SIRT1 is a nicotinamide adenosine dinucleotide (NAD+)-dependent deacetylase, which removes
acetyl groups from many target proteins, such as histone proteins, transcription factors and cofactors.
SIRT1-catalyzed deacetylation of these factors modulates the activity of downstream proteins, thus
influencing many biological processes. SIRT1 is involved in the regulation of metabolism, inflammation,
and tumor growth. The activity of this enzyme is related to the beneficial health effects of calorie restriction,
such as lifespan extension and, in particular, the activation of SIRT1 has a positive impact on the cardiovascular
system. Therefore, SIRT1 is considered as an attractive drug target and modulation of SIRT1
may represent a new therapeutic strategy against cardiovascular diseases, as small molecules able to activate
SIRT1 can be considered as cardioprotective agents. In this review, we summarize both natural and
synthetic compounds developed as SIRT1 activators, with a focus on their promising therapeutic applications
in cardiovascular pathologies.