Tracheal relaxation through calcium channel blockade of Achillea millefolium hexanic extract and its main bioactive compounds.

Autor: Arias-Durán L; Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico., Estrada-Soto S; Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico. Electronic address: enoch@uaem.mx., Hernández-Morales M; Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico., Chávez-Silva F; Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico., Navarrete-Vázquez G; Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico., León-Rivera I; Centro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico., Perea-Arango I; Centro de Investigación en Biotecnología, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico., Villalobos-Molina R; Unidad de Biomedicina, Facultad de Estudios Superiores Iztacala, Universidad Nacional Autónoma de México, Tlalnepantla, Estado de México, 54090, Mexico., Ibarra-Barajas M; Unidad de Biomedicina, Facultad de Estudios Superiores Iztacala, Universidad Nacional Autónoma de México, Tlalnepantla, Estado de México, 54090, Mexico.
Jazyk: angličtina
Zdroj: Journal of ethnopharmacology [J Ethnopharmacol] 2020 May 10; Vol. 253, pp. 112643. Date of Electronic Publication: 2020 Feb 05.
DOI: 10.1016/j.jep.2020.112643
Abstrakt: Ethnopharmacological Importance: Achillea millefolium L. (Asteraceae) is used for the treatment of respiratory diseases, diabetes, and hypertension.
Aim: to explore its tracheal relaxant properties and clarify its functional mechanism of action on smooth muscle cells, which allow us to propose it as a potential anti-asthmatic drug.
Material and Methods: organic and hydro-alcoholic extracts from A. millefolium were obtained by macerations, then their relaxing effect on ex vivo isolated rat trachea rings was determined. Most active extract (hexanic extract, EHAm) was studied to determine its functional mechanism of action using synergic, antagonist and inhibitor agents related with the contraction/relaxation process of the smooth muscle. Also, EHAm was subjected to bio-guided fractionation by open-column chromatography (on silica gel) using cyclohexane-EtOAc (80:20) in an isocratic way to isolate main bioactive compounds.
Results: organic and hydro-alcoholic extracts showed relaxant effect in a concentration-response dependent manner, being EHAm the most active. The functional mechanism of action indicates that EHAm induced a non-competitive antagonism to the muscarinic receptors ; in addition, the NO/cGMP pathway is involved in the relaxation process of the tracheal smooth muscle. However, the most important mechanism of action showed by EHAm was related with the calcium channel blockade influx into the smooth muscle cells. On the other hand, epimeric sesquiterpene lactones leucodin (1) and achillin (2) were isolated and purified, which are responsible for the observed smooth muscle relaxant activity of the extract.
Conclusion: hexanic extract of A. millefollium induced a significant relaxant effect on tracheal rat rings by calcium channel blockade and NO release.
Competing Interests: Declaration of competing interest The authors declare no conflict of interest. Author contributions to the paper were as follows: Extracts preparation, and leucodin and achillin isolation: L. A-D., M. H-M, F. Ch-S. Structural elucidation: G. N–V., I. L-R. Pharmacological evaluation: R. V-M., M. I–B., L. A-D., S. E-S. Identification and recollection of plant material: I. P-A. Study design: S. E-S. Manuscript preparation: all authors. Notes: The authors declare no competing financial interest.
(Copyright © 2020 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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