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Antihypertensive and vasorelaxant effect of leucodin and achillin isolated from Achillea millefolium through calcium channel blockade and NO production: In vivo, functional ex vivo and in silico studies.
- Source :
-
Journal of ethnopharmacology [J Ethnopharmacol] 2021 Jun 12; Vol. 273, pp. 113948. Date of Electronic Publication: 2021 Feb 19. - Publication Year :
- 2021
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Abstract
- Ethnopharmacological Relevance: Achillea millefolium L. (Asteraceae), known as yarrow (milenrama), is a plant used in Mexican traditional medicine for the treatment of hypertension, diabetes, and related diseases.<br />Aim: To determine the vasorelaxant and antihypertensive effect of A. millefollium and to isolate the main bioactive antihypertensive agents.<br />Materials and Methods: Organic (hexane, dichloromethane and methanol) and hydro-alcohol (Ethanol-H <subscript>2</subscript> O: 70:30) extracts obtained from flowers, leaves and stems were evaluated on isolated aorta rat rings with and without endothelium to determine their vasorelaxant effect. Hexane extract from flowers (HEAmF) was studied to evaluate its antihypertensive effect on spontaneously hypertensive rats (SHR). From HEAmF, bioactive compounds were obtained by bio-guided phytochemical separation through chromatography.<br />Results: Organic extracts showed the best vasorelaxant activity. Hexane extract from flowers was the most potent and efficient ex vivo vasorelaxant agent, showing significant decrease of systolic and diastolic blood pressure in SHR (p < 0.05). Phytochemical separation of HEAmF yielded two epimeric sesquiterpene lactones: leucodin (1) and achillin (2), the major components of the extract. Both 1 and 2 showed similar vasorelaxant action ex vivo (p < 0.05), and their effects where modified by L-NAME (10 μM, nitric oxide synthase inhibitor), by ODQ (1 μM, soluble guanylyl cyclase inhibitor), and also relaxed the contraction induced by KCl (80 mM). Finally, 1 and 2 intragastric administration (50 mg/kg) decreased systolic and diastolic blood pressure in SHR.<br />Conclusions: Achillea millefolium showed antihypertensive and vasorelaxant effects, due mainly to leucodin and achillin (epimers). Both compounds showed antihypertensive activity by vasorelaxation putatively by endothelium-dependent NO release and cGMP increase, as well as by calcium channels blockade.<br /> (Copyright © 2021 Elsevier B.V. All rights reserved.)
- Subjects :
- Animals
Antihypertensive Agents therapeutic use
Aorta drug effects
Blood Pressure drug effects
Calcium Channel Blockers therapeutic use
Calcium Channels metabolism
Computer Simulation
Heart Rate drug effects
Male
NG-Nitroarginine Methyl Ester pharmacology
Nitric Oxide metabolism
Nitric Oxide Synthase Type III chemistry
Oxadiazoles pharmacology
Plant Extracts therapeutic use
Quinoxalines pharmacology
Rats, Inbred SHR
Rats, Wistar
Sesquiterpenes chemistry
Sesquiterpenes isolation & purification
Sesquiterpenes therapeutic use
Vasodilator Agents therapeutic use
Rats
Achillea chemistry
Antihypertensive Agents pharmacology
Calcium Channel Blockers pharmacology
Plant Extracts pharmacology
Sesquiterpenes pharmacology
Vasodilator Agents pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1872-7573
- Volume :
- 273
- Database :
- MEDLINE
- Journal :
- Journal of ethnopharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 33610712
- Full Text :
- https://doi.org/10.1016/j.jep.2021.113948