Abstract
BackgroundXylopia frutescens Aubl. (embira, semente-de-embira or embira-vermelha), is used in folk medicine as antidiarrheal. The essential oil from its leaves (XF-EO) has been found to cause smooth muscle relaxation. Thus, the aim of this study was to investigate the spasmolytic action by which XF-EO acts on guinea pig ileum.MethodsThe components of the XF-EO were identified by gas chromatography-mass spectrometry. Segments of guinea pig ileum were suspended in organ bath containing modified Krebs solution at 37 °C, bubbled with carbogen mixture under a resting tension of 1 g. Isotonic contractions were registered using kymographs and isometric contractions using force transducer coupled to an amplifier and computer. Fluorescence measurements were obtained with a microplate reader using Fluo-4.ResultsForty-three constituents were identified in XF-EO, mostly mono- and sesquiterpenes. XF-EO has been found to cause relaxation on guinea pig ileum. The essential oil inhibited in a concentration-dependent manner both CCh- and histamine-induced phasic contractions, being more potent on histamine-induced contractions as well as antagonized histamine-induced cumulative contractions in a non-competitive antagonism profile. XF-EO relaxed in a concentration-dependent manner the ileum pre-contracted with KCl and histamine. Since the potency was smaller in organ pre-contracted with KCl, it was hypothesized that XF-OE would be acting as a K+ channel positive modulator. In the presence of CsCl (non-selective K+ channel blocker), the relaxant potency of XF-OE was not altered, indicating a non-participation of these channels. Moreover, XF-EO inhibited CaCl2-induced cumulative contractions in a depolarizing medium nominally without Ca2+ and relaxed the ileum pre-contracted with S-(-)-Bay K8644 in a concentration-dependent manner, thus, was confirmed the inhibition of Ca2+ influx through Cav1 by XF-EO. In cellular experiments, the viability of longitudinal layer myocytes from guinea pig ileum was not altered in the presence of XF-OE and the Fluo-4-associated fluorescence intensity in these intestinal myocytes stimulated by histamine was reduced by the essential oil, indicating a [Ca2+]c reduction.ConclusionSpasmolytic action mechanism of XF-EO on guinea pig ileum can involve histaminergic receptor antagonism and Ca2+ influx blockade, which results in [Ca2+]c reduction leading to smooth muscle relaxation.
Highlights
IntroductionXylopia frutescens Aubl. (embira, semente-de-embira or embira-vermelha), is used in folk medicine as antidiarrheal
Xylopia frutescens Aubl., is used in folk medicine as antidiarrheal
Identification of essential oil components Forty-three compounds of the XF-OE were identified by GC-MS, most of them being represented by monoterpenes (18 %) and sesquiterpenes (67.5 %)
Summary
Xylopia frutescens Aubl. (embira, semente-de-embira or embira-vermelha), is used in folk medicine as antidiarrheal. The aim of this study was to investigate the spasmolytic action by which XF-EO acts on guinea pig ileum. Diarrhea is characterized by change in bowel movements with symptoms of increment in water content, volume and frequency of stool [1] It is the second leading cause of death in children under five years old, and it is responsible for around 760.000 children deaths every year [2]. For this reason, international organizations have encouraged studies pertaining to treatment and prevention of diarrheal diseases using traditional medicinal practices [3]. The present study aimed to evaluate the spasmolytic activity and possible mechanism of action of the essential oil from X. frutescens (XF-EO) on guinea pig ileum, to ascertain ethnopharmacological claims
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