Papain-like protease (PLpro) inhibitory effects of cinnamic amides from Tribulus terrestris fruits.
Biol Pharm Bull
; 37(6): 1021-8, 2014.
Article
em En
| MEDLINE
| ID: mdl-24882413
ABSTRACT
Tribulus terrestris fruits are well known for their usage in pharmaceutical preparations and food supplements. The methanol extract of T. terrestris fruits showed potent inhibition against the papain-like protease (PLpro), an essential proteolylic enzyme for protection to pathogenic virus and bacteria. Subsequent bioactivity-guided fractionation of this extract led to six cinnamic amides (1-6) and ferulic acid (7). Compound 6 emerged as new compound possessing the very rare carbinolamide motif. These compounds (1-7) were evaluated for severe acute respiratory syndrome coronavirus (SARS-CoV) PLpro inhibitory activity to identify their potencies and kinetic behavior. Compounds (1-6) displayed significant inhibitory activity with IC50 values in the range 15.8-70.1 µM. The new cinnamic amide 6 was found to be most potent inhibitor with an IC50 of 15.8 µM. In kinetic studies, all inhibitors exhibited mixed type inhibition. Furthermore, the most active PLpro inhibitors (1-6) were proven to be present in the native fruits in high quantities by HPLC chromatogram and liquid chromatography with diode array detection and electrospray ionization mass spectrometry (LC-DAD-ESI/MS).
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Base de dados:
MEDLINE
Assunto principal:
Proteínas Virais
/
Extratos Vegetais
/
Inibidores de Cisteína Proteinase
/
Cinamatos
/
Tribulus
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article