Erucin exhibits vasorelaxing effects and antihypertensive activity by H2S-releasing properties

被引：56

作者：

Martelli, Alma ^{[1
,5
]}

Piragine, Eugenia ^{[1
]}

Citi, Valentina ^{[1
]}

Testai, Lara ^{[1
,5
]}

Pagnotta, Eleonora ^{[2
]}

Ugolini, Luisa ^{[2
]}

Lazzeri, Luca ^{[2
]}

Di Cesare Mannelli, Lorenzo ^{[3
]}

Manzo, Onorina Laura ^{[4
]}

Bucci, Mariarosaria ^{[4
]}

Ghelardini, Carla ^{[3
]}

Breschi, Maria Cristina ^{[1
]}

Calderone, Vincenzo ^{[1
,5
,6
]}

机构：

[1] Univ Pisa, Dept Pharm, Via Bonanno 6, I-56126 Pisa, Italy

[2] Council Agr Res & Econ, Res Ctr Cereal & Ind Crops, Bologna, Italy

[3] NEUROFARBA Sect Pharmacol & Toxicol, Dept Neurosci Psychol Drug Res & Child Drug Res, Florence, Italy

[4] Univ Naples Federico II, Dept Pharm, Naples, Italy

[5] Univ Pisa, Interdept Res Ctr Nutraceut & Food Hlth NUTRAFOOD, Pisa, Italy

[6] Univ Pisa, Interdept Res Ctr Ageing Biol & Pathol, Pisa, Italy

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 2020年 / 177卷 / 04期

关键词：

HYDROGEN-SULFIDE; BLOOD-PRESSURE; RESISTANT HYPERTENSION; CONCISE GUIDE; NITRIC-OXIDE; H2S DONORS; PHARMACOLOGY; ISOTHIOCYANATES; BIOAVAILABILITY; SULFORAPHANE;

D O I：

10.1111/bph.14645

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Background and Purpose Hydrogen sulfide (H2S)-releasing agents are viewed as potential antihypertensive drugs. Recently, natural isothiocyanates emerged as original H2S-donor agents. Among them, erucin, present in some edible cruciferous plants, shows suitable H2S-releasing properties and features of "druggability." The aim of this work was to investigate the erucin-mediated release of H2S inside vascular cells, its vasorelaxing effects, and activity on BP of normo and hypertensive animals. Experimental Approach Intracellular H2S-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 H2S 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 H2S 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

引用

页码：824 / 835

页数：12

共 48 条

[41] Hydrogen sulfide in hypertension [J].