Erucin exhibits vasorelaxing effects and antihypertensive activity by H2S‐releasing properties. - GreenMedInfo Summary

BACKGROUND AND PURPOSE: Hydrogen sulfide (HS)-releasing agents are viewed as potential antihypertensive drugs. Recently, natural isothiocyanates emerged as original HS-donor agents. Among them, erucin, present in some edible cruciferous plants, shows suitable HS-releasing properties and features of "druggability." The aim of this work was to investigate the erucin-mediated release of HS inside vascular cells, its vasorelaxing effects, and activity on BP of normo and hypertensive animals.

EXPERIMENTAL APPROACH: Intracellular HS-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 HS 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 HS donor endowed with vasorelaxing and antihypertensive effects.

LINKED ARTICLES: This article is part of a themed section on Hydrogen Sulfide in Biology&Medicine. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v177.4/issuetoc.