scholarly journals Synthesis, characterization and pharmacological activity of new 2- imino –thiazolidine-4-one derivatives

2019 ◽  
Vol 10 (3) ◽  
pp. 1763-1769 ◽  
Author(s):  
Raghdah M. Alwiswasy ◽  
Raheem Jameel M ◽  
Basim Jasim Hameed
Keyword(s):  
Acetic Acid ◽  
Pharmacological Activity ◽  
Analgesic Activity ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Edema Model ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Analgesic Activities

A new 2-iminothiazolidin-4-ones compound and its derivatives were synthesized and characterized by FT-IR, CHN, and 1HNMR techniques. The target compounds were assessed for their anti-inflammatory and analgesic activities, and the study was performed using Swiss albino mice (25-30 g) for investigation. A hind edema model caused by , while the analgesic activity was assessed using an acetic acid-induced writhing and a hot plate test evaluated the anti-inflammatory activity.

scholarly journals Anti-nociceptive and anti-inflammatory effects of an aqueous extract of blended leaves of Ocimum gratissimum and Psidium guajava

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Akinyinka O. Alabi ◽  
Abayomi M. Ajayi ◽  
Osarume Omorogbe ◽  
Solomon Umukoro
Keyword(s):  
Acetic Acid ◽  
Aqueous Extract ◽  
Psidium Guajava ◽  
Antinociceptive Activity ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Promising Alternative ◽  
Plate Test ◽  
Ocimum Gratissimum ◽  
Anti Inflammatory

Abstract Background To investigate the antinociceptive and anti-inflammatory activities of aqueous extract of a blended mixture of dried leaves of Ocimum gratissimum and Psidium guajava, a traditional analgesic drug polyherbal (TADP) used as a remedy for pain-related conditions. Methods Antinociceptive activity of TADP (100, 200 and 400 mg/kg) was evaluated in the hot plate test and acetic acid-induced nociception in mice while the anti-inflammatory was evaluated in carrageenan-induced paw oedema in rats. Levels of nitrite, myeloperoxidase, glutathione and malondialdehyde were assayed in carrageenan-induced paw tissue. Results TADP (200 and 400 mg/kg) significantly prolong the latency time in the hot-plate test. TADP (100–400 mg/kg) produced a dose-dependent significant inhibition of the acetic-acid induced abdominal constriction. The antinociceptive activity of TADP in the presence of naloxone and atropine was not reversed whereas yohimbine and glibenclamide significantly reversed it. TADP (100, 200 and 400 mg/kg) significantly reduced the swelling in the carrageenan-induced oedema model and also produced a reduction in the nitrite and myeloperoxidase level. TADP (400 mg/kg) significantly reduced malondialdehyde concentration and increase glutathione level in the carrageenan-induced rat paw. TADP significantly decrease the number of cellular infiltrates in the histopathological assessment. Conclusion These results indicate that polyherbal product containing blended leaves of Ocimum gratissimum and Psidium guajava possess antinociceptive and anti-inflammatory properties, hence represents a promising alternative remedy in inflammation-induced pain.

scholarly journals Borneol, a Bicyclic Monoterpene Alcohol, Reduces Nociceptive Behavior and Inflammatory Response in Mice

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Jackson Roberto Guedes da Silva Almeida ◽  
Grasielly Rocha Souza ◽  
Juliane Cabral Silva ◽  
Sarah Raquel Gomes de Lima Saraiva ◽  
Raimundo Gonçalves de Oliveira Júnior ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Motor Coordination ◽  
Nociceptive Behavior ◽  
Hot Plate ◽  
Rotarod Test ◽  
Hot Plate Test ◽  
Plate Test ◽  
Strength Tests ◽  
Anti Inflammatory ◽  
Motor Abnormality

Borneol, a bicyclic monoterpene, has been evaluated for antinociceptive and anti-inflammatory activities. Antinociceptive and anti-inflammatory activities were studied by measuring nociception by acetic acid, formalin, hot plate, and grip strength tests, while inflammation was prompted by carrageenan-induced peritonitis. The rotarod test was used to evaluate motor coordination. Borneol produced a significant (P<0.01) reduction of the nociceptive behavior at the early and late phases of paw licking and reduced the writhing reflex in mice (formalin and writhing tests, resp.). When the hot plate test was conducted, borneol (in higher dose) produced an inhibition (P<0.05) of the nociceptive behavior. Such results were unlikely to be provoked by motor abnormality. Additionally, borneol-treated mice reduced the carrageenan-induced leukocytes migration to the peritoneal cavity. Together, our results suggest that borneol possess significant central and peripheral antinociceptive activity; it has also anti-inflammatory activity. In addition, borneol did not impair motor coordination.

Evaluation of the Anti-Inflammatory and Analgesic Activities of the Total Saponins Extracted from Fermented Polygala japonica Houtt

2013 ◽  
Vol 641-642 ◽  
pp. 931-934
Author(s):  
Ming Xing Liu ◽  
Ting Zhu ◽  
She Ne Guo ◽  
Hong Da Zhu
Keyword(s):  
Experimental Study ◽  
Acetic Acid ◽  
Vascular Permeability ◽  
Analgesic Activity ◽  
Inflammatory Activity ◽  
Hot Plate ◽  
Plate Models ◽  
Anti Inflammatory ◽  
Analgesic Activities

This study was to investigate the anti-inflammatory and analgesic activities of the total saponins extracted from fermented Polygala japonica Houtt (FPH) compared with that of unfermented Polygala japonica Houtt (UFPH). The total saponins extracted from FPH and UFPH were evaluated for anti-inflammatory activity in xylene-induced ear swelling and acetic acid-induced vascular permeability models in mice, analgesic activity in acetic acid-induced writhing and hot plate models in mice. The total saponins extracted from FPH had the significant anti-inflammatory (p<0.001) and analgesic (p<0.01) activities with the doses of 6 g/kg b.w. in mice. The results of this experimental study thus strongly support the potential significant use of the total saponins extracted from FPH for pain and inflammatory.

scholarly journals Anti-inflammatory, antipyretic, analgesic, and antioxidant activities of Haloxylon salicornicum aqueous fraction

2019 ◽  
Vol 17 (1) ◽  
pp. 1034-1042
Author(s):  
Riaz Ullah ◽  
Mansour S. Alsaid ◽  
Ali S. Alqahtani ◽  
Abdelaaty A. Shahat ◽  
Almoqbil A. Naser ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Water Extract ◽  
Antioxidant Potential ◽  
High Dose ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Aqueous Fraction ◽  
Plate Test ◽  
Anti Inflammatory ◽  
Haloxylon Salicornicum

AbstractThe medicinal plant Haloxylon salicornicum is utilized for therapeutic purposes. We previously reported the antioxidant potential of hexane fraction and methanol extracts of the same species. However, since these solvents could be clinically toxic, the current findings investigated the pharmacological effects of the water fraction. The pain relieving, antioxidant, anti-inflammatory, and antipyretic potential of H. salicornicum water extract (HEW) were studied at two concentrations (250 and 500 mg/kg) in rodents. The carrageenan stimulated rat paw edema assay was exercised to assess anti inflammatory potential in rats; yeast-stimulated hyperthermia was utilized to test antipyretic activity in mice; analgesic properties were assessed based on acetic acid-induced writhing, tail flicking, and hot-plate test; and antioxidant potential was examined with the 2,2-diphenyl-1-picrylhydrazyl assay. We found that 500 mg/kg HEW inhibited edema by 44.03%. Yeast-induced hyperthermia in mice was reduced by 250 and 500 mg/kg HEW after 30, 60, and 120 min with significant level of (P < 0.001) compared to rectal temperature of yeast administered group. The high dose of HEW (500 mg/kg) improved the reaction time of mice in the hot-plate test from 6.66 ± 0.33 to 11.33 ± 0.49 s after 120 min. In the acetic acid-stimulated writhing test, 250 and 500 mg/kg HEW decreased writhing by 32.71% and 51.40%, respectively, after 20 min. HEW also showed antioxidant effects. These results demonstrate that HEW is bioactive and has therapeutic potential for treating a variety of ailments.

scholarly journals Anti-inflammatory and Analgesic Effects in Rodent Models of Ethanol Extract of Clausena anisata Roots and their Chemical Constituents

2017 ◽  
Vol 12 (1) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Emmanuel Kofi Kumatia ◽  
Kofi Annan ◽  
Rita Akosua Dickson ◽  
Abraham Yeboah Mensah ◽  
Isaac Kingsley Amponsah ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Crude Extract ◽  
Analgesic Effect ◽  
Chemical Constituents ◽  
Ethanol Extract ◽  
Phytochemical Analysis ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Anti Inflammatory

The in vivo anti-inflammatory and analgesic activities of the crude ethanol extract and chemical constituents of Clausena anisata roots were investigated. The crude extract, which was devoid of any visible acute toxicity, displayed significant anti-inflammatory effect at the dose of 1000 mg/kg (p.o.) when assessed using the carrageenan-induced oedema model. In the acetic acid-induced writhing and hot plate tests, it produced a very significant ( p < 0.001), dose-dependent analgesic effect, with maximum analgesic activity of 72.1% at 1000 mg/kg (p.o.). Phytochemical analysis of the crude extract resulted in the isolation of four coumarins (anisocoumarin B, osthol, imperatorin and xanthotoxol) and a carbazole alkaloid, heptaphylline. Among the isolated compounds, osthol and anisocoumarin B produced the highest anti-inflammatory activity at 9 mg/kg (p.o.): slightly better than the positive control, indomethacin. Except for xanthotoxol, all the isolated compounds administered at 6 mg/kg (p.o.) produced significant analgesic activity and higher than diclofenac; with heptaphylline being the most potent (48.7%). The analgesic activity of anisocoumarin B (50.4%) was the highest among the isolates tested and the standard, tramadol, in the hot plate test. The nonselective opioid receptor antagonist, naloxone, abolished the analgesic effect of the crude extract and the tested isolates (anisocoumarin B and xanthotoxol) in the hot plate test suggesting an effect via the central opioidergic system. These findings provide the scientific basis for the use of C. anisata roots in traditional medicine as anti-inflammatory and analgesic agents.

scholarly journals The Study of the Effect of Histidine Derivatives as a Novel Antinociceptive and Anti-Inflammatory Activity

2011 ◽  
Vol 8 (4) ◽  
pp. 1832-1842 ◽  
Author(s):  
Usama H. Ramadhan ◽  
Niran J. Al-Salihi
Keyword(s):  
Inflammatory Activity ◽  
Biochemical Activity ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Writhing Test ◽  
Plate Test ◽  
Chemical Structures ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Histidine Derivatives

This study explains the biochemical activity of histidine derivatives The compounds were identified by CHN analysis, FT-IR and H1NMR. The results certified that the chemical structures of the prepared compounds. The anti-inflammatory and antinociceptive activity was studied by two different tests; the hot plate test and writhing test for analgesic activity and two tests for anti-inflammatory activity they are formalin induced inflammation test and carrageen an induced inflammation test. The histidine derivatives were found to have potent activity as anti-inflammatory and antinociceptive. The active compounds were tested to acute toxicity. It was found that they are safety to the dose 5 g/kg orally in mice without any mortality.

Water Mediated One-Pot, Stepwise Green Synthesis, Anti-Inflammatory and Analgesic Activities of (3-Amino-1-Phenyl-1H-Benzo[f]Chromen-2-yl) (1H-Indol-3-yl) Methanone Catalysed by L-Proline

2021 ◽  
Vol 18 ◽  
Author(s):  
G. Ganga Reddy ◽  
Ch Venkata Ramana Reddy ◽  
B. Srinivasa Reddy
Keyword(s):  
Analgesic Activity ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Hot Plate ◽  
Plate Method ◽  
One Pot ◽  
Standard Drug ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Analgesic Activities

Aim: The reactions were carried out by one pot three-component synthesis, 3-cyanoacetylindole (1) on reaction with aromatic aldehydes (2) and β-naphthol (3) in an aqueous medium in presence of L-proline as a catalyst under reflux for 30 min, resulted (3-amino-1-phenyl-1H-benzo[f]chromen-2-yl) (1H-indol-3-yl)methanone (4). The method has many advantages like short reaction times, good yields and simple workup procedure besides being green in nature. Pharmacological evaluation of title compounds was done for anti-inflammatory and analgesic activities. Anti-inflammatory activity was carried carrageenan-induced paw edema model in which indomethacin was used as standard and analgesic activity was evaluated by eddy's hot plate method using diclofenac as standard drug. Background: Benzopyrans or chromenes are an important class of heterocyclic compounds due to their broad spectrum of biological activity and a wide range of applications in medicinal chemistry. The chromene moiety is found in various natural products with interesting biological properties. Chromenes constitute the basic backbone of various types of polyphenols and are widely found in alkaloids, tocopherols, flavonoids and anthocyanins. Indoles are omnipresent in various bioactive compounds like alkaloids, agrochemicals and pharmaceuticals. Objective: To synthesize one-pot stepwise Green synthesis, anti-inflammatory and analgesic activities of 3-amino-1-phenyl-1H-benzo[f]chromen-2-yl) (1H-indol-3-yl)methanones Methods: The acute anti-inflammatory effect was evaluated by carrageenan-induced mice paw edema (Ma Rachchh et al., 2011). Edema was induced by injecting carrageenan (1% w/v, 0.1 ml) in the right hind paw of mice. The test compounds 1-12, indomethacin (10 mg/kg) and the vehicle were administered orally one hour before injection of carrageenan. Paw volume was measured with digital plethysmometer at 0, 30, 60, 90, 120 min after injection. Percentage increase =A-B/ A *100 Results: Carrageenan Induced paw edema model was used for Anti-inflammatory activity in which animals treated with standard (indomethacin) and test compounds showed a significant decrease in the paw edema. Analgesic activity was estimated by using Eddy’s hot plate method; animals were treated with standard (diclofenac) and test compounds showed a significant increase in the reaction time. Conclusion: A green, One-pot, step-wise and three-component synthesis of 3-amino-1-phenyl-1H-benzo[f]chromen-2-yl) (1H-indol-3-yl) methanone was achieved by using water as a solvent, L-proline as catalyst under reflux conditions. The reactions were carried out in eco-friendly conditions with shorter reaction times, easier workup and high yields. Anti-inflammatory activity was evaluated by carrageenan-induced paw edema model where significant anti-inflammatory activity is shown by all the test compounds (4a-l) when compared to standard drug. Analgesic activity was studied by Eddy’s Hot plate method and Test compounds 4e, 4f, 4h, 4i, 4j, 4k, 4l showed significant activities when compared to the reference drug.

scholarly journals Analgesic, Anti-Inflammatory, and Antioxidant Activities of Byrsonima duckeana W. R. Anderson (Malpighiaceae)

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Maria Christina dos Santos Verdam ◽  
Fernanda Guilhon-Simplicio ◽  
Kleyton Cardoso de Andrade ◽  
Karina Lorena Meira Fernandes ◽  
Tallita Marques Machado ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Antioxidant Activities ◽  
Ethanol Extract ◽  
Quinic Acid ◽  
Polyphenol Content ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Writhing Test ◽  
Anti Inflammatory ◽  
Analgesic Activities

Background. Byrsonima is a promising neotropical genus, rich in flavonoids and triterpenes, with several proven pharmacological properties. Nevertheless, Byrsonima duckeana W. R. Anderson is an Amazonian species almost not studied. Objective. To assess the antioxidant, anti-inflammatory, and analgesic activities of Byrsonima duckeana leaves. Materials and Methods. We analyzed an ethanol extract and its fractions for polyphenol content and UHPLC-MS/MS, phosphomolybdenum, DPPH, TBARS antioxidant tests, formalin-induced pain, carrageenan-induced peritonitis, acetic acid-induced abdominal writhings, and hot plate assays. Results. All the samples showed high polyphenol content and antioxidant capacity in the phosphomolybdenum, DPPH, and TBARS tests. We identified ethyl gallate, quinic acid, gallic acid, catechin, epicatechin, quercetrin, and quercetin in the samples. B. duckeana was able to reduce leukocyte migration in the carrageenan-induced peritonitis by 43% and the licking time in the formalin test by 57%. In the acetic acid-induced writhing test, the chloroform (FCL) and ethyl acetate (FEA) fractions were the most active samples. FEA was selected for the hot plate test, where all the dosages tested (5, 50, and 200 mg·kg−1) showed significant analgesic activity. Conclusion. B. duckeana has interesting analgesic and antioxidant activities, due to its high phenolic content, especially phenolic acids.

scholarly journals STUDY OF THE ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF A NEW NON-OPIOID ANALGESIC BASED ON A SELECTIVE INHIBITOR OF TRPA1 ION CHANNELS

2019 ◽  
Vol 26 (1) ◽  
pp. 77-87
Author(s):  
Evgeniya A. Beskhmelnitsyna ◽  
Mikhail V. Pokrovskii ◽  
Aleksandr A. Dolzhikov ◽  
Tat’yana V. Avtina ◽  
Nina I. Zhernakova ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Conflict Of Interest ◽  
Inflammatory Activity ◽  
Laboratory Mice ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Reference Drug ◽  
Plate Test ◽  
Analgesic Effects ◽  
Anti Inflammatory

The aim is to study the analgesic and anti-inflammatory activity of an innovative molecule under the ZC02-0012 laboratory code belonging to the group of selective blockers of the TRPA1 ion channel.Materials and methods. The study of the ZC02-0012 analgesic activity was carried out by the hot plate and acetic acid writhing tests. The hot plate test was performed on white laboratory mice. ZC02-0012 substance was administered in doses of 1, 3 and 9 mg/kg. Ketorol at a dose of 3.48 mg/kg was chosen as the reference drug. To study the analgesic effects in the hot plate test, intact white laboratory mice were placed on a preheated at 55°C plate to determine the base level of pain sensitivity. Then the test substances were administered to the animals divided into groups, and the hot plate test was repeated after 30, 60, 90 and 120 minutes. To study the analgesic effects in the test of acetic acid writhing, white laboratory rats were injected with the ZC02-0012 substance at doses of 0.46, 1.38, and 4.15 mg/kg. Ketorol at a dose of 1.6 mg/kg was chosen as the reference drug. 30 minutes after intramuscular injection and 60 minutes after intragastric administration, the intraperitoneal administration of a 0.75% solution of acetic acid was carried out at the rate of 1 ml per 100 g of animal weight. Counting the number of writhings started 15 minutes after the injection of acetic acid and continued for 30 minutes. The anti-inflammatory effects of the ZC02-0012 substance were studied using a model of acute exudative inflammation in response to the subplantar introduction of 0.02 ml of 2% formaldehyde aqueous solution into the right hind paw of the mouse. 4 hours after the phlogistic introduction, the mass of the edematous paw was evaluated. ZC02-0012 substance at doses of 1, 3 and 9 mg/kg and the Diclofenac reference drug at a dose of 13.91 mg/kg were administered intragastrically or intramuscularly 45 minutes before the introduction of phlogistic. The presence and severity of anti-inflammatory activity was judged by the inhibitory effect, expressed in percentage.Results. The analgesic activity of ZC02-0012 is found to exceed that for Ketorol in both the intramuscular and intragastric ways of administration according to the results of hot plate tests in doses of 3 and 9 mg/kg and acetic acid writhing in doses of 1.38 and 4.15 mg/kg, while the anti-inflammatory activity of ZC02-0012 at doses of 3 and 9 mg/kg is shown to be comparable to that of Diclofenac. Conclusion. The innovative molecule under the ZC02-0012 laboratory code is established to exhibit a pronounced analgesic and anti-inflammatory activity, thus being prospective for further research.Conflict of interest: the authors declare no conflict of interest.

scholarly journals Synthesis, characterization and pharmacological activity of Ibuprofen Acyl Hydrazones and their Conversion into 1,3,4-Oxadiazoline Derivatives

2019 ◽  
Vol 10 (4) ◽  
pp. 3626-3635
Author(s):  
Mustafa Q. Alderawy ◽  
Leaqaa A. Alrubaie ◽  
Falah Hassan Sheri ◽  
Basim Jasim Hameed
Keyword(s):  
Acetic Acid ◽  
Ethyl Acetate ◽  
Pharmacological Activity ◽  
Uv Light ◽  
Hot Plate ◽  
Plate Method ◽  
Activity Assessment ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
New Compounds

This work implicates the synthesis of Ibuprofen Acyl Hydrazones and then Converted into the new 1,3,4-Oxadiazoline derivatives that characterized by proton-NMR, FT.IR and elemental microanalysis (CHN) techniques. The intermediates and final compounds were investigated for their physicochemical properties, including the melting point,  color, the yield percent, and thin-layer chromatography performed by using TLC silica gel (60) F254, Merck (Germany), to identify the purity of the products and to know the reaction endpoint. Compounds were monitored by UV light irradiation and the elution by using the following systems:: ethyl acetate: hexane ( 3:7), ethyl acetate, ethanol:dioxan (1:1) and methanol: chloroform (1:9). The study was performed using Swiss albino mice (25-30 g) for the pharmacological activity assessment. Hind edema template of carrageenan used for anti-inflammatory activity assessment and the analgesic activity evaluated using ( writhing induced by acetic acid ) and hot plate method, the results show that all the final compounds present with good anti-inflammatory plus analgesic activities exhibited in the animal model of our experimental work  , we observed that the standard compound and the synthesized derivatives substantially reduced carrageenan-induced edema at all-times (2,4,6,24) hours, all chemically synthesized new compounds actually significantly reduced the number of acetic acid writhings induced in mice and finally in hot plate method there is high increase in the reaction time to painful stimulation  

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