scholarly journals Quercetin action on pain modulation/ Ação da quercetina sobre a modulação da dor

2021 ◽  
Vol 7 (4) ◽  
pp. 43616-43634
Author(s):  
Maria Elvira Ribeiro Cordeiro ◽  
Flávio Klinpovous Kerppers ◽  
Luiza Ferreira Cunha ◽  
Ketllin Bragnholo ◽  
Luana Rodrigues Vasconcelos ◽  
...  

Background: Quercetin is a flavonoid widely found in plant kingdom and target of studies in pharmacological area due to its potent antinociceptive effect compared to analgesics used in conventional therapies. The aim was to evaluate its antinociceptive activity and antinociception mechanism. Methods: For this, 40 Norvegicus Wistar rats were used, divided into 4 groups: Q50 (treated with quercetin 50 mg/Kg), Q100 (treated with quercetin 100 mg/Kg), Q500 (treated with quercetin 500 mg/Kg) and Positive control (PC) without quercetin treatment), who were submitted through the pain induction methods by tail immersion and formalin in the first step to assess antinociceptive action and in the second step, tail immersion method receiving antagonists from opioid, cholinergic and nitric oxide - L-arginine to evaluate the action mechanism. Results: Quercetin antinociceptive activity was verified at the dose of 50 mg/kg and 100 mg/kg in tail immersion test after formalin injection, with better performance at the dose of 50 mg/kg. There were no statistically significant results in paw opening and capsaicin tests. Quercetin demonstrated a possible influence on opioid and cholinergic pathway, which was not observed on the nitric acid - L-arginine pathway in view of parameters tested. Conclusion: Quercetin performed the best antinociceptive activity at a dose 50 mg/kg and there was a possible influence on opioid and cholinergic pathways.

2021 ◽  
Vol 7 (4) ◽  
pp. 43667-43682
Author(s):  
Flávio Klinpovous Kerppers ◽  
Maria Elvira Ribeiro Cordeiro ◽  
Tatiane Budniak Mazur ◽  
Heron Bittencourt ◽  
Karoline Penteado da Luz ◽  
...  

Introduction: The use of medicinal plants for therapeutic purposes has been common practice since antiquity. Ruta graveolens L., commonly known as rue, has been shown to have antiparasitic, antioxidant, antibacterial and allelopathic activity. Objective: The objective was to investigate the antinociceptive effect of rue, as well as the mechanisms behind this effect. Materials and Methods: The sample consisted of 40 male Norvegicus (Wistar) rats, randomly divided into a positive control and three treatment groups administered Ruta graveolens L. aqueous extract at the following doses: 50 mg/kg, 100 mg/kg or 500 mg/kg, p.o. The experimental models of nociception used in this study to assess effectiveness of the treatments were the formalin and capsaicin tests. Five days prior to nociceptive challenges, the tail immersion assay was conducted to determine baseline pain threshold. Results: Antinociceptive activity was observed at Ruta graveolens L. aqueous extract concentrations of 50 mg/kg and 100mg/kg. 500 mg/kg induced pro-nociceptive activity with activation of the L-arginine-oxide-nitric system. Conclusion: These results suggest Ruta graveolens L. aqueous extract antinociceptive activity, and possible antagonism towards receptors


2016 ◽  
Vol 88 (3) ◽  
pp. 1471-1484
Author(s):  
GLAUCIEMAR DEL-VECHIO-VIEIRA ◽  
BRUNA C.S. SANTOS ◽  
MARIA SILVANA ALVES ◽  
AÍLSON L.A. ARAÚJO ◽  
CÉLIA H. YAMAMOTO ◽  
...  

ABSTRACT The present study was designed to investigate the antioxidant, antinociceptive and anti-inflammatory activities of the ethanol extract from Ageratum fastigiatum branches. Phytochemical screening and total phenol and flavonoid contents were determined. The antioxidant activity was assessed by 2,2-diphenyl-1-pycrilhydrazin (DPPH) and iron reducing power methods. The antinociceptive effect was evaluated using the acetic acid-induced writhing, formalin, hot plate and tail immersion assays; while the carrageenan-induced paw edema and pleurisy tests were performed to examine the anti-inflammatory activity against acute inflammation. The extract revealed the presence of flavonoids, tannins, coumarins, terpenes, sterols and saponins. Expressive levels of total phenols and flavonoids and a promising antioxidant effect were quantified. At the doses of 50, 100 and 200 mg/kg, the extract inhibited the writhing, reduced both phases of paw licking time and increased the reaction time on the hot plate. In the tail immersion test, the extract (50, 100 and 200 mg/kg) caused a significant inhibition of pain. In these doses, the paw edema, exudate volume and leucocyte mobilization were significantly reduced. These results suggest that A. fastigiatum can be an active source of substances with antioxidant, antinociceptive and anti-inflammatory activities, adding scientific support to the appropriate use in the Brazilian folk medicine.


2018 ◽  
Vol 68 (1) ◽  
pp. 108-118 ◽  
Author(s):  
Savić Vujović Katarina ◽  
Vučković Sonja ◽  
Stojanović Radan ◽  
Divac Nevena ◽  
Medić Branislava ◽  
...  

Abstract Ketamine and magnesium can interact in additive, supra-additive and antagonistic manners in analgesia or anesthesia. Ketamine is a non-competitive NMDA receptor antagonist. Magnesium is an endogenous non-competitive NMDA antagonist that causes anion channel blockade in a dose-dependent manner. It has been established that ketamine and magnesium interact synergistically in the tail-immersion test in rats. To determine the role of serotonergic, GABAergic and noradrenergic systems in analgesia induced by the ketamine-magnesium sulfate combination. Experiments were performed on male Wistar albino rats (200-250 g). Antinociception was evaluated by the tail-immersion test. Methysergide (0.5 and 1 mg/kg, sc) administered alone did not affect nociception in rats. Methysergide (0.5 and 1 mg/kg, sc) antagonized the antinociceptive effect of the ketamine (5 mg/kg)-magnesium sulfate (5mg/kg) combination. Bicuculline (0.5 and 1 mg/kg, sc) given alone did not change the threshold to thermal stimuli in rats. Bicuculline (0.5 and 1 mg/kg, sc) antagonized the antinociceptive effect of the ketamine (5 mg/kg)-magnesium sulfate (5 mg/kg) combination. Yohimbine (0.5, 1 and 3 mg/kg, sc) applied alone did not change nociception. Yohimbine at a dose of 0.5 mg/kg did not influence the effect of ketamine (5 mg/kg)-magnesium sulfate (5 mg/kg), while yohimbine at doses of 1 and 3 mg/kg antagonized the antinociceptive effect of this combination. Serotonergic, noradrenergic and GABAergic systems participate, at least in part, in the antinociceptive effect of the ketamine-magnesium sulfate combination in acute pain in rats.


2017 ◽  
Vol 41 (S1) ◽  
pp. S708-S709
Author(s):  
K. Savic Vujovic ◽  
A. Vujovic ◽  
S. Vuckovic ◽  
B. Medic ◽  
M. Prostran

ObjectivesStudy is aimed at evaluating the effects of ketamine and magnesium sulphate on acute nociceptive pain in rats and examination whether magnesium sulfate added to ketamine or morphine-ketamine combination produces higher level of analgesia.MethodsAnalgesic activity was assessed by tail-immersion test in male Wistar rats (200–250 g).ResultsMagnesium sulfate (2.5–60 mg/kg, s.c.) and ketamine (2.5-30 mg/kg, i.p.) given alone did not produce any effect on antinociception. However, there is a synergistic interaction between ketamine (2.5, 5 and 10 mg/kg) and magnesium sulfate (5 mg/kg). Both ketamine and magnesium sulfate, as well as their combination potentiated the antinociceptive effect of morphine (2.6 mg/kg, i.p.).ConclusionThis study revealed potentiation of ketamine and morphine-ketamine combination by magnesium sulphate in tail-immersion test in rats with higher activity when ketamine is given before magnesium sulfate. It is first time to demonstrate the synergistic interaction between magnesium sulphate and ketamine in lowering body temperature and in antinociception with statistical confirmation.Disclosure of interestThe authors have not supplied their declaration of competing interest.


2018 ◽  
Vol 29 (1) ◽  
pp. 81-93 ◽  
Author(s):  
Mir Muhammad Nasir Uddin ◽  
Mohammad Shah Hafez Kabir ◽  
Mahmud Hasan ◽  
Zobaer Al Mahmud ◽  
N. M. Mahmudul Alam Bhuiya ◽  
...  

AbstractBackground:The plant under investigation (Tetracera sarmentosa) is a dicotyledonous flowering plant and belongs to the family Dilleniaceae. The goal of our investigation was to determine whether the leaf extracts of this plant held any significant medicinal properties.Methods:Leaves ofT. sarmentosawere extracted with pure ethanol (EETS) and methanol (METS), and then methanol extract fractioned withn-hexane (NHFMETS) and chloroform (CHFMETS). The extracts and fractions were tested for antioxidant activity, which was measured by using qualitative and quantitative procedures. Thrombolytic activity was evaluated by the clot lysis test. Analgesic activity was evaluated employing the acidic acid-induced writhing test, the formalin-induced paw licking test and tail immersion on Swiss albino mice. The anti-inflammatory activity test was studied using the paw edema test. Forced swimming, tail suspension, elevated plus maze and hole board model tests were used to evaluate neuropharmacological activity.Results:All the extracts and fractions possessed antioxidant effects. All the extracts, fractions and streptokinase exhibited significant (p<0.0001) clot lysis. The extracts and fractions produced significant analgesic effects as evaluated by the acetic acid writhing test, the formalin-induced paw licking test and the tail immersion method. Similarly, carrageenan-induced inflammation was significantly antagonized by the treatments. The extracts and fractions also significantly showed neuropharmacological (antidepressant and anxiolytic) effects.Conclusions:The overall results suggested that this plant deserves further investigation to isolate the active compounds which are responsible for these activities and to establish the mechanism of action.


Author(s):  
Mario I Ortiz ◽  
Raquel Cariño-Cortés ◽  
Victor Manuel Muñoz Pérez ◽  
Andres Salas Casas ◽  
Gilberto Castañeda-Hernández

The aim of this study was to examine if the peripheral antinociception of α-bisabolol involve the participation of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) synthesis followed by K+ channel opening in the formalin test. Wistar rats were injected in the dorsal surface of the right hind paw with formalin (1%). Rats received a subcutaneous injection into the dorsal surface of the paw of vehicles or increasing doses of α-bisabolol (100-300 µg/paw). To determine whether the peripheral antinociception induced by α-bisabolol was mediated by either the opioid receptors or the NO-cGMP-K+ channels pathway, the effect of pretreatment (10 min before formalin injection) with the appropriate vehicles, naloxone, naltrexone, L-NAME, ODQ, glibenclamide, glipizide, apamin, charybdotoxin, tetraethylammonium or 4-aminopyridine on the antinociceptive effects induced by local peripheral α-bisabolol (300 µg/paw) were assessed. α-bisabolol produced antinociception during both phases of the formalin test. α-bisabolol antinociception was blocked by L-NAME, ODQ, and all the K+ channels blockers. The peripheral antinociceptive effect produced by α-bisabolol was not blocked by the opioid receptor inhibitors. α-bisabolol was able to active the NO-cGMP-K+ channels pathway in order to produce its antinoceptive effect. The participation of opioid receptors in the peripheral local antinociception induced by α-bisabolol is excluded.


2013 ◽  
Vol 11 (1) ◽  
pp. 54 ◽  
Author(s):  
. Widanarni ◽  
Puguh Widagdo ◽  
Dinamella Wahjuningrum

<p>The use of antibiotics for controlling of luminous vibriosis caused by <em>Vibrio harveyi</em> is restricted now, because it induces antibiotic-resistant bacteria and leave residue in shrimp’s body. An alternative solution that can be done to treat the disease is by using applications of probiotic, prebiotic, and synbiotic. The aim of this research was to examine the effect of probiotic, prebiotic, and synbiotic on the survival rate and growth of Pacific white shrimp against <em>V. harveyi</em> infection. Feed as a treatment was supplemented with probiotic 1%, prebiotic 2%, and probiotic 1%+prebiotic 2% (synbiotic). Shrimps feed without supplementation of probiotic and prebiotic was used as a control treatment. The shrimps were maintainedin the aquarium (60×30×35 cm<sup>3</sup>) with a density of 40 shrimps/40 L and an average weight of 0.4±0.1 g. After 30 days of feeding treatment, the shrimp was challenged by immersion method with <em>V. harveyi</em> solution containing 10<sup>6</sup> CFU/mL. The results showed that before challenge, synbiotic feed treated shrimp has a growth rate (5.89%), feed conversionrate (1.21), and a high survival rate (80%). After challenge, survival rate (83.33%) of shrimp fed diet supplemented with synbiotic was higher than prebiotic (51.67%) and positive control (31.67%).</p> <p>Keywords: probiotic, prebiotic, synbiotic, <em>Vibrio harveyi</em>,Pacific white shrimp</p>


Folia Medica ◽  
2021 ◽  
Vol 63 (3) ◽  
pp. 377-384
Author(s):  
Anita Mihaylova ◽  
Ilia Kostadinov ◽  
Nina Doncheva ◽  
Delian Delev ◽  
Hristina Zlatanova

Introduction: Parkinson&rsquo;s disease (PD) is &#1072; neurodegenerative disorder characterized mainly by its motor symptoms. The non-motor symptoms including pain are increasingly recognized in the last few decades. Existing evidence suggests that the dopaminergic neurotransmission has an essential role in pain control. Aim: The aim of the present study was to investigate the antinociceptive effect of dopaminergic drugs pramipexole and tolcapone against chemical and thermal stimuli in naive rats. Materials and methods: Male Wistar rats divided into 8 groups (n=8): saline; diclofenac 25 mg/kg body weight (bw) (positive control); pramipexole 0.5; 1 and 3 mg/kg bw; tolacapone 5; 15 and 30 mg/kg bw. Paw pressure and plantar tests were performed. Paw withdrawal pressure and latent time were measured. Statistical analysis was done by SPSS 19. Results: In the paw pressure test, pramipexole, in a dose of 1 and 3 mg/kg bw and tolcapone in a dose of 30 mg/kg bw, increased significantly the latency at 1, 2, and 3 hours compared to saline (p<0.05). In the plantar test, only the highest dose of pramipexole reached significance at 3 hours compared to the control rats (p<0.05). In contrast to pramipexole the three experimental groups with tolcapone markedly increased the latent time at 1 and 3 hours compared to saline (p<0.05). Conclusions: Pramipexole and tolcapone reduce mechanical and thermal nociception in na&iuml;ve rats by enhancing dopaminergic neurotransmission at both spinal and supraspinal levels. In addition, tolcapone stimulates noradrenergic mediation which may contribute to its antinociceptive effect.


Author(s):  
Manju Gari ◽  
Kumari Ranjeeta ◽  
Lakhan Majhee ◽  
Akhilesh Kumar ◽  
Sumit Kumar Mahato

Background: Pain is the most common reason patients seek medical care. Increased level of monoamines (serotonin and norepinephrine) in synaptic clefts lead to changes in pain threshold and induce antinociception. The study was carried out to evaluate antinociceptive effect of paroxetine in albino rats and to probe into its possible mechanism of action. The study was carried out to evaluate anti-nociceptive effect of paroxetine in albino rats.Methods: Male Albino rats of average weight 150-240gms were used. The drugs used were paroxetine 5mg/Kg, pethidine 5mg/kg (standard drug). Anti-nociceptive effect tested by using thermal method i.e. Tail flick response and Tail warm water immersion method.Results: In this study, Anti-nociceptive effect of respective drugs were measured by using two methods i.e. tail flick test and tail warm water immersion method at 0 min., 30 min., 60 min. and 90min.after administration of drugs. Reaction time started to increase from baseline at 0 min. and peak effect was seen at 60 min. then it started to decrease at 90 min. in almost all the groups except in control group.Conclusions: Paroxetine have significant analgesic effect in acute pain, which may be mediated via central and peripheral mechanisms. Efficacy of Paroxetine is almost equal to that of standard drug pethidine in acute pain management.


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