Vascular endothelium plays an important role in the physiological homeostasis of blood vessels. Endothelial injury is considered to be implicated in the pathogenesis of many
cardiovascular diseases, including
atherosclerosis.
Farrerol, a
flavonoid considered to be the major bioactive component in a traditional Chinese herb, "Man-shan-hong", which is the dried leaves of Rhododendron dauricum L., displays many bioactive properties, including antibechic, antibacterial, anti-inflammatory, and the inhibition of vascular smooth muscle cell (VSMC) proliferation. In this study, the protective effects of
farrerol on
hydrogen peroxide (H2O2)-induced apoptosis in human endothelium-derived EA.hy926 cells were investigated. The results showed that
farrerol significantly inhibited the loss of cell viability and enhanced
superoxide dismutase (SOD) and
glutathione peroxidase (GSH-Px) activities in H2O2-induced EA.hy926 cells. Meanwhile,
farrerol inhibited H2O2-induced elevation in the levels of intracellular
malondialdehyde and
reactive oxygen species, as well as cell apoptosis. Furthermore, real time RT-PCR and Western blot analysis showed that
farrerol significantly decreased the expression of Bax
mRNA, Bax, cleaved
caspase-3, and phosph-p38 MAPK, while increasing the exporession of Bcl-2
mRNA and Bcl-2 in H2O2-induced EA.hy926 cells. These results are the first demonstration that
farrerol has protective effects against H2O2-induced apoptosis in EA.hy926 cells, and suggests that
farrerol is a potential candidate for the intervention of endothelial-injury-associated
cardiovascular diseases.