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.

scholarly journals DETERMINATION OF BIOLOGICAL ACTIVITIES OF THREE MARINE ALGAE COLLECTED FROM VISAKHAPATNAM COAST

2017 ◽  
Vol 10 (12) ◽  
pp. 274 ◽  
Author(s):  
Satya Lakshmi S
Keyword(s):  
Antioxidant Activity ◽  
Marine Algae ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Inflammatory Activity ◽  
Diffusion Method ◽  
Dpph Method ◽  
Anti Inflammatory

  Objective: Determination of biological activities of marine algae collected from the Visakhapatnam coastal region.Methods: Antibacterial activity of algal extracts determined by the well diffusion method, antioxidant activity was determined by reducing power (RP) method and 1, 1-diphenyl-2-picryl-hydrazil (DPPH) radical scavenging method finally anti-inflammatory activity was determined by human red blood cell stabilization method and egg albumin method.Results: Methanolic extracts of three algae have potential inhibition activity against Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, and Staphylococcus aureus. Green alga Enteromorpha compressa has better antioxidant activity compared to the Gracilaria arcuata and Ulva fasciata when tested in RP and DPPH method. U. fasciata found good anti-inflammatory activity among the selected three algae.Conclusion: The three tested algae exhibited significant antibacterial and antioxidant activity compared to anti-inflammatory activity. These bioactive compounds containing macroalgae may find their commercial potential in medicine, food, and cosmetic industry

scholarly journals Anti-Inflammatory and Antioxidant Activities of Cordia Dichotoma Forst

2020 ◽  
Vol 13 (4) ◽  
pp. 2093-2099
Author(s):  
Nazim Hussain ◽  
Bibhuti Bhushan Kakoti ◽  
Mithun Rudrapal ◽  
Zubaidur Rahman ◽  
Mokinur Rahman ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Dpph Radical ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Dpph Radical Scavenging ◽  
Radical Scavenging Assay

Cordia dichotoma Forst.has been used in the management of pain and inflammations in traditional medicine. However, the anti-inflammatory activity of the methanolic extract of C. dichotoma(MECD) bark has not been reported so far. This work was, therefore, aimed at investigating the anti-inflammatory activity of C. dichotomabark extract. The antioxidant activity was evaluated to justify the anti-inflammatory action of MECD on the basis of its radical scavenging property. The extract of C. dichotomawas obtained by Soxhlation of bark powder using methanol as solvent. The anti-inflammatory activity was determined by the carrageenan induced paw edemamodel in ratsat two different dose levels, viz., 250 and 500 mg/kg. The antioxidant activity was evaluated using DPPH radical scavenging assay. The antioxidant activity was performed in vitro by DPPH radical scavenging assay using ascorbic acid as the standard drug. In anti-inflammatory activity, maximum inhibition of edema was observed after 4 hours of experimental period. At lower test dose (250 mg/kg b.w.), the percentage inhibition of paw edema was 29.7 %, while 48.6 % inhibition of edema was observed at higher dose (500 mg/kgb.w.). The percentage inhibition of paw edema was significant relative to the control group. The standard indomethacin group also exhibited sufficiently high level of anti-inflammatory effect with 56% inhibition of paw edema at 5 mg/kg dose. In in vitroantioxidant activity, the MECD exhibited good DPPHradical scavenging activity with the IC50 vale of 62.46 µg/ml, whereas the standard drug, ascorbic acid showed comparatively more antioxidant activity with IC50 of 27.66 µg/ml.However, our study scientifically validates the folkloric claim as well as traditional uses of C. dichotomaas anti-inflammatory medication. It is suggested that the anti-inflammatory activity of C. dichotomamay be due to the antioxidant potential of phenolic phytoconstituents or plant flavonoids present in the methanolic bark extract.

Synthesis and Evaluation of Substituted Aryl Thiazoles With Antioxidant Potential as Gastro-sparing Anti-inflammatory Agents

2020 ◽  
Vol 17 (12) ◽  
pp. 1566-1578
Author(s):  
Akhil Bansal ◽  
Alka Bali ◽  
Ajitesh Balaini
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Reducing Power ◽  
Structural Features ◽  
Inflammatory Activity ◽  
Standard Group ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Background: NSAIDs are used as first-line drugs for the treatment of various inflammatory disorders. Chronic use of NSAIDs is known to be associated with gastrointestinal and renal toxicity. Local generation of reactive oxygen species finally resulting in cellular apoptosis is one of the accepted mechanisms for NSAID-induced toxicity. Objective: The objective of the present study was to design and synthesize a series of 2-methane sulfonamido substituted arylthiazole derivatives by including structural features of combined antiulcer and anti-inflammatory activity utilizing as the structural core, thiazole nucleus with potential for antioxidant effect. Methods: Compounds were designed based on three dimensional and field similarity studies. The synthesized compounds were evaluated for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Rofecoxib and indomethacin were taken as standard drugs for comparison. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. Results: The compounds 6 and 7 showed good anti-inflammatory activity comparable to the standard group and were also non ulcerogenic at the test doses. Compounds 1-7 displayed varying degrees of reducing power in the PFRAP) assay and the methanesulphonamido derivatives 4-7 showed the highest antioxidant activity (EC50 values 3.7-5.1 μmol/ml vs ascorbic acid 7.4 μmol/ml). Theoretical ADME profiling of the compounds based on selected physicochemical properties showed excellent compliance with Lipinski’s rule. Conclusion: A series of compounds have been designed and synthesized having dual antioxidant and anti-inflammatory activity with activities comparable to standard drugs.

EVALUATION OF SALVIA LANATA LEAF EXTRACT FOR ANTI-INFLAMMATORY AND ANTIOXIDANT ACTIVITY

2020 ◽  
pp. 113-117
Author(s):  
LIPI NOGAI ◽  
TIRATH KUMAR ◽  
PANKAJ LOHUMI
Keyword(s):  
Nitric Oxide ◽  
Antioxidant Activity ◽  
Free Radical ◽  
Leaf Extract ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Free Radical Scavenging ◽  
Paw Edema ◽  
Standard Drug ◽  
Anti Inflammatory

Objective: The work is aimed to evaluate the anti-inflammatory and antioxidant activity of the ethanolic leaf extract of Salvia lanata. Methods: Anti-inflammatory activity of the leaf extract of S. lanata at a dose of 100 mg/kg and 200 mg/kg against the standard drug indomethacin at a dose of 10 mg/kg i.p. was evaluated by carrageenan-induced rat paw edema and protein denaturation method. Antioxidant activity was determined by 1, 1 diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging method, reducing power method, and nitric oxide scavenging assay. Results: S. lanata leaf extract showed highly significant dose-dependent efficacy against carrageenan-induced paw edema at a dose of 200 mg/kg and lesser effect at 100 mg/kg. It inhibited heat-induced albumin denaturation with a maximum inhibition of 79.26% at 160 μg/ml. DPPH free radical scavenging activity of extract exhibited inhibition of 25.96%–87.74% within the concentration range of 10 μg/ml–160 μg/ml, nitric oxide assay from 12.26% to 79.22% in the same concentration range. In reducing power assay with an increase in concentrations, an increase in the absorbance of the reaction mixture was observed. Antioxidant activity was compared to standard drug ascorbic acid. Conclusion: The leaf extract of S. lanata has potent anti-inflammatory and antioxidant activity.

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 Antioxidant and Potentially Anti-Inflammatory Activity of Anthocyanin Fractions from Pomace Obtained from Enzymatically Treated Raspberries

Antioxidants ◽  
2019 ◽  
Vol 8 (8) ◽  
pp. 299 ◽  
Author(s):  
Urszula Szymanowska ◽  
Barbara Baraniak
Keyword(s):  
Antioxidant Activity ◽  
Phenolic Compounds ◽  
Solid Phase ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Phase Extraction ◽  
Scavenging Activity ◽  
Hplc Technique ◽  
Anti Inflammatory

Raspberry pomace was obtained from raspberries subjected to enzymatic maceration using three commercial pectinolytic preparations (Pectinex Ultra SP-L, Pectinex Yield Mash, and Ultrazym AFP-L). Phenolic compounds were extracted and anthocyanin fractions were isolated using the SPE solid phase extraction technique. In the separated anthocyanin fractions, the content of individual compounds was determined by the HPLC technique and the antioxidant activity was assessed with four complementary methods (DPPH and ABTS radical scavenging activity, chelating Fe(II) power, and ferric reducing power). Potential anti-inflammatory properties were also identified as the ability to inhibit the activity of lipoxygenase and cyclooxygenase 2. For these enzymes, the type of inhibition was determined based on the Lineweaver–Burke plot.

scholarly journals Evaluation of Ethnopharmacological and Antioxidant Potential ofZanthoxylum armatumDC.

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Rabia Kanwal ◽  
Muhammad Arshad ◽  
Yamin Bibi ◽  
Saira Asif ◽  
Sunbal Khalil Chaudhari
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Antioxidant Potential ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Zanthoxylum Armatum

Zanthoxylum armatumDC. (syn.Z. alatumRoxb.) is an important medicinal plant commonly called Timur or Indian prickly ash. The ethnopharmacological study ofZ. armatumrevealed the use of different plant parts for curing various ailments including cholera, chest infection, fever, indigestion, stomach disorders, gas problems, piles, toothache, gum problems, dyspepsia, as carminative, antipyretic, aromatic, tonic, and stomachic. Keeping in view the medicinal potential of the plant, the antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, reducing power, and phosphomolybdate assay using different concentrations (7.81 μg/mL–250 μg/mL). Ascorbic acid was taken as standard. The results indicated that the free radical scavenging activity ranged from 40.12% to 78.39%, and the reductive potential ranged from 0.265 nm to 1.411 nm while the total antioxidant activity ranged from 0.124 nm to 0.183 nm. The antioxidant potential evaluated by three assays increased in a concentration dependent manner and ascorbic acid showed better antioxidant activity than leaf extract. Results obtained through different tests confirmed redox protective activities ofZanthoxylum armatum. Further in vitro and in vivo research should be performed, so this plant can be further utilized in drug development.

scholarly journals EVALUATION OF ETHANOLIC ROOT EXTRACT OF PARTHENIUM HYSTEROPHORUS LINN FOR ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITY

2017 ◽  
pp. 194-197 ◽  
Author(s):  
Pankaj Lohumi ◽  
Tirath Kumar ◽  
Lipi Nogai
Keyword(s):  
Nitric Oxide ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Parthenium Hysterophorus ◽  
Inflammatory Activity ◽  
Root Extract ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Soxhlet Apparatus ◽  
Anti Inflammatory

Objective: The work is aimed to draw out the health beneficial properties of a weed (Parthenium hysterophorus Linn). The present work is organized to evaluate the antioxidant and anti-inflammatory activity of the ethanolic root extract of Parthenium hysterophorus Linn.Methods: In the present work the ethanolic extract was determined by using soxhlet apparatus. The antioxidant scavenging activity of this extract was determined by applying three different assay methods: (1) DPPH (1, 1-diphenyl-2-picryl hydrazyl) free radical method. (2) Nitric oxide scavenging assay and (3) Reducing power method. The anti-inflammatory activity was determined by in vivo method i.e. Carrageenan induced rat paw edema.Results: DPPH radical scavenging activities of the standard antioxidant and extracts were found to be increased in dose dependent manner. The percentage inhibition increases from 4.19% to 97.09% within the concentration range of 10µg/ml to 160µg/ml. Parthenium hysterophorus Linn effectively reduced the generation of nitric oxide radicals from sodium nitroprusside solution in a concentration dependent manner and percentage inhibition increases from 3.53% to 55.21% within the concentration range 10µg/ml to 160µg/ml. All the concentrations of extract significantly showed higher absorbance than the absorbance of control reaction (0.9705) in reducing power assay. A Higher absorbance indicates high reducing power due to the formation of reduced intermediates. Parthenium hysterophorus Linn showed highly significant anti-inflammatory activity at a dose of 200 mg/kg and the lesser effect was observed at 100 mg/kg with the percentage change in paw volume at 0 min, 30 min, 60 min, 90 min and 120 min.Conclusion: Thus, from above experimental observations, it can be stated that Parthenium is a natural antioxidant and bearing anti-inflammatory activity. 

scholarly journals Anti-inflammatory and Antioxidant Potential of Hyaluronic Acid Mediated Zinc Nanoparticles

2020 ◽  
pp. 33-37
Author(s):  
N. Akash ◽  
Lakshminarayanan Arivarasu ◽  
S. Rajeshkumar
Keyword(s):  
Antioxidant Activity ◽  
Zinc Oxide ◽  
Hyaluronic Acid ◽  
Antioxidant Potential ◽  
Inflammatory Activity ◽  
Therapeutic Drug ◽  
Zinc Nanoparticles ◽  
Zinc Oxide Nanoparticle ◽  
Oxide Nanoparticle ◽  
Anti Inflammatory

Aim: The aim of the study is to interpret the hyaluronic acid mediated with zinc oxide nanoparticle and its anti-inflammatory and antioxidant activity. Introduction: Hyaluronic acid has a role as ‘physiological selector’ for spermatozoa prior to intracy to plasmic sperm injection (icsi). They are mostly seen in the synovial joints and act as a shock absorber. The objective of this study is to analyse the results achievable by the introduction of a routine HA. Hyaluronic acid is an immune neutral polysaccharide that is ubiquitous in the human body, and it is crucial for many cellular and tissue functions. Nanoparticles are the compounds which respond to the applied magnetic fields, magnetic separation labelled cells, therapeutic drug, gene and radionuclide delivery and other biological entities. Materials and Methods: Hyaluronic acid mediated with zno nanoparticles were evaluated for its anti inflammatory activity and antioxidant potential using photometry analysis. Results and Discussion: Zinc nanoparticles shows a higher efficiency of antibacterial activity, but sublethal concentration causes adverse effects and results in increased biofilm formation of V. cholerae Hyaluronic acid mediated zinc oxide nanoparticle show good result in anti inflammatory activity as well as in antioxidant activity. The biosynthesis of the nanoparticle was done by addition of hyaluronic acid with zinc nanoparticles in a scarese amount. This was kept in the orbital shaker, hence they take a long time for the synthesis. The colour change was observed, hence the synthesized nanoparticles proceeded with the anti-inflammatory and antioxidant tests.

scholarly journals ANTIOXIDATIVE AND FREE RADICAL SCAVENGING POTENTIALS OF HABENARIA PECTINATA

2020 ◽  
pp. 68-71
Author(s):  
CHARANJIT KAUR ◽  
RAJESH KUMAR ◽  
GURVINDER SINGH ◽  
CHANDER MOHAN
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Ethyl Acetate ◽  
Methanolic Extract ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Free Radical Scavenging ◽  
Antioxidant Potential ◽  
Flavonoid Content ◽  
Anti Oxidant

Objective: This study was designed to evaluate the antioxidative potential of tubers of Habenaria pectinata. Methods: The tubers of H. pectinata were extracted using hexane, ethyl acetate, methanol, and water as solvents. The anti-oxidant potential of extracts was evaluated using free radical scavenging and reducing power assays. The most active methanolic extract was then fractionated into four fractions using the above-mentioned solvents. Results: The phenol and flavonoid content was found to be maximum in the methanol extracts. All the extracts and fractions showed significant levels of antioxidant activity except hexane extract. Conclusion: The tubers of H. pectinata were found to possess a significant antioxidant potential and can be explored further for isolation and preclinical investigation for the ailment of various diseased states and disorders.

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