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Natural phosphodiesterase-4 (PDE4) inhibitors from Crotalaria ferruginea.
- Source :
-
Fitoterapia . Apr2014, Vol. 94, p177-182. 6p. - Publication Year :
- 2014
-
Abstract
- Abstract: Bioassay-guided fractionation of the ethanol extract of the Chinese folk medicine Crotalaria ferruginea led to the isolation of a new isoflavonoid, 4′-hydroxy-2′-methylalpinum-isoflavone (1), and eight known analogs (2–9). Their structures were elucidated by spectroscopic analysis. Compounds 1, 2, 5, and 8 showed inhibitory activities against phosphodiesterase-4 (PDE4), a therapeutic target of asthma, with IC50 values ranging from 2.57 to 8.94μM. The possible action mechanism and the structure–activity relationship (SAR) of the active isoflavonoids were explored by using molecular docking and molecular dynamics (MD) simulation methods. Our study herein may explain the anti-inflammatory function of this plant in Chinese folk medicine. [Copyright &y& Elsevier]
- Subjects :
- *MEDICINAL plants
*ALTERNATIVE medicine
*ANTI-inflammatory agents
*BIOLOGICAL models
*PHYSICAL & theoretical chemistry
*DOSE-effect relationship in pharmacology
*FLAVONOIDS
*MOLECULAR biology
*SPECTRUM analysis
*PLANT extracts
*PHOSPHODIESTERASE inhibitors
*DESCRIPTIVE statistics
*IN vitro studies
*PHARMACODYNAMICS
Subjects
Details
- Language :
- English
- ISSN :
- 0367326X
- Volume :
- 94
- Database :
- Academic Search Index
- Journal :
- Fitoterapia
- Publication Type :
- Academic Journal
- Accession number :
- 95387061
- Full Text :
- https://doi.org/10.1016/j.fitote.2014.02.010