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.

Analgesic and Anti-inflammatory Activity of Ficus glomerata in Experimental Animal Models

2011 ◽  
Vol 4 (3) ◽  
pp. 1501-1505
Author(s):  
Cylma Menezes ◽  
Kunal G ◽  
Reema N ◽  
Satyanarayana D ◽  
Jagadish K
Keyword(s):  
Analgesic Activity ◽  
Inflammatory Activity ◽  
Significant Activity ◽  
Paw Edema ◽  
Hot Plate ◽  
Plate Method ◽  
Swiss Albino Mice ◽  
Albino Mice ◽  
Anti Inflammatory ◽  
Ficus Glomerata

The anti-inflammatory and analgesic activity of various extracts of Ficus glomerata Roxb. were evaluated in experimental animals. We have determined the anti-inflammatory and analgesic activity of various extracts of the dried fruits of Ficus glomerata by oral administration at doses of 200 and 400 mg/kg of body weight to healthy animals. The extracts were studied for their anti-inflammatory activity in carageenan induced hind paw edema in rats and the paw volume was measured plethysmometrically after 3 hours of injection. The extracts were also evaluated for analgesic activity using Eddy’s hot plate method in Swiss albino mice. The extracts of Ficus glomerata significantly reduced carageenan induced hind paw edema in rats and analgesic activity evidenced by increase in the reaction time by Eddy’s hot plate method in Swiss albino mice. The extracts showed a similar anti-inflammatory and analgesic effect comparative to the standard drugs indomethacin and diclofenac sodium respectively. The present results indicated the ethanolic extract of Ficus glomerata exhibited more significant activity than other extracts in the treatment of pain and inflammation.

scholarly journals Evaluation of analgesic and anti-inflammatory activity of Levocetirizine in albino rats

2019 ◽  
Vol 8 (8) ◽  
pp. 1805
Author(s):  
Dipti R. Sonawane ◽  
Jugalkishor B. Jaju ◽  
Ganesh R. Pawar ◽  
Punam A. Gosavi
Keyword(s):  
Analgesic Activity ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Hot Plate ◽  
Plate Method ◽  
Standard Drug ◽  
Group I ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Tail Clip

Background: Levocetirizine, the R-enantiomer of Cetirizine has pharmacokinetically and pharmacodynamically favourable characteristics, with rapid onset of action, high bioavailability, high affinity for and occupancy of the H1-receptor, limited distribution, minimal hepatic metabolism together with minimal side effects. Non-steroidal anti-inflammatory drugs (NSAIDs) have been used for many years for analgesic, anti-inflammatory, and more recently in the case of aspirin, antithrombotic purposes. Because of the significant side effect profiles of steroidal and NSAID medications, there is a greater interest in newer compounds such as antihistaminic drugs. This article will consider the potential or otherwise of the reported analgesic and anti-inflammatory effects of levocetirizine to enhance its effectiveness in the treatment of allergic disease with pain.Methods: Albino Wistar rats of either sex weighing 150-250 grams were used. For both Analgesic activity and Anti-inflammatory activity, 4 groups consisting of 6 animals per group were used. Group I: Control: 1% Gum acacia. 2ml/kg, Group II: Standard drug: Diclofenac sodium 4.5mg/kg; Group III: Test Drug 1: Levocetirizine 1mg/kg; Group IV: Test Drugs 2: Levocetirizine 1mg/kg+Diclofenac sodium 4.5mg/kg. Drugs were administered orally. For analgesic activity, Tail clip method and Hot plate method was used. For acute anti-inflammatory activity Carrageenan induced rat paw oedema method was used.Results: Levocetirizine, is found to have significant analgesic activity in rats (1 mg/kg dose) alone and in combination with Diclofenac Sodium in Haffner’s Tail Clip method and Eddy’s Hot Plate Method. Levocetirizine also has got prominent anti-inflammatory activity in acute models evidenced by percentage inhibition of acute rat paw oedema.Conclusions: Levocetirizine possess analgesic and acute anti-inflammatory activity alone and in combination with Diclofenac sodium.

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.

scholarly journals Evaluation of analgesic and anti-inflammatory activity of ethanolic extract of Enhydra fluctuans on male wistar rats

2021 ◽  
Vol 9 (1) ◽  
pp. 1-7
Author(s):  
Kishor Kumar Roy ◽  
Md. Kabirul Islam Mollah ◽  
Md. Masud Reja ◽  
Dibyendu Shil ◽  
Ranjan Kumar Maji
Keyword(s):  
Wistar Rats ◽  
Pain Threshold ◽  
Ethanolic Extract ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Hot Plate ◽  
Plate Method ◽  
Traditional System ◽  
Male Wistar Rats ◽  
Anti Inflammatory

Enhydra fluctuations an edible semi-aquatic vegetable plant are widely used in the traditional system of medicine. Ethanolic extract of Enhydra fluctuans was screened for analgesic & anti-inflammatory activity. Analgesic activity was evaluated by the hot plate method and anti-inflammatory activity was evaluated by formalin induce paw edema in Wistar rats (male). Ethanolic extract dose of 300 mg/kg reduce formalin induce paw inflammation and also increased the pain threshold in rats evidenced by hot plate method. The experimental results concluded that Enhydra fluctuans have significant analgesic and anti-inflammatory activity may due to flavonoid and phenolic compound content.

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.

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 and anti-inflammatory effect of Clausena suffruticosa root extract in animal model

2011 ◽  
Vol 3 (3) ◽  
pp. 631-639 ◽  
Author(s):  
M. A. Rahman ◽  
J. S. Chakma ◽  
S. Islam ◽  
M. S. Rana ◽  
N. U. Ahmed
Keyword(s):  
Animal Model ◽  
Analgesic Activity ◽  
Root Extract ◽  
Paw Edema ◽  
Hot Plate ◽  
Plate Method ◽  
Albino Rat ◽  
Chemical Models ◽  
Anti Inflammatory ◽  
Inflammatory Effect

The aim of the study was to evaluate the analgesic and anti-inflammatory effects of Clausena suffruticosa root extract. The effect of different concentrations of ethanolic root extract were studied in animal model using acetic acid induced writhing response, formalin induced pain, hot plate method for analgesic activity in Swiss Albino mice and carrageenan induced paw edema for anti-inflammatory action in Wister Albino rat. The extract reduced writhing response 20% by 0.5g/kg, 57.6% by 1.5g/kg and 78% by 2 g/kg and showed significant analgesic activity as determined by formalin induced pain and hot plate method. In the carrageenan induced paw edema, the extract at a dose of 0.5, 1.0 and 2.0 g/kg showed the highest inhibition 17.23%, 26.30% and 42.46%, respectively, at the 4th hour of administration. The results indicate that the extract shows promising analgesic effect in chemical models of nociception (not related to the opioid system) and anti-inflammatory effect.

scholarly journals Synthesis, Characterization and Anti-inflammatory Activity of (2E)-3-(2-Bromo-6-hydroxy-4-methoxyphenyl)-1-(naphthalene-2-yl)prop-2-en-1-one

2020 ◽  
Vol 32 (3) ◽  
pp. 561-564
Author(s):  
Dileep Kumar M. Guruswamy ◽  
Shankar Jayarama
Keyword(s):  
1H Nmr ◽  
13C Nmr ◽  
Stair Climbing ◽  
Inflammatory Activity ◽  
Spectral Studies ◽  
Albino Rats ◽  
Paw Edema ◽  
Standard Drug ◽  
Edema Model ◽  
Anti Inflammatory

(2E)-3-(2-Bromo-6-hydroxy-4-methoxyphenyl)-1-(naphthalene-2-yl)prop-2-en-1-one (d1) was synthesized by the Claisen-Schmidt condensation method and characterized by 1H NMR, 13C NMR spectral studies. The anti-inflammatory activity was conducted in Swiss albino rats for paw edema model. Edema was actuated with 1 % carrageenan to every one of the animals following 1 h of the oral medicines. Paw thickness was checked at t = 1, 2, 3, 4, 5 and 24 h. Stair climbing score and motility score were surveyed at t = 24 h. Compound d1 signicant decline in paw thickness at p < 0.001 diminished by 32 % in paw thickness. The compound d1 signicantly expanded the stair climbing and motility score. This study suggested that the compound d1 exhibits remarkable anti-inflammatory activity when compared with that of the standard drug.

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 Analgesic and Anti-inflammatory Activity of Withania somnifera Root Extract

2021 ◽  
pp. 75-84
Author(s):  
Subasini Uthirapathy
Keyword(s):  
Toxic Effect ◽  
Analgesic Activity ◽  
Withania Somnifera ◽  
Methanolic Extract ◽  
Tail Flick ◽  
Paw Edema ◽  
Hot Plate ◽  
Standard Drug ◽  
Adjuvant Induced Arthritis ◽  
Anti Inflammatory

The anti-inflammatory and analgesic properties of the 85 % methanolic extract of Withania somnifera (WS) root was investigated and the anti-inflammatory effect was compared with the standard drug indomethacin. Analgesic activity was carried out by hot plate and tail flick method. Anti-inflammatory activity was carried out by carraggenan induced paw edema and Freund’s adjuvant induced arthritis. The results are related with evaluation of the analgesic activity in hot plate and tail flick method, they reveal that methanolic extract has exhibited significant activity (P<0.05) at 150 mg/kg b.wt, itself, whereas, the percentage inhibition exhibited by WS (350 mg/kg b.wt,) in carrageenan induced paw edema is found to be nearer to that of standard drug (10 mg/kg b.wt.). In Freund’s adjuvant induced arthritis, WS is seen to decrease the paw volume significantly (P<0.05). Significant (P<0.05) protection is also observed by elevating antioxidant enzymes. WS does not exhibit toxic effect which is observed in standard drug treatment. The 85 % crude methanolic extract does not present toxic effect as observed in indomethacin treatment. However, the extract has exhibited analgesic, anti-inflammatory and antioxidant activities.

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