Mechanism of the Antihypertensive and Vasorelaxant Effects of the
                    Flavonoid Tiliroside in Resistance Arteries

Grazielle C. Silva; Aline C. Pereira; Bruno A. Rezende; José P. Felippe da Silva; Jader S. Cruz; Maria de Fátima V. de Souza; Roosevelt A. Gomes; Yanna C. F. Teles; Steyner F. Cortes; Virginia S. Lemos

doi:10.1055/s-0032-1328765

Planta Medica, Inhaltsverzeichnis

Planta Med 2013; 79(12): 1003-1008
DOI: 10.1055/s-0032-1328765

Biological and Pharmacological Activity

Original Papers

Georg Thieme Verlag KG Stuttgart · New York

Mechanism of the Antihypertensive and Vasorelaxant Effects of the Flavonoid Tiliroside in Resistance Arteries

Grazielle C. Silva

¹Department of Pharmacology, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil

,

Aline C. Pereira

²Department of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil

,

Bruno A. Rezende

²Department of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil

,

José P. Felippe da Silva

²Department of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil

,

Jader S. Cruz

³Department of Biochemistry and Immunology, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil

,

Maria de Fátima V. de Souza

⁴Department of Pharmaceutical Sciences, Health Sciences Center, Universidade Federal da Paraíba, João Pessoa, PB, Brazil

,

Roosevelt A. Gomes

⁴Department of Pharmaceutical Sciences, Health Sciences Center, Universidade Federal da Paraíba, João Pessoa, PB, Brazil

,

Yanna C. F. Teles

⁴Department of Pharmaceutical Sciences, Health Sciences Center, Universidade Federal da Paraíba, João Pessoa, PB, Brazil

,

Steyner F. Cortes

¹Department of Pharmacology, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil

,

Virginia S. Lemos

²Department of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil

› Institutsangaben

Abstract

Hypertension is a leading cause of death and disability globally, and its prevalence continues to accelerate. The cardiovascular effects of the flavonoid tiliroside have never been reported. In this work, using complementary in vivo and in vitro approaches, we describe the antihypertensive effect of tiliroside and the underlying mechanisms involved in the reduction of blood pressure. Tiliroside (1, 5 or 10 mg/kg) induced a dose-dependent long-lasting decrease in blood pressure in conscious DOCA-salt hypertensive rats that was accompanied by an increased heart rate. Tiliroside also induced a concentration-dependent vasodilation of mesenteric resistance arteries precontracted with phenylephrine. Removal of the endothelium or pretreatment of the preparation with L-NAME or indomethacin did not modify the vasodilator response for tiliroside. When vessels were precontracted with a high K⁺ (50 mM) solution, tiliroside exhibited a vasodilator effect similar to that observed in vessels precontracted with phenylephrine. Experiments carried out in nominally Ca²⁺-free solution showed that tiliroside antagonized CaCl₂-induced contractions. Moreover, tiliroside reduced the rise in intracellular Ca²⁺ concentration induced by membrane depolarization in vascular smooth muscle cells. Finally, tiliroside decreased the voltage-activated peak amplitude of the L-type Ca²⁺ channel current in freshly dissociated vascular smooth muscle cells from mesenteric arteries. Altogether, our results point to an antihypertensive effect of tiliroside due to a reduction in peripheral resistance through blockage of voltage-activated peak amplitude of the L-type Ca²⁺ channel in smooth muscle cells.

Key words

flavonoids - tiliroside - antihypertensive effect - vasodilation - mesenteric artery - Ca_V 1.2

Volltext

Referenzen

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