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 Synthesis and Anti-inflammatory Activity of Some Novel Pyrazole Derivatives of Gallic Acid

2009 ◽  
Vol 6 (s1) ◽  
pp. S123-S128 ◽  
Author(s):  
S. Arunkumar ◽  
K. Ilango ◽  
R. S. Manikandan ◽  
N. Ramalakshmi
Keyword(s):  
Sodium Hydroxide Solution ◽  
Aromatic Aldehydes ◽  
Inflammatory Activity ◽  
Pyrazole Derivatives ◽  
Paw Edema ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Derivatives Of

In the present study, a new series of [5-substituted-3-(phenylamino)-1H-pyrazol-1yl] (3,4,5-trihydroxyphenyl)-methanone (4a-j) have been synthesized. 3, 4, 5-Trihydroxy benzohydrazide (1) was synthesized from propyl gallate and hydrazine hydrate in presence of ethanol. Chalcones (2a-j) were synthesized from acetanilide and various aromatic aldehydes in presence of ethanol and sodium hydroxide solution. By refluxing the compound (1) and compounds (2a-j) in presence of ethanol yielded [5-substituted-3-(phenylamino)-4.5-dihydropyrazol-1yl] (3,4,5-trihydroxy phenyl)-methanone (3a-j). The final compounds [5-substituted-3-(phenylamino)-1H-pyrazol-1yl] (3,4,5-trihydroxyphenyl)-methanone (4a-j) were synthesized by treating compounds (3a-j) with bromine water. The synthesized compounds have been characterized by IR,1HNMR and Mass spectral data. The compounds were evaluated forin vivoanti-inflammatory activity by carrageenan induced paw edema test. In general all compounds were found to exhibit good 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.

scholarly journals Anti-inflammatory activity of aqueous extracts of Ove Costa Rican medicinalplants in Sprague-Dawley rats

2015 ◽  
pp. 723-727
Author(s):  
Beatriz Badilla ◽  
Gerardo Mora ◽  
Luis Jorge Poveda
Keyword(s):  
Costa Rican ◽  
Inflammatory Activity ◽  
Control Group ◽  
Aqueous Extracts ◽  
Paw Edema ◽  
Sprague Dawley ◽  
Sprague Dawley Rats ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Lethal Doses

The anti-inflamrnatory properties of Loasa specic¡sa and Loasa triphylla (Loasaceae), Urtica leptuphylla and Urera baccifera (Urticaceae), and Chaptalia nutans (Astemceae) were studied using the carregeenan induced mt paw edema model. Aqueous extmcts of each plant were made according to the ethnoboranical use. The hippocratic assay was made with female mts; the dose used was 500 mglkg i.p. andthe control group received 0.5 mi of n.s.s .. A11 the lmimals treated showed hipothermia, and those treated with the extmcts of Chaptalia nutans, Urera baccifera and Urtica lept/lPhylla showed an increased colinergic activity. Acute toxicities of !he aqueous extmcts were studied in mice an tbe mean lethal doses ranged between 1.0226 and 1.2022 glkg. The extracts of Urera baccifera, Chaptalia nutans, Loasa speciosa and Loasa triphylla (500 mglkg i.p.) showed an antiinflarnmatory activity compamble with that of indomethacin. The extracts of U. baccifera and C. nutans, which showed the gI"tatest anti-inflamrtJatory activity, did not show it when used orally (500 mg/k:g p.o.).

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 and ulcerogenic activities of thiazolidine-4-ones in rats

2018 ◽  
Vol 8 (1) ◽  
pp. 8
Author(s):  
Shiva Murthy N. ◽  
Srinivas V. ◽  
Shanthi M.
Keyword(s):  
Dry Weight ◽  
Inflammatory Activity ◽  
In Vivo Studies ◽  
Control Group ◽  
Paw Edema ◽  
Acute Peritonitis ◽  
Anti Inflammatory ◽  
And Control

Background: NSAIDS are associated with side effects and research should continue for developing safer drugs. This study aims to evaluate newer thiazolidine-4-ones for their anti-inflammatory and ulcerogenic activities in wister rats.Methods: Five groups of wister rats, 6 in each were used.  Anti-inflammatory and ulcerogenic activities of diclofenac (30mg/kg), nimesulide (50mg/kg), thia-1 (50mg/kg) and thia-2 (50mg/kg) are compared with control group (4% Gum Acacia). Carrageenin-induced paw edema, formaline induced acute peritonitis and cotton pellet-induced granulomatous tissue formation models were used for evaluating anti-inflammatory activity. After removing cotton pellets with granuloma on 8th day gastric ulcerogenicity was assessed by using macroscopic and microscopic scoring of ulcers.Results: Diclofenac, nimesulide and thia 2 reduced both paw edema and peritoneal exudate volume significantly (p <0.01). Wet weight of cotton pellets reduced significantly (p <0.01) by diclofenac, nimesulide and thia 2. Diclofenac (p <0.01) and thia 2 (p <0.05) reduced dry weight of cotton pellets significantly. nimesulide and thia-1 reduced it by 19.14% and 2.68% respectively and was considered statistically not significant (p>0.05). Nimesulide, thia-1 and thia-2 did not increase gastric ulcer score significantly (p >0.05). Diclofenac increased ulcer score significantly (p <0.01).Conclusions: Thia-2 demonstrated significant anti-inflammatory activity in acute and chronic models. In addition to inhibition of cyclooxygenase pathway, PPAR agonistic activity may be involved in its anti-inflammatory activity.  No significant ulcerogenicity was observed on comparing with nimesulide and control. Further in-vitro and in-vivo studies are recommended to confirm the results of this study.

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 AKTIVITAS ANTIINFLAMASI EKSTRAK ETANOL 70% DAUN ASHITABA (Angelica keiskei) SECARA IN VIVO DENGAN PENGINDUKSI KARAGENAN

2019 ◽  
Author(s):  
Haka As'ada ◽  
Yardi Saibi ◽  
Hendri Aldrat
Keyword(s):  
Dose Range ◽  
White Male ◽  
Ethanol Extract ◽  
Negative Control ◽  
Inflammatory Activity ◽  
Male Rat ◽  
Control Group ◽  
Angelica Keiskei ◽  
Anti Inflammatory

Ashitaba leaves (Angelica keiskei) or also known as tommorow's leaf is plant that known to have various health benefit, one of them is as an anti-inflammatory activity. The anti-inflammatory activity of ashitaba leaves has been known through in vitro assays. This study aims to determine the anti-inflammatory activity of 70% ethanol extract of ashitaba leaves through in vivo assay. Anti-inflammatory activity was performed on white male rat of Sprague dawley strain with induction method of edema on rat's foot using 1% carrageenan 0.2 ml. Rats were divided into 5 groups. The negative control group was given a 0.5% Na-CMC suspension, a positive control group was given sodium diclofenac suspension of 5.14 mg / kgBW, and the test group was given 70% ethanol extract of ashitaba leaves at a dose of 1000; 2000; and 4000 mg / kgBW suspended in 0.5% Na-CMC. The results showed that in that dose range the 70% ethanol extract of ashitaba leaves had anti-inflammatory activity that did not depend on the dose. Percentage of edema of 70% ethanol extract of ashitaba leaves dose 1000; 2000; 4000 mg / kgBB was significantly different with negative control (p ≤ 0,05) and had percentage of edema inhibition respectively 83,95%, 79,01%, and 80,25%. The results of this study showed that 70% ethanol extract of ashitaba leaves have anti-inflammatory activity. Keywords: Ashitaba, Angelica keiskei, tommorow's leaf, anti-inflammatory, carrageenan.

Pharmacognostical Standardization, Isolation of Phytoconstituents (β-sitosterol), HPTLC analysis of extracts of Operculina turpethum (Linn.) roots and evaluation of cytotoxic, in vitro & in vivo anti-inflammatory activities

2021 ◽  
Vol 18 ◽  
Author(s):  
Akash Ved ◽  
Shweta Gupta ◽  
Namrata Singh ◽  
Karuna S. Shukla ◽  
Om Prakash ◽  
...  
Keyword(s):  
Column Chromatography ◽  
Inflammatory Activity ◽  
Control Group ◽  
Albino Rats ◽  
Cell Viability Assay ◽  
Edema Formation ◽  
Egg Albumin ◽  
Anti Inflammatory

Background: Operculina turpethum (Linn.) Silva Manso, family- convolvulaceae, is an important plant in Indian conventional system of medicine which is extensively employed by different tribes in many countries to cure edema and painful conditions like arthritis, back pain; hyperlipidemia, diabetes mellitus, liver disorders, skin disorders and to regulate bowel functions. Objective: The roots of O. turpethum (Linn.) was subjected to physicochemical, phytochemical standardization, the chromatographic separation which was accomplished by column chromatography, TLC, and HPTLC, further, the acute toxicity, cytotoxic and anti-inflammatory activities of Operculina turpethum roots were estimated by in vivo and in vitro models. Materials and Methods: This study includes percentage yield of extraction, organoleptic evaluation along with the analysis of its physicochemical investigations & preliminary phytochemical estimation. The isolation of active phytoconstituents was done by column chromatography, and the isolated compound was then exposed to TLC and HPTLC analysis. Cytotoxic activity was tested by WST-1 based cell viability assay on HepG2 cells. Anti-inflammatory activity of methanol extract (ME) was evaluated against inflammation occur by both in vitro and in vivo method. Results: The methanolic extract exhibited the presence of most of the phytoconstituents out of all the extracts, the phytoconstituent phytosterol, i.e., β-sitosterol was isolated by column chromatography, identified and quantified by TLC and HPTLC, which is liable for anti-inflammatory activity. The amount of β-sitosterol was estimated to be 14.09 µg in 10.00 mg fraction of MEOT. MEOT is devoid of toxicity up to 2000 mg/kg in Wistar albino rats. It was analysed that in vitro anti-inflammatory activity of MEOT by egg albumin denaturation method exhibited a incredible decrement in turbidity and increasing the percentage inhibition of albumin denaturation (60.52%) in MEOT treated group as compared with control group. In egg albumin-induced edema in rats, MEOT at the dose of 400 mg/kg reduced the edema formation (3.03 ± 0.02) induced by egg albumin at 4th h. In cotton pellet-induced granuloma in rats, MEOT at the dose of 400 mg/kg displayed maximum granuloma inhibition (51.06%) which is similar to that of indomethacin. Conclusion: From the obtained findings it is confirmed that O. turpethum contains β-sitosterol which is responsible for potent anti-inflammatory activity without causing cytotoxicity to the plant. The results suggested that ME of O. turpethum roots had high potential for application as an anti-inflammatory agent. The recognization and confirmation of the plant can be obtaineded from the study and will present data which is aidful in determining the quality and purity of a crude drug which further helps in preventing its adulteration.

scholarly journals PHYTOCHEMICAL SCREENING AND EVALUATION OF ANTI-INFLAMMATORY ACTIVITY OF AERIAL PART EXTRACTS OF PLANTAGO MAJOR L.

2017 ◽  
Vol 10 (9) ◽  
pp. 307
Author(s):  
Jyoti Vandana ◽  
Gupta A K ◽  
Alok Mukerjee
Keyword(s):  
Aerial Part ◽  
Iridoid Glycosides ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Plantago Major ◽  
Phytochemical Screening ◽  
Paw Edema ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Wistar Albino Rats

  Objective: This study aims to perform phytochemical screening and investigate anti-inflammatory activity of extract from aerial part of the plant Plantago major L.Methods: Preliminary phytochemical screening of plant extract was carried out using standard qualitative procedures and anti-inflammatory activity was evaluated using carrageenan-induced paw edema model in male Wistar albino rats using plethysmometer. Diclofenac sodium (10 mg/kg, b.w.) was used as standard drug.Results: Preliminary phytochemical screening of the different extracts revealed that they were rich in secondary metabolite compounds such as carbohydrates, tannins, steroids, flavonoids, terpenoids, glycosides, fats and oils, alkaloids, phenolic compounds, and iridoid glycosides. The anti-inflammatory activity was evaluated using carrageenan-induced paw edema models in Wistar albino rats. The anti-inflammatory activity of methanolic extract (ME) was found to be dose dependent in carrageenan-induced paw edema model. The ME has shown significant (p<0.05) inhibition of paw edema, 61.11% and 55.55% on 4th hr at the doses of 900 and 600 mg/kg, respectively.Conclusion: The results of the present study demonstrate that ME of the aerial parts of the plant possess significant (p<0.05) anti-inflammatory potential.

scholarly journals Antioxidant, Anti-Inflammatory, and Analgesic Activities ofAgrimonia eupatoriaL. Infusion

2017 ◽  
Vol 2017 ◽  
pp. 1-13 ◽  
Author(s):  
Telmo N. Santos ◽  
Gustavo Costa ◽  
J. Pinto Ferreira ◽  
Joana Liberal ◽  
Vera Francisco ◽  
...  
Keyword(s):  
Antiradical Activity ◽  
Inflammatory Activity ◽  
No Production ◽  
Hot Plate ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
First Time

Agrimony (Agrimonia eupatoriaL.) (Ae) is used in traditional medicine to treat inflammatory and oxidative related diseases. Therefore, this study focuses on the anti-inflammatory and analgesic potential of Ae infusion (AeI). Phenolic compounds characterization was achieved by HPLC-PDA-ESI/MSn. To evaluate antioxidant potential, 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide anion, hydroxyl radical, and SNAP assays were used. In vitro anti-inflammatory activity of AeI was investigated in LPS-stimulated macrophages by measuring the NO production. In vivo anti-inflammatory activity was validated using the mouse carrageenan-induced paw edema model. Peripheral and central analgesic potential was evaluated using the acetic acid-induced writhing and hot-plate tests, respectively, as well as the formalin assay to assess both activities. The safety profile was disclosed in vitro and in vivo, using MTT and hematoxylin assays, respectively. Vitexin, quercetinO-galloyl-hexoside, and kaempferolO-acetyl-hexosyl-rhamnoside were referred to in this species for the first time. AeI and mainly AePF (Ae polyphenolic fraction) showed a significant antiradical activity against all tested radicals. Both AeI and AePF decreased NO levels in vitro, AePF being more active than AeI. In vivo anti-inflammatory and analgesic activities were verified for both samples at concentrations devoid of toxicity. Agrimony infusion and, mainly, AePF are potential sources of antiradical and anti-inflammatory polyphenols.

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