Protección cardiovascular con flavonoidesenigma farmacocinético

  1. Juan Duarte
  2. Francisco Pérez-Vizcaíno
Revista:
Ars pharmaceutica

ISSN: 2340-9894,  0004-2927

Año de publicación: 2015

Volumen: 56

Número: 4

Páginas: 193-200

Tipo: Artículo

DOI: 10.4321/S2340-98942015000400002 DIALNET GOOGLE SCHOLAR lock_openAcceso abierto editor

Otras publicaciones en: Ars pharmaceutica

Resumen

Objetivos: Los flavonoides ejercen efectos beneficiosos en la prevención de las enfermedades cardiovasculares. En esta revisión trataremos de clarificar algunas preguntas fundamentales respecto a la eficacia, mecanismo de acción y biodisponibilidad de uno de los flavonoides dietéticos más abundante, la quercetina. Métodos: Se utilizó la base de datos de la National Library of Medicine, Washington, DC (MEDLINE: PubMed). Se recopilaron todos los estudios en animales y en humanos disponibles online desde la creación de la base de datos hasta Noviembre de 2015. Resultados: La quercetina produce un efecto vasodilatador y antihipertensor en modelos animales y en individuos hipertensos. Es eficaz en todos los modelos de hipertensión analizados, independientemente del origen de la hipertensión, del estado del sistema renina-angiotensina, del estrés oxidativo, del óxido nítrico y de otros factores. Paradójicamente, a pesar de ejercer efectos sistémicos biológicamente demostrables, no se encuentra en el plasma tras su administración oral y sus metabolitos circulantes muestran una débil actividad in vitro. La quercetina es extensamente metabolizada en derivados metilados y glucurono- y sulfo-conjugados, que son las formas circulantes en el plasma; y glucurono-, pero no sulfo-conjugados, pueden ser hidrolizados a nivel vascular, produciendo la aglicona matriz que se acumula en los tejidos. La conjugación es un proceso reversible y, al menos con respecto a los efectos vasodilatador y antihipertensivo, el ciclo de conjugación-deconjugación parece ser un requisito absoluto. Conclusiones: Los glucurono-conjugados transportan la quercetina y su forma metilada, y liberan en los tejidos la aglicona libre, que es el efector final.

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Fuente de los datos: Dialnet