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.

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 Preliminary screening of Waltheria indica (L.) plant for its anti-inflammatory activity

2017 ◽  
Vol 9 (2) ◽  
Author(s):  
Amol Chandekar ◽  
Amber Vyas ◽  
Neeraj Upamanyu ◽  
Atul Tripathi ◽  
Surendra Agrawal
Keyword(s):  
Inflammatory Activity ◽  
In Vivo Model ◽  
Significant Activity ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Test Models ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Acute And Chronic Inflammation

<p dir="ltr"><span>The investigation on anti-inflammatory activity of the various extract of </span><span>Waltheria indica </span><span>L. </span><span>was reported to find out the pharmacological basis for its ethnomedical use. </span><span>The anti-inflammatory activity of the pet ether (PEW) and methanol (MEW) extracts of the leaves of </span><span>Waltheria indica </span><span>L. (</span><span>Malvaceae</span><span>)</span><span>were evaluated by using in vivo (Carrageenan &amp; histamine induced rat paw edema, cotton pellet granuloma test) models. It was observed that, all the extracts showed significant activity in the in-vivo model at the dose of 500 mg/kg b.w. orally, when compared with control and standard drugs. Of the two extracts tested, methanol extract MEW showed most significant activity well in comparison to the standard drug.  Therefore, present study suggests, potential of leaves of </span><span>Waltheria indica </span><span>L. in both models of acute and chronic inflammation.</span></p><p dir="ltr"> </p>

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 ANTI-INFLAMMATORY PROFILING OF SEED AND RIND EXTRACTS OF AMOMUM SUBULATUM

2020 ◽  
pp. 204-208
Author(s):  
SUPRIYA AGNIHOTRI
Keyword(s):  
Inflammatory Activity ◽  
In Vivo Studies ◽  
Inflammatory Models ◽  
Rat Paw Edema ◽  
Soxhlet Apparatus ◽  
Anti Inflammatory ◽  
Amomum Subulatum ◽  
Rat Paw

Objective: The study aimed to evaluate the anti-inflammatory activity of Amomum subulatum (greater cardamom) seed and rind extracts in Wistar rats. Methods: The seed and rind of A. subulatum were air-dried in the shade, powdered, and subjected to 80% hydroalcoholic extraction in the Soxhlet apparatus. The anti-inflammatory activity of the seed and rind extracts of A. subulatum was evaluated by in vivo and in vitro methods. Results and Discussion: In vivo studies, namely, carrageenan-induced rat paw edema, cotton pellet granuloma, and formaldehyde-induced arthritis model confirmed the anti-inflammatory potential of seed and rind extracts of A. subulatum. It was found that rind extract exhibited better inhibition of inflammation as compared to seed extract. A. subulatum rind extract at the dose of 500 μg/ml exhibited best results for in vitro studies, namely, inhibition of albumin denaturation (73% inhibition), antiproteinase action (58% inhibition), membrane stabilization, heat-induced hemolysis, hypotonicity-induced hemolysis (54% inhibition), anti-lipoxygenase activity. Conclusions: The results of the study showed that the rind extract of A. subulatum (greater cardamom) possesses significant anti-inflammatory potential in various in vivo and in vitro anti-inflammatory models in the experimental animals.

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 ANTI-INFLAMMATORY EFFECTS OF PROPOXAZEPAM ON DIFFERENT MODELS OF INFLAMMATION

2020 ◽  
Vol 5 (2) ◽  
pp. 105-112 ◽  
Author(s):  
N. Ya. Golovenko ◽  
T. A. Kabanova ◽  
S. A. Andronati ◽  
O. I. Halimova ◽  
V. B. Larionov ◽  
...  
Keyword(s):  
Acute Inflammation ◽  
Experimental Models ◽  
Paw Edema ◽  
Preclinical Trial ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
First Time ◽  
Inflammatory Action

Background. Propoxazepam, 7-bromo-5-(2-chlorophenyl)-3-propoxy-1H-benzo[e][1,4]diazepin-2(3H)-one, is a promising analgesic and anticonvulsant and is on preclinical trial. Objective. The aim of the research was to study the anti-inflammatory and analgesic action of Propoxazepam. Methods. The anti-inflammatory action was evaluated by carrageenan induced rat paw edema, formalin-induced paw licking response in mice and bradykinin-induced pain response in rat models. Results. It was established for the first time that the administration of Propoxazepam caused a significant anti-inflammatory activity when tested in different in vivo chemical experimental models of induced inflammation, i.e. carrageenan-, bradykinin- and formalin-induced inflammation tests. Conclusions. Propoxazepam significantly reduced acute and sub-acute inflammation and proved its efficacy and similar to anti-inflammatory action.

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 Anti-inflarnmatory activity of Urera baccifera(Urticaceae) in Sprague-Dawley rats

1969 ◽  
pp. 365-371
Author(s):  
Beatriz Badilla ◽  
Gerardo Mora ◽  
Antonio José Lapa ◽  
José Arthur Silva Ernim
Keyword(s):  
Analgesic Activity ◽  
Preliminary Test ◽  
Inflammatory Activity ◽  
Sprague Dawley ◽  
In Vivo Models ◽  
Aqueous Fraction ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

On a preliminary test, anti-inflammatory and analgesic dose-related activities on rats were observed for the aqueous fraction of Urera baccifera; this extract was bioassay-guided fractionated and the final aqueous fraction was used according the ethnobotanical use. Carrageenan-induced edema (n=6), was used as an assay in the fractionating process. The anti-inflammatory and antinociceptive properties of the final aqueons fraction were studied using in vivo models. For the anti-inflammatory activity rat paw edema (n=6), pleurisy induced by carrageenan (n=6) and ear edema induced by topical croton oil (n=6) models were used, and tail-fIick test (n=6), abdominal constrictions induced by acetic acid (n=6), and formalin test (n=6), were used for the alltillociceptive activity. The tests perfonned showed an inhibition effeet on !eukocyte rnigration, and a reductioll on pleural exudate, as well as dose-dependant peripheral analgesic activity, al a range of 25-100 mglk:g i.p. The final aqueous fraction contains most of the anti-inflammatory activity of the plant U. baccifera. A possibJe mechanism of action is discussed and based on the results we conclude that this plant has a potential. for both anti-inflammalory and analgesic activity al the c1inical level.

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.

scholarly journals Anti-Tumor and Anti-Inflammatory Activity In Vivo of Apodanthera congestiflora Cogn. (Cucurbitaceae)

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 743
Author(s):  
Geovana F. G. Silvestre ◽  
Renally P. Lucena ◽  
Genil D. Oliveira ◽  
Helimarcos N. Pereira ◽  
Jhonatta A. B. Dias ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Phytochemical Investigation ◽  
Significant Toxicity ◽  
Biological Tests ◽  
Ehrlich's Carcinoma ◽  
Anti Inflammatory ◽  
Pharmacological Potential ◽  
First Time ◽  
Anti Tumor Activity

This work aimed to carry out a study of Apodanthera congestiflora by investigating its chemical composition and pharmacological potential. From the dichloromethane phase (Dic-Ac) of the A. congestiflora stems, three compounds were identified: cayaponoside C5b (Ac-1), cabenoside C (Ac-2) and fevicordin C2 glucoside (Ac-3), being last identified for the first time as a natural product. These compounds were obtained by chromatographic methods and their structures were elucidated by means of spectroscopic analysis of IR, MS and NMR. In the quantification of Dic-Ac, it was possible to observe the presence of 7% of cayaponoside C5b. Dic-Ac showed significant toxicity for in vivo tests, with macroscopic and biochemical changes. The anti-inflammatory activity of Dic-Ac was investigated using the paw edema model. A decrease in inflammatory signs was observed in the first 5 h and the most effective dose in reducing edema with was 7.5 mg kg−1 (66.6%). Anti-tumor activity of Dic-Ac was evaluated by Ehrlich’s carcinoma model, which showed inhibition rate of 78.46% at 15 mg kg−1 dosage. The phytochemical investigation, together with the biological tests carried out in this study, demonstrated that A. congestiflora is a promising species in the search for therapeutics, since it contains substances with high pharmacological potential in its composition.

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