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J Ethnopharmacol ; 274: 114048, 2021 Jun 28.
Artículo en Inglés | MEDLINE | ID: mdl-33781875

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Plectranthus vettiveroides (Jacob) N.P. Singh & B.D. Sharma is a traditional medicinal plant used in Siddha System of Medicine and its aromatic root is used to reduce the elevated blood pressure. AIM: The aim of the present study was to study vasorelaxant property of the root essential oil nanoemulsion (EON) of P. vettiveroides. METHODS: The EON was formulated to enhance the solubility and bioavailability and characterized. The preliminary screening was performed by treating the EON with aortic rings pre-contracted with phenylephrine (1 µM) and potassium chloride (80 mM). The role of K⁺ channels in EON induced vasorelaxation was investigated by pre-incubating the aortic rings with different K⁺ channel inhibitors namely, glibenclamide (a non-specific ATP sensitive K⁺ channel blocker, 10 µM), TEA (a Ca2⁺ activated non-selective K⁺ channel blocker, 10-2 M), 4-AP (a voltage-activated K⁺ channel blocker, 10-3 M) and barium chloride (inward rectifier K⁺ channel blocker, 1 mM). The involvement of extracellular Ca2+ was performed by adding cumulative dose of extracellular calcium in the presence and absence of EON and the concentration-response curve (CRC) obtained is compared. Similarly, the role of nitric oxide synthase, muscarinic and prostacyclin receptors on EON induced vasorelaxation were evaluated by pre-incubating the aortic rings with their inhibitors and the CRC obtained in the presence and absence of inhibitor were compared. RESULTS: The GC-MS and GC-FID analyses of the root essential oil revealed the presence of 62 volatile compounds. The EON exhibited significant vasorelaxant effect through nitric oxide-mediated pathway, G-protein coupled muscarinic (M3) receptor pathway, involvement of K+ channels (KATP, KIR, KCa), and blocking of the calcium influx by receptor-operated calcium channel. CONCLUSION: It is concluded that the root essential oil of P. vettiveroides is possessing marked vasorelaxant property. The multiple mechanisms of action of the essential oil of P. vettiveroides make it a potential source of antihypertensive drug.


Asunto(s)
Antihipertensivos/farmacología , Aorta Torácica/efectos de los fármacos , Aceites Volátiles/farmacología , Plectranthus , Vasodilatadores/farmacología , Animales , Antihipertensivos/química , Aorta Torácica/fisiología , Calcio/fisiología , Canales de Calcio/fisiología , Emulsiones , Receptores de Inositol 1,4,5-Trifosfato/fisiología , Canales KATP/fisiología , Masculino , Óxido Nítrico/fisiología , Aceites Volátiles/química , Fitoquímicos/análisis , Fitoquímicos/farmacología , Raíces de Plantas , Canales de Potasio de Rectificación Interna/fisiología , Ratas Wistar , Receptor Muscarínico M3/fisiología , Vasodilatación/efectos de los fármacos , Vasodilatadores/química
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