrieno B4/antagonistas & inibidores , Neutrófilos/efeitos dos fármacos , Neutrófilos/metabolismo , Farmacognosia
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