scholarly journals New ibuprofen derivatives with thiazolidine-4-one scaffold with improved pharmaco-toxicological profile

2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Ioana-Mirela Vasincu ◽  
Maria Apotrosoaei ◽  
Sandra Constantin ◽  
Maria Butnaru ◽  
Liliana Vereștiuc ◽  
...  
Keyword(s):  
Analgesic Effect ◽  
Visceral Pain ◽  
Biological Effects ◽  
Maximum Effect ◽  
Tail Flick ◽  
Paw Edema ◽  
Cell Viability Assay ◽  
Thermal Nociception ◽  
Analgesic Effects ◽  
Anti Inflammatory

Abstract Background Aryl-propionic acid derivatives with ibuprofen as representative drug are very important for therapy, being recommended especially for anti-inflammatory and analgesic effects. On other hand 1,3-thiazolidine-4-one scaffold is an important heterocycle, which is associated with different biological effects such as anti-inflammatory and analgesic, antioxidant, antiviral, antiproliferative, antimicrobial etc. The present study aimed to evaluated the toxicity degree and the anti-inflammatory and analgesic effects of new 1,3-thiazolidine-4-one derivatives of ibuprofen. Methods For evaluation the toxicity degree, cell viability assay using MTT method and acute toxicity assay on rats were applied. The carrageenan-induced paw-edema in rat was used for evaluation of the anti-inflammatory effect while for analgesic effect the tail-flick test, as thermal nociception in rats and the writhing assay, as visceral pain in mice, were used. Results The toxicological screening, in terms of cytotoxicity and toxicity degree on mice, revealed that the ibuprofen derivatives (4a-n) are non-cytotoxic at 2 μg/ml. In addition, ibuprofen derivatives reduced carrageenan-induced paw edema in rats, for most of them the maximum effect was recorded at 4 h after administration which means they have medium action latency, similar to that of ibuprofen. Moreover, for compound 4d the effect was higher than that of ibuprofen, even after 24 h of administration. The analgesic effect evaluation highlighted that 4 h showed increased pain inhibition in reference to ibuprofen in thermal (tail-flick assay) and visceral (writhing assay) nociception models. Conclusions The study revealed for ibuprofen derivatives, noted as 4 m, 4 k, 4e, 4d, a good anti-inflammatory and analgesic effect and also a safer profile compared with ibuprofen. These findings could suggest the promising potential use of them in the treatment of inflammatory pain conditions.

scholarly journals New ibuprofen derivatives with thiazolidin-4-one scaffold with improved pharmaco-toxicological profile

2020 ◽  
Author(s):  
Ioana-Mirela Vasincu ◽  
Maria Apotrosoaei ◽  
Sandra Madalina Constantin ◽  
Maria Butnaru ◽  
Liliana Vereștiuc ◽  
...  
Keyword(s):  
Analgesic Effect ◽  
Visceral Pain ◽  
Biological Effects ◽  
Maximum Effect ◽  
Tail Flick ◽  
Paw Edema ◽  
Cell Viability Assay ◽  
Thermal Nociception ◽  
Analgesic Effects ◽  
Anti Inflammatory

Abstract Background Aryl-propionic acid derivatives with ibuprofen as representative drug are very important for therapy, being recommended especially for anti-inflammatory and analgesic effects. On other hand 1,3-thiazolidine-4-one scaffold is an important heterocycle, which is associated with different biological effects such as anti-inflammatory and analgesic, antioxidant, antiviral, antiproliferative, antimicrobial etc. The present study aimed to evaluated the toxicity degree and the anti-inflammatory and analgesic effects of new 1,3-thiazolidine-4-one derivatives of ibuprofen. Methods For evaluation the toxicity degree, cell viability assay using MTT method and acute toxicity assay on rats were applied. The carrageenan-induced paw-edema in rat was used for evaluation of the anti-inflammatory effect while for analgesic effect the tail-flick test, as thermal nociception in rats and the writhing assay, as visceral pain in mice, were used. Results The toxicological screening, in terms of cytotoxicity and toxicity degree on mice, revealed that the ibuprofen derivatives (4a-n) are non-cytotoxic at 2 µg/ml. In addition, ibuprofen derivatives reduced carrageenan-induced paw edema in rats, for most of them the maximum effect was recorded at 4 h after administration which means they have medium action latency, similar to that of ibuprofen. Moreover, for compound 4d the effect was higher than that of ibuprofen, even after 24 h of administration. The analgesic effect evaluation highlighted that 4 h showed increased pain inhibition in reference to ibuprofen in thermal (tail-flick assay) and visceral (writhing assay) nociception models. Conclusions The study revealed for ibuprofen derivatives, noted as 4 m, 4 k, 4e, 4d, a good anti-inflammatory and analgesic effect and also a safer profile compared with ibuprofen. These findings could suggest the promising potential use of them in the treatment of inflammatory pain conditions.

scholarly journals Preliminary assessment of the anti-inflammatory and analgesic effects of methanol leaf extract of Cussonia barteri (Araliaceae) in rodents

2019 ◽  
Vol 65 (3) ◽  
pp. 22-31
Author(s):  
Ighodaro Igbe ◽  
Osaze Edosuyi ◽  
Agbonlahor Okhuarobo ◽  
Adarki Pongri ◽  
Nkechi Maduako ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Analgesic Effect ◽  
Leaf Extract ◽  
Methanol Extract ◽  
Tail Flick ◽  
Hot Plate ◽  
Analgesic Effects ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Ear Oedema

Summary Introduction: Potato (Solanum tuberosum L.) is an important vegetable crop in Syria. Potato tuber moth Cussonia barteri is a small tree that grows in the sub-Saharan part of Africa. Various parts of the plant are used for the treatment of a variety of ailments in ethno-medicine. Objective: To evaluate the anti-inflammatory and analgesic effect of the methanol leaf extract of Cussonia barteri. Material and methods: The leaves were air-dried, powdered and repeatedly extracted with methanol using a Soxhlet apparatus. The resulting methanol extract (100, 200 and 400 mg/kg) was evaluated for anti-inflammatory activity using carrageenan-induced paw oedema, xylene-induced ear oedema and formalin-induced arthritis tests. Analgesic effect was evaluated using acetic acid-induced mouse writhing, hot plate and tail flick tests. Results: All doses of the extract significantly (p<0.05) reduced carrageenan-induced paw oedema, however the 400 mg/kg dose gave a sustained effect. The extract significantly inhibited xylene induced ear oedema at all doses. There were no significant (p>0.05) reductions in paw swellings due to formalin. In the acetic acid induced writhing test, the extract significantly (p<0.05) decreased writhing at 400 mg/kg only. Reaction times were not significantly different from the control in the hot plate and tail flick tests. Conclusion: This study has shown that the methanol extract possesses acute anti-inflammatory and peripherally mediated analgesic effects.

The nitric oxide–cGMP signaling pathway plays a significant role in tolerance to the analgesic effect of morphine

2011 ◽  
Vol 89 (2) ◽  
pp. 89-95 ◽  
Author(s):  
Ercan Ozdemir ◽  
Ihsan Bagcivan ◽  
Nedim Durmus ◽  
Ahmet Altun ◽  
Sinan Gursoy
Keyword(s):  
Nitric Oxide ◽  
Analgesic Effect ◽  
Soluble Guanylate Cyclase ◽  
Morphine Tolerance ◽  
Cyclic Guanosine Monophosphate ◽  
Guanosine Monophosphate ◽  
Albino Rats ◽  
Tail Flick ◽  
Analgesic Effects ◽  
Cgmp Signaling

Although the phenomenon of opioid tolerance has been widely investigated, neither opioid nor nonopioid mechanisms are completely understood. The aim of the present study was to investigate the role of the nitric oxide (NO)–cyclic guanosine monophosphate (cGMP) pathway in the development of morphine-induced analgesia tolerance. The study was carried out on male Wistar albino rats (weighing 180–210 g; n = 126). To develop morphine tolerance, animals were given morphine (50 mg/kg; s.c.) once daily for 3 days. After the last dose of morphine was injected on day 4, morphine tolerance was evaluated. The analgesic effects of 3-(5′-hydroxymethyl-2′-furyl)-1-benzylindazole (YC-1), BAY 41-2272, S-nitroso-N-acetylpenicillamine (SNAP), NG-nitro-l-arginine methyl ester (L-NAME), and morphine were considered at 15 or 30 min intervals (0, 15, 30, 60, 90, and 120 min) by tail-flick and hot-plate analgesia tests (n = 6 in each study group). The results showed that YC-1 and BAY 41-2272, a NO-independent activator of soluble guanylate cyclase (sGC), significantly increased the development and expression of morphine tolerance, and L-NAME, a NO synthase (NOS) inhibitor, significantly decreased the development of morphine tolerance. In conclusion, these data demonstrate that the nitric oxide–cGMP signal pathway plays a pivotal role in developing tolerance to the analgesic effect of morphine.

5-HT1A Receptors Mediate Analgesia Induced by Emulsified Sevoflurane in Thermal Nociception but Have Little Effect on Chemical Nociception

Pharmacology ◽  
2017 ◽  
Vol 100 (1-2) ◽  
pp. 25-30
Author(s):  
Chen Yan ◽  
Dai Ti-jun ◽  
Li Xin ◽  
Cao Gao ◽  
Jiang Shen ◽  
...  
Keyword(s):  
Analgesic Effect ◽  
Intraperitoneal Injection ◽  
Serotonin Receptor ◽  
Intrathecal Injection ◽  
Tail Flick ◽  
Hot Plate Test ◽  
Thermal Nociception ◽  
Tail Flick Latency ◽  
Specific Antagonist ◽  
The Relationship

Objective: The study aimed to investigate the relationship between the analgesic effect of sevoflurane and 5-serotonin receptor 1A (5-HT1A R) in the spinal cords of mice. Methods: Analgesic mouse models were established by intraperitoneal injection of emulsified sevoflurane, and the influence of p-MPPF (a specific antagonist of 5-HT1A Rs) intrathecal injection on the changes in tail-flick latency in tail-withdrawal test, pain threshold in hot-plate test (HPPT), and writhing times in acetic acid-induced writhing test were recorded. Results: Intraperitoneal injection of emulsified sevoflurane alone produced an analgesic effect (p < 0.05). p-MPPF (2, 4, and 8 μg) alone had no impact on tail-flick latency, HPPT, and writhing times in mice (p > 0.05). The 3 doses of p-MPPF reduced the tail-flick latency or HPPT. p-MPPF 8 μg can increase the writhing times (p < 0.05) in analgesic mice with sevoflurane, while p-MPPF 2 and 4 μg did not affect the writhing times. Conclusion: 5-HT1A Rs in the spinal cord may be an important target for the analgesic effect of sevoflurane on the thermal nociception, but it has little relation to the anti-chemical chemical nociceptive effect of sevoflurane.

scholarly journals Cashew (Anacardium occidentale L.) Nuts Counteract Oxidative Stress and Inflammation in an Acute Experimental Model of Carrageenan-Induced Paw Edema

Antioxidants ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 660 ◽  
Author(s):  
Marika Cordaro ◽  
Rosalba Siracusa ◽  
Roberta Fusco ◽  
Ramona D’Amico ◽  
Alessio Filippo Peritore ◽  
...  
Keyword(s):  
Inflammatory Cytokines ◽  
Radical Scavenging ◽  
Oxygen Free Radical ◽  
Anacardium Occidentale ◽  
Oxidative Enzymes ◽  
Paw Edema ◽  
Analgesic Effects ◽  
Carrageenan Injection ◽  
Anti Inflammatory ◽  
The Right

Background: Anacardium occidentale L. is a medicinal plant with powerful anti-oxidative and anti-inflammatory properties. Acute inflammatory events cause tissue alterations, decrease of anti-oxidative endogenous enzymes such as superoxide dismutase, catalase and glutathione, neutrophils infiltration, increase in the activities of myeloperoxidase, malondialdehyde, and pro-inflammatory release. Methods: Paw edema was induced by subplantar injection of carrageenan into the right hind paw in rats, but 30 min before a group of animals were orally treated with 100 mg/kg of cashew nuts to evaluate the anti-inflammatory and anti-oxidative response. Results: In the present work, we found that (1) cashew nuts reduced the development of carrageenan-induced paw edema limiting the formation of edema and pain; (2) cashew nuts ameliorated the diminutions of the anti-oxidative enzymes caused by carrageenan injection; (3) cashew nuts decreased myeloperoxidase malondialdehyde activity induced by carrageenan; and (4) cashew nuts acted by blocking pro-inflammatory cytokines response and nitrate/nitrite formation stimulated by carrageenan injection. Conclusions: The mechanisms of anti-inflammatory and analgesic effects exerted by cashew nuts were relevant to oxygen free radical scavenging, anti-lipid peroxidation, and inhibition of the formation of inflammatory cytokines.

scholarly journals Analgesic and Anti-Inflammatory Activities of Methanol Extract ofFicus pumilaL. in Mice

2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Chi-Ren Liao ◽  
Chun-Pin Kao ◽  
Wen-Huang Peng ◽  
Yuan-Shiun Chang ◽  
Shang-Chih Lai ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Methanol Extract ◽  
Inflammatory Diseases ◽  
Paw Edema ◽  
Tissue Destruction ◽  
Hplc Fingerprint ◽  
Analgesic Effects ◽  
Inflammatory Mechanism ◽  
Tnf Α ◽  
Anti Inflammatory

This study investigated possible analgesic and anti-inflammatory mechanisms of the methanol extract ofFicus pumila(FPMeOH). Analgesic effects were evaluated in two models including acetic acid-induced writhing response and formalin-induced paw licking. The results showedFPMeOHdecreased writhing response in the acetic acid assay and licking time in the formalin test. The anti-inflammatory effect was evaluated by λ-carrageenan-induced mouse paw edema and histopathological analyses.FPMeOHsignificantly decreased the volume of paw edema induced by λ-carrageenan. Histopathologically,FPMeOHabated the level of tissue destruction and swelling of the edema paws. This study indicated anti-inflammatory mechanism ofFPMeOHmay be due to declined levels of NO and MDA in the edema paw through increasing the activities of SOD, GPx, and GRd in the liver. Additionally,FPMeOHalso decreased the level of inflammatory mediators such as IL-1β, TNF-α, and COX-2. HPLC fingerprint was established and the contents of three active ingredients, rutin, luteolin, and apigenin, were quantitatively determined. This study provided evidence for the classical treatment ofFicus pumilain inflammatory diseases.

scholarly journals Pre-treatment Effect of Kombucha Tea on Analgesia and Inflammation in Male Rat

2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Zahra Rabiei ◽  
Zahra Lorigooini ◽  
Fatemeh Firuzi ◽  
Mohammad Rahimi-Madiseh
Keyword(s):  
Acetic Acid ◽  
Pain Tolerance ◽  
Male Rat ◽  
Control Group ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Analgesic Effects ◽  
Kombucha Tea ◽  
Anti Inflammatory

Background: The use of natural compounds in relieving pain has been commonplace since ancient times and their use is currently increasing. Objectives: Given that analgesic and anti-inflammatory effects of Kombucha have not been studied, this study was designed to examine these effects in vitro. Methods: In this experimental study, rats were divided into four groups. The control group received normal saline i.p in the same amount of the drug. The other groups received Kombucha tea i.p at 250, 500, and 1000 mg/kg. Tail-flick and acetic acid tests were used to evaluate the analgesic effects of Kombucha tea and the xylene-induced ear inflammation test to evaluate the anti-inflammatory effects of Kombucha tea. Results: Kombucha tea at three doses 250, 500, and 1000 mg/kg significantly reduced the number of writhings in the acetic acid test. Kombucha tea at 1000 mg/kg significantly increased pain tolerance in the tail-flick test. Kombucha tea at 250 and 500 mg/kg could significantly reduce inflammation in the rat’s ear. Conclusions: The results of this study indicate that Kombucha has analgesic effects in rats and can be considered in future treatments.

scholarly journals Novel N-Pyrrolylcarboxylic Acid Derivative as a Potential New Analgesic and Anti-Inflammatory Drug

2017 ◽  
Vol 1 (1) ◽  
pp. 1-11
Author(s):  
Hristina Zlatanova ◽  
Stanislava Vladimirova ◽  
Ilia Kostadinov ◽  
Delian Delev ◽  
Tanya Deneva ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Tail Flick ◽  
Analgesic Action ◽  
Paw Edema ◽  
Pentanoic Acid ◽  
Experimental Conditions ◽  
Organ Toxicity ◽  
Multiple Administration ◽  
Chemical Stimuli ◽  
Anti Inflammatory

The objective of our study was to evaluate the analgesic and anti-inflammatory activity, as well as possible organ toxicity of 2-3-3-methyl-pentanoic acid (compound 3d), a newly synthesized pyrrolic derivative, structurally similar to Celecoxib. Antinociception was assessed using animal pain models with thermal and chemical stimuli (paw withdrawal, tail-flick and formalin test). Anti-inflammatory activity was measured using the carrageenan-induced paw edema model. Blood samples were collected from the animals to study possible organ toxicity. All experiments were performed on male Wistar rats. The results in our study show that in experimental conditions 2-3-3-methyl-pentanoic acid has analgesic action against thermal and chemical stimuli. This effect is registered after both single and multiple administration of the compound. In the carrageenan model after single administration compound 3d did not inhibit formation of paw edema. After multiple administration all doses of compound 3d significantly suppressed paw edema at second, third and fourth hours. Hematological tests showed that compound 3d did not affect red blood cells and platelets but decreased white blood cell levels and the highest used dose decreased hemoglobin as well. Compound 3d decreased blood sugar levels and liver transaminases, compared to the control. Compound 3d did not affect creatinine levels but the smallest dose used lowered blood urea. We concluded antinociception in the tested compound is most likely mediated by supraspinal, spinal and peripheral mechanisms. Possible tolerance develops towards the analgesic action on spinal level after continuous administration. Anti-inflammatory activity, though significant, is probably not the leading cause for antinociception.

scholarly journals Comparative Anti-Inflammatory and Analgesic Activities of Qurs-Saffron and Quknar Polyherbal Tablets in Mouse Model

2020 ◽  
Vol 7 (4) ◽  
pp. 199-205
Author(s):  
Muhammad Shoaib Akhtar ◽  
Abdul Malik ◽  
Haroon Arshad ◽  
Nabiha Pervez ◽  
Nadeem Irshad
Keyword(s):  
Radical Scavenging ◽  
Toxicity Testing ◽  
Paw Edema ◽  
Standard Drug ◽  
Analgesic Effects ◽  
Parametric Data ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Radical Scavenging Properties ◽  
One Way Anova

Objective: We aimed to study the anti-inflammatory and analgesic effects for two polyherbal tablets in animal model. Methods: Suspensions of Qurs-Saffron and Quknar polyherbal formulations (p.o.) were evaluated for their anti-inflammatory (in carrageenan-induced paw edema) and analgesic activities (in formalin-induced paw licking test) in albino mice using Ibuprofen (50 mg/kg, orally) as standard drug. Acute toxicity testing of suspensions from Qurs-Saffron and Quknar tablets was also performed at doses 1, 2 and 3 gm/kg, orally. Parametric data were evaluated by one way ANOVA followed by Tukey’s test while graphics were made using GraphPad Prism. Results: Administration of Qurs-Saffron (1000, 1500, 2000 mg/kg) and Quknar (500, 750, 1000 mg/kg) suspensions showed significant (P < 0.05) inhibition of paw edema and at later time point (after 3 hours), both suspensions showed highly significant (P < 0.001) inhibition of paw edema. In another experiment (formalin-induced paw licking test), Qurs-Saffron (2000 mg/kg) and Quknar (1000 mg/kg) showed the highly significant (P < 0.001) analgesic activity. Conclusion: Qurs-Saffron and Quknar tablets possessed anti-inflammatory and analgesic effects that were most likely due to flavonoids and phenolic compounds with free radical scavenging properties which significantly reduced inflammation and pain in treated mice and were also found safe in toxicity testing.

scholarly journals Analgesic and Anti-Inflammatory Activities of Eurycoma longifolia root in Mice

2018 ◽  
Vol 16 (2) ◽  
pp. 182
Author(s):  
Phebe Hendra ◽  
Wina Susana ◽  
Indriyani Permatasari ◽  
Jessy Florensia ◽  
Monita Natalia Siregar
Keyword(s):  
Analgesic Effect ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Eurycoma Longifolia ◽  
Peripheral Pain ◽  
Chemical Stimuli ◽  
Anti Inflammatory

This study was conducted to evaluate the analgesic and anti-inflammatory acitvities of Eurycoma longifolia root in mice. The analgesic effect was assessed using chemical stimuli (wrihting test) to induce peripheral pain in mice. The anti-inflammatory activity was determined using carrageenan-induced paw edema in mice. This study exhibites that Eurycoma longifolia root possesses analgesic and anti-inflammatory activities in mice.

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