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.

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

Martelli, A.
Primo
;
Piragine, E.;Citi, V.;Testai, L.;Di Cesare Mannelli, L.;Ghelardini, C.;Breschi, M. C.;Calderone, V.
Ultimo
2020-01-01

Abstract

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.
2020
Martelli, A.; Piragine, E.; Citi, V.; Testai, L.; Pagnotta, E.; Ugolini, L.; Lazzeri, L.; Di Cesare Mannelli, L.; Manzo, O. L.; Bucci, M.; Ghelardini, C.; Breschi, M. C.; Calderone, V.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/990113
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