The circadian clock regulates many aspects of (patho)physiology in the central nervous system and in the peripheral tissues. RAR-related orphan receptor α (RORα), an
orphan nuclear receptor, is involved in circadian rhythm regulation, including regulation of cardiovascular function.
Bavachalcone, a prenylchalcone, is a major bioactive
chalcone isolated from Psoralea corylifolia. This natural ingredient activated RORα1
luciferase reporter activity on
drug screening. In addition,
bavachalcone induced RORα1 expression in
mRNA and
protein levels in a dose-dependent manner and enhanced the circadian amplitude of Bmal1
mRNA expression after serum
shock. Moreover,
bavachalcone suppressed senescence in human endothelial cells and
mRNA expression of
p16(ink4a) (a marker of replicative senescence) and IL-1α (a proinflammatory
cytokine of the senescence-associated secretory phenotype). These inhibitory effects were partially reversed by the RORα inhibitor VPR-66. Our results demonstrate that
bavachalcone, as a natural medicine ingredient, has a pharmacological function in regulating RORα1.