Abstract
This study aims to evaluate the antinociceptive effect of the C. rhamnifolioides leaf essential oil (OEFC) and the β-cyclodextrin inclusion complex (COEFC) and investigate the pain signaling pathways involved in the antinociceptive response. The effects of the OEFC and COEFC on the central nervous system (CNS) were determined by open field and rota-rod assays, and the antinociceptive effect was evaluated via the acetic acid-induced abdominal contortions, formalin, and hot plate models. Swiss (Mus musculus) male mice (20–30 g) were used in both trials. The OEFC (200 mg/kg/v.o-orally) and COEFC (83.5 mg/kg/v.o.) did not present alterations in the CNS. The OEFC (25, 50, 100, and 200 mg/kg/vo.) and COEFC (8.35, 41.75, and 83.5 mg/kg/v.o.) demonstrated antinociceptive effects in the abdominal contortions, formalin, and hot plate tests. The OEFC (25 mg/kg/v.o.) and COEFC (8.35 mg/kg/v.o.) doses showed that the antinociceptive effect involves the activation of the opioid, cholinergic, and vanilloid systems, as well as the L-arginine/NO and α-2 adrenergic receptor pathways. The antinociceptive potential the OEFC and COEFC demonstrate possible alternatives for the therapy of pain. However, the COEFC presented more significant effects at lower doses than the isolated OEFC, where this action may be justified by the properties and advantages of the complexation.
Highlights
The Croton rhamnifolioides species belonging to the Croton genus and Euphorbiaceae family is known in popular medicine as “quebra-faca” or “caatinga-branca”, where the first name refers to the stiffness of its trunk, while the second refers to its aroma and stem color.This species is used for the treatment of stomachaches, gastric upset, vomiting, bloody diarrhea, and to reduce fever [1]
The essential oil was analyzed by gas-phase chromatography coupled to mass spectrometry (GC/MS) and the complexations were characterized by different physical methods as differential scanning calorimetry (DSC), TG/DTG, Karl Fischer method, and electronic microscope
Given the results presented in the present study, the OEFC and COEFC may act on α2-adrenergic receptors, given the reversal of their antinociceptive effect when these were associated with the selective antagonist; when the OEFC and COEFC were evaluated with respect to α1-adrenergic receptors, neither one presented an effect
Summary
The Croton rhamnifolioides species belonging to the Croton genus and Euphorbiaceae family is known in popular medicine as “quebra-faca” or “caatinga-branca”, where the first name refers to the stiffness of its trunk, while the second refers to its aroma and stem color. This species is used for the treatment of stomachaches, gastric upset, vomiting, bloody diarrhea, and to reduce fever [1]. Essential oils complexed with cyclodextrins are considered as important in medicinal chemistry due to changes in physicochemical properties, which allow the administration of lower doses and, a reduction in side effects [6]. Cyclodextrins possess unique physicochemical properties, including the ability to solubilize in aqueous media and simultaneously encapsulate hydrophobic molecules within their cavity [7], facilitating the transfer of hydrophobic guest molecules from a solution to lipophilic cell membranes, promoting absorption [8], in addition to having the ability to improve the bioavailability of some substances [9], which is associated with solubility, dissolution, and permeability that is promoted indirectly to the guest drug [10]
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