Withapubesides A-D: natural inducible nitric oxide synthase (iNOS) inhibitors from Physalis pubescens.
Org Biomol Chem
; 15(47): 10016-10023, 2017 Dec 06.
Article
em En
| MEDLINE
| ID: mdl-29164214
ABSTRACT
Four new steroid glycosides, withapubesides A-D (1-4), were isolated from the stems of Physalis pubescens L. Their structures were elucidated primarily by NMR experiments. The absolute configurations of 1 and 2 were deduced by single-crystal X-ray diffraction and ECD data analysis, respectively. Compound 3 has shown significant inhibitory activity against LPS-induced nitric oxide production in RAW 264.7 macrophages with an IC50 value of 12.8 µM and moderate cytostatic activity against human carcinoma cells (786-O, C4-2B, 22Rvl, A375 and A375S2) with IC50 values in the range of 3.05-9.47 µM. Molecular docking simulation demonstrated that 3 is bound in the inducible nitric oxide synthase (iNOS) active site heme pocket very well, which suggests that 3 might be a candidate for the development of iNOS inhibitors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Esteroides
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Inibidores Enzimáticos
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Óxido Nítrico Sintase Tipo II
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Citostáticos
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Glicosídeos
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Antineoplásicos Fitogênicos
Limite:
Animals
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Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article