scholarly journals In vivo investigation of antihyperalgesic and antinociceptive effects of peat formulations

2018 ◽  
Vol 68 (3) ◽  
pp. 373-380
Author(s):  
Plamen Ivanov Zagorchev ◽  
Elisaveta Georgieva Apostolova ◽  
Bissera Asenova Pilicheva ◽  
Milena Nenkova Draganova-Filipova ◽  
Vesela Yulieva Kokova ◽  
...  

Abstract The aim of this study is to evaluate the antihyperalgesic and antinociceptive effects of two formulations containing peat water extracts using a model of carrageenan-induced hyperalgesia, combined with a test with a mechanical stimulus, and a hot plate test. Rats were divided into seven groups (n = 6) and received local treatment with two peat formulations and two diclofenac formulations dissolved in carbopol gel and Wolff® basis creme, respectively. Carbopol gel, Wolff® basis creme and 0.9 % NaCl without tested substances were used as controls. Both peat formulations exerted an unambiguous antihyperalgesic effect 60 minutes after the treatment. In the hot plate test, the rats treated with the Wolff® basis creme peat formulation showed a tendency to prolonged latency on the first hour. The results could be explained by partial activation of peripheral α2-adrenoceptors and the possible COX-2 suppressive activity.

Molecules ◽  
2019 ◽  
Vol 24 (24) ◽  
pp. 4584 ◽  
Author(s):  
Thais Biondino Sardella Giorno ◽  
Carlos Henrique Corrêa dos Santos ◽  
Mario Geraldo de Carvalho ◽  
Virgínia Cláudia da Silva ◽  
Paulo Teixeira de Sousa ◽  
...  

Infusions of roots of Siolmatra brasiliensis (Cogn.) Baill, (“taiuiá”, “cipó-tauá”) are used for toothache pain and ulcers. We aimed to study the antinociceptive effects and identify the possible mechanism of action of this plant and its isolated substances (cayaponoside A1, cayaponoside B4, cayaponoside D, and siolmatroside I). Hydroethanol extract (HE), ethyl acetate fraction (EtOAc), and isolated saponins were evaluated in chemical and thermal models of pain in mice. Animals were orally pretreated and evaluated in the capsaicin- or glutamate-induced licking and in the hot plate tests. The antinociceptive mechanism of action was evaluated using the hot plate test with the following pretreatments: Atropine (cholinergic antagonist), naloxone (opioid antagonist), or L-NAME (nitric oxide synthase inhibitor). All extracts and isolated saponins increased the area under the curve in the hot plate test. Tested substances induced a higher effect than the morphine-treated group. Our data suggest that stems of S. brasiliensis and their isolated substances present antinociceptive effects. Cholinergic and opioidergic pathways seem to be involved in their mechanism of action. Taken together our data corroborate the traditional use of the plant and expands the information regarding its use.


2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Jo-Young Son ◽  
Jae-Seong Lim ◽  
Jae-Hyung Park ◽  
Jae-Hyeong Park ◽  
Myeong-Shin Kim ◽  
...  

Mannitol has recently been reported to be effective in enhancing the antinociceptive efficacy of lidocaine. No single study to date, however, has compared diphenhydramine with and without mannitol for nociceptive processing as an alternative local anesthetic. In this study, we examined the antinociceptive efficacy enhancements of diphenhydramine when combined with mannitol. Male Sprague-Dawley rats weighing 230–260 g were used in a hot plate test to evaluate the antinociceptive effects of diphenhydramine. All chemicals were dissolved in isotonic normal saline and administered subcutaneously into the plantar surface of the right hind paw at 10 min before the hot plate test. A subcutaneous injection of 0.5% or 1% diphenhydramine produced significant inhibition of the withdrawal latency time compared with the vehicle treatment. Antinociceptive effects appeared 10 min after the diphenhydramine injections and persisted for over 30 min. The antinociceptive effects of 1% diphenhydramine were not statistically different from those of 1% lidocaine. Although a subcutaneous injection of a 0.5 M mannitol solution alone did not affect the withdrawal latency time, 1% diphenhydramine with 0.5 M mannitol significantly enhanced antinociception. A subcutaneous injection of 1% diphenhydramine with epinephrine (1 : 100,000) solution did not increase the antinociceptive effect of the diphenhydramine. These results suggest that diphenhydramine with mannitol can be used as an alternative local anesthetic.


2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Amjad Ali ◽  
Abdul Nasir ◽  
Syed Wadood Ali Shah ◽  
Atif Ali Khan Khalil ◽  
Mi-jeong Ahn ◽  
...  

Abstract Background In order to find a new natural resource for pain-relief, the analgesic effects of Ilex dipyrena crude extract, fractions, and subfractions were evaluated in in-vivo mouse models with possible mechanism of action. Methods Analgesic effects of crude extract (100 and 200 mg/kg body weight), fractions and subfractions (75 mg/kg body weight) were screened using heat-induced (tail-immersion and hot plate test) and chemical-induced (formalin and acetic acid) nociception models in mice. The samples were also tested for the elucidation of a possible mechanism through opioidergic and GABAergic systems. Results The administration of crude extract, fractions and subfractions produced analgesic responses in acetic acid, formalin, tail immersion, and hot plate model for pain similar to those obtained with the standard. Naloxone antagonized the antinociceptive effects of the tested samples, whereas bicuculline showed partial inhibition. Considering the analgesic response, crude extract, fractions, and subfractions demonstrated promising inhibitory activity against all test models for pain, which was further supported by the possible involvement of opioidergic and GABAergic systems. Conclusion The results suggest that this plant may be useful in the development of new analgesic drugs. Further research with regard to the isolation of bioactive compounds is required to verify these findings.


Author(s):  
E.Yu. Bibik ◽  
◽  
L.I. Kurbanov ◽  
S.A. Grygoryan ◽  
D.S. Krivokolysko ◽  
...  

Nowadays the search of new high-efficiency and safe drugs for the pharmacotherapy of diseases accompanied by pain syndrome is an active area of modern pharmacological research. 170 new derivatives of di- and tetrahydropyridines synthesized on the basis of the Chemex Research Laboratory, Vladimir Dahl Lugansk State University were exposed to the virtual bioscreening using the Swiss Target Prediction software. The paper describes screening studies in vivo of 5 samples of sulfur-containing di- and tetrahydropyridines (laboratory codes d02-138, as-262, f02-079, cv-074, cv-143) in the standard hot plate test in comparison with the reference drug — metamizole sodium. The compounds in the dose of 5 mg/kg were given intragastrically 1 hour and a half before placing the rats on the hot plate, the reference drug in the dose of 7 mg/kg also was given intragastrically 1 hour and a half before placing the rats on the hot plate. The compounds with laboratory codes as-262 (allyl 6-({2-[(4-acetylphenyl)amino]-2-oxoethyl}thio)-5-cyano-4-(2-furyl)-2-methyl-1,4-dihydropyridine-3-carboxylate) and d02-138 (ethyl 4-[({[3-cyano-5-{[(2,4-dichlorophenyl)amino]carbonyl}-4-(2-furyl)-6-methyl-1,4-dihydropyridinе-2-yl]thio}acetyl)amino]benzoate) possess the most pronounced analgesic activity in the dose of 5 mg/kg, they demonstrated 2.03 and 1.9-fold efficiency in comparison to metamizole sodium respectively. The rest three specimens demonstrated metamizole sodium-like analgesic activity.


Toxins ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 589
Author(s):  
Elena Lucia Anna Malpezzi-Marinho ◽  
Cristiane Isabel Silva Zanoni ◽  
Graziella Rigueira Molska ◽  
Camila Paraventi ◽  
Raphael Wuo-Silva ◽  
...  

Pain is a distressful experience that can have a major impact on an individual’s quality of life. The need for new and better analgesics has been further intensified in light of the current opioid epidemic. Substances obtained from amphibians have been shown to contain bioactive peptides that exert analgesic effects. The genus Phyllomedusa represents an important source of peptides and bioactive components. The aim of this study was to investigate the antinociceptive effects of the skin secretion of Phyllomedusa rohdei in rodent models of pain. The crude skin extract of P. rohdei was tested in different pain models: acetic acid-induced writhing test (mice), formalin test (rats), Von Frey electronic test for hypernociception induced by PGE2 (rats), and hot plate test (mice). Motor-impairing effects were tested using the rota-rod test. The results showed that the skin extract of P. rohdei exerted antinociceptive effects in all pain models tested. Particularly, the highest dose tested of the skin extract decreased acetic acid-induced writhing by 93%, completely blocked formalin-induced nociception both during the acute and inflammatory phases of the test, PGE2-induced hypernociception by 73% and increased latency to paw withdrawal in the hot plate test by 300%. The effects observed in the hot plate test were reversed by pretreatment with selective µ and κ, but not δ, opioid receptor antagonists, indicating a mechanism of action dependent on µ and κ opioid receptors. The results were not influenced by sedative effects. Further studies remain necessary to reveal the specific compounds involved in the antinociceptive effects of P. rohdei skin extract as a new therapeutic tool in pain management.


2010 ◽  
Vol 29 (10) ◽  
pp. 881-886 ◽  
Author(s):  
Danish Mahmood ◽  
M. Akhtar ◽  
Divya Vohora ◽  
Razia Khanam

Antidepressants (ADs) are frequently used for the treatment of persistent pain associated with diabetic neuropathy. The aim of this study is to investigate the antinociceptive effects of sertraline (Ser) and amitriptyline (Ami) in diabetic rats, and additionally monitoring their effects on grip strength, blood glucose and percentage glycosylated hemoglobin (GHb%) levels. Streptozotocin (STZ; 55 mg/kg, intraperitoneal [ip]) was injected in rats to induce diabetes. After 7 days, Ser (30 mg/kg) or Ami (15 mg/kg) was administered in diabetic rats orally. After 28 days drug treatment, the antinociceptive effects were evaluated using hot plate test both in diabetic and non-diabetic rats. The effects of these drugs on grip strength, blood glucose and GHb% were also measured. Ser and Ami showed antinociceptive effects in diabetic and non-diabetic rats. Both the drugs increased the grip strength reduction in STZ-induced diabetic rats. Ser reduces and Ami increases the serum glucose levels in diabetic and normal rats. Administration of Ami per se increased GHb% levels, while Ser per se has no effects. The effects of Ser (30 mg/kg, per os [po]) on glucose, GHb% and antinociceptive action on hot plate test showed an association between improved blood glucose levels and analgesia. However, the results of Ami treatment are controversial and needs further studies.


Author(s):  
Venkatesh Sama ◽  
Azmathunnisa Begum ◽  
Rajesh Bolleddu ◽  
Ravi Alvala ◽  
Jaya Prakash D

Barleria prionitis Linn.(Acanthaceae) is a prickly shrub and traditionally whole plant is used as anti-inflammatory, expectorant, analgesic, diuretic, antirheumaticand antidiabetic. This study was conducted to investigate the antinociceptive and CNS depressant activity of ethanolic extract and the fractions of B. prionitis in mice. Ethanol extract and its fractions were tested at a dose of 200 and 400 mg/kg. Ethanol, petroleum ether and chloroform fractions demonstrated significant antinociceptive activity at 400 mg/kg and significantly increased the latency in hot plate test and the action was antagonised by naloxone, indicating a potential opioid-like mechanism. In conclusion, the ethanol, pet ether and chloroform fractions of B. prionitis markedly demonstrated the antinociceptive action. The CNS depressant and good protective effect on pain stimuli suggest that the possible mechanisms appear to be due to involvement of opioid and/or peripheral receptors. 


2018 ◽  
Vol 2018 ◽  
pp. 1-6 ◽  
Author(s):  
Liping Sun ◽  
Lei Liao ◽  
Bei Wang

Propolis is an important bee product which has been applied to the treatment of several diseases. The aim of this study was to understand the material basis of Chinese propolis on pain relief; different Chinese propolis fractions (40W, 40E, 70E, and 95E raw propolis extracted followed by 40%, 70%, or 95% ethanol) were prepared, and their antinociceptive effects were evaluated. By analyzing using UPLC-Q-TOF-MS, we showed that 40W was rich in phenolic acids, like caffeic acid, while 40E, 70E, and 95E have relatively high levels in flavonoids, like galangin, pinocembrin, and chrysin. Notably, chrysin amounts in 70E and 95E are much higher than those in 40E fraction. Antinociceptive effects by these propolis fractions were evaluated in mice using acetic acid-induced writhing test, hot plate test, and tail immersion test, respectively. We noticed that only 40E fraction showed a significant reduction on acetic acid-induced writhing test. Importantly, in the hot plate test, all groups showed their effectiveness, except for the 70E group. We also noticed that 40W, 40E, and 95E administration caused an increase in the tail withdrawal latency of the mice. These data suggested that the different antinociceptive effects of different fractions from Chinese propolis extracts are directly link to their flavonoid composition.


2010 ◽  
Vol 34 (2) ◽  
pp. 73-78
Author(s):  
Ahmed Najim Abed saleh

In the present work, the antinociceptive action was assayed in several experiment models in mice, Hot plate, writhing and formalin test. The alcoholic extract of MP leaves at a dose of 150mg/kg B.W and 300 mg/kgB.W showed antinociceptive effects in different methods, where the dose of 300 mg/kg B.W showed significant reduction of the nociception by acetic acid. In the formalin test, the extract (300mg/kg B.W) also significantly reduced painful stimulus in both phases of the test. Treatment with extract (300mg/kg B.W) when given orally produced significant increase of the reaction time in hot plate test. These results showed that the leaves extract of MP contain active analgesic principles acting both centrally and peripherally.


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