scholarly journals Anti-Inflammatory Effects of 3-Formyl, 7-Flavonols Derivatives by Microwave Enhanced Chemistry Assisted - Vilsmeier Haack Synthesis

2019 ◽  
Vol 12 (04) ◽  
pp. 1779-1791
Author(s):  
M. Karpakavalli ◽  
A.Y. Sangilimuthu ◽  
A.Usha Raja Nanthini ◽  
G.Nagaraja Perumal ◽  
S. Mohan ◽  
...  
Keyword(s):  
Protein Denaturation ◽  
Population Increase ◽  
Spectral Studies ◽  
Dimethyl Formamide ◽  
Mass Spectral ◽  
Paw Oedema ◽  
Rf Values ◽  
Anti Inflammatory

In the modern medicines the novel and active molecules are essential to act against various diseases and increase the needs day by day due to population increase. In view of that, we attempt to make a variety of synthetic molecules against inflammation by a new and popular greener microwave assisted and faster method such as Microwave Enhanced Chemistry assisted Vilsmeier Haack Synthesis (MEC-VHS). In this paper, we report the synthesis of nitro- dinitro- and acetyl- derivatives of 3- formyl, 7-flavonols using MEC-VHS techniques against inflammation as anti-inflammatory agent. These derivatives were synthesized via pinkish formylation complex of dimethyl formamide and phosphorous oxychloride by microwave irradiation resulted as suspension by base. The re-crystallized products were characterized through Co-TLC, λmax, IR, HPTLC, 1HNMR, CHN analysis and mass spectral studies. The HPTLC finger print profiles obtained were of with a prominent single peak and with a matching Rf values compared to that obtained by an ordinary Co-TLC technique. All the synthesized compounds were screened for their anti-inflammatory activity by in vitro protein denaturation method and in vivo carrageenan induced paw oedema method and it was found that all the compounds excepting the un-substituted 3-formyl, 7-flavonols gave an equi- or more potent activity as compared to that of the standard.

scholarly journals Anti-inflammatory properties of Dirinaria consimilis extracts in albino rats

2018 ◽  
Vol 4 (1) ◽  
pp. 3-8 ◽  
Author(s):  
Vinay Bharadwaj Tatipamula ◽  
Girija Sastry Vedula
Keyword(s):  
Protein Denaturation ◽  
Chloroform Extract ◽  
Acetone Extract ◽  
Albino Rats ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

BackgroundEarlier, the lichens are used in traditional medicines by different cultures across the world. As the Dirinaria genus has been shown to be biologically active against inflammation in folklore, we assessed the in vitro and in vivo anti-inflammatory profile of Dirinaria consimilis.Material and methodsInitially, the hydroalcoholic extract of lichen, D. consimilis (Dc-HE) was prepared and re-extracted with n-hexane, chloroform, ethyl acetate, acetone and methanol. The resultant extracts were evaluated for their in vitro (protein denaturation method), acute toxicity and in vivo (formalin-induced rat paw oedema assay) anti-inflammatory studies.ResultsAmong all the tested extracts, the acetone and chloroform extract of D. consimilis depicted prominent anti-inflammatory activity in both the bioassays. The acetone extract inhibited protein denaturation with IC50 value of about 468 µg/mL while the standard (Indomethacin) with 120 µg/mL. Moreover, the Dc-HE was screened for acute toxicity studies in male albino rats up to 2000 mg/Kg b.w dosage. The in vivo anti-inflammatory analysis of acetone extract (200 mg/mL) showed potent reduction of rat paw oedema nearer to that of the standard, whereas chloroform extract depicted moderate depletion and the other extracts revealed mild inhibitory profile against inflammation.ConclusionThis study reveals that the lichen, D. consimilis might be a good source of anti-inflammatory agents.

Fibrinolytic, Anti-Inflammatory and Cytotoxic Potentialities of Extracts and Chemical Constituents of Manglicolous Lichen, Graphis ajarekarii Patw. & C. R. Kulk

2020 ◽  
Vol 10 (1) ◽  
pp. 87-93 ◽  
Author(s):  
Vinay Bharadwaj Tatipamula ◽  
Girija Sastry Vedula
Keyword(s):  
Protein Denaturation ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Fibrin Clot ◽  
Hydroalcoholic Extract ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Background: Lichens which are betide to mangroves are termed as Manglicolous Lichens (ML). As these ML are habituated under stress conditions, they are screened for unique metabolites and biological activities. Objective: The study aimed to establish the chemical and biological profile of ML, Graphis ajarekarii. Methods: The Ethyl Acetate Extract of G. ajarekarii (EAE) was subjected to chromatographic techniques and the obtained isolates were characterized by spectroscopic analysis. The hydroalcoholic extract of G. ajarekarii (AE), EAE, isolates and Hydroalcoholic Extract of host (HE) were evaluated for fibrinolytic (fibrin clot method), in vitro (protein denaturation method) and in vivo (formalin-induced rat paw oedema assay), anti-inflammatory and cytotoxicity (MTT assay) activities. Results: Chemical investigation of the EAE led to the isolation of two known compounds namely atranorin (1) and ribenone (2), which were confirmed by spectral data. The AE and EAE gradually lysed the fibrin clot with 94.54 and 65.07%, respectively, at 24 h. The AE inhibited protein denaturation of about 88.06%, while the standard (Indomethacin) with 93.62%. Similarly, the in vivo antiinflammatory analysis of AE (200 mg/mL) showed potent reduction of rat paw oedema than the standard, whereas EAE and 1 depicted moderate depletion. In addition, the AE revealed prominence inhibition on MCF-7, DU145 and K-562 with IC50 values of 69.5, 42.5 and 38 µg/mL, respectively, whereas the HE exhibited mild inhibitory profile against fibrin clot, inflammation and cancer. Conclusion: From the results, it can be concluded that the G. ajarekarii has an aptitude to act against coagulation, inflammation and cancer cells.

scholarly journals In Vitro Anti-Inflammatory and In Vivo Antiarthritic Activities of Aqueous and Ethanolic Extracts of Dissotis thollonii Cogn. (Melastomataceae) in Rats

2019 ◽  
Vol 2019 ◽  
pp. 1-17 ◽  
Author(s):  
Stephanie Flore Djuichou Nguemnang ◽  
Eric Gonzal Tsafack ◽  
Marius Mbiantcha ◽  
Ateufack Gilbert ◽  
Albert Donatien Atsamo ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Protein Denaturation ◽  
Inflammatory Diseases ◽  
Ros Production ◽  
Zymosan A ◽  
Ethanolic Extracts ◽  
Anti Inflammatory ◽  
Promising Source

Dissotis thollonii Cogn. (Melastomataceae) is a tropical plant widely used in traditional Cameroonian medicine to relieve and treat many pathologies. It is widespread in the western region where it is used to treat typhoid fever, gastrointestinal disorders, and inflammatory diseases. The purpose of this study is to scientifically demonstrate the anti-inflammatory and antiarthritic properties of the aqueous and ethanolic extracts of the leaves of Dissotis thollonii. The anti-inflammatory properties were evaluated in vitro by inhibition tests for cyclooxygenase, 5-lipoxygenase, protein denaturation, extracellular ROS production, and cell proliferation; while antiarthritic properties were evaluated in vivo in rats using the zymosan A-induced monoarthritis test and the CFA-induced polyarthritis model. This study shows that aqueous and ethanolic extracts at a concentration of 1000 μg/ml inhibit the activity of cyclooxygenase (47.07% and 63.36%) and 5-lipoxygenase (66.79% and 77.7%) and protein denaturation (42.51% and 44.44%). Similarly, both extracts inhibited extracellular ROS production (IC50 = 5.74 μg/ml and 2.96 μg/ml for polymorphonuclear leukocytes, 7.47 μg/ml and 3.28 μg ml for peritoneal macrophages of mouse) and cell proliferation (IC50 = 16.89 μg/ml and 3.29 μg/ml). At a dose of 500 mg/kg, aqueous and ethanolic extracts significantly reduce edema induced by zymosan A (69.30% and 81.80%) and CFA (71.85% and 79.03%). At the same dose, both extracts decreased sensitivity to mechanical hyperalgesia with 69.00% and 70.35% inhibition, respectively. Systemic and histological analyzes show that both extracts maintain the studied parameters very close to normal and greatly restored the normal architecture of the joint in animals. Dissotis thollonii would therefore be a very promising source for the treatment of inflammatory diseases.

scholarly journals New oxadiazole derivatives of isonicotinohydrazide in the search for antimicrobial agents: Synthesis and in vitro evaluation

2012 ◽  
Vol 77 (1) ◽  
pp. 9-16 ◽  
Author(s):  
Manav Malhotra ◽  
Mohit Sanduja ◽  
Abdul Samad ◽  
Aakash Deep
Keyword(s):  
Antimicrobial Agents ◽  
Fungal Strain ◽  
Spectral Studies ◽  
Dilution Method ◽  
Mass Spectral ◽  
Oxadiazole Derivatives ◽  
Derivatives Of ◽  
And Staphylococcus Aureus

Structural modification of the front line antitubercular drug isoniazid provide a lipophilic adaptations of the drug in which hydrazide moiety of isoniazid is replaced by 1,3,4-oxadiazole heterocycles to eliminate in-vivo acetylation by arylamine N-acetyltransferase which results to form inactive acetylated drug. In the present study a series of sixteen oxadiazole derivatives were synthesized and characterized by (IR, 1H NMR, 13C NMR and Mass spectral) studies. All the synthesized compounds were evaluated for their antimicrobial activity by broth dilution method against two Gram positive strains (Bacillus subtilis and Staphylococcus aureus), two Gram negative strains (Pseudomonas aeruginosa and Escherichia coli) and fungal strain (Candida albicans and Aspergillus niger). The minimum inhibitory concentration of the compounds was in the range of 1.56-50 ?g ml-1 against bacterial and fungal strain. The results revealed that all synthesized compounds have a significant biological activity against the tested microorganisms. Among the synthesized derivatives 4g, 4h, 4m and 4p were found to be most effective antimicrobial compounds.

scholarly journals In vitro anti-inflammatory, antioxidant and qualitative phytochemical evaluation of the Phytexponent preparation of selected plants

2020 ◽  
Author(s):  
Gervason Moriasi ◽  
Elias Nelson ◽  
Epaphrodite Twahirwa
Keyword(s):  
Oxidative Stress ◽  
Protein Denaturation ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Scientific Data ◽  
Etiologic Factor ◽  
Phytochemical Screening ◽  
Anti Inflammatory

Abstract Oxidative stress is a critical etiologic factor and driver of inflammatory responses, witnessed in chronic and persistent conditions. The current anti-oxidative stress and anti-inflammatory drugs are associated with detrimental effects, high dependence, high costs, inaccessibility, among other drawbacks; therefore, a need for alternatives is imperative. Despite the remarkable potential of medicinal plants, there are scanty empirical studies on their pharmacologic efficacy. The Phytexponent is an alcoholic polyherbal preparation of Allium sativum, Triticum repens, Echinacea purpurea, Viola tricolor and Matricaria chamomilla. In complementary medicine, the Phytexponent is used to boost immunity, to treat inflammatory disorders, oxidative stress, blood pressure, diabetes, stress/depression, among other conditions. However, there is no sufficient scientific data to support these healing claims. Therefore, in the current study evaluated the in vitro anti-inflammatory, antioxidant activities and qualitative phytochemical composition of the Phytexponent. The in vitro anti-inflammatory activities were evaluated using the inhibition of protein denaturation and the human erythrocyte (HRBC) membrane stabilization techniques. Antioxidant activities were evaluated by the 1,1-diphenyl-picryl-1-hydrazyl (DPPH) radical scavenging-, the hydroxyl radical scavenging- and catalase activities. Qualitative phytochemical screening was performed using standard procedures. The results showed a significantly higher percentage inhibition of heat-induced- and hypotonicity induced HRBC hemolysis by the Phytexponent at concentrations of 50 % and 100 %, compared with the percentage inhibitions of etanercept (p<0.05). No significant differences in percentage inhibitions of protein denaturation were observed among concentrations of 12.5 %,25.0 %,50.0 %,100.0 % of the Phytexponent and etanercept (25 mg/ml) (p˃0.05). Furthermore, the Phytexponent demonstrated high antioxidant activities against the DPPH- (IC50=0.00733%) and the hydroxyl- (IC50 = 0.716 %) radicals in vitro.The Phytexponent recorded significantly higher catalase activities at concentrations of 1 % and 0.1 % than those recorded by ascorbic acid at similar concentrations. Qualitative phytochemical screening revealed the presence of phenols, flavonoids, tannins, among other antioxidant associated phytochemicals. The bioactivities of the Phytexponent reported herein, were attributed to the presence of these phytochemicals. Further studies to establish specific mode(s) through which the Phytexponent exerts in vitro anti-inflammatory and antioxidant effects are encouraged. Moreover, in vivo anti-inflammatory and antioxidant activities should be done to determine the replicability of these findings in vivo. Bioassay-guided isolation of compounds responsible for the reported bioactivities herein should be done.

Synthesis of novel thiadiazole derivatives as selective COX-2 inhibitors

MedChemComm ◽  
2016 ◽  
Vol 7 (12) ◽  
pp. 2309-2327 ◽  
Author(s):  
Fatma A. Ragab ◽  
Helmi I. Heiba ◽  
Marwa G. El-Gazzar ◽  
Sahar M. Abou-Seri ◽  
Walaa A. El-Sabbagh ◽  
...  
Keyword(s):  
Paw Oedema ◽  
Analgesic Agents ◽  
Thiadiazole Derivatives ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Cox 2 Inhibitors ◽  
Rat Paw Oedema

A novel series of thiadiazole derivatives were designed and synthesized for evaluation as selective COX-2 inhibitors in vitro and were investigated in vivo as anti-inflammatory and analgesic agents against carrageenan-induced rat paw oedema model in irradiated rats.

The acute anti-inflammatory action of xylopic acid isolated from Xylopia aethiopica

2018 ◽  
Vol 29 (6) ◽  
pp. 659-669 ◽  
Author(s):  
Newman Osafo ◽  
David D. Obiri ◽  
Aaron O. Antwi ◽  
Oduro K. Yeboah
Keyword(s):  
Acute Inflammation ◽  
Protein Denaturation ◽  
Prostaglandin E ◽  
Paw Oedema ◽  
Dependent Inhibition ◽  
Dried Fruit ◽  
Anti Inflammatory ◽  
Xylopia Aethiopica ◽  
Inflammatory Action

AbstractBackgroundOur earlier studies had given evidence of the traditional application ofXylopia aethiopicain the management of inflammation. The principal constituent obtained from its bio-fractionation is xylopic acid. It is a crystalline diterpene that belongs to the class of kauranes. This work sets out to investigate the anti-inflammatory potential of the xylopic acid isolated from the dried fruit ofX. aethiopica.MethodsA preliminary anti-inflammatory study, using the protein denaturation model, andin vivoanti-inflammatory assay were employed in the investigation of acute inflammation. The modulation of the effect of the pro-inflammatory markers histamine, serotonin, bradykinin, and prostaglandin E2by xylopic acid was investigated byin vivomice paw oedema models.ResultsXylopic acid showed a concentration-dependent inhibition of albumen denaturation with an IC50of 15.55 μg mL−1. Xylopic acid (10, 30, 100 mg kg−1) inhibited the maximal oedema and the average paw thickness (oedema) over the period of each study considerably for all phlogistic agents employed (i.e. carrageenan, histamine, serotonin, bradykinin, and prostaglandin E2) in the inflammation induction for both prophylactic and therapeutic protocols.ConclusionThis study establishes that xylopic acid has anti-inflammatory action in acute inflammation.

scholarly journals In vitro anti-inflammatory, antioxidant and qualitative phytochemical evaluation of the Phytexponent preparation of selected plants

2020 ◽  
Author(s):  
Gervason Moriasi ◽  
Elias Nelson ◽  
Epaphrodite Twahirwa
Keyword(s):  
Oxidative Stress ◽  
Protein Denaturation ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Scientific Data ◽  
Etiologic Factor ◽  
Phytochemical Screening ◽  
Anti Inflammatory

Abstract Oxidative stress is a critical etiologic factor and driver of inflammatory responses, witnessed in chronic and persistent conditions. The current anti-oxidative stress and anti-inflammatory drugs are associated with detrimental effects, high dependence, high costs, inaccessibility, among other drawbacks; therefore, a need for alternatives is imperative. Despite the remarkable potential of medicinal plants, there are scanty empirical studies on their pharmacologic efficacy. The Phytexponent is an alcoholic polyherbal preparation of Allium sativum, Triticum repens, Echinacea purpurea, Viola tricolor and Matricaria chamomilla. In complementary medicine, the Phytexponent is used to boost immunity, to treat inflammatory disorders, oxidative stress, blood pressure, diabetes, stress/depression, among other conditions. However, there is no sufficient scientific data to support these healing claims. Therefore, in the current study evaluated the in vitro anti-inflammatory, antioxidant activities and qualitative phytochemical composition of the Phytexponent. The in vitro anti-inflammatory activities were evaluated using the inhibition of protein denaturation and the human erythrocyte (HRBC) membrane stabilization techniques. Antioxidant activities were evaluated by the 1,1-diphenyl-picryl-1-hydrazyl (DPPH) radical scavenging-, the hydroxyl radical scavenging- and catalase activities. Qualitative phytochemical screening was performed using standard procedures. The results showed a significantly higher percentage inhibition of heat-induced- and hypotonicity induced HRBC hemolysis by the Phytexponent at concentrations of 50 % and 100 %, compared with the percentage inhibitions of etanercept (p<0.05). No significant differences in percentage inhibitions of protein denaturation were observed among concentrations of 12.5 %,25.0 %,50.0 %,100.0 % of the Phytexponent and etanercept (25 mg/ml) (p˃0.05). Furthermore, the Phytexponent demonstrated high antioxidant activities against the DPPH- (IC50=0.00733%) and the hydroxyl- (IC50 = 0.716 %) radicals in vitro.The Phytexponent recorded significantly higher catalase activities at concentrations of 1 % and 0.1 % than those recorded by ascorbic acid at similar concentrations. Qualitative phytochemical screening revealed the presence of phenols, flavonoids, tannins, among other antioxidant associated phytochemicals. The bioactivities of the Phytexponent reported herein, were attributed to the presence of these phytochemicals. Further studies to establish specific mode(s) through which the Phytexponent exerts in vitro anti-inflammatory and antioxidant effects are encouraged. Moreover, in vivo anti-inflammatory and antioxidant activities should be done to determine the replicability of these findings in vivo. Bioassay-guided isolation of compounds responsible for the reported bioactivities herein should be done.

Appraisal of Anti-Arthritic and Anti-Inflammatory Potential of Folkloric Medicinal Plant Peganum Harmala

2021 ◽  
Vol 21 ◽  
Author(s):  
Muhammad Furqan Akhtar ◽  
Syed Ahmad Raza ◽  
Ammara Saleem ◽  
Irfan Hamid ◽  
Mirza Muhammad Faran Ashraf Baig ◽  
...  
Keyword(s):  
Plant Extract ◽  
Protein Denaturation ◽  
In Vitro Assays ◽  
Peganum Harmala ◽  
Reactive Protein ◽  
Inflammatory Conditions ◽  
Anti Inflammatory ◽  
Dpph Scavenging

Background: Peganum harmala is traditionally used to manage rheumatoid arthritis (RA) and other inflammatory conditions. However, its use against RA has not been scientifically evaluated. The current study was designed to assess the anti-arthritic and anti-inflammatory activities of the methanolic extract of P. harmala leaves by in vitro and in vivo methods. Methods: The in vitro assays were carried out to determine the effect of plant extract on inhibition of egg albumin denaturation and human red blood cell membrane (HRBC) stabilization. Moreover, 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity was performed to determine the antioxidant potential. In vivo anti-arthritic activity was performed by determining the curative effect against Complete Freund’s adjuvant (0.1 ml). The plant extract was administered to rats orally at 200, 400 and 600 mg/kg/day for 21 days. Results: The values of IC50 of plant extract in protein denaturation, stabilization of HRBC and DPPH assays were 77.54 mg/ml, 23.90 mg/ml and 58.09 µg/ml respectively. Moreover, the plant extract significantly attenuated the poly-arthritis and weight loss, anemia and paw edema. The plant extract restored the level of C-reactive protein, rheumatoid factor, alanine transaminase, aspartate transaminase and alkaline phosphatase in poly-arthritic rats. Moreover, the plant extract restored the immune organs weight in treated rats. Treatment with P. harmala also significantly subdued the oxidative stress by reinstating superoxide dismutase, reduced glutathione, catalase and malondialdehyde in poly-arthritic rats. The plant extract notably restored the prostaglandin-E2 and tumor necrosis factor (TNF)-α in the serum of poly-arthritic rats. Conclusion: It was concluded that P. harmala extract had potential antioxidant, anti-inflammatory and antiarthritic activities which primarily might be attributed to alkaloids, flavonoids and phenols.

Formulation, Optimization, in Vitro and in Vivo Investigation of Ketoprofen - Fumaric Acid Co-crystal for the Solubility Enhancement of Ketoprofen

2021 ◽  
Author(s):  
Meenakshi Bhatia ◽  
Ashwani Kumar ◽  
Vikas Verma ◽  
Snehlata Yadav ◽  
SUNITA DEVI
Keyword(s):  
Fumaric Acid ◽  
Protein Denaturation ◽  
Research Work ◽  
Molar Ratio ◽  
Scanning Calorimetry ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Analgesic Activities

Abstract The present piece of research work is framed as improving the solubility of ketoprofen by forming co-crystal using fumaric acid as a coformer. Co-crystal of ketoprofen and fumaric acid were prepared by simple solvent assisted grinding. The independent variables i.e. drug and coformer were mixed in 1:1 molar ratio and dependent variables were assumed to be solubility and % drug release. Differential scanning calorimetry, fourier transform infrared spectroscopy, X-ray diffraction, nuclear magnetic resonance and scanning electron microscopy techniques were used to characterize the preparation of optimized batch of co-crystal and further, evaluated for in-vitro and in-vivo anti-inflammatory and analgesic activities. Based on results of solubility and dissolution rate studies the drug showed 4-5 fold improvement in both the properties on co-crystallisation. The values of Gibbs free energy are negative at all levels of carrier demonstrating spontaneity of drug solubilization process. The IC50 value of optimized batch of co-crystal formulation and pure drug was observed as 327.33 µg/ml and 556.11 µg/ml, respectively, demonstrating that co-crystal formulation possesses more percentage protection against protein denaturation than the drug ketoprofen. In-vivo (anti-inflammatory and analgesic) activities revealed that optimized batch of co-crystal formulation delivered a rapid pharmacological response in wistar rats and albino mice when compared with standard drug.

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