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

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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Assessment ofOpuntia ficus-indicain vivo Following Ethnobotanical Survey: Confirmation of its Analgesic Activity

Phytothérapie ◽

10.3166/phyto-2019-0144 ◽

2018 ◽

Vol 16 (S1) ◽

pp. S191-S196

Author(s):

A. Mouhaddach ◽

A. El-hadi ◽

K. Taghzouti ◽

M. Bendaou ◽

R. Hassikou

Keyword(s):

Body Weight ◽

Analgesic Activity ◽

Prickly Pear ◽

Tail Flick ◽

Ethnobotanical Study ◽

Ethnobotanical Survey ◽

Hot Plate ◽

Traditional Use ◽

Opuntia Ficus Indica ◽

Plant Parts

Opuntia ficus-indica(the cactus or prickly pear) is a cactus belonging to the Opuntiae family. Several Opuntiae plant parts have been used in traditional Moroccan medicine. In this study, we investigated its most common use as an analgesic. An ethnobotanical study ofOpuntia ficus-indicawas first conducted in 10 areas in Morocco. Extracts fromOpuntia ficus-indicacladodes were obtained using a decoction method and its analgesic activity in mice was investigated by the hot plate and tail flick methods. Cladode extracts had significant (p<0.05) analgesic activity at intraperitoneal doses of 300, 500, and 1000 mg/kg body weight. Both methods revealed significantly increased latency at all three doses (p<0.05) compared to controls. These data suggest that the traditional use of this plant as an analgesic is valid; in fact, perhaps it may be a centrally-acting analgesic.

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5-HT1A Serotonergic, α-Adrenergic and Opioidergic Receptors Mediate the Analgesic Efficacy of Vortioxetine in Mice

Molecules ◽

10.3390/molecules26113242 ◽

2021 ◽

Vol 26 (11) ◽

pp. 3242

Author(s):

Nazlı Turan Yücel ◽

Ümmühan Kandemir ◽

Ümide Demir Özkay ◽

Özgür Devrim Can

Keyword(s):

Analgesic Activity ◽

Time Course ◽

Motor Coordination ◽

Antidepressant Drug ◽

Area Under The Curve ◽

Analgesic Efficacy ◽

Synthesis Inhibitor ◽

Tail Immersion ◽

Adrenoceptor Blocker ◽

The Central Nervous System

Vortioxetine is a multimodal antidepressant drug that affects several brain neurochemicals and has the potential to induce various pharmacological effects on the central nervous system. Therefore, we investigated the centrally mediated analgesic efficacy of this drug and the mechanisms underlying this effect. Analgesic activity of vortioxetine (5, 10 and 20 mg/kg, p.o.) was examined by tail-clip, tail-immersion and hot-plate tests. Motor performance of animals was evaluated using Rota-rod device. Time course measurements (30–180 min) showed that vortioxetine (10 and 20 mg/kg) administrations significantly increased the response latency, percent maximum possible effect and area under the curve values in all of the nociceptive tests. These data pointed out the analgesic effect of vortioxetine on central pathways carrying acute thermal and mechanical nociceptive stimuli. Vortioxetine did not alter the motor coordination of mice indicating that the analgesic activity of this drug was specific. In mechanistic studies, pre-treatments with p-chlorophenylalanine (serotonin-synthesis inhibitor), NAN-190 (serotonin 5-HT1A receptor antagonist), α-methyl-para-tyrosine (catecholamine-synthesis inhibitor), phentolamine (non-selective α-adrenoceptor blocker), and naloxone (non-selective opioid receptor blocker) antagonised the vortioxetine-induced analgesia. Obtained findings indicated that vortioxetine-induced analgesia is mediated by 5-HT1A serotonergic, α-adrenergic and opioidergic receptors, and contributions of central serotonergic and catecholaminergic neurotransmissions are critical for this effect.

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EVALUATION OF ANALGESIC ACTIVITY OF MURRAYA KOENIGII AND CORIANDRUM SATIVUM LEAVES EXTRACT IN ANIMAL MODEL.

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v11i1.22718 ◽

2018 ◽

Vol 11 (1) ◽

pp. 328

Author(s):

Kartik Salwe J ◽

Mirunalini R ◽

Jervin Mano ◽

Manimekalai K

Keyword(s):

Analgesic Activity ◽

Analgesic Effect ◽

Coriandrum Sativum ◽

Control Group ◽

Tail Flick ◽

Murraya Koenigii ◽

Hot Plate ◽

Plate Method ◽

Standard Drug ◽

Soxhlet Apparatus

Objective: The objective of the study was to investigate the analgesic activity of hydroalcoholic extract of Murraya koenigii and Coriandrum sativum leaves and compared it with standard drug in an animal model.Methods: Hydroalcoholic extracts of M. koenigii and C. sativum leaves were obtained using Soxhlet apparatus. The central analgesic property was screened by hot plate method in mice and tail flick method in rats. The pain reaction time (PRT) was measured at 30, 60, and 120 min. The peripheral analgesic activity was evaluated by acetic acid induced writhing in mice.Results: In hot plate method M. koenigii leaves extract at both doses and tramadol showed significant increase in PRT at 30, 60, and 120 min compared with control group. C. sativum leaves extract showed significant increase in PRT only at 60 and 120 min compared to control group. In tail flick method M. koenigii leaves extract at both doses, higher dose of C. sativum leaves extract and tramadol showed significant increase in PRT at 30, 60, and 120 min compared with control group. Higher dose of M. koenigii leaves extract (200 mg/kg) was comparable with standard drug tramadol in both the methods. M. koenigii leaves extract at both dose showed significant reduction in the number of writhing but C. sativum leaves extract failed to show any significant reduction in the number of writhing compared with control. Higher dose of M. koenigii leaves extract was comparable with standard drug tramadol.Conclusion: M. koenigii leaves extract showed both peripheral and central analgesic effect while C. sativum leaves extract showed only peripheral analgesic effect.

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Dipeptide mimetic of the bdnf loop 4 possesses analgetic activity

Доклады Академии наук ◽

10.31857/s0869-56524853366-369 ◽

2019 ◽

Vol 485 (3) ◽

pp. 366-369

Author(s):

T. A. Gudasheva ◽

M. A. Konstantinopolsky ◽

A. V. Tarasiuk ◽

L. G. Kolik ◽

S. B. Seredenin

Keyword(s):

Analgesic Activity ◽

Neurotrophic Factor ◽

Intraperitoneal Injection ◽

Brain Derived Neurotrophic Factor ◽

Tail Flick ◽

Hot Plate ◽

The Brain

Previously, we synthesized a dimeric dipeptide mimetic of the brain-derived neurotrophic factor (BDNF) loop 4, GSB-106, which, similarly to BDNF, activated TrkB, PI3K/AKT, and MAPK/ERK. When administered systemically, it exhibited neuroprotective, antidepressant, and antidiabetic activities and stimulated neurogenesis and synaptogenesis. In this study, we established that GSB-106 also exhibits the analgesic activity, typical for BDNF, which was revealed in rats in hot plate and tail flick tests 0.5–48 h after intraperitoneal injection at doses of 0.1 and 1 mg/kg.

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Evaluation of analgesic activity of the methanol extract from the galls of Quercus infectoria alone and as an adjuvant in wistar rats

International Journal of Basic & Clinical Pharmacology ◽

10.18203/2319-2003.ijbcp20201521 ◽

2020 ◽

Vol 9 (5) ◽

pp. 701

Author(s):

Abishek P. Raichurkar ◽

Shashikala Gowdara Hanumanth Reddy

Keyword(s):

Analgesic Activity ◽

Wistar Rats ◽

Methanolic Extract ◽

Inflammatory Diseases ◽

Syringic Acid ◽

Tail Flick ◽

Hot Plate ◽

Anti Inflammatory ◽

Group 2 ◽

Quercus Infectoria

Background: Non-steroidal anti-inflammatory drugs and opioids are the most preferred drugs for pain relief. Considering the gastrointestinal toxicity, dependence and other side effects, search for better analgesic drug continues. Quercus infectoria (QI) is from the family Fagaceae. The galls of QI are comprised of tannin (36 to 60%), gallic acid, ellagic acid, and syringic acid. They possess antioxidant, anti-inflammatory, antimicrobial, and anti-diabetic properties. In India, galls of QI have been used for the treatment of toothache, diarrhoea, sore throat and inflammatory diseases as a home remedy. This study was conducted to evaluate the analgesic activity of methanolic extract of galls of QI on wistar rats using tail-flick and Eddy’s hot-plate methods. The objective of the study was to evaluate the analgesic activity of methanolic extract of galls of QI alone and as an adjuvant with tramadol on Wistar rats.Methods: Total of 24 wistar rats were included in the study and divided into 4 groups. They received drugs intra-peritoneally as follows. In group 1, normal saline, in group 2, tramadol, in group 3, methanolic extract of galls of QI and in group 4, tramadol with methanolic extract of galls of QI was available.Results: Methanolic extract of galls of QI produced significant maximal possible analgesia (<0.001) at 30 and 60 minutes in tail-flick method whereas it failed to produce analgesia in hot-plate method during all time intervals.Conclusions: Methanolic extract of galls of QI showed analgesic activity in tail-flick method indicating that its possible mechanism of action is spinally mediated.

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Pharmacological Evaluation of Antipyretic, Analgesic and Anti-inflammatory Activities of Ethanolic Extract of Cassia fistula

Indian Journal of Animal Research ◽

10.18805/ijar.b-4531 ◽

2021 ◽

Author(s):

D.K. Sharma ◽

S.K. Sharma ◽

M.K. Lonare ◽

Rajdeep Kaur ◽

V.K. Dumka

Keyword(s):

Analgesic Activity ◽

Ethanolic Extract ◽

Inflammatory Activity ◽

Bark Extract ◽

Control Group ◽

Albino Rats ◽

Hot Plate ◽

Antipyretic Activity ◽

Tail Immersion ◽

Anti Inflammatory

Background: The antipyretic, analgesic and anti-inflammatory activities of two concentrations (100 and 200 mg/kg) of ethanolic extract of leaf, bark, flower and fruit pulp of C. fistula were determined in male wistar albino rats. Methods: Antipyretic activity was assessed by E. coli endotoxin induced pyrexia. Analgesic activity was assessed by hot plate, tail immersion and acetic acid induced writhing test. Anti-inflammatory activity was evaluated by carrageenan-induced rat paw edema assay. Result: Significant (p less than 0.05) antipyretic activity was exhibited from 2h onwards by bark extract @ 200 mg/kg and from 3h onwards by bark extract @100 mg/kg and leaves extract @ 200mg/kg as compared to control group. Significant (p less than 0.05) analgesic activity was shown by extract of bark @ 200 mg/kg as it is evident by increase in reflex time in hot plate (90,120,180 min), tail immersion test (120,180 min) and inhibition of writhing (32.12%). Significant (p less than 0.05) anti-inflammatory activity was exhibited from 3h post administration by bark @ 200 and leaves @ 100 and 200 mg/kg.

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A Original Article ANALGESIC ACTIVITY OF BARK AND LEAVES OF FICUS RELIGIOSA L. FROM NEPAL

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2020v12i7.37783 ◽

2020 ◽

pp. 32-35

Author(s):

DHARMA RAJ MARASINI ◽

JITENDRA PANDEY ◽

LAXMAN PAUDEL SHARMA ◽

LAXMI PAUDEL ◽

ROSHNI GYAWALI ◽

...

Keyword(s):

Acetic Acid ◽

Analgesic Activity ◽

Test Group ◽

Ethanolic Extract ◽

Stem Bark ◽

Latency Time ◽

Hot Plate ◽

Ficus Religiosa ◽

Standard Drug ◽

Ethanolic Extracts

Objective: Because of adverse side effects, caused by NSAIDs, tolerance, and dependence induced by opiates, the use of these analgesic agents has not been successful in all cases. Therefore, alternative analgesic drugs from plant sources are the new target now days. The objective of this study was to evaluate the analgesic activity of ethanolic extracts of stem barks and leaves of Ficus religiosa. Methods: The analgesic activity of ethanolic extract of stem barks and leaves was evaluated in the Swiss albino mice model using acetic acid-induced writing response and Eddy’s hot plate method. Analgesic activity was demonstrated with the percentage inhibition of acetic acid induced writings and the percentage increased in latency time of paw licking. The potency of test extracts was compared with standard drug, Diclofenac. Results: Ethanolic extract of leaves and bark of F. religiosa showed potential analgesic activity from both methods. From Eddy’s hot plate model, it was observed that the percentage of increased latency time at 90 min by ethanolic extract of leaves and stem bark was found to be 70.81 % (8.54 min) and 70.78 % (8.53 min) respectively at a dose of 400 mg/kg. Both of these results are statistically significant (p<0.05) as compared to the test group. Furthermore, both of these extracts showed the dose-dependent and time-dependent increased in latency time and these results are compared to that of standard drug Diclofenac. Similarly, ethanolic extract of leaves and stem at 400 mg/kg significantly inhibited the number of writhings induced by acetic acid. The percentage inhibition of writhings by ethanolic extract of leaves at a dose of 400 mg/kg was 68.47 % which was similar to that of standard drug Diclofenac (68.47 %). However, ethanolic extract of bark showed relatively lower percentage inhibition (60.79 %) as compared to leaf extract and standard, but the result was significant as compared to that of the test group (p<0.05). Conclusion: Ethanolic extracts of F. religiosa stem bark and leaf possess both central and peripheral analgesic properties and these effects may be beneficial for the management of pain.

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Evaluation of analgesic activity of turmeric (Curcuma longa Linn.) in Wister rats

International Journal of Basic & Clinical Pharmacology ◽

10.18203/2319-2003.ijbcp20170814 ◽

2017 ◽

Vol 6 (3) ◽

pp. 568 ◽

Cited By ~ 2

Author(s):

Sangita Jogdand ◽

Jagruti Bhattacharjee

Keyword(s):

Analgesic Activity ◽

Normal Saline ◽

Curcuma Longa ◽

Ethanolic Extract ◽

Albino Rats ◽

Time Intervals ◽

Hot Plate ◽

Hot Plate Test ◽

Analgesic Activities

Background: NSAIDs like Aspirin etc. are randomly used for mild to severe types of pain but long-term and injudicious use of NSAIDs lead to a number of side effects. The present study is designed for exploring the analgesic potential of Curcuma longa Linn (Turmeric) in albino rats, which may widen the therapeutic horizon for the said agent.Methods: Ethanolic extract of Curcuma longa in the doses 100, 200 and 400mg/kg is given orally to 6 Wister rats against a control of normal saline and a standard using Aspirin (300mg/kg) and the animals were subjected to Eddy’s hot plate test at different time intervals i.e., 30, 60, 90 and 120 minutes after administration of the drugs and the parameters were noted.Results: The analgesic activity of Curcuma longa showed significant (p<0.05) increase in mean basal reaction time in Hot plate method when compared to the control (Normal saline). As the dose of the ethanolic extract of Curcuma longa was gradually increased from 100, 200 and 400mg/kg respectively, the analgesic activity significantly increased (<0.05). Effect of curcuma longa at a dose of 400mg/kg is found to be comparable with Aspirin.Conclusions: The results of this study suggest that turmeric (Curcuma longa) has significant analgesic activities in rats.

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Phytochemical & Pharmacological Investigation of Stems of Passiflora foetida

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i58b34218 ◽

2021 ◽

pp. 408-414

Author(s):

N. Michael Antony ◽

Jennifer Fernandes ◽

Jane Mathew

Keyword(s):

Analgesic Activity ◽

Ethanolic Extract ◽

Tail Flick ◽

Phytochemical Analysis ◽

Significant Activity ◽

Dependent Manner ◽

Phytochemical Investigation ◽

Soxhlet Apparatus ◽

Passiflora Foetida

Aims: To carry out extraction, preliminary phytochemical analysis and invivo analgesic screening of extract of the stem of Passiflora foetida L. Methodology: Passiflora foetida L; Family: Passifloraceae, is an exotic fast-growing perennial and medicinal vine occurring in Germany, France and other European countries and USA and grown in different parts of India. Dried stems of Passiflora foetida L was coarsely powdered and maceration was done using Soxhlet apparatus. The ethanolic extract of stems of Passiflora foetida L was subjected to preliminary phytochemical tests. Then subjected to in vivo analgesic activity. Results: Phytochemical investigation of the stem of Passiflora foetida L preliminary test showed the presence of carbohydrates, glycosides, flavonoids and steroids. Acute toxicity study of ethanolic extract of stems of Passiflora foetida L was carried out and extracts were found to be safe up to 2000 mg/kg body weight. Pharmacological activities of stems of Passiflora foetida L was carried out from ethanolic extract. Conclusion: Phytochemical investigation of ethanolic extract of stems were carried out and Analgesic activity by tail flick method in rats and acetic acid induced writhing method in mice, showed statistically significant activity (P=.05) when compared to control. The ethanolic stem extract of Passiflora foetida L proved to have significant pain relieving action in a dose dependent manner.

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Structural and Functional Characterization of Conotoxins from Conus achatinus Targeting NMDAR

Marine Drugs ◽

10.3390/md18030135 ◽

2020 ◽

Vol 18 (3) ◽

pp. 135 ◽

Cited By ~ 1

Author(s):

Xiujie Liu ◽

Ge Yao ◽

Kang Wang ◽

Yanli Liu ◽

Xiukun Wan ◽

...

Keyword(s):

Analgesic Activity ◽

Functional Characterization ◽

Tail Flick ◽

Snail Species ◽

Thermal Stimulus ◽

Dependent Manner ◽

Amino Acid Residues ◽

Cone Snail ◽

Hot Plate ◽

Linear Peptide

Conotoxin-Ac1 and its variant conotoxin-Ac1-O6P, were isolated from the venom duct of Conus achatinus, a fish-hunting cone snail species collected in the Sea of Hainan, China. Conotoxin-Ac1 is linear peptide that contain 15 amino acids. In the present study, we synthesized and structurally and functionally characterized conotoxin-Ac1 as well as 19 variants. Electrophysiological results showed that conotoxin-Ac1 inhibited N-methyl-D-aspartate receptor subunit 2B (NR2B) with an IC50 of 8.22 ± 0.022 μM. Further structure-activity studies of conotoxin-Ac demonstrated that polar amino acid residues were important for modulating its active, and the replacement of N1, O9, E10, and S12 by Ala resulted in a significant decrease in potency to NR2B. °Furthermore, conotoxin-Ac1 and conotoxin-Ac1-O6P were tested in hot-plate and tail-flick assays to measure the potential analgesic activity to an acute thermal stimulus in a dose-dependent manner. Subsequently, the analgesic activity of conotoxin-Ac1 mutants was analyzed by the hot-plate method. The results show that N1, Y2, Y3, E10, N11, S12, and T15 play an important role in the analgesic activity of conotoxin-Ac1. N1 and S12 have significant effects on conotoxin-Ac1 in inhibiting NR2B and analgesic activity. In conclusion, we have discovered that conotoxin-Ac1 is an inhibitor of NMDAR and displays antinociceptive activity.

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