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Aristoteline, an Indole-Alkaloid, Induces Relaxation by Activating Potassium Channels and Blocking Calcium Channels in Isolated Rat Aorta.
Romero, Fernando; Palacios, Javier; Jofré, Ignacio; Paz, Cristian; Nwokocha, Chukwuemeka R; Paredes, Adrián; Cifuentes, Fredi.
Afiliação
  • Romero F; Vicerrectoría de Investigación y Postgrado, Programa de Doctorado en Ciencias Médicas, Universidad de la Frontera, Temuco 4780000, Chile. fernando.romero@ufrontera.cl.
  • Palacios J; Laboratorio de Bioquímica Aplicada, Departamento de Química y Farmacia, Facultad Ciencias de la Salud, Universidad Arturo Prat, Iquique 1110939, Chile. clpalaci@unap.cl.
  • Jofré I; Laboratorio de Neurociencias y Biología de Péptidos, Centro de Excelencia en Biotecnología de La Reproducción, Facultad de Medicina, Universidad de La Frontera, Temuco 4811230, Chile.
  • Paz C; Laboratorio de Productos Naturales y Descubrimiento de Fármacos, Departamento de Ciencias básicas, Universidad de La Frontera, Temuco 4811230, Chile.
  • Nwokocha CR; Department of Basic Medical Sciences Physiology Section, Faculty of Medical Sciences, The University of the West Indies, Mona, Kingston 7, KGN, Jamaica (W.I.).
  • Paredes A; Laboratorio de Química Biológica, Instituto Antofagasta, Universidad de Antofagasta, Antofagasta 1270300, Chile.
  • Cifuentes F; Laboratorio de Fisiología Experimental, Instituto Antofagasta, Universidad de Antofagasta, Antofagasta 1270300, Chile.
Molecules ; 24(15)2019 Jul 29.
Article em En | MEDLINE | ID: mdl-31362388
Alkaloids derived from plants have shown great medicinal benefits, and are often reported for their use in cardiovascular disease management. Aristotelia chilensis (Molina) Stuntz (Maqui) has shown important medicinal properties in traditional useage. In this study, we evaluated the effect of the indole-alkaloid aristoteline (ARI), isolated from leaves of Maqui, on vascular reactivity of isolated aortic rings from normotensive rats. ARI induced relaxation (100%) in a concentration-dependent manner in intact or denuded-endothelium aortic rings pre-contracted with phenylephrine (PE; 1 µM). However, a specific soluble guanylyl cyclase inhibitor (ODQ; 1 µM) significantly reduced the relaxation to ARI in aortic rings pre-contracted with PE. In the presence of ARI, the contraction induced by KCl or PE was significantly (p < 0.05) decreased. Interestingly, the potassium channel blockade with 10 µM BaCl2 (Kir), 10 µM glibenclamide (KATP), 1 mM tetraethylammonium (TEA; KCa1.1), or 1 mM 4-aminopyridine (4-AP; Kv) significantly (p < 0.05) reduced the ARI-induced relaxation. ARI significantly (p < 0.05) reduced the contractile response to agonist of CaV1.2 channels (Bay K8644; 10 nM), likely reducing the influx of extracellular calcium through plasma membrane. The mechanisms associated with this process suggest an activation of the potassium channels, a calcium-induced antagonism and endothelium independent vasodilation that possibly involves the nitric oxide-independent soluble guanylate cyclase pathway.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Bloqueadores dos Canais de Cálcio / Canais de Cálcio / Canais de Potássio / Alcaloides Limite: Animals Idioma: En Revista: Molecules Assunto da revista: BIOLOGIA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Chile País de publicação: Suíça
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Bloqueadores dos Canais de Cálcio / Canais de Cálcio / Canais de Potássio / Alcaloides Limite: Animals Idioma: En Revista: Molecules Assunto da revista: BIOLOGIA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Chile País de publicação: Suíça