Intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from Oxandra xylopioides leaves.

Autor: Gavilánez Buñay TC; Cátedra de Farmacología, Grupo de Farmacología Experimental y Energética Cardíaca (GFEYEC) y Maestría en Plantas Medicinales, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, La Plata, Argentina; Departamento de Ciencias de Agricultura y Recursos Naturales, Universidad Técnica de Cotopaxi, La Maná, Ecuador., Colareda GA; Cátedra de Farmacología, Grupo de Farmacología Experimental y Energética Cardíaca (GFEYEC) y Maestría en Plantas Medicinales, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, La Plata, Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas de la República Argentina (CONICET), Argentina., Ragone MI; Cátedra de Farmacología, Grupo de Farmacología Experimental y Energética Cardíaca (GFEYEC) y Maestría en Plantas Medicinales, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, La Plata, Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas de la República Argentina (CONICET), Argentina., Bonilla M; Cátedra de Farmacología, Grupo de Farmacología Experimental y Energética Cardíaca (GFEYEC) y Maestría en Plantas Medicinales, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, La Plata, Argentina., Rojano BA; Laboratorio de Ciencias de los Alimentos, Universidad Nacional de Colombia (sede Medellín), Colombia., Schinella GR; Cátedra de Farmacología Básica, Facultad de Ciencias Médicas, Universidad Nacional de La Plata. CIC-PBA, La Plata, Argentina., Consolini AE; Cátedra de Farmacología, Grupo de Farmacología Experimental y Energética Cardíaca (GFEYEC) y Maestría en Plantas Medicinales, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, La Plata, Argentina. Electronic address: dinamia@biol.unlp.edu.ar.
Jazyk: angličtina
Zdroj: Phytomedicine : international journal of phytotherapy and phytopharmacology [Phytomedicine] 2018 Dec 01; Vol. 51, pp. 20-28. Date of Electronic Publication: 2018 Jun 05.
DOI: 10.1016/j.phymed.2018.06.001
Abstrakt: Background: Isoespintanol is a monoterpene isolated from the leaves of Oxandra xylopioides Diels. (Annonaceae) with antioxidant and antiinflammatory effects. It was of interest to know whether it has antispasmodic effects such as other known drugs, phloroglucinol and trimethoxybenzene, used in therapeutics for treating biliary, urinary and uterine spasms.
Purpose: To assess whether isoespintanol possesses antispasmodic effects on intestine, uterus and bladder.
Study Design: A preclinical study was performed in which isoespintanol, phloroglucinol and trimethoxybenzene were evaluated with concentration-contractile response curves (CRC) of carbachol in isolated rat intestine and bladder, and with CRC of serotonin (5-HT) in rat uterus. Moreover, it was assessed whether isoespintanol interferes with Ca 2+ influx by making CRC of Ca 2+ in high-K + medium in intestine and bladder.
Results: Isoespintanol non-competitively inhibited the CRC of carbachol with affinity constant (pK) of 4.78 ± 0.09 in intestine and 4.60 ± 0.09 in bladder. Phloroglucinol and trimethoxybenzene were also non-competitive antagonists, but isoespintanol was 8 times more potent than trimethoxybenzene and similarly potent than phloroglucinol in intestine. In bladder, isoespintanol resulted 8 times more potent than trimethoxybenzene. The maximal inhibition of contraction followed the order of isoespintanol > trimethoxybenzene > phloroglucinol in intestine, and isoespintanol > trimethoxybenzene in bladder. Moreover, isoespintanol also completely and non-competitively inhibited the CRC of Ca 2+ , with a pK of 5.1 ± 0.1 in intestine, and 4.32 ± 0.07 in bladder. In uterus isoespintanol reduced, completely and non-competitively, the contraction produced by 5-HT with pK of 5.05 ± 0.07.
Conclusion: Results demonstrate that isoespintanol is a very good intestinal, urinary and uterine antispasmodic, with higher potency than the other drugs used in therapeutics. The mechanism of action of isoespintanol is the interference with Ca 2+ influx, at a difference of trimethoxybenzene and phloroglucinol.
(Copyright © 2018 Elsevier GmbH. All rights reserved.)
Databáze: MEDLINE
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