Autor según el artículo: Guerrero, Ligia; Castillo, Julian; Quinones, Mar; Garcia-Vallve, Santiago; Arola, Lluis; Pujadas, Gerard; Muguerza, Begona;
Departamento: Bioquímica i Biotecnologia
Autor/es de la URV: Arola Ferrer, Luis Maria / Garcia Vallve, Santiago / Muguerza Marquínez, Maria Begoña / Pujadas Anguiano, Gerard
Resumen: Previous studies have demonstrated that certain flavonoids can have an inhibitory effect on angiotensin-converting enzyme (ACE) activity, which plays a key role in the regulation of arterial blood pressure. In the present study, 17 flavonoids belonging to five structural subtypes were evaluated in vitro for their ability to inhibit ACE in order to establish the structural basis of their bioactivity. The ACE inhibitory (ACEI) activity of these 17 flavonoids was determined by fluorimetric method at two concentrations (500 µM and 100 µM). Their inhibitory potencies ranged from 17 to 95% at 500 µM and from 0 to 57% at 100 µM. In both cases, the highest ACEI activity was obtained for luteolin. Following the determination of ACEI activity, the flavonoids with higher ACEI activity (i.e., ACEI >60% at 500 µM) were selected for further IC50 determination. The IC50 values for luteolin, quercetin, rutin, kaempferol, rhoifolin and apigenin K were 23, 43, 64, 178, 183 and 196 µM, respectively. Our results suggest that flavonoids are an excellent source of functional antihypertensive products. Furthermore, our structure-activity relationship studies show that the combination of sub-structures on the flavonoid skeleton that increase ACEI activity is made up of the following elements: (a) the catechol group in the B-ring, (b) the double bond between C2 and C3 at the C-ring, and (c) the cetone group in C4 at the C-ring. Protein-ligand docking studies are used to understand the molecular basis for these results.
Áreas temáticas: Zootecnia / recursos pesqueiros Sociology Sociología Serviço social Saúde coletiva Química Psychology Psicología Planejamento urbano e regional / demografia Odontología Nutrição Multidisciplinary sciences Multidisciplinary Medicine (miscellaneous) Medicina veterinaria Medicina iii Medicina ii Medicina i Materiais Matemática / probabilidade e estatística Linguística e literatura Letras / linguística Interdisciplinary research in the social sciences Interdisciplinar Human geography and urban studies History & philosophy of science Historia Geografía Geociências General medicine General biochemistry,genetics and molecular biology General agricultural and biological sciences Farmacia Environmental studies Ensino Engenharias iv Engenharias iii Engenharias ii Engenharias i Enfermagem Educação física Educação Economia Direito Demography Comunicação e informação Ciências sociais aplicadas i Ciências biológicas iii Ciências biológicas ii Ciências biológicas i Ciências ambientais Ciências agrárias i Ciência política e relações internacionais Ciência de alimentos Ciência da computação Biotecnología Biology Biodiversidade Biochemistry, genetics and molecular biology (miscellaneous) Astronomia / física Arquitetura, urbanismo e design Archaeology Antropologia / arqueologia Anthropology Agricultural and biological sciences (miscellaneous) Administração, ciências contábeis e turismo Administração pública e de empresas, ciências contábeis e turismo
Acceso a la licencia de uso: https://creativecommons.org/licenses/by/3.0/es/
Direcció de correo del autor: santi.garcia-vallve@urv.cat gerard.pujadas@urv.cat lluis.arola@urv.cat begona.muguerza@urv.cat
Identificador del autor: 0000-0002-0348-7497 0000-0003-2598-8089 0000-0003-2767-1974 0000-0001-7384-8588
Fecha de alta del registro: 2024-11-16
Versión del articulo depositado: info:eu-repo/semantics/publishedVersion
Enlace a la fuente original: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0049493
URL Documento de licencia: https://repositori.urv.cat/ca/proteccio-de-dades/
Referencia al articulo segun fuente origial: Plos One. 7 (11): e49493-e49493
Referencia de l'ítem segons les normes APA: Guerrero, Ligia; Castillo, Julian; Quinones, Mar; Garcia-Vallve, Santiago; Arola, Lluis; Pujadas, Gerard; Muguerza, Begona; (2012). Inhibition of Angiotensin-Converting Enzyme Activity by Flavonoids: Structure-Activity Relationship Studies. Plos One, 7(11), e49493-e49493. DOI: 10.1371/journal.pone.0049493
DOI del artículo: 10.1371/journal.pone.0049493
Entidad: Universitat Rovira i Virgili
Año de publicación de la revista: 2012
Tipo de publicación: Journal Publications