Background:: The endothelium is a monolayer of cells that extends on the vascular inner surface, responsible for the modulation of vascular tone. By means of the release of nitric oxide (NO), the endothelium has an important protective function against cardiovascular diseases.

Objective:: Verify if cis- [Ru(bpy)2(NO2)(NO)](PF6)2 (BPY) improves endothelial function and the sensibility of conductance (aorta) and resistance (coronary) to vascular relaxation induced by BPY.

Methods:: Normotensive (2K) and hypertensive (2K-1C) Wistar rats were used. For vascular reactivity study, thoracic aortas were isolated, rings with intact endothelium were incubated with: BPY(0.01 to10 µM) and concentration effect curves to acetylcholine were performed. In addition, cumulative concentration curves were performed to BPY (1.0 nM to 0.1 µM) in aortic and coronary rings, with intact and denuded endothelium.

Results:: In aorta from 2K-1C animals, the treatment with BPY 0.1µM increased the potency of acetylcholine-induced relaxation and it was able to revert the endothelial dysfunction. The presence of the endothelium did not modify the effect of BPY in inducing the relaxation in aortas from 2K and 2K-1C rats. In coronary, the endothelium potentiated the vasodilator effect of BPY in vessels from 2K and 2K-1C rats.

Conclusion:: Our results suggest that 0.1 µM of BPY is able to normalize the relaxation endothelium dependent in hypertensive rats, and the compound BPY induces relaxation in aortic from normotensive and hypertensive rats with the same potency. The endothelium potentiate the relaxation effect induced by BPY in coronary from normotensive and hypertensive rats, with lower effect on coronary from hypertensive rats.

Fundamento:: O endotélio é uma monocamada de células que se estende sobre a superfície interna vascular, responsável pela modulação do tônus vascular. Por meio da liberação de óxido nítrico (NO), o endotélio tem uma função protetora importante contra doenças cardiovasculares.

Objetivo:: Verificar se o cis- [Ru (BPY)2 (NO2) (NO)] (PF6) 2 (BPY) melhora a função endotelial e a sensibilidade da condutância (aorta) e da resistência (coronária) ao relaxamento vascular induzido por BPY.

MÉtodos:: Foram utilizados ratos Wistar normotensos (2K) e hipertensos (2K-1C). Para o estudo de reatividade vascular, as aortas torácicas foram isoladas, os anéis com endotélio intacto foram incubados com: BPY (0,01 a 10 µM) e se realizaram curvas de efeito de concentração para acetilcolina. Adicionalmente, foram feitas curvas de concentração cumulativas para BPY (1,0 nM a 0,1 µM) nos anéis aórticos e coronários, com endotélio intacto e nu.

Resultados:: Na aorta de animais 2K-1C, o tratamento com BPY 0,1 µM aumentou a potência do relaxamento induzido pela acetilcolina e foi capaz de reverter a disfunção endotelial. A presença do endotélio não modificou o efeito da BPY na indução do relaxamento em aortas de ratos 2K e 2K-1C. Na coronária, o endotélio potencializou o efeito vasodilatador do BPY em vasos de ratos 2K e 2K-1C.

ConclusÃo:: Nossos resultados sugerem que 0,1 µM de BPY é capaz de normalizar o relaxamento dependente do endotélio em ratos hipertensos, e o composto BPY induz relaxamento na aorta de ratos normotensos e hipertensos com a mesma potência. O endotélio potencializa o efeito de relaxamento induzido pela BPY em coronárias de ratos normotensos e hipertensos, com menor efeito em coronárias de ratos hipertensos.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5576116PMC
http://dx.doi.org/10.5935/abc.20170090DOI Listing

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