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Bioorg Med Chem Lett ; 26(12): 2755-2759, 2016 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-27210437

RESUMEN

Three new withanolides, physaperuvin G (1), with physaperuvins I (2), and J (3), along with seven known derivatives (4-10), were isolated from the aerial parts of Physalis peruviana. The structures of 1-3 were determined by NMR, X-ray diffraction, and mass spectrometry. Compounds 1-10 were evaluated in lipopolysaccharide (LPS)-activated murine macrophage RAW 264.7 cells. Compounds 4, 5, and 10 with potent nitric oxide inhibitory activity in LPS-activated RAW 264.7 cells, with IC50 values in the range of 0.32-7.8µM. In addition, all compounds were evaluated for potential to inhibit tumor necrosis factor-alpha (TNF-α)-activated nuclear factor-kappa B (NF-κB) activity with transfected human embryonic kidney cells 293. Compounds 4-7 inhibited TNF-α-induced NF-κB activity with IC50 values in the range of 0.04-5.6µM.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , FN-kappa B/antagonistas & inhibidores , Physalis/química , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores , Witanólidos/farmacología , Animales , Antiinflamatorios no Esteroideos/síntesis química , Antiinflamatorios no Esteroideos/química , Línea Celular , Relación Dosis-Respuesta a Droga , Células HEK293 , Humanos , Ratones , Modelos Moleculares , Conformación Molecular , FN-kappa B/metabolismo , Relación Estructura-Actividad , Factor de Necrosis Tumoral alfa/metabolismo , Witanólidos/síntesis química , Witanólidos/química
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