6 research outputs found
Erucin exhibits vasorelaxing effects and antihypertensive activity by H2 S-releasing properties.
BACKGROUND AND PURPOSE: Hydrogen sulfide (H2 S)-releasing agents are viewed as
potential antihypertensive drugs. Recently, natural isothiocyanates emerged as
original H2 S-donor agents. Among them, erucin, present in some edible
cruciferous plants, shows suitable H2 S-releasing properties and features of
"druggability." The aim of this work was to investigate the erucin-mediated
release of H2 S inside vascular cells, its vasorelaxing effects, and activity on
BP of normo and hypertensive animals.
EXPERIMENTAL APPROACH: Intracellular H2 S-release and the hyperpolarizing effect
of erucin were tested using fluorescent dye, in human aortic smooth muscle cells
(HASMCs). Its direct vasorelaxing effect and ability to inhibit
noradrenaline-induced vasoconstriction were evaluated on endothelium-intact or
-denuded rat aortic rings. Its vasodilator properties were tested in coronary
arteries using Langendorff-perfused rat hearts. Finally, erucin's
antihypertensive activity was evaluated in vivo in normotensive and spontaneously
hypertensive rats (SHRs) by recording systolic BP using the tail-cuff method.
KEY RESULTS: Erucin induced the release of H2 S inside HASMCs. Moreover, erucin
hyperpolarized the membrane of HASMCs membrane in a concentration-dependent
manner. It induced vasodilatation of rat aortic rings, in endothelium-denuded
vessels. This effect was further improved by the presence of endothelial NO. When
pre-incubated with rat aortic rings, erucin induced concentration-dependent
inhibition of noradrenaline-induced vasoconstriction. Erucin did not affect basal
coronary flow but restored the flow to normal in pre-contracted coronary vessels.
Finally, in vivo, erucin decreased systolic BP in SHRs by about 25%, and restored
the BP to values observed in normotensive rats.
CONCLUSIONS AND IMPLICATIONS: Erucin is an H2 S donor endowed with vasorelaxing
and antihypertensive effects