THE PHARMACOLOGICAL EFFECT OF STILBENES ISOLATED FROM KANGAROO ISLAND PROPOLIS ON SIRT-1 ENZYME ACTIVITY
Keywords:
SIRT-1 enzyme, Resveratrol, Piceatannol, Tetrahydroxystilbenes, Stilbenes, PropolisAbstract
Objective: Resveratrol, a trihydroxystilbene, has been claimed to be a potent activator to SIRT-1 enzyme activity, which in turn could have a useful future application in the management of many chronic conditions such as metabolic syndrome and obesity. A group of novel tetrahydroxystilbene derivatives were isolated from Kangaroo Island propolis in Australia. Due to its structural similarities with resveratrol, the aim of this research was to explore the activity of Kangaroo Island prenylated stilbenes on SIRT-1 enzyme.
Methods: In vitro fluorometry measurement of SIRT-1 enzyme activity using SIRT-1 assay kit (Cayman®).
Results: None of the tested compounds had shown any activation to SIRT-1 enzyme, on contrary, they produced mild inhibition to the enzyme. Compound 3 (C20H22O4, 3,5,4'-trihydroxy-3'-methoxy-2-prenyl-E-stilbene) was the most potent inhibitor.
Conclusion: Compound 3, in addition to compounds 2, 4, and 6 are candidate compounds for further investigation. A discussion of the results as well as the contradictory results in the literature has been presented in this article.Â
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