Erucin exhibits vasorelaxing effects and antihypertensive activity by H 2 S-releasing properties

Background and Purpose: Hydrogen sulfide (H 2 S)-releasing agents are viewed as potential antihypertensive drugs. Recently, natural isothiocyanates emerged as original H 2 S-donor agents. Among them, erucin, present in some edible cruciferous plants, shows suitable H 2 S-releasing properties and features of “druggability.” The aim of this work was to investigate the erucin-mediated release of H 2 S inside vascular cells, its vasorelaxing effects, and activity on BP of normo and hypertensive animals. Experimental Approach: Intracellular H 2 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 H 2 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 H 2 S donor endowed with vasorelaxing and antihypertensive effects.