scholarly journals Amarisolide A and pedalitin as bioactive compounds in the antinociceptive effects of Salvia circinata

2019 ◽  
Vol 97 (3) ◽  
pp. 355 ◽  
Author(s):  
Gabriel Fernando Moreno-Pérez ◽  
María Eva González-Trujano ◽  
Martha Juana Martínez-Gordillo ◽  
Rubén San Miguel-Chávez ◽  
Francisco Alberto Basurto-Peña ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Folk Medicine ◽  
Gastrointestinal Diseases ◽  
Antinociceptive Activity ◽  
Bioactive Constituents ◽  
Response Curves ◽  
Reference Drug ◽  
Writhing Test ◽  
H Nmr ◽  
Antinociceptive Effects

<p align="left"><strong>Background</strong>: <em>Salvia circinata</em> is an endemic species of Mexico used in the folk medicine of Santiago Huauclilla, Oaxaca, mainly as remedy for gastrointestinal diseases.</p><p align="left"><strong>Hypothesis</strong>: If the extracts of <em>Salvia circinata</em> have secondary metabolites with antinociceptive activity, then the behavior of nociception in the model of “whriting” in mice will decrease.</p><p align="left"><strong>Specie studied</strong>:<strong> </strong><em>Salvia circinata </em>Cav. (Lamiaceae).</p><p align="left"><strong>Study site and years of study</strong>: <em>Salvia circinata </em>was collected in Santiago Huauclilla, Oaxaca, in July 2014.</p><p align="left"><strong>Methods</strong>: Firstly, the acute toxicity of <em>S. circinata</em> extracts was evaluated to calculate the LD<sub>50 </sub>with OECD method. Then, dose-response curves of the antinociceptive effect of <em>S. circinata</em> organic and aqueous extracts (1, 10, 30, 100, and 300 mg/kg) were obtained in the writhing test in mice. Furthermore, chromatographic techniques were applied to isolate the compounds and were identified by comparison of the values of <sup>1</sup>H NMR, <sup>13</sup>C NMR and ESIMS reported in the literature.</p><p align="left"><strong>Results</strong>: Our data showed significant antinociceptive activity in all the tested extracts. Amarisolide A and pedalitin were isolated in the ethyl acetate and methanol extracts, respectively and assayed at doses of 1, 5 and 10 mg/kg, i.p. All the compounds decreased nociception in mice in at least 50 % from a minimal dosage of 1 mg/kg, i.p. and in a similar manner than the reference drug ketorolac (1 mg/kg, i.p.).</p><p align="left"><strong>Conclusions</strong>: Our findings give evidence that <em>Salvia circinata </em>possesses antinociceptive activity depending on the presence of several known bioactive constituents, reinforcing its use in the Mexican traditional medicine to alleviate abdominal pain.</p>

scholarly journals Chemical Composition and Antinociceptive Potential of Plinia edulis Fruits Peels

2018 ◽  
Vol 13 (5) ◽  
pp. 1934578X1801300
Author(s):  
Luciane Angela Nottar Nesello ◽  
Adriana Campos ◽  
Karla Capistrano ◽  
Fátima de Campos Buzzi ◽  
Valdir Cechinel Filho
Keyword(s):  
Chemical Composition ◽  
Antinociceptive Effect ◽  
Reference Drug ◽  
Writhing Test ◽  
Maslinic Acid ◽  
Pain Model ◽  
Antinociceptive Effects ◽  
Dose Dependent ◽  
Dose Dependent Effect ◽  
Different Doses

The present study deals with the chemical composition and antinociceptive effects of Plinia edulis fruit peels, analyzed by writhing, formalin, glutamate and capsaicin tests and comparison with two reference analgesic drugs, acetylsalicylic acid and acetaminophen. Phytochemical analyses of the nonpolar fraction (dichloromethane) obtained from the peels of P. edulis fruits revealed the presence of two triterpenes, maslinic acid and ursolic acid. The methanol extract of P. edulis peels showed a pronounced antinociceptive activity in the writhing test, with inhibition of 91.3% at 10 mg/kg, and its dichloromethane and ethyl acetate fractions presented inhibition of 68.3% and 51.5%, respectively. Maslinic acid showed a dose-dependent effect with inhibition of 60.8% at a dose of 10 mg/kg and ID50 value of 3.31 (2.75 to 4.0) mg/kg. The dichloromethane fraction, evaluated in the formalin-induced pain model at a dose of 10 mg/kg, showed a significant effect on both phases of pain. Maslinic acid was evaluated at different doses (1, 3 and 6 mg/kg) and presented a dose-dependent profile in both phases of pain, being more effective than the reference drug (acetaminophen), which was evaluated at 10 mg/kg. The dichloromethane fraction also inhibited the pain induced by glutamate and capsaicin by around 54% and 44%, respectively, whereas maslinic acid was more effective against glutamate, with 62.5% inhibition at 6 mg/kg, and 32% inhibition against capsaicin-induced pain. The results demonstrated that the pronounced antinociceptive effect presented by P. edulis fruits peels is related, at least in part, to the presence of the triterpenes evidenced in this study.

Antinociceptive Activity of Structural Analogues of Rotundifolone: Structure-Activity Relationship

2007 ◽  
Vol 62 (1-2) ◽  
pp. 39-42 ◽  
Author(s):  
Damião P. de Sousa ◽  
Edison V. M. Júnior ◽  
Fernando S. Oliveira ◽  
Reinaldo N. de Almeida ◽  
Xirley P. Nunes ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Structural Modification ◽  
Functional Group ◽  
Present Report ◽  
Antinociceptive Effect ◽  
Antinociceptive Activity ◽  
Writhing Test ◽  
Structure Activity ◽  
Structural Analogues ◽  
Limonene Oxide

Rotundifolone, a monoterpene isolated from the essential oil of the leaves of Mentha x villosa, is a constituent of several essential oils and known to have antinociceptive activity. Our recent study demonstrated that the analogues of rotundifolone showed also a significant antinociceptive effect. In the present report, to investigate the correlation between the structure and antinociceptive activity, rotundifolone and its analogues were evaluated in the acetic acid-induced writhing test in mice. All compounds showed to be more antinociceptive than rotundifolone against the pain response induced by acetic acid. Comparing the antinociceptive effect of rotundifolone with limonene oxide and (+)-pulegone, the results demonstrated that the epoxide group contributes as much as the ketone group to the antinociceptive activity of rotundifolone. Similarly, pulegone oxide and carvone epoxide were more antinociceptive than rotundifolone, thereby suggesting that the position of the functional group on the ring also influences the antinociceptive activity. (D)-Carvone produced maximal inhibition of the writhing response and was slightly more active than (+)-carvone. The study showed that by appropriate structural modification it may be possible to develop novel antinociceptive agents.

Antinociceptive Activity and Preliminary Structure-Activity Relationship of Chalcone-Like Compounds

2008 ◽  
Vol 63 (11-12) ◽  
pp. 830-836 ◽  
Author(s):  
Rogério Corrêa ◽  
Bruna Proiss Fenner ◽  
Fátima de Campos Buzzi ◽  
Valdir Cechinel Filho ◽  
Ricardo José Nunes
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Antinociceptive Effect ◽  
Experimental Models ◽  
Antinociceptive Activity ◽  
Dominant Factor ◽  
Writhing Test ◽  
Aromatic Ketones ◽  
Structure Activity ◽  
Relationship Of

Abstract Chalcones belong to a class of α,β unsaturated aromatic ketones which occur abundantly in nature, especially in plants. They are promising and interesting compounds due to their vast applications in pharmaceuticals, agriculture and industry. Several studies have shown that these compounds exert important biological activities in different experimental models. The present work deals with the antinociceptive activity, evaluated against the writhing test, of three series of chalcone-like compounds obtained by the Claisen-Schmidt condensation, using different aldehydes and substituted acetophenones. The results reveal that the compounds synthesized show a significant antinociceptive effect compared with nonsteroidal drugs such as aspirin, paracetamol and diclofenac. They also show that the electronic demand of the substituents is the dominant factor of the biological activity.

scholarly journals Synergistic Herb-Herb Interaction of the Antinociceptive and Anti-Inflammatory Effects of Syzygium aromaticum and Rosmarinus officinalis Combination

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
Myrna Déciga-Campos ◽  
Karla Lizet Beltrán-Villalobos ◽  
Hidemi Aguilar-Mariscal ◽  
María Eva González-Trujano ◽  
Guadalupe Esther Ángeles-López ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Folk Medicine ◽  
Ethanolic Extract ◽  
Rosmarinus Officinalis ◽  
Syzygium Aromaticum ◽  
Response Curves ◽  
Pharmacological Interaction ◽  
Pharmacological Studies ◽  
Anti Inflammatory ◽  
Rosmarinus Officinalis L

The use of alternative medicine to treat pain has been increased, and the combination of several medicinal plants for its relief is a common practice in traditional medicine. The present study is aimed at determining whether a combination of Syzygium aromaticum (S. aromaticum) and Rosmarinus officinalis L. (R. officinalis) potentiates their antinociceptive and anti-inflammatory effects. These effects were explored using the formalin and carrageenan assays in rats, respectively. Animals received local pretreatment with S. aromaticum oil or R. officinalis ethanolic extract (0.1–100 μg/paw) alone or combined in a 1 : 1 rate. Concentration-response curves were built to compare pharmacological responses after an individual administration of S. aromaticum, R. officinalis, or their combination. The pharmacological interaction was investigated by an isobolographic study using the EC50 of each component in a fixed 1 : 1 ratio. S. aromaticum and R. officinalis administered alone showed significant and concentration-dependent antinociceptive and anti-inflammatory effects, but R. officinalis was more potent than S. aromaticum in both the antinociceptive and anti-inflammatory effects (EC50 = 7.96 ± 0.6 μg/paw vs. EC50 = 41.6 ± 1.7 μg/paw; EC50 = 1.97 ± 0.3 μg/paw vs. EC50 = 26.9 ± 2.5 μg/paw, respectively). The isobolographic analysis of the combination of these species in a 1 : 1 ratio showed a synergistic interaction between S. aromaticum and R. officinalis since Zmix (experimental value) was lower than Zadd (theoretical value) for both the antinociceptive effect (Zmix = 0.45 ± 0.1 < Zadd = 24.8 ± 1.3) and the anti-inflammatory effect (Zmix = 5.2 ± 0.6 < Zadd = 14.4 ± 2.2), suggesting a potentiation for both pharmacological effects. These results prove evidence of the efficacy of mixture herb-herb used in folk medicine for pain therapy. It also emphasizes the requirement of pharmacological studies to explore the efficacy and safety of herb interactions.

scholarly journals Synthesis and Antinociceptive Effect of Some Thiazole-Piperazine Derivatives: Involvement of Opioidergic System in the Activity

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3350
Author(s):  
Nazlı Turan Yücel ◽  
Derya Osmaniye ◽  
Ümmühan Kandemir ◽  
Asaf Evrim Evren ◽  
Özgür Devrim Can ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Reaction Times ◽  
Docking Studies ◽  
Antinociceptive Activity ◽  
Opioidergic System ◽  
Piperazine Derivatives ◽  
Antinociceptive Effects ◽  
Using Data ◽  
Δ Opioid Receptor

In this study, we aimed to design and synthesize novel molecules carrying both the thiazole and piperazine rings in their structures and to investigate their antinociceptive activity. Targeted compounds were obtained by reacting thiosemicarbazide derivative and appropriate 2-bromoacetophenone in ethanol. The structures of the obtained compounds were determined using data from various spectroscopic methods (IR, 1H-NMR, 13C-NMR, and LCMSMS). Experimental data from in vivo tests showed that test compounds 3a–3c, 3f, and 3g (50 mg/kg) significantly prolonged reaction times of animals in tail-clip and hot-plate tests compared to the controls, indicating that these compounds possess centrally mediated antinociceptive activities. Furthermore, these compounds reduced the number of writhing behaviors in the acetic acid-induced writhing tests, showing that the compounds also possess peripheral antinociceptive activity. In the mechanistic studies, naloxone pre-treatments abolished the antinociceptive activities of compounds 3a–3c, 3f, and 3g, indicating that opioidergic mechanisms were involved in their antinociceptive effects. Molecular docking studies demonstrating significant interactions between the active compounds and µ- and δ-opioid receptor proteins supported the pharmacological findings. This study is the first showing that molecules designed to bear thiazole and piperazine moieties together on their structure exert centrally and peripherally mediated antinociceptive effects by activating the opioid system.

Carbachol interactions with nonsteroidal anti-inflammatory drugs

2002 ◽  
Vol 80 (12) ◽  
pp. 1173-1179 ◽  
Author(s):  
H F Miranda ◽  
F Sierralta ◽  
G Pinardi
Keyword(s):  
Test Dose ◽  
Antinociceptive Activity ◽  
Simultaneous Administration ◽  
Response Curves ◽  
Additional Mechanism ◽  
Writhing Test ◽  
Prostaglandin Biosynthesis ◽  
Isobolographic Analysis ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

The inhibition of cyclooxygenase enzymes by nonsteroidal anti-inflammatory drugs (NSAIDs) does not completely explain the antinociceptive efficacy of these agents. It is known that cholinergic agonists are antinociceptive, and this study evaluates the interactions between carbachol and some NSAIDs. Antinociceptive activity was evaluated in mice by the acetic acid writhing test. Dose–response curves were constructed for NSAIDs and carbachol, administered either intraperitoneally (i.p.) or intrathecally (i.t.). The interactions of carbachol with NSAIDs were evaluated by isobolographic analysis after the simultaneous administration of fixed proportions of carbachol with each NSAID. All of the drugs were more potent after spinal than after systemic administration. The combinations of NSAIDs and carbachol administered i.p. were supra-additive; however, the i.t. combinations were only additive. Isobolographic analysis of the coadministration of NSAIDs and carbachol and the fact that atropine antagonized the synergistic effect suggest that carbachol may strongly modulate the antinociceptive activity of NSAIDs; thus, central cholinergic modulation would be an additional mechanism for the antinociceptive action of NSAIDs, unrelated to prostaglandin biosynthesis inhibition.Key words: antinociception, nonsteroidal anti-inflammatory drugs, cholinergic, carbachol, writhing test.

scholarly journals Intrathecal administration of neuronostatin induces an antinociceptive effect in a mouse visceral pain model

2020 ◽  
Vol 6 (4) ◽  
pp. 344-354
Author(s):  
Tingji Shao ◽  
Shaobin Yang ◽  
Peng Yu
Keyword(s):  
Visceral Pain ◽  
Antinociceptive Effect ◽  
Intrathecal Administration ◽  
Writhing Test ◽  
New Approach ◽  
Pain Model ◽  
Antinociceptive Effects ◽  
Μ Opioid Receptor ◽  
G Protein Coupled ◽  
Dose Dependent

Neuronostatin (NST) is a peptide encoded by the somatostatin gene that serves important physiological functions in diverse tissues. Previous studies have shown that intracerebroventricular administration of NST induces antinociceptive effects and hyperalgesic effects as determined by the tail immersion assay and formalin test, respectively. In the present study, we aimed to evaluate the effects of intrathecal (i.t.) injection of NST on nociception in a model of visceral pain, and determine possible mechanisms of action in mice. NST (1, 3, 6, or 12 nmol) was administered to mice, leading to a dose‐dependent antinociceptive effect as determined by the acetic acid‐induced writhing test in mice. NST (1 nmol) also enhanced the antinociceptive effect of morphine (2.5 and 5 μg/kg) in the spine. Naloxone and β‐funaltrexamine hydrochloride significantly antagonized the antinociceptive effect of NST. The expression of G‐protein‐coupled receptor 107 (GPR107) protein and the phosphorylation of PKA at Thr197 were increased after i.t. administration of NST, suggesting that the μ‐opioid receptor and GPR107/PKA signaling pathway are involved in the analgesic response. In conclusion, i.t. injection of NST may potentially be used as a new approach in the mediation of visceral pain.

Contribution of spinal 5-HT5A receptors to the antinociceptive effects of systemically administered cannabinoid agonist WIN 55,212-2 and morphine

2018 ◽  
Vol 96 (6) ◽  
pp. 618-623 ◽  
Author(s):  
Ahmet Goktan Aksu ◽  
Ozgur Gunduz ◽  
Ahmet Ulugol
Keyword(s):  
Receptor Antagonist ◽  
Motor Coordination ◽  
Antinociceptive Effect ◽  
Antinociceptive Activity ◽  
Tail Flick ◽  
Hot Plate ◽  
Rotarod Test ◽  
Antinociceptive Effects ◽  
Cb2 Agonist ◽  
Cannabinoid Agonist

The antinociceptive effects of cannabinoids and opioids have been known for centuries. Serotonin and its receptors are also known to play important roles in nociception. However, the contribution of spinal 5-HT5A receptors in antinociceptive effects of cannabinoids and opioids has not been studied. We conducted this study to clarify spinal mechanisms of the actions of the antinociceptive effects of cannabinoids and opioids. Hot plate and tail flick tests were used to assess the antinociceptive activity in Balb/c mice. WIN 55,212-2, a nonselective CB1 and CB2 agonist, and morphine exerted significant antinociceptive effects at 1, 3, and 10 mg/kg doses administered intraperitoneally in both hot plate and tail flick tests. The selective 5-HT5A receptor antagonist SB-699551 (10 nmol/mouse) was administered intrathecally 10 min before the agonists. SB-699551 significantly reduced the antinociceptive effect of both WIN 55,212-2 and morphine. In the rotarod test, WIN 55,212-2 disrupted the motor coordination at a dose of 10 mg/kg, while morphine did not affect this function at any dose. Our findings show that spinal 5-HT5A receptors are involved in the antinociceptive effects of WIN 55,212-2 and morphine.

scholarly journals Perillyl Alcohol: Antinociceptive Effects and Histopathological Analysis in Rodent Brains

2017 ◽  
Vol 12 (9) ◽  
pp. 1934578X1701200
Author(s):  
Rubens Batista Benedito ◽  
Mateus Feitosa Alves ◽  
Wendel Batista Pereira ◽  
Paula de Arruda Torres ◽  
Jéssica Pereira Costa ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Natural Compound ◽  
Perillyl Alcohol ◽  
Antinociceptive Activity ◽  
Histopathological Analysis ◽  
Histological Changes ◽  
Writhing Test ◽  
Antinociceptive Effects ◽  
Histopathological Evaluation ◽  
Tissue Changes

Perillyl alcohol (PA) is a natural compound found in essential oils. In this study, the antinociceptive activity of PA was evaluated using acetic acid and formalin tests. The involvement of the opioid system in its mechanism of action was investigated. Potential histological changes in the hippocampus and striatum were also assessed. In the acetic acid induced writhing tests, the mice pretreated with PA exhibited significant reductions in writhing. PA inhibited formalin injected paw licking response, and naloxone partially reversed the antinociceptive activity of perillyl alcohol during the writhing test. And as for the histopathological evaluation, PA did not cause significant tissue changes. This study suggests that PA possesses antinociceptive effects without significant hippocampus or striatum neurotoxicity, and that its activity involves opioid.

Antinociceptive Effects of Aza-Bicyclic Isoxazoline-Acylhydrazone Derivatives in Different Models of Nociception in Mice

2022 ◽  
Vol 22 ◽  
Author(s):  
Fernanda Virginia Barreto Mota ◽  
Felipe Neves Coutinho ◽  
Vanessa Mylenna Florêncio de Carvalho ◽  
Julyanne Cunha de Assis Correia ◽  
Isla Vanessa Gomes Alves Bastos ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Acetic Acid ◽  
Potassium Channels ◽  
Antinociceptive Activity ◽  
Writhing Test ◽  
Cholinergic Pathways ◽  
Chemical Models ◽  
Pain Models ◽  
Antinociceptive Effects ◽  
Adrenergic Systems

Background: In a study recently published by our research group, the compounds isoxazoline-acylhydrazone derivatives R-99 and R-123 presented promising antinociceptive activity. However, the mechanism of action of this compound is still unknown. Objective: This study aimed to assess the mechanisms involved in the antinociceptive activity of these compounds in chemical models of pain. Methods: Animals were orally pretreated and evaluated in the acetic acid-, formalin-, capsaicin-, carrageenan- and Complete Freund's Adjuvant (CFA)-induced pain models in mice. The effects of the compounds after pretreatment with naloxone, prazosin, yohimbine, atropine, L-arginine, or glibenclamide were studied, using the acetic acid-induced writhing test to verify the possible involvement of opioid, α1-adrenergic, α2-adrenergic or cholinergic receptors, and nitric oxide or potassium channels pathways, respectively. Results: R-99 and R-123 compounds showed significant antinociceptive activity on pain models induced by acetic acid, formalin, and capsaicin. Both compounds decreased the mechanical hyperalgesia induced by carrageenan or CFA in mice. The antinociceptive effects of R-99 and R-123 on the acetic acid-induced writhing test were significantly attenuated by pretreatment with naloxone, yohimbine or atropine. R-99 also showed an attenuated response after pretreatment with atropine and glibenclamide. However, on the pretreatment with prazosin, there was no change in the animals' response to both compounds. Conclusion: R-99 and R-123 showed antinociceptive effects related to mechanisms that involve, at least in part, interaction with the opioid and adrenergic systems and TRPV1 pathways. The compound R-99 also interacts with the cholinergic pathways and potassium channels.

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