The Study of Analgesic Effects of Leonurus cardiaca L. in Mice by Formalin, Tail Flick and Hot Plate Tests

Leonurus cardiaca, commonly known as motherwort, is a member of the Lamiaceae family. It has a number of interesting biological activities, for example, sedative and hypotensive, antioxidant, anti-inflammatory, and antimicrobial activities. The aim of the present study was to investigate the effect of alcoholic extract of aerial part of Leonurus cardiaca on nociceptive response using formalin, tail flick, and hot plate tests in mice. The acute treatment of mice with an ethanolic extract at doses of 500 and 250 mg/kg by intraperitoneal administration produced a significant antinociceptive in the first and second phases of formalin test, respectively. The hot plate and tail flick tests showed an increase in the antinociceptive effect at dose 500 mg/kg. These results suggest that Leonurus cardiaca possesses central and peripheral antinociceptive actions.

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Anodyne activities of New Tetrazole derivatives from Triazine

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11i3.2474 ◽

2020 ◽

Vol 11 (3) ◽

pp. 3377-3383

Author(s):

Arulmozhi R ◽

Abirami N ◽

Helen P Kavitha ◽

Arulmurugan S ◽

Vinoth Kumar J

Keyword(s):

Heterocyclic Compounds ◽

Biological Activities ◽

Pharmaceutical Chemistry ◽

Tail Flick ◽

Structural Fragment ◽

Hot Plate ◽

Standard Drug ◽

New Class ◽

Novel Drugs ◽

Tetrazole Derivatives

The creation of novel drugs containing a tetrazole ring as a structural fragment has contributed considerably to the outstanding achievements of the pharmaceutical chemistry in the last decade. Tetrazoles are the heterocyclic compounds having diverse biological activities such as analgesic, antiinflammation, antimicrobial, anticancer, antidiabetic, etc., and an impending source in biosciences. In this paper, the authors describe the synthesis of novel tetrazoles from N, N-( 6-Phenyl-1,3,5-triazine-2,4-diyl) dibenzamide (PTDDB) and 2-phenyl-4, 6-di(2H-tetrazole-2-yl)-1,3,5-triazine(5a-i) were prepared per the proposed scheme. A new class of tetrazole heterocycles were synthesised and characterised. I n vivo analysis was carried out on the analgesic property of synthesised tetrazole derivatives (5a, 5b, 5c). Characterisation studies such as IR, 1H NMR, 13C NMR, Mass and elemental analysis were performed for the synthesised tetrazole derivatives. Some of the tetrazole derivatives 5a, 5b, and 5c were tested for anodyne activity using morphine as the standard drug. The data reveals that all the three compounds 5a, 5b and 5c taken for the study show analgesic activity by hot plate method and tail flick methods. Among tested compounds, compound 5c is found to have potent analgesic (anodyne) activity. The results of the study indicate that the sample taken for the study show fairly good business using morphine as the standard drug.

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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

Journal of Neurosciences in Rural Practice ◽

10.4103/0976-3147.83577 ◽

2011 ◽

Vol 02 (02) ◽

pp. 130-136 ◽

Cited By ~ 9

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.

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Ellagic Acid ameliorates Streptozotocin-Induced Diabetic Hyperalgesia in Rat: Involvement of Oxidative Stress

Basic and Clinical Neuroscience Journal ◽

10.32598/bcn.2021.2413.1 ◽

2021 ◽

Author(s):

Siamak Shahidi ◽

◽

Alireza Komaki ◽

Safoura Raoufi ◽

Iraj Salehi ◽

...

Keyword(s):

Oxidative Stress ◽

Ellagic Acid ◽

Therapeutic Potential ◽

Biological Activities ◽

Antinociceptive Effect ◽

Diabetic Rats ◽

Diabetic Rat ◽

Tail Flick ◽

Stress Markers ◽

Total Antioxidant

Background/Aim: Hyperalgesia is one of the current complications of diabetes mellitus that Oxidative stress and inflammation have principal role in its development. Ellagic Acid (EA) as a herbal component, has some biological activities, including antioxidant and anti-inflammatory effects. This study was designed to evaluate the possible beneficial effect of EA on hyperalgesia in streptozotocin (STZ)-induced diabetic rat. Materials and Methods: Rats were divided into control(vehicle received), diabetic, EA (25, 50 mg/kg)-treated control and EA(25, 50 mg/kg)-treated diabetic groups. Diabetes was induced by a single intraperitoneal (IP) injection of streptozotocin (STZ) (60 mg/Kg). EA was administered daily by oral gavage for 4 weeks. Hyperalgesia was assessed using tail flick (TF) and hot plate (HP) tests. Also, oxidative stress markers including malondialdehyde (MDA), total oxidant status (TOS) and total antioxidant capacity (TAC) in the serum were evaluated. Results: Diabetic animals showed marked reductions in TF and HP latencies, elevation of serum MDA level and TOS and diminution of serum TAC compared to controls significantly. Treatment of Diabetic rats with EA ameliorated reduction of TF latency at the dose of 25 mg/kg and HP latency at the dose of 50 mg/kg. Furthermore EA significantly increased TAC and decreased MDA level at dose of 50 mg/kg and reduced TOS at both doses in the serum of diabetic animals. In EA treated normal rats we could see no significant alterations in the parameters studied. Conclusion: These results displayed potent antinociceptive effect of EA in diabetic rats via attenuating oxidative stress. This proposes therapeutic potential of EA for damping diabetic hyperalgesia.

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Evaluation of Analgesic Activity ofPapaver libanoticumExtract in Mice: Involvement of Opioids Receptors

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2017/8935085 ◽

2017 ◽

Vol 2017 ◽

pp. 1-13 ◽

Cited By ~ 7

Author(s):

Mohamad Ali Hijazi ◽

Ahmed El-Mallah ◽

Maha Aboul-Ela ◽

Abdalla Ellakany

Keyword(s):

Opioid Receptors ◽

Analgesic Activity ◽

Time Course ◽

Ethanolic Extract ◽

Maximum Activity ◽

Tail Flick ◽

Endemic Plant ◽

Hot Plate ◽

The Central Nervous System ◽

Opioid Withdrawal Syndrome

Papaver libanoticumis an endemic plant to Lebanese region (family Papaveraceae) that has not been investigated before. The present study aimed to explore the analgesic activity of dried ethanolic extract ofPapaver libanoticum(PLE) using tail flick, hot plate, and acetic acid induced writhing models in mice. The involvement of opioid receptors in the analgesic mechanism was investigated using naloxone antagonism. Results demonstrated that PLE exhibited a potent dose dependent analgesic activity in all tested models for analgesia. The analgesic effect involved activation of opioid receptors in the central nervous system, where both spinal and supraspinal components might be involved. The time course for analgesia revealed maximum activity after three hours in both tail flick and hot plate methods, which was prolonged to 24 hours. Metabolites of PLE could be responsible for activation of opioid receptors. The EC50 of PLE was 79 and 50 mg/kg in tail flick and hot plate tests, respectively. The total coverage of analgesia by PLE was double that of morphine in both tests. In conclusion, PLE proved to have opioid agonistic activity with a novel feature of slow and prolonged effect. The present study could add a potential tool in the armaments of opioid drugs as a natural potent analgesic and for treatment of opioid withdrawal syndrome.

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Effect of Rosmarinic and Caffeic Acids on Inflammatory and Nociception Process in Rats

ISRN Pharmacology ◽

10.5402/2011/451682 ◽

2011 ◽

Vol 2011 ◽

pp. 1-6 ◽

Cited By ~ 35

Author(s):

Giovana Duzzo Gamaro ◽

Edna Suyenaga ◽

Milene Borsoi ◽

Joice Lermen ◽

Patrícia Pereira ◽

...

Keyword(s):

Caffeic Acid ◽

Rosmarinic Acid ◽

Pleural Cavity ◽

Biological Activities ◽

Control Group ◽

Tail Flick ◽

Nociceptive Response ◽

Tail Flick Latency ◽

Balanced Distribution ◽

Anti Inflammatory

Rosmarinic acid is commonly found in species of the Boraginaceae and the subfamily Nepetoideae (Lamiaceae). It has a number of interesting biological activities, for example, antiviral, antibacterial, anti-inflammatory, and antioxidant. The aim of the present study was to investigate the effect of the i.p. administration of caffeic and rosmarinic acid (5 and 10 mg/kg) on anti-inflammatory and nociceptive response using carrageenan-induced pleurisy model and tail-flick assay in rats. The analysis of cells in the pleural exudates revealed a reduction of 66% of the number of leukocytes that migrated to the pleural cavity in the animals treated with 5 mg/kg caffeic acid, and of 92.9% for the animals treated with 10 mg/kg in comparison with the control group. These exudates showed a balanced distribution of polymorphonuclear (PMN) and mononuclear (MN) cells, differently from the control group, in which PMN cells were predominant. The analysis to tail-flick latency was increased in the group treated with 10 mg/kg caffeic acid characterizing a nociceptive response. While there was no difference between control group and animals treated with rosmarinic.

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The mineralocorticoid receptor antagonist spironolactone enhances morphine antinociception

Scandinavian Journal of Pain ◽

10.1016/j.sjpain.2013.07.013 ◽

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.

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The Anti-Nociceptive Potential of Tulathromycin against Chemically and Thermally Induced Pain in Mice

Pharmaceutics ◽

10.3390/pharmaceutics13081247 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1247

Author(s):

Mohamed Elbadawy ◽

Amira Abugomaa ◽

Hussein M. El-Husseiny ◽

Ahmed S. Mandour ◽

Mohamed M. Abdel-Daim ◽

...

Keyword(s):

Acetic Acid ◽

Acute Pain ◽

Symptomatic Relief ◽

Late Phase ◽

Control Group ◽

Tail Flick ◽

Nociceptive Response ◽

Hot Plate ◽

Significant Prolongation ◽

Dose Dependent

The present study was conducted to evaluate the analgesic potential of the new triamilide macrolide antibiotic, tulathromycin, at 20 and 40 mg/kg of body weight (BW), subcutaneously against acute pain in mice. Acute pain was induced either chemically (using acetic acid-induced writhing and formalin-induced pain tests) or thermally (using hot-plate, and tail-flick tests). In the acetic acid-induced writhing test, tulathromycin induced a dose-dependent and significant decrease in the number of writhes compared with the control group. In the late phase of the formalin test, a significant decline in hind paw licking time compared with the control group was observed. In the hot-plate and tail-flick tests, tulathromycin caused a dose-dependent and significant prolongation of latency of nociceptive response to heat stimuli, compared with the control group. These findings may indicate that tulathromycin possesses significant peripheral and central analgesic potentials that may be valuable in symptomatic relief of pain, in addition to its well-established antibacterial effect.

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PHYTOCHEMICAL SCREENING, ANTIOXIDANT AND ANTIMICROBIAL ASSESSMENT OF PLUCHEA INDICA (L.) LESS EXTRACT AS AN ACTIVE INGREDIENT IN NATURAL LOTION BAR

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2021v13i2.41555 ◽

2021 ◽

pp. 51-57

Author(s):

SIRIKHWAN TINRAT

Keyword(s):

Broad Spectrum ◽

Antioxidant Activities ◽

Biological Activities ◽

Radical Scavenging ◽

Ethanolic Extract ◽

Antimicrobial Activities ◽

Dilution Method ◽

Reducing Ability ◽

Phytochemical Compounds ◽

Antioxidant And Antimicrobial Activities

Objective: To screen phytochemical compounds and study antioxidant and antimicrobial activities of Pluchea indica (L.) Less (PI) leaves extracts for assessment the moisturizing lotion bar formulation containing it’s as a bioactive ingredient. Methods: PI leaves were extracted in different solvents. Crude extracts were screened phytochemical compounds and evaluated antioxidant and antimicrobial activities before formulating to antibacterial moisturizing lotion bar. Results: 95% ethanolic extract displayed high antioxidant activities. DPPH radical scavenging capacity with IC50 was 6.80±0.04 mg/ml (61.37±0.41%) and the ferric reducing ability power was 381.20±0.10 mg AAE/100 gDW. Additionally, 95% ethanolic extract served as a broad spectrum bacteriostatic agents against gram-positive and gram-negative species with an inhibition zone of 6.50±0.00-46.67±0.58 mm. It also was simultaneously as a broad spectrum bactericidal agents (MIC and MBC value of 25-200 mg/ml) by broth micro-dilution method. The screened phytochemical constituents (saponins, tannins, flavonoids, terpenoids, steroids, and alkaloids) in PI leaves extract may be responsible for high biological activities. Thus, 95% ethanolic extract was the most appropriate bioactive ingredient for formulated the product development. Conclusion: The developed moisturizing lotion bar with 0.0041% of 95% ethanolic extract was the most eligible formula that showed good appearance, odor, color, homogeneity, after feel and stability. This extract-containing lotion bar formulation achieved a high level of customer satisfaction by sensory evaluation and development of this specific formulation should be subject to further clinical investigation.

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Antinociceptive and Toxicological Effects ofDioclea grandifloraSeed Pod in Mice

Journal of Biomedicine and Biotechnology ◽

10.1155/2010/606748 ◽

2010 ◽

Vol 2010 ◽

pp. 1-6 ◽

Cited By ~ 4

Author(s):

Rita de Cássia da Silveira e Sá ◽

Leandra Eugênia Gomes de Oliveira ◽

Franklin Ferreira de Farias Nóbrega ◽

Jnanabrata Bhattacharyya ◽

Reinaldo Nóbrega de Almeida

Keyword(s):

Motor Performance ◽

Formalin Test ◽

Antinociceptive Effect ◽

Intraperitoneal Administration ◽

Ethanolic Extract ◽

Neurogenic Pain ◽

Hot Plate Test ◽

Writhing Test ◽

Toxicological Effects ◽

Observation Period

The acute treatment of mice with an ethanolic extract from the seed pod ofDioclea grandiflora(EDgP) at doses of 75, 150 and 300 mg/kg by intraperitoneal administration produced a significant antinociceptive effect as displayed by the acetic acid-induced writhing test and the formalin test. The antinociception was observed through the first (neurogenic pain) and second (inflammatory pain) phases in the formalin test. The hot plate test did not show an increase in the antinociceptive latency whereas the motor performance was affected by the administration at 300 mg/kg at the beginning (30 minutes) of the observation period but not at later periods (60 and 120 minutes). These results suggest that EDgP has a central antinociceptive action and a possible anti-inflammatory activity in mice.

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Examining the Effects of (α4)3(β2)2 Nicotinic Acetylcholine Receptor-Selective Positive Allosteric Modulator on Acute Thermal Nociception in Rats

Molecules ◽

10.3390/molecules25122923 ◽

2020 ◽

Vol 25 (12) ◽

pp. 2923

Author(s):

Farah Deba ◽

Kara Ramos ◽

Matthew Vannoy ◽

Kemburli Munoz ◽

Lois S. Akinola ◽

...

Keyword(s):

Acetylcholine Receptor ◽

Nicotinic Acetylcholine Receptor ◽

Antinociceptive Effect ◽

Tail Flick ◽

Allosteric Modulator ◽

Positive Allosteric Modulator ◽

Hot Plate ◽

Nicotinic Acetylcholine ◽

Thermal Nociception ◽

Nociceptive Responses

Neuronal nicotinic acetylcholine receptor (nAChR)-based therapeutics are sought as a potential alternative strategy to opioids for pain management. In this study, we examine the antinociceptive effects of 3-(2-chlorophenyl)-5-(5-methyl-1-(piperidin-4-yl)-1H-pyrazol-4-yl)isoxazole (CMPI), a novel positive allosteric modulator (PAM), with preferential selectivity to the low agonist sensitivity (α4)3(β2)2 nAChR and desformylflustrabromine (dFBr), a PAM for α4-containing nAChRs. We used hot plate and tail flick tests to measure the effect of dFBr and CMPI on the latency to acute thermal nociceptive responses in rats. Intraperitoneal injection of dFBr, but not CMPI, dose-dependently increased latency in the hot plate test. In the tail flick test, the effect achieved at the highest dFBr or CMPI dose tested was only <20% of the maximum possible effects reported for nicotine and other nicotinic agonists. Moreover, the coadministration of dFBr did not enhance the antinociceptive effect of a low dose of nicotine. Our results show that the direct acute effect of dFBr is superior to that for CMPI, indicating that selectivity to (α4)3(β2)2 nAChR is not advantageous in alleviating responses to acute thermal nociceptive stimulus. However, further studies are necessary to test the suitability of (α4)3(β2)2 nAChR-selective PAMs in chronic pain models.

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