Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats

Background: Ayanin (3,7,4’-Tri-O-methylquercetin) and 3,7-Di-O-methylquercetin (DMQ) are the main active metabolites isolated by bioguided fractionation from Croton schiedeanus, species known popularly in Colombia as “almizclillo”, which has been studied in experimental models in rats, exerting vas...

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Autores principales:	Mario Francisco Guerrero Pabón, Alejandra P Ortiz S., Dra. Pilar Puebla Ibáñez
Formato:	article
Lenguaje:	EN
Publicado:	Universidad de Antioquia 2021
Materias:	Ayanin, Flavonoids Nitric oxide Guanylate cyclase Synergism Croton. Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675
Acceso en línea:	https://doaj.org/article/751f1f2968f544c591200579958bce15
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spelling	oai:doaj.org-article:751f1f2968f544c591200579958bce152021-12-02T18:20:59ZVascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats10.17533/udea.vitae.v28n2a3439230121-40042145-2660https://doaj.org/article/751f1f2968f544c591200579958bce152021-05-01T00:00:00Zhttps://revistas.udea.edu.co/index.php/vitae/article/view/343923https://doaj.org/toc/0121-4004https://doaj.org/toc/2145-2660 Background: Ayanin (3,7,4’-Tri-O-methylquercetin) and 3,7-Di-O-methylquercetin (DMQ) are the main active metabolites isolated by bioguided fractionation from Croton schiedeanus, species known popularly in Colombia as “almizclillo”, which has been studied in experimental models in rats, exerting vasodilator and antihypertensive effects. Also, when the effect of these flavonoids was studied separately, important vasodilation was observed. Objective: To evaluate whether flavonoids from Croton schiedeanus have synergistic vasodilator properties when different combinations are used in isolated aorta rings. Methods: Cumulative concentrations of ayanin (10-8 M - 6x10-5 M or 0.01 μM - 60 μM) were assayed in the absence and presence of an increasing concentration of 3,7-Di-O-methylquercetin (DMQ) (10-8 – 3x10-5 M or 0.01–30 μM) in isolated rings from Wistar rats, pre-contracted with phenylephrine. The concentration-response curve with the maximal effect was compared with that obtained by Croton schiedeanus whole ethanolic extract (10-6 – 3x10-4 g/mL). Also, this combination was assayed in the presence of the nitric oxide synthetase inhibitor L-NAME (10-4 M) and the guanylate cyclase inhibitor methylene blue (10-4 M) to assess the role of the NO/cGMP pathway in this interaction. Results: Ayanin and DMQ display a dual interaction in vascular relaxant response: agonism at higher concentration ranges (10-6 – 3x10-5 M or 1–30 μM) and antagonism at lower concentration ranges (10-8 – 3x10-7 M or 0.01–0.3 μM). The efficacy at the highest concentration was greater than that obtained by the whole extract (Emax: 98.4% vs. 33.9%). This response was decreased but not reverted in the presence of L-NAME and methylene blue. Thus, the vasodilator effect of this combination does not depend entirely on the NO/cGMP cyclic pathway. Conclusion: The combined use of appropriate concentrations of these flavonoids could represent an advantage over Croton schiedeanus whole extract for vasodilator purposes. Mario Francisco Guerrero PabónAlejandra P Ortiz S.Dra. Pilar Puebla IbáñezUniversidad de AntioquiaarticleAyanin,FlavonoidsNitric oxideGuanylate cyclaseSynergismCroton.Food processing and manufactureTP368-456Pharmaceutical industryHD9665-9675ENVitae, Vol 28, Iss 2 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Ayanin, Flavonoids Nitric oxide Guanylate cyclase Synergism Croton. Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675
spellingShingle	Ayanin, Flavonoids Nitric oxide Guanylate cyclase Synergism Croton. Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675 Mario Francisco Guerrero Pabón Alejandra P Ortiz S. Dra. Pilar Puebla Ibáñez Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats
description	Background: Ayanin (3,7,4’-Tri-O-methylquercetin) and 3,7-Di-O-methylquercetin (DMQ) are the main active metabolites isolated by bioguided fractionation from Croton schiedeanus, species known popularly in Colombia as “almizclillo”, which has been studied in experimental models in rats, exerting vasodilator and antihypertensive effects. Also, when the effect of these flavonoids was studied separately, important vasodilation was observed. Objective: To evaluate whether flavonoids from Croton schiedeanus have synergistic vasodilator properties when different combinations are used in isolated aorta rings. Methods: Cumulative concentrations of ayanin (10-8 M - 6x10-5 M or 0.01 μM - 60 μM) were assayed in the absence and presence of an increasing concentration of 3,7-Di-O-methylquercetin (DMQ) (10-8 – 3x10-5 M or 0.01–30 μM) in isolated rings from Wistar rats, pre-contracted with phenylephrine. The concentration-response curve with the maximal effect was compared with that obtained by Croton schiedeanus whole ethanolic extract (10-6 – 3x10-4 g/mL). Also, this combination was assayed in the presence of the nitric oxide synthetase inhibitor L-NAME (10-4 M) and the guanylate cyclase inhibitor methylene blue (10-4 M) to assess the role of the NO/cGMP pathway in this interaction. Results: Ayanin and DMQ display a dual interaction in vascular relaxant response: agonism at higher concentration ranges (10-6 – 3x10-5 M or 1–30 μM) and antagonism at lower concentration ranges (10-8 – 3x10-7 M or 0.01–0.3 μM). The efficacy at the highest concentration was greater than that obtained by the whole extract (Emax: 98.4% vs. 33.9%). This response was decreased but not reverted in the presence of L-NAME and methylene blue. Thus, the vasodilator effect of this combination does not depend entirely on the NO/cGMP cyclic pathway. Conclusion: The combined use of appropriate concentrations of these flavonoids could represent an advantage over Croton schiedeanus whole extract for vasodilator purposes.
format	article
author	Mario Francisco Guerrero Pabón Alejandra P Ortiz S. Dra. Pilar Puebla Ibáñez
author_facet	Mario Francisco Guerrero Pabón Alejandra P Ortiz S. Dra. Pilar Puebla Ibáñez
author_sort	Mario Francisco Guerrero Pabón
title	Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats
title_short	Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats
title_full	Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats
title_fullStr	Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats
title_full_unstemmed	Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats
title_sort	vascular interactions of croton schiedeanus major flavonoids in isolated aortic rings from wistar rats
publisher	Universidad de Antioquia
publishDate	2021
url	https://doaj.org/article/751f1f2968f544c591200579958bce15
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Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats

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