The novel inhibitory effect of Pangdahai on fatty acid synthase.
IUBMB Life
; 60(3): 185-94, 2008 Mar.
Article
em En
| MEDLINE
| ID: mdl-18380011
ABSTRACT
Recently, animal fatty acid synthase (FASN) is reported as a potential therapeutic target for obesity and cancer. Considerable interest has been developed in searching for novel inhibitors of this enzyme. An extract from Pangdahai has been found to inhibit FASN in both reversible and irreversible manners, with an IC(50) of 3.5 microg/ml and an apparent inactivation rate constant of k(obs) of 2.2 x 10(-3)/min. The kinetic study showed that the Pangdahai extract inhibited the overall FASN reaction uncompetitively with acetyl-CoA, but it presented in a mixed manner both with NADPH and with malonyl-CoA. Its major reacting site on this enzyme, as compared between two IC(50) values, is not in the beta-ketoacyl reduction domain. A weight reducing experiment in rats showed that the extract significantly reduced the adipose and food intake, but in view of statistics (P < 0.05), a correlation between the reductions in the adipose and in the food consumption and the inhibition of hepatic FASN could not be established. Three known flavonoid compounds were isolated from the extract and the structure-activity relationship was discussed.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Flavonoides
/
Medicamentos de Ervas Chinesas
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Inibidores Enzimáticos
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Ácido Graxo Sintases
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
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Humans
/
Male
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article