scholarly journals Effect of the Croton rhamnifolioides Essential Oil and the Inclusion Complex (OEFC/β-CD) in Antinociceptive Animal Models

Macromol ◽  
2021 ◽  
Vol 1 (2) ◽  
pp. 94-111
Author(s):  
Anita Oliveira Brito Pereira Bezerra Martins ◽  
Maria Rayane Correia de Oliveira ◽  
Isabel Sousa Alcântara ◽  
Lindaiane Bezerra Rodrigues ◽  
Francisco Rafael Alves Santana Cesário ◽  
...  
Keyword(s):  
Essential Oil ◽  
Inclusion Complex ◽  
Antinociceptive Effect ◽  
Hot Plate ◽  
Cyclodextrin Inclusion ◽  
Antinociceptive Effects ◽  
Plate Models ◽  
Leaf Essential Oil ◽  
The Central Nervous System ◽  
Therapy Of Pain

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.

scholarly journals Antinociceptive and anti-inflammatory effect of Lippia pedunculosa Hayek essential oil and its β-cyclodextrin inclusion complex

2021 ◽  
Vol 20 (2) ◽  
pp. 162-176
Author(s):  
Renan Marinho Braga ◽  
◽  
Humberto Hugo Nunes de Andrade ◽  
Humberto de Carvalho Aragao Neto ◽  
Ryldene Marques Duarte da Cruz ◽  
...  
Keyword(s):  
Essential Oil ◽  
Inclusion Complex ◽  
Antinociceptive Effect ◽  
Experimental Models ◽  
Complex Formulation ◽  
Cyclodextrin Inclusion ◽  
Leucocyte Migration ◽  
Prevalence Of Pain ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Lippia pedunculosa Hayek (EOLp) presents tripanocid and amebicid effects. However essential oil needs to be further studied in experimental models of analgesia and inflammation once the prevalence of pain in the population generates great suffering and disability and the drugs most often used have undesirable side effects. We also evaluated whether the inclusion complex formulation EOLp/β-cyclodextrin (β-CD) was able to improve the antinociceptive activity of the EOLp alone. Data were evaluated by analysis of variance (ANOVA), followed by Tukey’s test. Differences were considered significant if p<0.05. EOLp presented better antinociceptive effect when compared to the EOLp/β-CD inclusion complex. Thus, cyclodextrins appear not to be efficient for essential oils with peroxide substances. However, in peritonitis, EOLp reduced total leucocyte migration and IL-1β levels in the peritoneal fluid, which confirmed its anti-inflammatory effect. The observed effects suggest that EOLp is the best promising option for the treatment of inflammation and pain-related disorders.

scholarly journals Preparation, Characterization, and Pharmacological Activity ofCymbopogon winterianusJowitt ex Bor (Poaceae) Leaf Essential Oil ofβ-Cyclodextrin Inclusion Complexes

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Priscila L. Santos ◽  
Adriano A. S. Araújo ◽  
Jullyana S. S. Quintans ◽  
Makson G. B. Oliveira ◽  
Renan G. Brito ◽  
...  
Keyword(s):  
Essential Oil ◽  
Motor Coordination ◽  
Antinociceptive Effect ◽  
Nociceptive Behavior ◽  
Scanning Calorimetry ◽  
Standard Drug ◽  
Main Compound ◽  
Rota Rod Test ◽  
Leaf Essential Oil ◽  
The Central Nervous System

This study aimed to evaluate the orofacial antinociceptive effect of theCymbopogon winterianusessential oil (LEO) complexed inβ-cyclodextrin (LEO-CD) and to assess the possible involvement of the central nervous system (CNS). The LEO was extracted, chromatographed, and complexed inβ-cyclodextrin. The complex was characterized by differential scanning calorimetry (DSC) and thermogravimetry derivative (TG/DTG). Male Swiss mice (2-3 months) were treated with LEO-CD (50–200 mg/kg, p.o.), vehicle (distilled water, p.o.), or standard drug (i.p.) and subjected to the orofacial nociception formalin-, capsaicin-, and glutamate-induced. After the formalin test, the animals were perfused and the brains subjected to immunofluorescence for Fos. The rota-rod test (7 rpm/min) was carried out. Geraniol (37.57%) was the main compound of LEO. DSC and TG/DTG proved the complexation. The orofacial nociceptive behavior was significantly (p<0.05) reduced. The number of Fos-positive cells was significantly changed in the dorsal raphe nucleus (p<0.01), locus coeruleus (p<0.001), trigeminal nucleus (p<0.05), and trigeminal thalamic tract (p<0.05). LEO-CD did not cause changes in motor coordination in the rota-rod test. Thus, our results suggested that LEO-CD has an orofacial antinociceptive profile, probably mediated by the activation of the CNS without changing the motor coordination.

scholarly journals Aristolochia trilobata: Identification of the Anti-Inflammatory and Antinociceptive Effects

Biomedicines ◽  
2020 ◽  
Vol 8 (5) ◽  
pp. 111
Author(s):  
Dayana da Costa Salomé ◽  
Natália de Morais Cordeiro ◽  
Tayná Sequeira Valério ◽  
Darlisson de Alexandria Santos ◽  
Péricles Barreto Alves ◽  
...  
Keyword(s):  
Enzyme Inhibitor ◽  
Interleukin 1 ◽  
Antinociceptive Effect ◽  
Cholinergic Receptor ◽  
Hot Plate ◽  
Nitric Oxide Synthase Inhibitor ◽  
Antinociceptive Effects ◽  
Anti Inflammatory ◽  
Skin Affection ◽  
Synthase Inhibitor

Aristolochia trilobata, popularly known as “mil-homens,” is widely used for treatment of stomach aches, colic, asthma, pulmonary diseases, diabetes, and skin affection. We evaluated the antinociceptive and anti-inflammatory activities of the essential oil (EO) and the main constituent, 6-methyl-5-hepten-2-yl acetate (sulcatyl acetate, SA). EO and SA (1, 10, and 100 mg/kg, p.o.) were evaluated using chemical (formalin-induced licking) and thermal (hot-plate) models of nociception or inflammation (carrageenan-induced cell migration into the subcutaneous air pouch, SAP). The mechanism of antinociceptive activity was evaluated using opioid, cholinergic receptor antagonists (naloxone and atropine), or nitric oxide synthase inhibitor (L-NAME). EO and SA presented a central antinociceptive effect (the hot-plate model). In formalin-induced licking response, higher doses of EO and SA also reduced 1st and 2nd phases. None of the antagonists and enzyme inhibitor reversed antinociceptive effects. EO and SA reduced the leukocyte migration into the SAP, and the cytokines tumor necrosis factor and interleukin-1 (TNF-α and IL-1β, respectively) produced in the exudate. Our results are indicative that EO and SA present peripheral and central antinociceptive and anti-inflammatory effects.

scholarly journals Comparison of antinociceptive effect of the antiepileptic drug gabapentin to that of various dosage combinations of gabapentin with lamotrigine and topiramate in mice and rats

2011 ◽  
Vol 02 (02) ◽  
pp. 130-136 ◽  
Author(s):  
Keshab Raj Paudel ◽  
SK Bhattacharya ◽  
GP Rauniar ◽  
BP Das
Keyword(s):  
Pain Perception ◽  
Late Phase ◽  
Antinociceptive Effect ◽  
Experimental Pain ◽  
Mechanical Hyperalgesia ◽  
Tail Flick ◽  
Hot Plate ◽  
Analgesic Effects ◽  
Pain Models ◽  
Antinociceptive Effects

ABSTRACT Introduction: Newer anticonvulsants have a neuromodulatory effect on pain perception mechanisms in a hyperexcitable and damaged nervous system. Aim: This study was designed to study the analgesic effects of gabapentin alone and in combination with lamotrigine and topiramate in experimental pain models. Materials and Methods: Adult albino mice (n = 490) weighing 20–30 g and rats (n = 130) weighing 100–200 g were injected intraperitoneally with gabapentin, lamotrigine, and topiramate alone and in different dose combinations. The hot-plate method, tail-flick method, capsaicin-induced mechanical hyperalgesia, and formalin assay were used to assess the antinociceptive effects. Results: Of the three antiepileptic drugs, when given separately, gabapentin was more efficacious than either topiramate or lamotrigine in all the pain models. Combination of 25 mg/kg gabapentin with 25 mg/kg topiramate was more efficacious (P <.05) than 50 mg/kg gabapentin alone in the capsaicin-induced mechanical hyperalgesia test. Similarly, 50 mg/kg gabapentin with 50 mg/kg topiramate or 5 mg/kg lamotrigine was more efficacious (P <.05) than 50 or 100 mg/kg gabapentin alone in late-phase formalin-induced behaviors. Conclusions: Combination of gabapentin with either lamotrigine or topiramate produced better results than gabapentin alone in capsaicin-induced mechanical hyperalgesia test and in late-phase formalin-induced behaviors.

Thermal analysis and gas chromatography coupled mass spectrometry analyses of hydroxypropyl-β-cyclodextrin inclusion complex containing Lippia gracilis essential oil

2008 ◽  
Vol 475 (1-2) ◽  
pp. 53-58 ◽  
Author(s):  
Ricardo N. Marreto ◽  
Elis E.C.V. Almeida ◽  
Péricles B. Alves ◽  
Edenilson S. Niculau ◽  
Rogéria S. Nunes ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Thermal Analysis ◽  
Gas Chromatography ◽  
Essential Oil ◽  
Inclusion Complex ◽  
Cyclodextrin Inclusion ◽  
Cyclodextrin Inclusion Complex

The mineralocorticoid receptor antagonist spironolactone enhances morphine antinociception

2013 ◽  
Vol 4 (4) ◽  
pp. 259-259
Author(s):  
Viljami Jokinen ◽  
Tuomas O. Lilius ◽  
Mikko S. Neuvonen ◽  
Antti J. Väänänen ◽  
Mikko O. Niemi ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Morphine Tolerance ◽  
Tail Flick ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Mineralocorticoid Receptor Antagonist ◽  
P Glycoprotein ◽  
Antinociceptive Effects ◽  
The Brain ◽  
Glycoprotein Inhibition

Abstract Aims Spironolactone, an antimineralocorticoid, has been reported to potentiate the cataleptic effect of morphine in the rat. Since no previous research exists on the matter and the interaction might be clinically significant, the effects of spironolactone on morphine antinociception and pharmacokinetics in the rat were investigated. Methods Male SD rats were used to assess the effects of spironolactone on acute morphine-induced antinociception, development of morphine tolerance, and established morphine tolerance in the tail-flick and hot plate tests. Spironolactone was also administered with loperamide to assess whether spironolactone enhances the brain distribution of the acknowledged P-glycoprotein substrate across the blood-brain barrier. Results Spironolactone had no antinociceptive effects of its own but when co-administrated with morphine the antinociceptive effect of morphine was greatly enhanced. Morphine concentrations in the brain were increased fourfold in the spironolactone co-administrated group. Spironolactone did not inhibit the formation of pro-nociceptive morphine-3-glucuronide, nor did inhibit the development of tolerance. The peripherally restricted opioid, loperamide, had no antinociceptive effects by itself, but co-administration with spironolactone produced a clear change in the hot plate test. Conclusions Although mineralocorticoids have been proposed to take part in pain signaling, in our setting spironolactone did not have antinociceptive properties of its own. The increased antinociceptive effect of morphine is apparently caused by the increased morphine brain concentrations. We suggest this to be due to P-glycoprotein inhibition, as indicated by the loperamide assay. The clinical relevance of P-glycoprotein inhibition by spironolactone should be studied.

scholarly journals Characterization of the Antinociceptive Activity from Stevia serrata Cav

Biomedicines ◽  
2020 ◽  
Vol 8 (4) ◽  
pp. 79
Author(s):  
Millena S. Cordeiro ◽  
Daniel L. R. Simas ◽  
Juan F. Pérez-Sabino ◽  
Max S. Mérida-Reyes ◽  
Manuel A. Muñoz-Wug ◽  
...  
Keyword(s):  
Essential Oil ◽  
Mechanism Of Action ◽  
Enzyme Inhibitor ◽  
Antinociceptive Effect ◽  
Area Under The Curve ◽  
Treated Group ◽  
Hot Plate ◽  
Gastrointestinal Problems ◽  
Higher Doses

Background: Stevia serrata Cav. (Asteraceae), widely found in Guatemala, is used to treat gastrointestinal problems. The aim of this study was to demonstrate the antinociceptive and anti-inflammatory effects of the essential oil (EO) and the mechanism of action. Methods: EO was tested in chemical (capsaicin- and glutamate-induced licking response) or thermal (hot plate) models of nociception at 10, 30 or 100 mg/kg doses. The mechanism of action was evaluated using two receptor antagonists (naloxone, atropine) and an enzyme inhibitor (L-NAME). The anti-hyperalgesic effect was evaluated using carrageenan-induced nociception and evaluated in the hot plate. Results: All three doses of EO reduced licking response induced by glutamate, and higher doses reduced capsaicin-induced licking. EO also increased area under the curve, similar to the morphine-treated group. The antinociceptive effect induced by EO was reversed by pretreatment of mice with naloxone (1 mg/kg, ip), atropine (1 mg/kg, ip) or L-NAME (3 mg/kg, ip). EO also demonstrated an anti-hyperalgesic effect. The 100 mg/kg dose increased the latency time, even at 1 h after oral administration and this effect has been maintained until the 96th hour, post-administration. Conclusions: Our data suggest that essential oil of S. serrata presents an antinociceptive effect mediated, at least in part, through activation of opioid, cholinergic and nitrergic pathways.

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