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 Biological Screening of Novel Structural Analog of Celecoxib as Potential Anti-Inflammatory and Analgesic Agent

Medicina ◽  
2019 ◽  
Vol 55 (4) ◽  
pp. 93
Author(s):  
Hristina Zlatanova ◽  
Stanislava Vladimirova ◽  
Ilia Kostadinov ◽  
Delian Delev ◽  
Tanya Deneva ◽  
...  
Keyword(s):  
Propionic Acid ◽  
Inflammatory Activity ◽  
Saline Control ◽  
Tail Flick ◽  
Analgesic Action ◽  
Paw Edema ◽  
Continuous Administration ◽  
Organ Toxicity ◽  
Multiple Administration ◽  
Anti Inflammatory

Background and objectives: The clinical use of non-steroidal anti-inflammatory drugs is limited due to high incidence of adverse drug reactions. The pyrrole heterocycle is included in the chemical structure of a number of drugs with various activities and shows relatively good tolerability and safety. The objectives of our study were to evaluate the analgesic and anti-inflammatory activity, as well as possible organ toxicity, of 2-[3-acetyl-5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-3-(1H-indol-3-yl)-propionic acid (compound 3g), a novel N-pyrrolylcarboxylic acid structurally similar to celecoxib. Materials and methods: All experiments were performed on 6-week-old male Wistar rats divided into parallel groups (n = 8). Antinociception was assessed using animal pain models with thermal and chemical stimuli (paw withdrawal, tail-flick, and formalin tests). Criteria for the analgesic effect were increased latency in the paw withdrawal and tail-flick tests and decreased paw licking time in the formalin test compared to animals treated with saline (control). Anti-inflammatory activity was measured using a carrageenan-induced paw edema model; the criterion for anti-inflammatory effect was decreased edema compared to control. Blood samples were obtained after animals were sacrificed to assess possible organ toxicity. Statistical analysis was performed with IBM SPSS 20.0. Results: 2-[3-Acetyl-5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-3-(1H-indol-3-yl)-propionic acid had analgesic action against chemical stimulus after single and multiple administration and against thermal stimulus after single administration. Compound 3g significantly suppressed carrageenan-induced paw edema after both single and continuous administration. After continuous administration, hematological tests showed that compound 3g decreased leukocyte and platelet levels and elevated serum creatinine levels. Conclusions: Antinociception with the tested compound is most likely mediated by spinal, peripheral, and anti-inflammatory mechanisms. Possible tolerance of the analgesic action at the spinal level develops after continuous administration. Anti-inflammatory activity is significant and probably the leading cause of antinociception. After multiple administration, compound 3g showed signs of potential nephrotoxicity and antiplatelet activity, as well as suppression of leukocyte levels.

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.

scholarly journals ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF VARIOUS EXTRACTS OF CLAUSENA DENTATA (WILLD.) ROEM

2018 ◽  
Vol 11 (2) ◽  
pp. 413
Author(s):  
Raju Kamaraj ◽  
Annamalai Maduram
Keyword(s):  
Tamil Nadu ◽  
Tween 80 ◽  
Volatile Oil ◽  
Stem Bark ◽  
Inflammatory Activity ◽  
Control Group ◽  
Tail Flick ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory

 Objectives: The present study was undertaken to study the analgesic and anti-inflammatory activity of various extracts of Clausena dentata. Clausena (Rutaceae) is a genus of about 23 species of unarmed trees and shrubs. The stem bark of C. dentata is used in veterinary medicine for the treatment of wounds and sprains. Even though C. dentata has a lot of potential medical uses, the study of pharmacological properties is very scarce.Methods: The plant C. dentata was collected in May 1999 from Kadagaman, near Tiruvannamalai, Tamil Nadu, India, and authenticated by Centre for Advanced Study in Botany, University of Madras, Chennai. The dry powder of stem bark was extracted with hexane, chloroform, and methanol. The extracts were subjected to thin-layer chromatography and phytochemical screening. Further, the extracts were tested for analgesic by the tail flick and anti-inflammatory by carrageenan-induced rat paw edema using plethysmometer.Results: Qualitative chemical tests revealed the presence of various phytochemicals such as alkaloids, glycosides, carbohydrate, proteins and amino acids, phytosterols, and volatile oil. The hexane, chloroform, and methanol extracts exhibited significant analgesic activity as compared to control group (Tween 80, 1%). The anti-inflammatory activity of C. dentata extracts revealed that the percent inhibition of carrageenan-induced rat hind paw edema was highly significant as compared to control group after 4 h of injection.Conclusion: The presence of coumarin and alkaloids all the extracts promising properties of analgesic and anti-inflammatory.

scholarly journals Evaluation of Analgesic and Anti-Inflamatory Activity of Ventilago calyculata

2015 ◽  
Vol 9 (1) ◽  
pp. 43-47
Author(s):  
G. Pranaya ◽  
P. Venkata Smitha ◽  
N. Srinivasa Reddy ◽  
R. Vinay ◽  
Ch. Murali Mohan ◽  
...  
Keyword(s):  
Formalin Test ◽  
Methanolic Extract ◽  
Life Sciences ◽  
Inflammatory Activity ◽  
Tail Flick ◽  
Paw Edema ◽  
Hot Plate ◽  
Plate Method ◽  
Ear Edema ◽  
Anti Inflammatory

Ventilago calyculata was traditionally used to treat sprains and pain. The purpose of this study was to evaluate the analgesic and anti-inflammatory activity of methanolic extract of bark of Ventilago calyculata (MVC). For evaluating analgesic activity, Hot plate method, Tail-flick method, Formalin test and Writhing methods were used. For evaluating anti-inflammatory activity Carrageenan induced paw edema and Xylene induced ear edema methods were used. Administration of MVC (100 and 200mg/kg) significantly reduced the total number of writhings in Acetic acid induced writhing method. In Hot plate and Tail-Flick methods there was a significant increase in baseline. There was a significant reduction in ear edema in Xylene induced ear edema method. The results suggest that the methanolic extract of bark of Ventilago calyculata might have analgesic and anti-inflammatory activity.DOI: http://dx.doi.org/10.3126/ijls.v9i1.11925 International Journal of Life Sciences Vol.9(1) 2015 43-47

Thiazole-Based Chalcone Derivatives as Potential Anti-inflammatory Agents: Biological Evaluation and Molecular Modelling

2020 ◽  
Vol 21 ◽  
Author(s):  
Michelyn Haroun ◽  
Christopher Tratrat ◽  
Evangelia Tsolaki ◽  
Anthi Petrou ◽  
Antonis Gavalas ◽  
...  
Keyword(s):  
Aromatic Aldehyde ◽  
Molecular Modelling ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Chalcone Derivatives ◽  
Treat Ment ◽  
Anti Inflammatory

Background.: Inflammation is a multifactorial process reflecting response of the organismto various stimuli and is associated to a number of disorders such as arthritis, asthma and psoriasis, which require long-lasting or repeated treat-ment. Objective.: The aim of this paper is to evaluate the anti-inflammatory activity of previous synthesized thiazole-based chal-cone derivatives. Method.: Chalcones were synthesized via Cliazen-Schmidt condensation1-(4-methyl-2-alkylamino)thiazol-5-yl) ethanone with corresponding aromatic aldehyde. For the evaluation of possible anti-inflammatory activity carrageneen mouse paw edema was used. Results.: Eight out of thirteen tested chalcones showed anti-inflammatory activity in range of 51-55%. Prediction of toxicity revealed that these compounds are not toxic. Conclusion.: In general, it can be concluded that these compounds can be used for further modifications in order to develop more active and safe agents.

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.

ANTIULCER AND ANTI-INFLAMMATORY ACTIVITIES OF HYDROALCOHOLIC EXTRACTS OF STEM BARK AND LEAF OF ANOGEISSUS PENDULA EDGEW

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (01) ◽  
pp. 41-46
Author(s):  
Deeksha Singh ◽  
◽  
Amit Nayak ◽  
Rakesh Yadav ◽  
Uttam Singh Baghel ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Stem Bark ◽  
Inflammatory Activity ◽  
Antiulcer Activity ◽  
Paw Edema ◽  
Ulcer Index ◽  
Pylorus Ligation ◽  
Anti Inflammatory ◽  
Anogeissus Pendula

Anogeissus pendula Edgew has been reported to be used in gastric disorder even though no attempt has been made to evaluate the same. The present study was designed to evaluate the hydroalcoholic extracts of stem bark and leaves for in vivo acute antiulcer and anti-inflammatory activities. Antiulcer activity was studied by pylorus ligation induced ulcers while anti-inflammatory activities was studied by carrageenan induced paw edema. The extract of stem bark at 200 and 400 mg/kg b. w., significantly (P<0.05) reduced ulcer index whereas extracts of both stem bark and leaves significantly (P<0.001) reduced paw diameter at the fifth hour. The hydroalcholic extract of stem bark of A. pendula possesses more significant antiulcer and anti-inflammatory activity than the hydroalcholic extract of leaves may be due to the presence of higher amount of phenolic compounds.

scholarly journals Anti-inflammatory activity and modulate oxidative stress of Bucida buceras in lipopolysaccharide-stimulated RAW 264.7 macrophages and Carrageenan-induced acute paw edema in rats

2017 ◽  
Vol 11 (12) ◽  
pp. 239-252 ◽  
Author(s):  
B. Iloki Assanga Simon ◽  
M. Lewis Luján Lidianys ◽  
A. Gil-Salido Armida ◽  
L. Lara Espinoza Claudia ◽  
Fernandez Angulo Daniela ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Inflammatory Activity ◽  
Raw 264.7 ◽  
Paw Edema ◽  
Raw 264.7 Macrophages ◽  
Anti Inflammatory

scholarly journals SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF NEW NAPROXEN ANALOGUES HAVING 1, 2, 4-TRIAZOLE-3-THIOL

2017 ◽  
Vol 9 (7) ◽  
pp. 66
Author(s):  
Monther F. Mahdi ◽  
Noor H. Naser ◽  
Nethal H. Hammud
Keyword(s):  
Aromatic Aldehydes ◽  
Heterocyclic Ring ◽  
Inflammatory Activity ◽  
Control Group ◽  
Paw Edema ◽  
Dose Equivalent ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: The objective of this search was to synthesize a new naproxen analogues having a 1,2,4-triazole-3-thiol heterocyclic ring, and preliminary pharmacological assessment of the anti-inflammatory activity of the synthesized compounds. Methods: The synthesis of naproxen analogues that having 1,2,4-triazole-3-thiol heterocyclic ring occur through esterification of naproxen, and then its reaction with hydrazine hydrate, and carbon disulfide, finally different aromatic aldehydes reacted with triazole derivatives of naproxen containing amino group to produce schiff bases.Results: In vivo acute anti-inflammatory activity of the synthesize compounds (Va-Vd) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (50 mg/kg) of naproxen. All tested compounds were produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Compound Vd produced superior anti-inflammatory activity compared to naproxen.Conclusion: The results obtained in this work give evidence about the valid synthesis of 1,2,4 triazole-3-thiol derivatives of naproxen, which reacted with different aldehydes to yield several schiff bases. The incorporation of benzaldehyde possess para-electron donating group (para-hydroxyl benzaldehyde) will increase the anti-inflammatory activity of naproxen.

scholarly journals Evaluation of analgesic and anti-inflammatory activity of ethanolic extract of Enhydra fluctuans on male wistar rats

2021 ◽  
Vol 9 (1) ◽  
pp. 1-7
Author(s):  
Kishor Kumar Roy ◽  
Md. Kabirul Islam Mollah ◽  
Md. Masud Reja ◽  
Dibyendu Shil ◽  
Ranjan Kumar Maji
Keyword(s):  
Wistar Rats ◽  
Pain Threshold ◽  
Ethanolic Extract ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Hot Plate ◽  
Plate Method ◽  
Traditional System ◽  
Male Wistar Rats ◽  
Anti Inflammatory

Enhydra fluctuations an edible semi-aquatic vegetable plant are widely used in the traditional system of medicine. Ethanolic extract of Enhydra fluctuans was screened for analgesic & anti-inflammatory activity. Analgesic activity was evaluated by the hot plate method and anti-inflammatory activity was evaluated by formalin induce paw edema in Wistar rats (male). Ethanolic extract dose of 300 mg/kg reduce formalin induce paw inflammation and also increased the pain threshold in rats evidenced by hot plate method. The experimental results concluded that Enhydra fluctuans have significant analgesic and anti-inflammatory activity may due to flavonoid and phenolic compound content.

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