Antioxidant Activity of DLω-Phenyl-Amino Acid Octyl Esters with Anti-inflammatory Activity

2011 ◽  
Vol 51 (06) ◽  
pp. 485-488
Author(s):  
Christos Kontogiorgis ◽  
Dimitra Hadjipavlou-Litina ◽  
Elisabeth Schulz
Keyword(s):  
Antioxidant Activity ◽  
Amino Acid ◽  
Inflammatory Activity ◽  
Anti Inflammatory

Design and Synthesis of Novel Anti-inflammatory/Anti-ulcer Hybrid Molecules with Antioxidant Activity

2020 ◽  
Vol 16 ◽  
Author(s):  
Bhim Bahadur Chaudhari ◽  
Alka Bali ◽  
Ajitesh Balaini
Keyword(s):  
Antioxidant Activity ◽  
Oral Absorption ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Antioxidant Potential ◽  
Inflammatory Activity ◽  
In Vivo Models ◽  
Standard Drug ◽  
Hybrid Molecules ◽  
Anti Inflammatory

Background: NSAIDs are the most widely prescribed medications worldwide for their anti-inflammatory, antipyretic, and analgesic effects However, their chronic use can lead to several adverse drug events including GI toxicity. The selective COX-2 inhibitors developed as gastro-sparing NSAIDs also suffer from serious adverse effects which limit their efficacy. Objective: Local generation of reactive oxygen species is implicated in NSAID-mediated gastric ulceration and their combination with H2 antagonists like famotidine reduces the risk of ulcers. The objective of this work was to design and synthesize novel methanesulphonamido isoxazole derivatives by hybridizing the structural features of NSAIDs with those of antiulcer drugs (ranitidine, famotidine, etc.) to utilize a dual combination of anti-inflammatory activity and reducing (antioxidant) potential. Method: The designing process utilized three dimensional similarity studies and utilized an isoxazole core having a potential for anti-inflammatory as well as radical scavenging antioxidant activity. The compounds were assayed for their antiinflammatory activity in established in vivo models. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. Results: Compounds (5, 6, 9 and 10) showed anti-inflammatory activity comparable to the standard drugs and were also found to be non-ulcerogenic at the test doses. Compounds 6-10 exhibited good antioxidant effect in the concentration range of 1.0-50.0 µmol/ml. The test compounds were also found to comply with the Lipinski rule suggesting good oral absorption. Conclusion: A new series of isoxazole based compounds is being reported with good anti-inflammatory activity coupled with antioxidant potential as gastro-sparing anti-inflammatory agents.

Identification of phytoconstituents of Tragia involucrata leaf extracts and evaluate their correlation with anti-inflammatory & antioxidant properties

2021 ◽  
Vol 20 ◽  
Author(s):  
Vinodhini Velu ◽  
Swagata Banerjee ◽  
Vidya Rajendran ◽  
Gaurav Gupta ◽  
Dinesh Kumar Chellappan ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Petroleum Ether ◽  
Ethyl Acetate Extract ◽  
Petroleum Ether Extract ◽  
Inflammatory Activity ◽  
Ether Extract ◽  
Membrane Stabilization ◽  
Leaf Extracts ◽  
Anti Inflammatory

Aims: The present investigation was aimed at exploring the phytoconstituents using Gas Chromatography Mass Spectroscopy and to evaluate antioxidant and anti-inflammatory properties of the leaf extracts. Materials and Methods: The extracts were obtained sequentially with petroleum ether, ethyl acetate and water using soxhlet apparatus. The anti-inflammatory property of the identified compounds using GC- MS spectroscopy was evaluated in silico. The antioxidant activity was performed by DPPH and H2O2 method whereas anti-inflammatory study was carried out by HRBC membrane stabilization method. Terpenoids were found to be major constituents in petroleum ether extract while, phenols and flavonoids were predominantly found in ethyl acetate extract. Results and Discussion: The GC-MS analysis of the extract revealed six major molecules including Squalene, 19β, 28- epoxyleanan-3-ol and 2-tu-Butyl-5-chloromethyl-3-methyl-4-oxoimidazolidine-1-carboxylic acid. The ethyl acetate extract showed a significant antioxidant activity (P<0.01) in both DPPH method (70.87 %) and H2O2 method (73.58%) at 200 µg mL-1 . Increased membrane stabilization of petroleum ether extract was observed in the in vitro anti-inflammatory activity study. A strong relationship between the terpenoid content and anti-inflammatory activity was obtained from the correlation (0.971) and docking study. Conclusion: These results justify T. involucrata to be a rich source of terpenoids with potent antiinflammatory property.

scholarly journals SYNTHESIS, ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITIES OF ETHYL 2-(2-CYANO-3- (SUBSTITUTED PHENYL)ACRYLAMIDO)-4,5-DIMETHYLTHIOPHENE-3-CARBOXYLATES

2017 ◽  
Vol 10 (7) ◽  
pp. 95 ◽  
Author(s):  
Madhavi K ◽  
Sree Ramya G
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Antioxidant Properties ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

Objective: Objective of the study was to synthesize and evaluate a series of novel compounds, ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)- 4,5-dimethylthiophene-3-carboxylates, for in vitro antioxidant and in vivo anti-inflammatory activities.Methods: Ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylates were synthesized by knoevenagel condensation of active methylene group of ethyl 2-(2-cyanoacetamido)-4,5-dimethylthiophene-3-carboxylate with substituted benzaldehydes. The synthesized compounds were evaluated for their in vitro antioxidant properties in three different models, viz., reduction of 1,1-diphenyl-2-pycrylhydrazyl free radical, scavenging of nitric oxide free radical, and ferric ion-induced lipid peroxidation using rat brain homogenate. Few selected compounds with good antioxidant properties were pharmacologically evaluated for anti-inflammatory activity by carrageenan-induced rat paw edema model.Results: Clean and efficient synthetic procedure was used for the preparation of series of compounds. The structures of synthesized compounds were confirmed by infrared, 1H nuclear magnetic resonance and mass spectra. The antioxidant activity data revealed that the compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant activity. Hence, the active compounds were evaluated for anti-inflammatory activity and found to possess good activity. The percentage inhibition of rat paw edema obtained for the evaluated compounds was in the range of 70.2-83.1, comparable to the standard drug diclofenac (85.0%).Conclusion: The use of inexpensive, eco-friendly and readily available reagents, easy work-up and high purity of products makes the procedure a convenient and robust method for the synthesis of title compounds. The compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5- dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant and anti-inflammatory activities.

scholarly journals Anti-inflammatory activity of Jefea gnaphalioides (a. gray), Astereaceae

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Axel Villagómez-Rodríguez ◽  
Julia Pérez-Ramos ◽  
Ana Laura Esquivel-Campos ◽  
Cuauhtémoc Pérez-González ◽  
Claudia Angélica Soto-Peredo ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Inflammatory Activity ◽  
Total Phenolic ◽  
Oral Toxicity ◽  
Alternative Source ◽  
Ear Edema ◽  
Tnf Α ◽  
Dpph Method ◽  
Anti Inflammatory ◽  
Commercial Kits

Abstract Background Inflammation is a symptom associated with many diseases. This symptom is treated with steroidal and non-steroidal anti-inflammatory drugs, which can cause severe side effects when used as long-term treatments. Natural products are an alternative source of new compounds with anti-inflammatory activity. Jefea gnaphalioides (Astereaceae) (A. Gray) is a plant species used to treat inflammatory problems, in Mexico. This study determined the anti-inflammatory activity and the composition of the methanol extract of Jefea gnaphalioides (MEJG). Methods The extract was obtained by heating the plant in methanol at boiling point for 4 h, and then the solvent was evaporated under vacuum (MEJG). The derivatization of the extract was performed using Bis-(trimethylsilyl) trifluoroacetamide, and the composition was determined by GC-MS. Total Phenols and flavonoids were determined by Folin-Ciocalteu AlCl3 reaction respectively. The antioxidant activity of MEJG was determined by DPPH method. The acute and chronic anti-inflammatory effects were evaluated on a mouse ear edema induced with 12-O-Tetradecanoylphorbol-13-acetate (TPA). Acute oral toxicity was tested in mice at doses of MEJG of 5000, 2500 and 1250 mg/kg. The levels of NO, TNF-α, IL-1β and IL-6 were determinate in J774A.1 macrophages stimulated by Lipopolysaccharide. The production of inflammatory interleukins was measured using commercial kits, and nitric oxide was measured by the Griess reaction. Results The anti-inflammatory activity of MEJG in acute TPA-induced ear edema was 80.7 ± 2.8%. This result was similar to the value obtained with indomethacin (IND) at the same dose (74.3 ± 2.8%). In chronic TPA-induced edema at doses of 200 mg/kg, the inhibition was 45.7%, which was similar to that obtained with IND (47.4%). MEJG have not toxic effects even at a dose of 5000 mg/kg. MEJG at 25, 50, 100 and 200 μg/mL decreased NO, TNF-α, IL-1β and IL-6 production in macrophages stimulated with LPS. The major compounds in MEJG were α-D-Glucopyranose (6.71%), Palmitic acid (5.59%), D-(+)-Trehalose (11.91%), Quininic acid (4.29%) and Aucubin (1.17%). Total phenolic content was 57.01 mg GAE/g and total flavonoid content was 35.26 mg QE/g MEJG had antioxidant activity. Conclusions MEJG has anti-inflammatory activity.

scholarly journals In Vitro Antioxidant Activity of Crude Extracts of Harpagophytum Zeyheri and Their Anti-Inflammatory and Cytotoxicity Activity Compared With Diclofenac.

2021 ◽  
Author(s):  
Sibonokuhle F. Ncube ◽  
Lyndy J. McGaw ◽  
Emmanuel Mfotie Njoya ◽  
Hilton G.T. Ndagurwa ◽  
Peter J. Mundy ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Inflammatory Activity ◽  
In Vitro Assays ◽  
Cytotoxicity Activity ◽  
Tnf Α ◽  
Low Toxicity ◽  
Anti Inflammatory ◽  
Ethyl Acetate Extracts

Abstract Background This study evaluated the in vitro antioxidant activity and comparison of anti-inflammatory and cytotoxic activity of Harpagopytum zeyheri with diclofenac. Methods In vitro assays were conducted using water, ethanol and ethyl acetate extracts of H.zeyheri. The antioxidant activity was evaluated using the 2,2'-diphenyl-1-picrylhydrazy (DPPH) and 2,2'- azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS)assays. The anti-inflammatory activity was determined by measuring the inhibition of nitric oxide (NO) on lipopolysaccharide (LPS)-induced RAW 264.7 mouse macrophages as well as cytokine (TNF-α and IL-10) expression on LPS-induced U937 human macrophages. For cytotoxicity, cell viability was determined using the 3-(4, 5-dimethylthiazol- 2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Results The ethyl acetate extract had the lowest IC50 values in the DPPH (5.91µg/ml) and ABTS (20.5µg/ml) assay compared to other extracts. Furthermore, the ethyl acetate extracts effectively inhibited NO and TNF-α and proved to be comparable to diclofenac at some concentrations. All extracts of H. zeyheri displayed dose dependent activity and were associated with low levels of human-IL-10 expression compared to quercetin. Furthermore, all extracts displayed low toxicity relative to diclofenac. Conclusions These findings show that H. zeyheri has significant antioxidant activity. Additionally, similarities exist in inflammatory activity of H. zeyheri to diclofenac at some concentrations as well as low toxicity in comparison to diclofenac.

scholarly journals Antibacterial, Anti-inflammatory and Antioxidant Potential of Ethanol Extract of Ipomoea staphylina Roem. & Schult

2021 ◽  
pp. 97-106
Author(s):  
G. Kokila ◽  
P. Jeevan
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Medicinal Plant ◽  
Ethanol Extract ◽  
Inflammatory Activity ◽  
Diffusion Method ◽  
Drug Candidate ◽  
Dependent Manner ◽  
Human Beings ◽  
Anti Inflammatory

In the present study we evaluate the antibacterial, anti-inflammatory and antioxidant activity of medicinal plant Ipomoea staphylina Roem & Schult. Many bacteria are harmful to human beings and animals. Theses bacteria make diseases the host organisms. Many antibiotics are available in the marker for the treatment of bacterial diseases. However, antibiotics cause unwanted side effect. Thus, the study focused to evaluate ethanol extract of Ipomoea staphylina against bacterial pathogens. Antibacterial activity was evaluated by the method of well diffusion method. Antiinflamatory and antioxidant activity was evaluated by in vitro study method. Ethanol extract of Ipomoea staphylina showed antibacterial activity against different bacteria isolated from chicken at dose depended manner ie., higher dose of plant extract possessed maximum inhibition zone (21.67 ± 1.45 mm) (P<0.05) against selected bacteria. Moreover, plant ethanol extract possessed anti-inflammatory activity and antioxidant activity at dose dependent manner (P<0.05). Higher dose (100 μg/ml) of ethanol extract of Ipomoea staphylina showed maximum anti-inflammatory activity (68.38 %) and antioxidant activity (72%). From this result it is concluded that the medicinal plant Ipomoea staphylina Roem. & Schult. possessed antibacterial, anti-inflammatory and antioxidant activity. Further detailed study will be conducted for the new drug candidate discovery.

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