scholarly journals SYNTHESIS, CHARACTERIZATION, AND BIOLOGICAL EVALUATION OF OXAZOLONE ANALOGS

2018 ◽  
Vol 11 ◽  
Author(s):  
Muthuboopathi G
Keyword(s):  
Fourier Transform ◽  
Infrared Spectroscopy ◽  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
The Other ◽  
Inflammatory Activity ◽  
Stabilization Method ◽  
Membrane Stabilization ◽  
Standard Drug ◽  
Anti Inflammatory

Objective: The main objective of the study is to synthesize some novel oxazolone derivatives to evaluate for anti-inflammatory activity.Methods: Acetylglycine was prepared using glycine and acetic anhydride, and the prepared acetylglycine was condensed with different aromatic aldehydes to get novel oxazolone derivatives. The synthesized compound was carried out the characterization by Fourier-transform infrared spectroscopy and find the anti-inflammatory by human red blood cell (HRBC) membrane stabilization method.Results: The anti-inflammatory activity was performed using novel oxazolone derivatives (Cpd1, Cpd2, Cpd3, and Cpd4) and nimesulide (as standard) on HRBC membrane stabilization method. The percentage protection was observed using colorimeter. The synthesized oxazolone was compared with the standard drug nimesulide for anti-inflammatory using HRBC membrane stabilizing method. All the synthesized oxazolone derivatives have shown the anti-inflammatory activity as that of standard. The results can be easily interpreted using histograms.Conclusions: Among all the synthesized compounds, oxazolone with 4-chlorobenzaldehyde shows more anti-inflammatory activity when compared with the other oxazolone derivatives.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF METHANOL EXTRACT OF NIEBUHRIA APETALA (ROTH) DUNN – IN VITRO MODELS

2019 ◽  
pp. 278-281
Author(s):  
RAJESH A ◽  
DOSS A ◽  
TRESINA PS ◽  
MOHAN VR
Keyword(s):  
Methanol Extract ◽  
Protein Denaturation ◽  
In Vitro Models ◽  
Inflammatory Activity ◽  
Membrane Stabilization ◽  
Standard Drug ◽  
Inflammatory Agent ◽  
Potential Source ◽  
Anti Inflammatory

Objective: The objective of this study was to determine the anti-inflammatory activity of methanol extract of Niebuhria apetala and its possible mechanism of action. Methods: Methanol extract of Niebuhria apetala leaf (NAL) was assessed for its anti-inflammatory activity by in vitro methods. Using albumin denaturation assay, proteinase inhibitory activity, membrane stabilization, and antilipoxygenase activity at different concentrations, in vitro anti-inflammatory activity was estimated. The standard drug used for this purpose was aspirin. Results: Methanol extract NAL at a concentration range of 100–500 μg/ml significant (p<0.01) protects the heat-induced protein denaturation. At the concentration of 500 mg/ml, NAL showed significant (p<0.01) inhibition of protease inhibitory action. Heat-induced hemolysis of erythrocyte, hypotonicity-induced hemolysis, and lipooxygenase activity were significant (p<0.01) inhibited at the concentration of 500 μg/ml. Conclusion: Finally, the present study indicates that methanol extract of Niebuhria apetala can be a potential source of anti-inflammatory agent.

scholarly journals DESIGN, SYNTHESIS, AND EVALUATION OF NEW DERIVATIVE OF 1,2,4-TRIAZOLES FOR ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTIVITY

2018 ◽  
Vol 10 (4) ◽  
pp. 29 ◽  
Author(s):  
Prabhu C. Jalihal ◽  
Vaibhav Rajoriya ◽  
Varsha Kashaw
Keyword(s):  
Biological Evaluation ◽  
Study Data ◽  
Inflammatory Activity ◽  
Basic Medium ◽  
Paw Edema ◽  
Zone Of Inhibition ◽  
Design Synthesis ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Objective: The object of the study is to design, synthesize and biological evaluation of isoniazid derived 1,2,4-triazoles compounds.Methods: Isoniazid based 1,2,4-triazoles derivatives have been synthesized by reaction of Isoniazid with carbon disulfide in basic medium (KOH) to form Potassium dithiocarbazinate salt and reaction with hydrazine hydrate converted into 4-amino-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol. These compounds were reacted with seven different benzaldehyde to form 4-[(substituted phenyl)-methylene]-amino-5-(pyridine-4-yl)-4H-1,2,4-triazol-3-thiol (4). The final compounds were synthesized by reaction with four different acetanilide to form 4-[substituted phenyl)-methylene]-amino-3-(N-substitutedcarboxamidomethylthio)-5-(pyridine-4-yl)-4H-1,2,4-triazoles derivatives. All these compounds were characterized by IR, 1H-NMR, [13]C-NMR and elemental analysis. The antimicrobial activity was determined by the cup plate method. Acute anti-inflammatory activity determined by using carrageenan-induced rat paw edema model.Results: Series PJ-A4, PJ-A7 and PJ-A13 showed more than 90% of the zone of inhibition against both Gram positive and Gram negative organisms. The antifungal study suggested that among synthesized compounds series PJ-A4, A7, A9, A11 and A13 showed more than 90% of zone of inhibition, A2, A10 and A12 shows more than 80% of the zone of inhibition. Anti-inflammatory study data indicate that compounds PJ-A4, PJ-A8, PJ-A9 and PJ-A13 produced 70 to 76% of paw edema inhibition compare to standard drug Ibuprofen which showed 83.3% after 5 h. Conclusion: Results suggested that the isoniazid based 1,2,4-triazole derivatives have significant antibacterial, antifungal and anti-inflammatory activity.

scholarly journals A scientific validation of In vitro anti-inflammatory activity of Punica granatum L. by human red blood cell membrane stabilization

2018 ◽  
Vol 6 (7) ◽  
pp. 2430
Author(s):  
Karunakar Kota ◽  
Sandhya Sharma ◽  
Jameela Tahashildar
Keyword(s):  
Methanolic Extract ◽  
Punica Granatum ◽  
Inflammatory Activity ◽  
Membrane Stabilization ◽  
Fruit Peel ◽  
Standard Drug ◽  
Membrane Lysis ◽  
Anti Inflammatory ◽  
Punica Granatum L

Background: In recent years there has been growing interest in therapeutic use of natural products, especially those derived from plants. P. granatum is very common dietary ingredient in many parts of India and has remarkable biological and medicinal properties.Methods: In the present study, the methanolic extract of fruit peels of Punica granatum Linn. (MEPG) were investigated for anti-inflammatory activity by simple, reliable, less toxic and less time consuming HRBC membrane stabilization method. The presentation of hypo tonicity induced HRBC membrane lysis was taken a measure of anti-inflammatory activity. Their activities were compared with standard drug diclofenac.Results: The results of the study demonstrated that P. granatum contains active constituents, which possess anti-inflammatory activity which is probably related to the inhibition of prostaglandin synthesis.Conclusions: It is concluded that methanolic extract of P. granatum fruit peel possesses significant anti-inflammatory activity and this is a possible rationale for its folkloric use as an anti-inflammatory agent.

scholarly journals POTENTIAL ANTIOXIDANT, ANTI-INFLAMMATORY AND ANTIBACTERIAL EVALUATION OF EXTRACTS OF LEUCAS ASPERA USING IN VITRO MODELS

2016 ◽  
Vol 8 (12) ◽  
pp. 292 ◽  
Author(s):  
Tahareen S. ◽  
Shwetha R. ◽  
Myrene R. D.
Keyword(s):  
Inflammatory Activity ◽  
Total Phenolic ◽  
Scavenging Activity ◽  
Membrane Stabilization ◽  
Standard Drug ◽  
Leucas Aspera ◽  
Ic50 Value ◽  
Anti Inflammatory ◽  
Stabilization Assay

<p><strong>Objective: </strong>To evaluate the potential antioxidant, anti-inflammatory and antibacterial activities of aqueous and methanolic extracts of leaves of <em>Leucas aspera</em> (Thumbae).</p><p><strong>Methods: </strong>Phytochemical screening of the leaves of <em>L. aspera</em> was followed by analysis of antioxidant activity by means of DPPH (2, 2-diphenyl-1-picrylhydrazyl) radical scavenging activity. <em>In vitro</em> anti‐inflammatory activity was evaluated using lipoxygenase inhibition, albumin denaturation assay, membrane stabilization assay and proteinase inhibitory activity at different concentrations. Aspirin was used as a standard drug for the study of anti‐inflammatory activity. Linear regression analysis was used to calculate half maximal inhibitory concentration, IC50 value. The zone of inhibition was performed against common pathogens to determine the antimicrobial activity at different concentrations of plant extracts (60%, 70%, 80%).</p><p><strong>Results: </strong>The phytochemical analysis revealed the presence of carbohydrates, amino acid, alkaloids, tannins, flavonoids, glycosides, xanthoproteins, and phenols. The total phenolic and flavonoid content was found to be 2.25±0.04 mg GAE/g (gallic acid equivalents) and 1.2±0.05 mg QE/g (Quercetin equivalents) of fresh weight tissue respectively. The IC50 values for hydrogen peroxide scavenging activity were found to be 244.6 µg/ml. The extract inhibited the lipoxygenase enzyme activity with an IC50 value of 356.3 µg/ml. Maximum inhibition of heat-induced protein denaturation of 69% was observed at 400 μg/ml, IC50 249.6 μg/ml. Proteinase activity was also significantly inhibited (IC50 = 421.6 μg/ml). Membrane stabilization assay attributed minor protection by the leaf extract with an IC50 of 206.7. It was observed that <em>E. coli</em> were inhibited at all concentrations, followed by <em>Klebsiella</em> and <em>Pseudomonas</em>.</p><p><strong>Conclusion: </strong>Results indicate that L. aspera possess anti-inflammatory properties due to the strong occurrence of polyphenolic compounds such as alkaloids, flavonoids, tannins and steroids that serve as free radical inhibitors or scavenger. Compounds of the plant L. aspera may hence be used as lead compounds for designing potent anti-inflammatory drug which can be used for treatment of various diseases.</p><p> </p>

scholarly journals Synthesis, characterization and biological evaluation of some novel N-Mannich bases of heterocyclic 1,3,4-thiadiazole.

2019 ◽  
Vol 9 (4-A) ◽  
pp. 220-228
Author(s):  
Piush Sharma ◽  
Charanjeet Singh
Keyword(s):  
Mannich Reaction ◽  
Mannich Bases ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Plate Method ◽  
Standard Drug ◽  
Excellent Activity ◽  
Anti Inflammatory

A series of some novel N-Mannich bases of heterocyclic 1,3,4-thiadiazole were synthesized through the condensation reaction of 1,3,4-thiadiazole containing a aromatic secondary amine, aromatic aldehydes and cyclic compounds employing Mannich reaction and using conventional synthesis. All the synthesized compounds were obtained in the range of 57.41-83.3 % yield. The structures of synthesized compounds were confirmed by UV, IR, 1H NMR spectroscopy. the essential structural features responsible for interaction with receptor site are established within a suggested pharmacophore. The in vitro antibacterial activity of the synthesized compounds was determined, against two Gram-positive bacteria, viz. S. aureus & B. subtilis and Gram-negative, viz. E. coli and K. pneumoniae, by cup-plate method using the standard drug ciprofloxacin. Minimum inhibitory concentrations (MIC) changed in the range of 1.56_ _ 200 mg mL_1. Compound 3b exhibited excellent activity against both bacteria. The in vitro antifungal activity of the synthesized compound was also evaluated by cup-plate method against the fungi A. niger and C. albicans compared with the standard drug Fluconazole. Compound 4a, 8a exhibited excellent activity against both fungi. The result has shown that the compounds are quite active against pathogens under study and were nontoxic. The anti-inflammatory activity of the compound was evaluated, on albino rats, by carageenan induced rat paw oedema method using the standard drug diclofenac sodium. Compound 7b and 8c exhibited excellent anti-inflammatory and analgesic pharmacological activities. Structurally the compound 7b has a greater number of unsaturated hydrocarbons in schiff base, which shows good lipophilic properties within electron rich morpholine ring in Mannich base. Statistical significance of differences between group was determined by one-way analysis of variance (ANOVA). Among the synthesized compounds 3a, 4b, 5c, 7b, 8a and 8c were found be the most active. All the synthesized compounds were found to be low lethal as ascertained by LD50 test. Keywords: N- Mannich bases of heterocyclic 1,3,4-thiadiazole derivatives; Mannich reaction; antimicrobial agents; anti-inflammatory activity;

scholarly journals PHYTOCHEMICAL ANALYSIS AND SUPPRESSION OF INFLAMMATORY TARGETS BY ADATHODA VASICA

2018 ◽  
Vol 11 (5) ◽  
pp. 162
Author(s):  
Amala Reddy ◽  
Sujatha Sundaresan
Keyword(s):  
Methanolic Extract ◽  
Maximum Yield ◽  
Foot Ulcer ◽  
Significant Inhibition ◽  
Inflammatory Activity ◽  
Phytochemical Analysis ◽  
Membrane Stabilization ◽  
Standard Drug ◽  
Anti Inflammatory

 Objectives: A persistent and chronic inflammation may act as an underlying definition for many of the long-term illness such as diabetic foot ulcer, Alzheimer’s disease and rheumatoid arthritis. Folklore medicinal plants provide immense health benefits with new remedies. Active compounds from plants containing alkaloids and phenolic compounds (flavonoids and tannins) possess antioxidant and anti-inflammatory activity. The leaves of Adhatoda vasica are most known for its effectiveness in treating respiratory diseases such as asthma, chronic bronchitis, and other respiratory conditions. In this report, we investigated the possible action of A. vasica against inflammation.Methods: Solvents with varying polarity (Hexane, dichloromethane, ethyl acetate, and methanol) were used for the sequential extraction of leaves of A. vasica Linn (Family: Acanthaceae). The anti‐inflammatory activity was assessed using simple in vitro methods. Phenols, flavonoids, phytosterols, saponins, alkaloids, and tannins were analyzed qualitatively using standard protocols. Anti‐inflammatory activity was evaluated using albumin denaturation assay, membrane stabilization assay and proteinase inhibitory activity. Aspirin (diclofenac) was used as a standard drug for the study of anti-inflammatory activity.Results: Our results substantiated that methanolic extract of A. vasica gave a maximum yield of 12.5% and apparently all bioactive phytochemical constituents were at a higher concentration in the methanolic extract. Methanolic extract of A. vasica showed a significant inhibition of the heat-induced albumin denaturation, red blood cells membrane stabilization, and proteinase inhibitory effects with 86±1.46, 88±1.24, and 96±0.93% for 1000 μg/ml, respectively.Conclusion: The above results delineate that the bioactive components were extracted using high polar solvent are mostly flavonoids and related polyphenols. These compounds may be the active constituents to render the anti-inflammatory activity to A. vasica.

scholarly journals Anti-inflammatory activity of leaves of Jatropha gossypifolia L. by hrbc membrane stabilization method

2013 ◽  
Vol 2 (2) ◽  
pp. 156-158 ◽  
Author(s):  
Yerramsetty Nagaharika ◽  
Valluri kalyani ◽  
Shaik Rasheed ◽  
Ramadosskarthikeyan
Keyword(s):  
Inflammatory Activity ◽  
Stabilization Method ◽  
Membrane Stabilization ◽  
Jatropha Gossypifolia ◽  
Anti Inflammatory

Synthesis, Anti-Arthritic, and Anti-Inflammatory Activity of N-Tosyl aza Cyclophanes

2012 ◽  
Vol 65 (2) ◽  
pp. 186 ◽  
Author(s):  
Perumal Rajakumar ◽  
Ramar Padmanabhan
Keyword(s):  
Bovine Serum Albumin ◽  
Serum Albumin ◽  
Blood Cells ◽  
Bovine Serum ◽  
Protein Denaturation ◽  
Inflammatory Activity ◽  
Stabilization Method ◽  
Membrane Stabilization ◽  
Human Red Blood Cells ◽  
Anti Inflammatory

The synthesis of novel N-tosyl tetraaza cyclophanes and N-tosyl diaza cyclophane incorporating m-terphenyl as spacer units is described. Anti-arthritic activity was studied by inhibition of the protein denaturation method (bovine serum albumin). All the N-tosyl aza cyclophanes exhibit excellent anti-arthritic activity. Anti-inflammatory activity of the synthesized cyclophanes was investigated using the human red blood cells (HRBC) membrane stabilization method and some of the N-tosyl aza cyclophanes exhibited good anti-inflammatory activity.

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