scholarly journals Antiinflammatory activity of 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates on carrageenan model of inflammation

2019 ◽  
pp. 82-87
Author(s):  
B. V. Pristupa ◽  
I. O. Shyshkin ◽  
Ya. V. Rozhkovsky ◽  
V. O. Gelmboldt
Keyword(s):  
Antiinflammatory Activity ◽  
Biologically Active ◽  
Inflammatory Activity ◽  
Male Rats ◽  
Control Group ◽  
Paw Edema ◽  
Commercial Preparation ◽  
Reference Drug ◽  
Anti Inflammatory ◽  
Inflammatory Effect

In the last decade, high cariesprophylactic efficacy of ammonium hexafluorosilicates, including salts with substituted biologically active ammonium cations, has been demonstrated. Among the promising anti-caries agents are recently synthesized 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates, for whose cations anti-inflammatory activity is expected. The aim of the work is to assess the presence of anti-inflammatory activity in the series of 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates in the experiment. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates (I–III, respectively) were synthesized according to the previously proposed technique, carrageenan is a commercial preparation, reference drug is a indomethacin. Experiments on the anti-inflammatory activity of hexafluorosilicates were performed on 77 white Wistar male rats weighing 174–190 g using the carrageenan model of inflammation. The inflammatory reaction was reproduced by subplantary administration of 0.1 ml of a 0.2% solution of carrageenan, the studied compounds were administered orally in doses 1/10, 1/20, 1/50 from LD50 for the compound III. It was established that after administration of carrageenan, animals of the control group showed marked paw edema, which gradually increased and was maximal after 24 hours of observation. According to the data obtained, the indices for compounds I-III practically do not differ from those of the control group. This indicates that, despite the results of the PASS forecast and the presence of acetic acid residue, an anti-inflammatory pharmacofor, in compounds I-III, the compounds under study do not have an anti-inflammatory effect in the carrageenan model. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates do not show the expected anti-inflammatory activity in the carrageenan model of inflammation.

scholarly journals Anti-inflammatory Activity of Ethanol Extract of Lotus (Nelumbo nucifera G.) Seed Against White Male Rats Using Paw Edema Method

2021 ◽  
Vol 11 (4) ◽  
pp. 1-4
Author(s):  
Khairani Fitri ◽  
Tetty Noverita Khairani ◽  
Kristin Tiurma Sianturi ◽  
Leny Leny ◽  
Ihsanul Hafiz
Keyword(s):  
White Male ◽  
Ethanol Extract ◽  
Nelumbo Nucifera ◽  
Inflammatory Activity ◽  
Male Rats ◽  
Control Group ◽  
Paw Edema ◽  
White Rats ◽  
Activity Test ◽  
Anti Inflammatory

The purpose of this study was to determine the anti-inflammatory activity test of ethanol extract of lotus seeds in rats induced by carrageenan. The research method used was experimental. The object used in this study was male white rats. Observations were made for 6 hours and then the data were analyzed using the one way analysis of variance (ANOVA) test. The anti-inflammatory activity test was carried out on the test animals which were divided into 5 groups, 3 each with the suspension test group with a dose of 200, 300, 400 mg/kg bw, the negative control group was the CMC Na 1% suspension and the positive control was diclofenac Na 2, 25 mg/kg bw. The results showed that the ethanol extract of the seeds of lotus (Nelumbo nucifera G) was proven to have an anti-inflammatory effect on carrageenan-induced male white rats at doses of 200, 300 and 400 mg/kg BW with the percentage value of inflammation inhibition at the 6th hour was 65.79, 74.65 and 80.77%, with the most effective dose in reducing anti-inflammatory drugs being 400 mg/kg bw. The ethanol extract of the seeds of lotus (Nelumbo nucifera) has anti-inflammatory activity. Keywords: anti-inflammatory activity, Nelumbo nucifera, paw edema

scholarly journals The Anti-Inflammatory Effect of a γ-Lactone Isolated from Ostrich Oil of Struthio camelus (Ratite) and Its Formulated Nano-Emulsion in Formalin-Induced Paw Edema

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3701
Author(s):  
Salah E. M. Eltom ◽  
Ahmed A. H. Abdellatif ◽  
Hamzah Maswadeh ◽  
Mohsen S. Al-Omar ◽  
Atef A. Abdel-Hafez ◽  
...  
Keyword(s):  
Oral Administration ◽  
Standard Procedure ◽  
P Value ◽  
Skin Thickness ◽  
Paw Edema ◽  
Reference Drug ◽  
Struthio Camelus ◽  
Anti Inflammatory ◽  
Nano Emulsion ◽  
Inflammatory Effect

The ostrich oil of Struthio camelus (Ratite) found uses in folk medicine as an anti-inflammatory in eczema and contact dermatitis. The anti-inflammatory effect of a γ-lactone (5-hexyl-3H-furan-2-one) isolated from ostrich oil and its formulated nano-emulsion in formalin-induced paw edema was investigated in this study. Ostrich oil was saponified using a standard procedure; the aqueous residue was fractionated, purified, and characterized as γ-lactone (5-hexyl-3H-furan-2-one) through the interpretation of IR, NMR, and MS analyses. The γ-lactone was formulated as nano-emulsion using methylcellulose (MC) for oral solubilized form. The γ-lactone methylcellulose nanoparticles (γ-lactone-MC-NPs) were characterized for their size, shape, and encapsulation efficiency with a uniform size of 300 nm and 59.9% drug content. The γ-lactone was applied topically, while the formulated nanoparticles (NPs) were administered orally to rats. A non-steroidal anti-inflammatory drug (diclofenac gel) was used as a reference drug for topical use and ibuprofen suspension for oral administration. Edema was measured using the plethysmograph method. Both γ-lactone and γ-lactone-MC-NPs showed reduction of formalin-induced paw edema in rats and proved to be better than the reference drugs; diclofenac gel and ibuprofen emulsion. Histological examination of the skin tissue revealed increased skin thickness with subepidermal edema and mixed inflammatory cellular infiltration, which were significantly reduced by the γ-lactone compared to the positive control (p-value = 0.00013). Diuretic and toxicity studies of oral γ-lactone-MC-NPs were performed. No diuretic activity was observed. However, lethargy, drowsiness, and refusal to feeding observed may limit its oral administration.

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, Characterization and Acute Anti-inflammatory Evaluation of New Mefenamic Acid Derivatives Having 4-Thiazolidinone Nucleus

2019 ◽  
Vol 28 (1) ◽  
pp. 138-146
Author(s):  
Mustafa H. Ali Alsafi ◽  
Muthanna S. Farhan
Keyword(s):  
Side Effects ◽  
Mefenamic Acid ◽  
Paw Edema ◽  
Compound I ◽  
Reference Drug ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Derivatives Of ◽  
Cox 1 ◽  
Inflammatory Effect

Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect.

scholarly journals Scientific Evaluation of anti-inflammatory potential of Macrotyloma uniflorum seeds extracts

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1883-1888
Author(s):  
Anandarajagopal K ◽  
Abdullah Khan ◽  
Sugalia S ◽  
Bama Menon ◽  
Tan Ching Siang ◽  
...  
Keyword(s):  
Antioxidant Properties ◽  
Water Extract ◽  
Ethanol Extract ◽  
Inflammatory Activity ◽  
Leguminous Plant ◽  
Paw Edema ◽  
Reference Drug ◽  
Macrotyloma Uniflorum ◽  
Phenolic Constituents ◽  
Anti Inflammatory

Phytochemicals possessing the antioxidant properties naturally present in food attract a greater interest to healthcare researchers due to their desirable health effects on human health as they can be explored for protection against oxidative deterioration. Macrtotyloma uniflorum is a leguminous plant belonging to the family Fabaceae and commonly known as Horse gram. Aqueous and ethanol extracts of seeds of Macrotyloma uniflorum were evaluated for their anti-inflammatory effects using the scientific protocol on experimental rats. Extraction was carried out using the cold maceration method, and the anti-inflammatory activity was evaluated using a digital plethysmometer in the experimental rats injected with carrageenan to produce paw edema. Preliminary phytochemical studies confirmed the presence of various bioactive compounds such as alkaloids, glycosides, carbohydrates, proteins and amino acids, terpenoids, tannins, and phenolic compounds in both extracts while flavonoids were found only in ethanol extract. Both extracts of M. uniflorum seeds (200 mg/ml) significantly (p<0.01) reduced the paw edema volume induced by carrageenan. The ethanol extract of M. uniflorum seeds exhibited more potent anti-inflammatory activity than water extract, that might be due to the presence of flavonoids in ethanol extract. The activity of the extracts was compared with diclofenac sodium (10mg/kg b.wt.) as a reference drug. From the results, it may be suggested that the antioxidative potential of phenolic constituents and flavonoids is the primary factors for the anti-inflammatory activity of M. uniflorum seeds extracts.

scholarly journals Study to Investigate the anti-inflammatory effect of Codelac® Broncho with Thymus Serpyllum (elixir) in comparison with reference drug Fenspiride (syrup) using accute Carrageenan-induced Paw Inflammation Model

2019 ◽  
Vol 5 (1) ◽  
pp. 45-52
Author(s):  
Pavel D. Kolesnichenko ◽  
Anna A. Peresypkina ◽  
Artem A. Poromov ◽  
Elena N. Kareva ◽  
Alexey N. Demidenko
Keyword(s):  
Inflammatory Activity ◽  
C Reactive Protein ◽  
Reference Drug ◽  
Reactive Protein ◽  
Model Control ◽  
Anti Inflammatory ◽  
Thymus Serpyllum ◽  
Carrageenan Inflammation ◽  
Subplantar Injection ◽  
Inflammatory Effect

Introduction: Evaluation of anti-inflammatory action of Codelac® Broncho with Thymus Serpyllum (elixir) in comparison with Fenspiride was carried out on the model of acute carrageenan inflammation of the paws in rats. Materials and methods: Edema was caused by subplantar injection of 0.1 ml of 1% λ- carrageenan gel into the hind paw. The severity of edema was assessed by using 37140 plethysmometer (UGO BASILE, Italy). The measurements were performed before edema induction and 1, 2, 4, 12, 24, 48, 72, 96 and 120 hours afterwards. Anti-inflammatory activity of the drugs was also evaluated based on the analysis of rats’ blood, C-reactive protein concentration and histological examination results. Results and discussion: A decrease in the paw volume increment was revealed in the group with the studied drug in comparison with the group with the carrageenan edema model (control) 4, 12, 24 hours after injection of carrageenan (p&lt;0.05). As a result of plethysmometry, a more pronounced anti-inflammatory effect of the studied drug than that of Fenspiride was revealed. There was a significant decrease in the levels of leukocytes (p&lt;0.05), lymphocytes (p&lt;0.05), monocytes (p&lt;0.05) and neutrophils (p&lt;0.05) in the group with the studied drug compared to those the the control 48 hours after the initiation of edema, while in the group with Fenspiride, there was only a decrease in the levels of leukocytes (p&lt;0.05) and lymphocytes (p&lt;0.05). There were no differences in the concentration of C-reactive protein between the groups. Conclusion: The obtained data indicate a more pronounced anti-inflammatory activity of Codelac® Broncho with Thymus Serpyllum in comparison with Fenspiride, on the model of acute carrageenan inflammation of the paw in rats.

scholarly journals Anti-Inflammatory Activity and Composition ofSenecio salignusKunth

2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Cuauhtemoc Pérez González ◽  
Roberto Serrano Vega ◽  
Marco González-Chávez ◽  
Miguel Angel Zavala Sánchez ◽  
Salud Pérez Gutiérrez
Keyword(s):  
Medicinal Plant ◽  
Methanol Extract ◽  
Chloroform Extract ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Active Fraction ◽  
Ear Edema ◽  
Methanol Extracts ◽  
Anti Inflammatory ◽  
Inflammatory Effect

We investigated the anti-inflammatory activity ofSenecio salignus. This medicinal plant is often used in Mexico for the treatment of fever and rheumatism. Chloroform and methanol extracts of the plant were tested on 12-O-tetradecanoylphorbol-13-acetate- (TPA-) induced edema in mice ears. The methanol extract of the plant inhibited edema by36±4.4% compared with the control, while the chloroform extract exhibited an even greater level of inhibition (64.1%). The chloroform extract was then fractionated, and the composition of the active fraction was determined by GC-MS. The anti-inflammatory activity of this fraction was then tested on TPA-induced ear edema in mice, and we found that the active fraction could inhibit edema by 46.9%. The anti-inflammatory effect of the fraction was also tested on carrageenan-induced paw edema in rats at doses of 100 mg/kg; a58.9±2.8% reduction of the edema was observed 4 h after administration of carrageenan, and the effect was maintained for 5 h.

scholarly journals In Vivo Evaluation of the Anti-Inflammatory Effect ofPistacia lentiscusFruit Oil and Its Effects on Oxidative Stress

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Sameh Ben Khedir ◽  
Masarra Mzid ◽  
Sana Bardaa ◽  
Dorsaf Moalla ◽  
Zouheir Sahnoun ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
New Drugs ◽  
Inflammatory Activity ◽  
Natural Health Products ◽  
Paw Edema ◽  
In Vivo Evaluation ◽  
Anti Inflammatory ◽  
Fruit Oil ◽  
Inflammatory Effect

In order to find new topical anti-inflammatory agents, we had recourse to a medicinal plant. This work was designed to determine the topical anti-inflammatory effect ofPistacia lentiscusfruit oil (PLFO), using carrageenan-induced paw edema rat model, and to evaluate its effects on oxidative stress. The topical anti-inflammatory activity of PLFO was compared to Inflocine® and estimated by measuring the diameter of paw edema, for 5 hours at a 1-hour interval. After that the rats were scarified and the inflamed paw tissue was removed for the exploration of some parameters of oxidative stress and histopathology. PLFO showed a significant anti-inflammatory activity in comparison with the Inflocine. The percentages of edema inhibition were 70% and % 51.5% (p<0.01), respectively, after five hours. The treatment with PLFO and Inflocine led to significant increases (p≤0.05) in the activities of CAT, SOD, and GPX and significant decreases in the MDA level and AOPP activity in the paw tissue after Carr injection, in comparison with the Carr group. Therefore, our findings demonstrate that PLFO might accelerate the development of new drugs which could be used scientifically as a source for natural health products in the treatment of topical inflammation.

scholarly journals Investigation of anti-inflammatory and antipyretic activity of polymorphic modification of n-(trifluoromethylphenyl)-4-hydroxy-2,2-dioxo-1h-2λ6,1-benzothiazine-3-carboxamide derivative in rats

2021 ◽  
Vol 25 (1) ◽  
pp. 27-31
Author(s):  
P. S. Bondarenko ◽  
N. І. Voloshchuk
Keyword(s):  
Inflammatory Reaction ◽  
White Male ◽  
Statistical Processing ◽  
Biologically Active ◽  
Inflammatory Activity ◽  
Polymorphic Modification ◽  
Reference Drug ◽  
Antipyretic Effect ◽  
Antipyretic Activity ◽  
Anti Inflammatory

Annotation. Polymorphism among biologically active substances is an extremely important factor that modifies the therapeutic properties of pharmaceutical substances and dosage forms, significantly affects the parameters of their biological activity and pharmacokinetics. Chemical synthesis among the derivatives of 4-R-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxylic acids gave the leader compound N-(4-trifluoromethylphenyl)-4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide, the crystalline polymorph of which in the form of plates has a pronounced analgesic activity. The aim of the study was to investigate the anti-inflammatory activity of compound B by its effect on various components of the inflammatory reaction, as well as the antipyretic effect of this compound in rats. The anti-alterative activity was determined on the model of planar skin wounds, the antiproliferative effect - on the model of cotton granuloma, the anti-exudative effect - on the model of toxic pulmonary edema in rats. The antipyretic effect was studied in a model of milk fever in rats. The study was performed on 91 white male Wistar rats. Statistical processing of the obtained results was performed using the program "STATISTICA 6.1" by methods of variation statistics using parametric and nonparametric methods. The results showed that the polymorphic compound B has anti-inflammatory activity on all components of the inflammatory reaction - alteration, exudation and proliferation. In terms of efficacy in the model of experimental inflammation, this substance is superior to meloxicam, as its ED50 when administered orally is 5.2 mg/kg, while the reference drug - 9.1 mg/kg. Compound B exhibits a pronounced antipyretic effect in a rat fever model. Therefore, the polymorphic modification of the carboxamide derivative in the form of plates is promising for further research in order to create on its basis a drug with analgesic, anti-inflammatory and antipyretic properties.

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.).

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