scholarly journals Evaluation of in vivo anti-inflammatory activity of Ariflex tablet in comparison with diclofenac and aceclofenac tablet in carrageenan induced rat paw edema model

2021 ◽  
Vol 9 (10) ◽  
pp. 2966
Author(s):  
Sanjay Nipanikar ◽  
Sohan S. Chitlange
Keyword(s):  
Lateral Malleolus ◽  
Inflammatory Activity ◽  
Control Group ◽  
Paw Edema ◽  
Surgical Interventions ◽  
Locomotor Disability ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

Background: Osteoarthritis is a major cause of pain and locomotor disability worldwide. Though various pharmacological, mechanical and surgical interventions are used, there is no known cure for OA. The present study was conducted to evaluate anti-inflammatory activity of Ariflex tablet (conceptualized and developed by Ari Healthcare Pvt. Ltd.) in comparison with diclofenac and aceclofenac tablet in carrageenan induced rat paw edema model.Methods: Wistar rats of either sex weighing 150-180 g were taken and divided into 4 groups with 6 animals in each group i.e. group 1 (control group), group 2 (diclofenac tablet), group 3 (aceclofenac tablet) and group 4 (ariflex tablet). The study drugs were orally administered with feeding needle, 30 minutes prior to carrageenan injection. After 30 min 1% w/v of 0.05 ml carrageenan was injected subcutaneously in the rat paw. The paw was marked with ink at the level of lateral malleolus and immersed in mercury up to lateral malleolus mark. The paw volume was measured plethysmographically after injection at 30 minutes, 1 hour, 2 hour, 3 hour, 4 hour and eventually at 5 hour.Results: All the test formulations possess statistically significant (p<0.05) anti-inflammatory activity as compared to control group. The maximum percentage inhibition for Ariflex tablet was 96.97% at the end of 5 hours. When compared to control group, statistically significant reduction of paw edema was observed. The anti-inflammatory activity of Ariflex tablet from 2 hours onwards is comparable to that of diclofenac tablet and aceclofenac tablet.Conclusions: Ariflex tablet possesses significant anti-inflammatory activity.

scholarly journals EVALUATION OF ANTI-INFLAMMATORY (IN VIVO) ACTIVITY OF ARIFLEX LINIMENT IN COMPARISON WITH DICLOFENAC GEL IN CARRAGEENAN INDUCED RAT PAW EDEMA MODEL

2021 ◽  
pp. 67-70
Author(s):  
SANJAY NIPANIKAR ◽  
S. S. CHITLANGE
Keyword(s):  
Significant Inhibition ◽  
Lateral Malleolus ◽  
Inflammatory Activity ◽  
Control Group ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Rat Paw

Objective: The present study was conducted to evaluate anti-inflammatory activity of Ariflex liniment (conceptualized and developed by Ari Healthcare Pvt. Ltd) in comparison with Diclofenac gel in carrageenan induced rat paw edema model. Methods: Wistar rats of either sex weighing 150-180 g were taken and divided into 3 groups with 6 animals in each group i.e. Group 1 (Controlled Group), Group 2 (Diclofenac gel) and Group 3 (Ariflex liniment). The study drugs were topically applied 30 min prior to carrageenan injection. After 30 min 1% w/v of 0.05 ml carrageenan was injected subcutaneously in the paw. The paw was marked with ink at the level of lateral malleolus and immersed in mercury up to the lateral malleolus mark. The paw volume was measured plethysmographically, immediately after injection i.e. on 0 min, and then on 30 min,1h, 2h,3h, 4h and 5hr after injection. Results: Diclofenac gel sodium treated group showed significant inhibition (p<0.01) of paw edema at 30 min, 1, 2, 3, 4 and 5th hrs as compared to control group. Ariflex Liniment showed significant inhibition (p<0.05) of paw edema at 30 min, 1, 2, 3, and 4th hrs as compared to the control group. Group treated with Ariflex Liniment did not show any significant decrease in paw edema volume at 5th hrs when compared to the control group. Conclusion: Ariflex Liniment possesses anti-inflammatory activity.

Inhibition of iNOS by Benzimidazole Derivatives: Synthesis, Docking, and Biological Evaluations

2021 ◽  
Vol 17 ◽  
Author(s):  
Richa Minhas ◽  
Yogita Bansal
Keyword(s):  
Inflammatory Activity ◽  
Benzimidazole Derivatives ◽  
Critical Study ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Inos Inhibitors ◽  
Rat Paw

Background: Inducible nitric Oxide Synthase (iNOS) plays a key role in the progression of inflammatory diseases by accelerating the production of NO, which makes it an intriguing target to treat inflammation in complex diseases. Therefore, the search is on to develop molecules as selective iNOS inhibitors. Objective: The present work was aimed to design, synthesize and evaluate benzimidazole-coumarin coupled molecules as anti-iNOS agents through in silico and pharmacological studies. Methods: A critical study of literature reports on iNOS inhibitors led to the selection of a (un)substituted coumarin nucleus, 2-aminobenzimidazole, and a 4-atom linker as important structural components for iNOS inhibition. Two series of compounds (7-16 and 17-26) were designed and synthesized by coupling these components. The compounds were subjected to docking using iNOS (1QW4) and nNOS (1QW6) as targets. All compounds were evaluated for NO and iNOS inhibitory activities in vitro. The selected compound was finally evaluated for anti-inflammatory activity in vivo using the carrageenan-induced rat paw edema model. Results : All compounds showed moderate to good inhibition of NO and iNOS in vitro. Compound 12 was the most potent inhibitor of NO and iNOS. Hence, it was evaluated in vivo for toxicity and anti-inflammatory activity. It was found to be safe in acute toxicity studies, and effective in reducing the rat paw edema significantly. Its anti-inflammatory behaviour was similar to that of aminoguanidine, which is a selective iNOS inhibitor. Conclusion: The newly synthesized benzimidazole-coumarin hybrids may serve as potential leads for the development of novel anti-iNOS agents.

scholarly journals Synthesis and Evaluation of Anti-inflammatory Activity of some Thiazolo[4,5-b]pyridines

2021 ◽  
Vol 12 (6) ◽  
pp. 7226-7238
Keyword(s):  
Mass Spectrometry ◽  
1H Nmr Spectroscopy ◽  
Functional Model ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Acylation Reactions

The 18 new thiazolo[4,5-b]pyridin-2-one derivatives have been synthesized using alkylation, cyanethylation, hydrolysis, and acylation reactions. The structures of the obtained compounds have been confirmed by 1H NMR spectroscopy, mass spectrometry, and elemental analysis. The study of the in vivo anti-inflammatory activity of the synthesized substances was assessed by using the functional model of carrageenan-induced rat paw edema. The present results of anti-inflammatory activity have shown that the synthesized compounds demonstrated considerable anti-inflammatory effects. Some of them approach or exceed the comparative drug Ibuprofen in terms of activity.

scholarly journals Synthesis of some new thiazolo[4,5-b]pyridin-2-ones and research of their anti-inflammatory activity

2019 ◽  
pp. 52-60
Author(s):  
T. I. Chaban
Keyword(s):  
Acetic Acid ◽  
Structural Modification ◽  
Acid Hydrazide ◽  
Inflammatory Activity ◽  
In Vivo Studies ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

In modern theoretical and clinical medicine inflammation problem remains one of the main.Deregulation of inflammatory processes leads to specific pathologies.There is a significant amount of drugs used to treat inflammation. But all of them have varying degrees of ulcerogenic properties. To overcome these limitations search is ongoing throughout the World to find new effective and safe anti-inflammatory agent. Therefore, of course, the synthesis of thiazolidines annelated with the pyridine cycle and the study of their anti-inflammatory properties is an interesting and relevant area. The objective of the present work was to synthesize a series of novel thiazolo[4,5-b]pyridine-2-ones by the structural modification of the (5,7-dimethyl-2-oxo-thiazolo[4,5-b]pyridine-3-yl)-acetic acid hydrazide for further pharmacological screening in vivo as anti-inflammatory activities. The objects of the study were thiazolo[4,5-b]pyridines, obtained by the structural modification of the (5,7-dimethyl-2-oxo-thiazolo[4,5-b]pyridine-3-yl)-acetic acid hydrazide. Anti-inflammatory activity was evaluated using carrageenan induced rat paw edema method in rats In vivo studies were carried out  for anti-inflammatory activity employing the carrageenan-induced rat paw edema method. Anti-inflammatory activity was defined by measuring the paw edema volume 4 h after the carrageenan injection.The NSAID drug Ibuprofen in effective therapeutic doses were tested inparallel as an activity references. Inhibition of the inflammatory response was expressed as a percentage of the paw volume reduction. Studies of anti-inflammatory activity showed that the synthesized compounds had pronounced diuretic properties, and some of them according to activity indicators were approaching or exceeding comparative preparations. The results of the anti-inflammatory activity of the synthesized compounds derivatives (5,7-dimethyl-2-oxo-thiazolo[4,5-b]pyridine-3-yl)-acetic acid hydrazide show the potential for the search for anti-inflammatory agents among thiazolo[4,5-b]pyridine-2-ones.

scholarly journals Bioactivity-Guided Investigation of the Anti-Inflammatory Activity of Hippophae rhamnoides Fruits

Planta Medica ◽  
2017 ◽  
Vol 84 (01) ◽  
pp. 26-33 ◽  
Author(s):  
Dóra Rédei ◽  
Norbert Kúsz ◽  
Nikoletta Jedlinszki ◽  
Gábor Blazsó ◽  
István Zupkó ◽  
...  
Keyword(s):  
Hippophae Rhamnoides ◽  
Inflammatory Activity ◽  
Hippophaë Rhamnoides ◽  
Rat Paw Edema ◽  
In Vivo Animal Models ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
First Time ◽  
Peel Extract

AbstractAccording to modern ethnobotanical records, the fruit of Hippophae rhamnoides is effective in the treatment of different allergic symptoms. In order to obtain pharmacological evidence for this observation, the fruit was investigated for anti-inflammatory activity using in vivo animal models. Aqueous and 70% MeOH extracts were tested in 48/80-induced rat paw edema assay after oral administration, and it was found that the 70% MeOH extract (500 mg/kg) reduced significantly edema volume (0.660 ± 0.082 mL vs. control 0.935 ± 0.041 mL). Extracts of different parts of the fruit (pulp, peel, seed) were investigated in the same assay, and the peel extract was shown to exhibit maximum edema-reducing effect (0.470 ± 0.124 mL vs. control 0.920 ± 0.111 mL). This extract was used to elucidate the mode of action. Different inflammation inducers (serotonin, histamine, dextran, bradykinin, and carrageenan) were applied in the rat paw model, but the extract inhibited only the compound 48/80 elicited inflammation. The active extract was then fractionated by solvent-solvent partitioning and chromatographic methods with the guidance of the 48/80-induced anti-inflammatory assay, and the main compounds responsible for the activity were identified as ursolic acid and oleanolic acid. Our data suggest that the activity is most probably based on a membrane stabilizing effect caused by the inhibition of degranulation of mast cells. Moreover, previously unknown 2,5-bis-aryl-3,4-dimethyltetrahydrofuran lignans, nectandrin B, fragransin A2, and saucernetindiol were isolated and identified from H. rhamnoides for the first time.

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 Anti-Inflammatory Activity of Chrozophora rottleri Extracts on Carrageenan-Induced Rat Paw Edema

2016 ◽  
Vol 3 ◽  
pp. 20-26
Author(s):  
Mallikarjuna Rao Talluri ◽  
Battu Ganga Rao ◽  
Y. Venkateswaea Rao
Keyword(s):  
Ethyl Acetate ◽  
Methanol Extract ◽  
Bioactive Molecules ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Isolation And Characterization ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

The present study was intended to evaluate Anti-inflammatory activity ofC. rottleriextracts (Hydroalcoholic, Methanol, Ethyl acetate and Hexane). The Anti-inflammatory activity ofC.rottleriextracts at doses of 125mg/kg, 250mg/kg and 500mg/kg using carrageenan induced rat paw edema model compared with standard drug (Indomethacin). The selected plant extracts significantly inhibited paw edema along with the standard drug Indomethacin. Of all extracts, methanol extract produced significant effect on reduction of increased paw thickness, hydro alcoholic and ethyl acetate extracts produced moderate percentage inhibition and hexane extract produced low level of percentage inhibition in reducing paw edema on carrageenan induced rats. In all extracts, methanol extract at a dose of 500mg/kg showed more percentage inhibition i.e . 53.47±2.19. From the results obtained during the study it is concluded thatC. rottlerihaving the bioactive molecule responsible for Anti-inflammatory activity by individually or by combination of different bio-active compounds present in it. Further is necessary for isolation and characterization of bioactive molecules which are responsible for the selected plant biological activities.

scholarly journals SYNTHESIS, ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITIES OF ETHYL 2-(2-CYANO-3- (SUBSTITUTED PHENYL)ACRYLAMIDO)-4,5-DIMETHYLTHIOPHENE-3-CARBOXYLATES

2017 ◽  
Vol 10 (7) ◽  
pp. 95 ◽  
Author(s):  
Madhavi K ◽  
Sree Ramya G
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Antioxidant Properties ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

Objective: Objective of the study was to synthesize and evaluate a series of novel compounds, ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)- 4,5-dimethylthiophene-3-carboxylates, for in vitro antioxidant and in vivo anti-inflammatory activities.Methods: Ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylates were synthesized by knoevenagel condensation of active methylene group of ethyl 2-(2-cyanoacetamido)-4,5-dimethylthiophene-3-carboxylate with substituted benzaldehydes. The synthesized compounds were evaluated for their in vitro antioxidant properties in three different models, viz., reduction of 1,1-diphenyl-2-pycrylhydrazyl free radical, scavenging of nitric oxide free radical, and ferric ion-induced lipid peroxidation using rat brain homogenate. Few selected compounds with good antioxidant properties were pharmacologically evaluated for anti-inflammatory activity by carrageenan-induced rat paw edema model.Results: Clean and efficient synthetic procedure was used for the preparation of series of compounds. The structures of synthesized compounds were confirmed by infrared, 1H nuclear magnetic resonance and mass spectra. The antioxidant activity data revealed that the compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant activity. Hence, the active compounds were evaluated for anti-inflammatory activity and found to possess good activity. The percentage inhibition of rat paw edema obtained for the evaluated compounds was in the range of 70.2-83.1, comparable to the standard drug diclofenac (85.0%).Conclusion: The use of inexpensive, eco-friendly and readily available reagents, easy work-up and high purity of products makes the procedure a convenient and robust method for the synthesis of title compounds. The compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5- dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant and anti-inflammatory activities.

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