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Bioorg Med Chem Lett ; 27(20): 4765-4769, 2017 10 15.
Artigo em Inglês | MEDLINE | ID: mdl-28911817

RESUMO

Because of the critical role of over-activated microglia in the progress of neurodegenerative diseases, it has been selected as a potential therapeutic target for drug discovery. In order to find natural neuroinflammatory inhibitors, we carried out a bioactivity-oriented phytochemical research of Caragana turfanensis Kom. (Krassn.), which is a folk medicine widely distributed in Xinjiang. As a result, a new coumarin lactone caraganolide A (1) and 35 known components were characterized from the effective extract of C. turfanensis. Furthermore, their anti-neuroinflammatory effects were evaluated in LPS-induced BV2 microglial cells using Griess assay to determine the release of nitric oxide (NO). Compounds 1, 2, 4-6, 9, 13-15, 20, 29 and 30 exhibited significant inhibitory activities and no obvious cytotoxicities were observed at their effective concentrations. It is noteworthy, the new compound caraganolide A (1) (IC50 1.01±1.57µM) and 3',7,8-trihydroxy-4'-methoxyisoflavone (5) (IC506.87±2.23µM) exhibited more excellent action than that of positive control minocycline (IC50 9.07±0.86µM).


Assuntos
Anti-Inflamatórios/química , Caragana/química , Cumarínicos/química , Extratos Vegetais/química , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Caragana/metabolismo , Linhagem Celular , Cumarínicos/isolamento & purificação , Cumarínicos/metabolismo , Concentração Inibidora 50 , Lipopolissacarídeos/toxicidade , Espectroscopia de Ressonância Magnética , Microglia/citologia , Microglia/efeitos dos fármacos , Microglia/metabolismo , Conformação Molecular , Óxido Nítrico/metabolismo
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