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  

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 AN INVESTIGATION OF THE ANALGESIC AND ANTI-INFLAMMATORY EFFECTS OF AERIAL PARTS OF FLACOURTIA JANGOMAS

2021 ◽  
pp. 77-81
Author(s):  
C. JOTHIMANIVANNAN ◽  
P. LALITHA ◽  
K. MEENA ◽  
A. MEENAJESILIYA ◽  
J. C. MOGANAPRIYA ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Aqueous Extract ◽  
Inflammatory Activity ◽  
Dependent Manner ◽  
Hot Plate ◽  
Plate Method ◽  
Standard Drug ◽  
Stem Extract ◽  
Anti Inflammatory ◽  
Analgesic Activities

Objective: The present study was aimed to evaluate the analgesic and anti-inflammatory effects of leaf and stem part aqueous extract of Flacourtia jangomas. Methods: Aqueous extract of leaves (ALE) and aqueous extract stem (ASE) part of Flacourtia jangomas were sequentially prepared by maceration process and subjected to a preliminary phytochemical screening. The anti-inflammatory activity was assessed by the carrageenan-induced acute rat paw oedema model and Analgesic activity was evaluated by acetic acid-induced writhing model and hot plate method in mice. The data were analysed by one-way ANOVA followed by post hoc Dunnet’s test by using SPSS V.15 (student trail version). Results: The preliminary phytochemical analysis of extracts of leaves and stems indicated the presence of carbohydrate, alkaloids flavonoids, phenols, tannins, saponins. The extracts showed significant anti-inflammatory and analgesic activities with a dose-dependent manner. The ethanolic extract from the leave extract of Flacourtia jangomas at the dose 200 mg/kg has 55.6% significant anti-inflammatory activity compared to the standard drugs (44.4%). Even at the low dose leave extract has more potent than aqueous stem extract. Where in analgesic effect by Hot plate method basal reaction time results showed that aqueous extract of stem part at the dose of 200 mg /kg has a significant effect at 120 mts 10.0 sec when compared with std pentazocine 13.0 sec. In peripheral analgesic method Acetic acid-induced writhing model results have not shown much more significant when compared with standard drug (42.1%). The potential to cause anti-inflammation by stem extract was comparatively less than that of leave extract. Thus it could be concluded that Flacourtia jangomas leave extract possess significant anti-inflammatory activity Conclusion: Our findings suggest that Flacourtia jangomas extract is safe and has potential anti-inflammatory and analgesic activities, which promote this use as a food supplement against pain and inflammation related to inflammatory diseases.

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 ANALGESIC, ANTI-INFLAMMATORY, ANTIPYRETIC EVALUATION OF ETHANOLIC EXTRACT OF LEAF OF POLYALTHIA LONGIFOLIA

2021 ◽  
Vol 10 (3) ◽  
Author(s):  
Ramjith.U. S ◽  
Faby Salim ◽  
Ashamol.K. S ◽  
Cyril Mathews Jacob
Keyword(s):  
Acetic Acid ◽  
Ethanolic Extract ◽  
Percentage Increase ◽  
Hot Plate ◽  
Plate Method ◽  
Percentage Decrease ◽  
Antipyretic Activity ◽  
Ethanolic Extracts ◽  
Anti Inflammatory ◽  
Polyalthia Longifolia

Polyalthia longifolia leaves ethanolic extracts produced significant analgesic activity in both Hot plate and acetic acid induced writhing models in mice. In hot plate method percentage increase in reaction time was determined where as in acetic acid induced writhing model percentage decrease in writhings was determined. From the results obtained it can be concluded that Polyalthia longifolia leaves has analgesic, anti inflammatory and antipyretic activity. Keywords: Analgesic, Anti-inflammatory, Antipyretic, Hot plate method, Acetic acid induced writhing model.

The Essential Oil of the Fruits of Ferula stenocarpa Boiss. & Hausskn: Powerful Analgesic and Anti-inflammatory Effects

2021 ◽  
Author(s):  
H. Shafaroodi ◽  
J. Asgarpanah ◽  
J. Asgarpanah
Keyword(s):  
Animal Model ◽  
Acetic Acid ◽  
Essential Oil ◽  
Acute Inflammation ◽  
Central Pain ◽  
Paw Edema ◽  
Hot Plate ◽  
Anti Inflammatory ◽  
Analgesic Activities

Ferula stenocarpa is an aromatic herb whose fruits are widely used in Persian traditional medicine as a painkiller and to relive inflammation-based disorders. Considering the higher content of essential oil in the fruits, the oil’s anti-inflammatory and analgesic activities were investigated in an animal model in vivo. The analgesic effect of Ferula stenocarpa fruits essential oil was evaluated via testing the writhing triggered by acetic acid examination and hot plate technique. Moreover, the acute anti-inflammatory effects were studied through the paw edema triggered in mice. Using 20 and 40 mg/kg of the oil revealed an analgesic impact considering the increment in the reaction time needed for the hot plate approach. Furthermore, all examined doses of the oil caused a reduction in the frequency of writhes in the mice. It was observed that the oil (40 mg/kg) followed by 10 and 20 mg/kg caused inflammatory reduction. The findings indicated that the oil may possess significant activities against acute inflammation. It had both peripheral and central pain-killing impacts. α-Pinene (43.1%) and β-pinene (22.9%) as the main constituents of the oil, can be considered as the responsible compounds to manage inflammation and pain.

scholarly journals Anti-inflammatory and analgesic activities of Clerodendrum capitatum (Willd) Schum. & Thonn. (Verbenaceae) leaves

2020 ◽  
Vol 17 (1) ◽  
pp. 1-7
Author(s):  
Abdulrahman Adamu ◽  
Abdulmumin Z. Abubakar ◽  
Adamu A. Ambi ◽  
Ibrahim M. Aliyu ◽  
Hamza Mohammed ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Ethyl Acetate ◽  
Aqueous Ethanol ◽  
Lethal Dose ◽  
Ethanol Extract ◽  
Perennial Herb ◽  
North East ◽  
South Central ◽  
Anti Inflammatory ◽  
Analgesic Activities

Clerodendrum capitatum (Willd) Schumach and Thonn. (Verbenaceae) is a perennial herb, which grows up to 0.5 m to 2 m high. It is widespread over North-East, East, and South Central Africa. It is known as “bambaro or maashayi” by the Hausas of Northern Nigeria. The leaves are used traditionally to treat intercostal pain, headaches and toothaches. The aim of this study is to evaluate the anti-inflammatory and analgesic activities of the aqueous ethanol extract and fractions of C. capitatum. The anti-inflammatory activity was investigated using carrageenan induced rat paw oedema model, while acetic acid induced mice writhing model was used to evaluate the anti-nociceptive property. The oral median lethal dose values were found to be greater than 5,000 mg/kg for the aqueous ethanol extract, ethyl acetate and n-butanol fractions, while that of dichloromethane fraction was less than 2000 mg/kg using OECD method. The acetic acid induced writhing was significantly (P<0.05-0.001) reduced particularly for the EF and NF fractions at 200 mg/kg (93.12% and 98.79%). DF showed percentage inhibition of 87.59% and 81.75% at 50 and 100 mg/kg respectively. The extracts and fractions also caused a significant (P<0.05-0.001) dose dependent reduction of inflammation induced by carrageenan when compared with the negative control with the maximum inhibitory effect of 43.69% observed in Ethyl acetate fraction at 50 mg/kg dose at the 3rd hour. It can be concluded that the leaf extracts of C. capitatum possess anti-inflammatory and analgesic effects in animal models, which may be mediated through the phytochemical constituents present in the extract and fractions of the plant. Keywords: Clerodendrum capitatum; Anti-inflammatory; Analgesic; OECD

scholarly journals Analgesic, Anti-Inflammatory, and GC-MS Studies onCastanospermum australeA. Cunn. & C. FraserexHook.

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Thankarajan Sajeesh ◽  
Thangaraj Parimelazhagan
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Ethanol Extract ◽  
Hot Plate ◽  
Plate Method ◽  
Writhing Test ◽  
Paw Oedema ◽  
Soxhlet Apparatus ◽  
Anti Inflammatory ◽  
Ethanol Extracts

The present study was aimed to evaluate the analgesic and anti-inflammatory properties ofCastanospermum australeand to profile phytochemicals by GC-MS. The ethanolic extracts were prepared by successive solvent extraction using Soxhlet apparatus. The analgesic activity was analyzed by hot plate method and acetic acid-induced writhing test whereas anti-inflammatory study was done by carrageenan induced paw oedema model. The acute toxicity study revealed that ethanol extracts of leaf and bark ofC. australewere safe even at a higher dose of 2000 mg/kg whereas ethanol extract of seed was toxic at the same dose. In both hot plate method (5.85 s) and acetic acid-induced writhing test (57%), the leaf ethanol extract exhibited significant analgesic activity (P<0.001) at a dose of 400 mg/kg. The anti-inflammatory activity of leaf extract was exhibited by the reduction in paw linear diameter by 64.76% at 400 mg/kg in carrageenan induced paw oedema. The GC-MS analysis of the ethanol extract of leaf revealed sixteen major compounds of which 1,7-dimethyl-4,10-dioxa-1,7-diazacyclododecane, (+)-N-methylephedrine, and permethylspermine were found to be pharmaceutically and the most important. These findings justify thatC. australecan be a valuable natural analgesic and anti-inflammatory source which seemed to provide potential phytotherapeutics against various ailments.

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 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.

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