scholarly journals Synthesis and Anti-Inflammatory Activity of Some O-Propargylated-N-acetylpyrazole Derived from 1,3-Diarylpropenones

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Ashwani Kumar Dhingra ◽  
Bhawna Chopra ◽  
Rameshwar Dass ◽  
Sanjeev K. Mittal
Keyword(s):  
Acetic Acid ◽  
Glacial Acetic Acid ◽  
Oral Route ◽  
Therapeutic Agents ◽  
Inflammatory Activity ◽  
Spectroscopic Techniques ◽  
Paw Oedema ◽  
Aryl Ketones ◽  
Anti Inflammatory

In search of novel effective potent therapeutic agents delivered by oral route for inflammation treatment, some novel O-propargylated-N-acetylpyrazole analogs (5a–j) were prepared by treating N-acetylpyrazole (4a–j) derived from 1,3-diarylpropenones (3a–j) with propargyl bromide. Claisen-Schmidt condensation of a series of substituted aryl ketones 1 and benzaldehydes 2 in glacial acetic acid afforded 1,3-diarylpropenones which on further treatment with hydrazine hydrate in acetic acid under reflux conditions afforded 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles (4a–j). The products were characterized by using spectroscopic techniques such as IR and NMR. In addition, the in vivo anti-inflammatory activity of the synthesized compounds was determined using the carrageenan-induced paw oedema method in rats.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF CURCUMIN AND CAPSAICIN AUGMENTED IN COMBINATION

2017 ◽  
Vol 9 (6) ◽  
pp. 145
Author(s):  
Thriveni Vasanth Kumar ◽  
Manjunatha H. ◽  
Rajesh Kp
Keyword(s):  
Acetic Acid ◽  
Protective Effect ◽  
Vascular Permeability ◽  
Diclofenac Sodium ◽  
Significant Inhibition ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
The Individual

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.

scholarly journals Synthesis and Prognosis of Anti-inflammatory Activity of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3h)-one

2021 ◽  
Vol 7 (12) ◽  
pp. 25-33
Author(s):  
A. Chiriapkin ◽  
I. Kodonidi ◽  
A. Ivchenko ◽  
L. Smirnova
Keyword(s):  
Acetic Acid ◽  
Biological Activity ◽  
Dimethyl Sulfoxide ◽  
In Silico ◽  
Glacial Acetic Acid ◽  
Inflammatory Activity ◽  
Modified Method ◽  
Anti Inflammatory ◽  
Catalytic Addition ◽  
Derivatives Of

The article presents a modified method for the synthesis of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one and the predict of their anti-inflammatory activity. The proposed method for obtaining tetrahydrothienopyrimidine derivatives is preparatively effective and simple. Their synthesis was carried out by heterocyclization of azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide in the medium of glacial acetic acid with the catalytic addition of dimethyl sulfoxide. Preliminary prognosis of anti-inflammatory activity in silico method allowed us to identify the most promising compounds. Of these, the 4b structure containing a 2-hydroxyphenyl fragment in the second position of pyrimidine-4(3H)-one may be of the greatest interest. It seems appropriate to further study the spectrum of biological activity of the studied compounds.

scholarly journals Biological Evaluation and Docking Analysis of Daturaolone as Potential Cyclooxygenase Inhibitor

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Abdur Rauf ◽  
Francesco Maione ◽  
Ghias Uddin ◽  
Muslim Raza ◽  
Bina S. Siddiqui ◽  
...  
Keyword(s):  
In Silico ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Active Constituent ◽  
Ligand Complex ◽  
Reference Drug ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Dose Dependent

This study deals with the isolation of the active constituent(s) from a methanolic extract ofPistacia integerrimaJ. L. Stewart barks and it was also oriented to evaluate thein vivoandin silicoanti-inflammatory activity. By NMR and crystallography techniques, we have isolated a triterpenoid identified as daturaolone (compound1). This compound showedin vivoa significant and dose dependent (1–30 mg/kg) anti-inflammatory activity on carrageenan-induced mouse paw oedema (ED50= 10.1 mg/kg) and on acetic acid-induced writhing responses in mice (ED50= 13.8 mg/kg). In thein vivoexperiments, the effect of tested compound was also evaluated in presence of the reference drug diclofenac (1–30 mg/kg). Moreover,in silicoanalysis of receptor ligand complex shows that compound1interacts with cyclooxygenases (COXs) binding sites displaying an interesting interaction with COX-1. These findings suggest that compound1isolated fromP.integerrimapossessesin vivoanti-inflammatory and antinociceptive potentials, which are supportedin silicoby an interaction with COXs receptors.

scholarly journals Anti-Inflammatory Activity of Oxycarotenoid Extracts Isolated from Coriander Leaves (Coriandrum Sativum) and Curry Leaves (Murraya koenigii) on Carrageenan Induced Acute Inflammation in Rats

2021 ◽  
Author(s):  
AM ANUSHA ◽  
PA SHERENA ◽  
PT ANNAMALA ◽  
JK Mukkadan
Keyword(s):  
Body Weight ◽  
Coriandrum Sativum ◽  
Leafy Vegetables ◽  
Inflammatory Activity ◽  
Murraya Koenigii ◽  
Curry Leaves ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Coriander Leaves

Introduction: Green leafy vegetables are important sources of polyphenols and carotenoids which possess both antioxidant and anti-inflammatory activities. Aim: To study the anti-inflammatory activity of oxycarotenoid extracts isolated from coriander leaves (Coriandrumsativum) and curry leaves (Murraya koenigii) in carrageenan induced acute paw oedema in rats. Materials and Methods: Oxycarotenoid extracts were isolated from the coriander leaves (Coriandrum sativum) and curry leaves (Murraya koenigii) and they were assessed for anti-inflammatory activities by in-vivo methods. The in-vivo anti-inflammatory activity was evaluated in carrageenan induced acute paw oedema model. Indomethacin at a dose of 20 mg/Kg body weight was used as standard anti-inflammatory drug. Results: The results revealed that oxycarotenoids extracted from coriander leaves administered at a dose of 40 mg/kg body weight showed an inhibition of 53.33% whereas the oxycarotenoids extracted from curry leaves showed an inhibition of 60% at the sixth hour after carrageenan injection. The results are comparable with those of indomethacin (20 mg/Kg body weight) administered group which showed an inhibition of 55.53% Conclusion: These findings suggest that oxycarotenoid extracts isolated from leafy vegetables (coriander leaves and curry leaves) have significant anti-inflammatory activities.

scholarly journals “EVALUATION OF GALPHIMIA GLAUCA STEM METHANOL EXTRACT FRACTIONS FOR ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES”

2019 ◽  
pp. 266-272
Author(s):  
GARIGE BABA SHANKAR RAO ◽  
SRISAILAM K ◽  
V UMA MAHESHWARA RAO ◽  
VASUDHA B
Keyword(s):  
Acetic Acid ◽  
Methanol Extract ◽  
Dose Range ◽  
Experimental Studies ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Methanol Fraction ◽  
Cotton Pellet ◽  
Anti Inflammatory

Objective: This current investigation assesses in vivo central and peripheral analgesic effects and anti-inflammatory properties of fractions obtained from Galphimia glauca (GG) stem methanol extract. Methods: The laboratory models such as Swiss albino mice and Wistar albino rats were employed in the studies. The GG stem methanol extract was subjected to fractionation with solvents such as hexane, chloroform, ethyl acetate, and methanol. Orally, the dose range of 100, 200, and 400 mg/kg was given for 1 day for evaluating analgesic (hotplate test, tail clip test, writhing test, and formalin test) and weekdays for assessing anti-inflammatory activity (carrageenan and cotton pellet test methods), respectively. The experimental studies were further conducted for determining the involvement of central and peripheral receptor actions in the analgesic activity of the extract by prechallenging it with naloxone and acetic acid, respectively. The in vivo anti-inflammatory studies were conducted using carrageenan-induced rat paw edema model and cotton pellet granuloma test. Results: The LD50 of the extract was found to be >2000 mg/kg b.w. The methanol fraction of 400 mg/kg dose exhibited significant (p≤0.001) and dose-dependent analgesic and anti-inflammatory activity. It also exhibited central and peripheral analgesic actions when treated with naloxone and acetic acid, respectively. Conclusion: The results revealed that the stem methanol fraction has more potential in terms of analgesic and anti-inflammatory properties.

scholarly journals Analgesic and Anti-Inflammatory Properties of Extracts from the Bulbils ofDioscorea bulbiferaL. varsativa(Dioscoreaceae) in Mice and Rats

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
M. Mbiantcha ◽  
A. Kamanyi ◽  
R. B. Teponno ◽  
A. L. Tapondjou ◽  
P. Watcho ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Oral Administration ◽  
Inflammatory Mediators ◽  
Methanol Extract ◽  
Inflammatory Activity ◽  
Maximum Effect ◽  
Methanol Extracts ◽  
Paw Oedema ◽  
Dioscorea Bulbifera ◽  
Anti Inflammatory

The aqueous and methanol extracts from the dry bulbils ofDioscorea bulbiferaL. var sativa (Dioscoreaceae)—evaluated orally at the doses of 300 and 600 mg/kg against pain induced by acetic acid, formalin, pressure and against inflammation induced by carrageenan, histamine, serotonin and formalin in mice and rats, showed a dose dependant inhibition of pain and inflammation with a maximum effect of 56.38%, 73.06% and 42.79% produced by the aqueous extract, respectively on pain induced by acetic acid, formalin and pressure while the methanol extract at the same dose respectively inhibited these models of pain by 62.70%, 84.54% and 47.70%. The oral administration of aqueous and methanol extracts caused significant anti-inflammatory activity on paw oedema induced by histamine, serotonin and formalin. The present results show that the bulbils ofDioscorea bulbiferavar sativa possess potent analgesic and anti-inflammatory activities. These activities may results from the inhibition of inflammatory mediators such as histamine, serotonin and prostaglandins. Thus, the analgesic activity of the bulbils ofDioscorea bulbiferamay be at least partially linked to its anti-inflammatory activity.

Synthesis, Anti-inflammatory, Antimicrobial Potential and Molecular Docking Studies of 4,5-Disubstituted-1,2,4-Triazole Thioacetate Derivatives

2019 ◽  
Vol 16 (7) ◽  
pp. 734-745 ◽  
Author(s):  
Muhammad Nouman Arif ◽  
Humaira Nadeem ◽  
Rehan Zafar Paracha ◽  
Arif-ullah Khan ◽  
Muhammad Imran ◽  
...  
Keyword(s):  
Docking Studies ◽  
Inflammatory Activity ◽  
Biological Assessment ◽  
Maximum Effect ◽  
Docking Analysis ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw

Background: In the present study synthesis and biological assessment of nine new ethyl [(4,5-disubstituted- 4H-1,2,4-triazol-3-yl)sulfanyl]acetate derivatives 2(a-i) is performed. Methods: The title compounds were characterized by their analytical and spectral data. All the synthesized compounds were screened for their in vivo anti-inflammatory activity using carrageenaninduced rat paw oedema method and in vitro antimicrobial activity. All the compounds exhibited good anti-inflammatory activity; especially compound 2h produced the maximum effect i.e., 62.5 % comparable to that of standard, diclofenac. The antimicrobial screening results indicated that some of the newly synthesized compounds showed good antibacterial activity, especially against Escherichia coli. Results: All the synthesized thioacetate derivatives of triazoles were also studied for their interactions with the enzymes COX-I and COX-II, two important targets of inflammation pathway, through docking analysis. All the compounds showed good binding affinities with both the enzymes with a maximum value of -8.1 for 2e kcal/mol against COX-I. Conclusion: Docking analysis predicted that our compounds reduce inflammation nonselectively by inhibiting both COX-I and COX-II of inflammatory pathway just like other nonselactive NSAIDS.

scholarly journals Anti-inflammatory activity of methanolic extract of Ficus hispida dried fruit

2021 ◽  
Vol 10 (8) ◽  
pp. 997
Author(s):  
Asif Choudhury ◽  
Deepak Kumar Jha ◽  
U. Rajashekhar
Keyword(s):  
Inflammatory Cytokines ◽  
Methanolic Extract ◽  
Inflammatory Activity ◽  
Bioactive Metabolites ◽  
Paw Oedema ◽  
Tnf Α ◽  
Ficus Hispida ◽  
Anti Inflammatory ◽  
Pro Inflammatory Cytokines

Background: Natural products are a valuable resource of novel bioactive metabolites and these products exist in which the anti-inflammatory activity. The present investigation studies the in vivo and in vitro anti-inflammatory activity of methanolic extract of Ficus hispida in rat’s model.Methods: Plant material was extracted with methanol in a Soxhlet extraction apparatus. Indomethacin was used as a standard drug here, which is a known potent inhibitor of PG synthesis. The carrageenin and histamine induced paw oedema were selected to represent models of acute inflammations. The test compounds and standard drugs were administered orally. After 60 minutes paw oedema was induced by giving 0.1 ml of 1% Carrageenan and 0.1 % histamine by sub-plantar administration. Paw volume-Plethysmometer by mercury displacement method, before and after 1 hr to 4 hours of carrageenan and histamine administration. Performed MTT-based cytotoxicity assay of the Ficus hispida on the RAW264.7 cell line to determine the IC50 and calculate the pro-inflammatory cytokines viz, IL-6, IL-1β and TNF-α and compared to the LPS control.Results: The result obtained from the in-vivo study shows that the Ficus hispida has significant anti- inflammatory activity in a dose dependent manner. This effect is similar to that produced by NSAIDS such as Indomethacin. The concentrations of IL-6, IL-1β and TNF-α, secreted by the cells after challenging with bacterial LPS (2 µg/ml) and subsequent treatment with 50 µg Ficus hispida has been found to reduce the production of all the three pro-inflammatory cytokines viz, IL-6, IL-1β and TNF-α as compared to the LPS control. The activity, in fact, is comparable to the standard NSAID Indomethacin.Conclusions: All these findings and phytoconstituents present in the extract could be the possible chemicals involved in the prevention of inflammations.

scholarly journals Synthesis of some new thiazolo[4,5-b]pyridin-2-ones and research of their anti-inflammatory activity

2019 ◽  
pp. 52-60
Author(s):  
T. I. Chaban
Keyword(s):  
Acetic Acid ◽  
Structural Modification ◽  
Acid Hydrazide ◽  
Inflammatory Activity ◽  
In Vivo Studies ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

In modern theoretical and clinical medicine inflammation problem remains one of the main.Deregulation of inflammatory processes leads to specific pathologies.There is a significant amount of drugs used to treat inflammation. But all of them have varying degrees of ulcerogenic properties. To overcome these limitations search is ongoing throughout the World to find new effective and safe anti-inflammatory agent. Therefore, of course, the synthesis of thiazolidines annelated with the pyridine cycle and the study of their anti-inflammatory properties is an interesting and relevant area. The objective of the present work was to synthesize a series of novel thiazolo[4,5-b]pyridine-2-ones by the structural modification of the (5,7-dimethyl-2-oxo-thiazolo[4,5-b]pyridine-3-yl)-acetic acid hydrazide for further pharmacological screening in vivo as anti-inflammatory activities. The objects of the study were thiazolo[4,5-b]pyridines, obtained by the structural modification of the (5,7-dimethyl-2-oxo-thiazolo[4,5-b]pyridine-3-yl)-acetic acid hydrazide. Anti-inflammatory activity was evaluated using carrageenan induced rat paw edema method in rats In vivo studies were carried out  for anti-inflammatory activity employing the carrageenan-induced rat paw edema method. Anti-inflammatory activity was defined by measuring the paw edema volume 4 h after the carrageenan injection.The NSAID drug Ibuprofen in effective therapeutic doses were tested inparallel as an activity references. Inhibition of the inflammatory response was expressed as a percentage of the paw volume reduction. Studies of anti-inflammatory activity showed that the synthesized compounds had pronounced diuretic properties, and some of them according to activity indicators were approaching or exceeding comparative preparations. The results of the anti-inflammatory activity of the synthesized compounds derivatives (5,7-dimethyl-2-oxo-thiazolo[4,5-b]pyridine-3-yl)-acetic acid hydrazide show the potential for the search for anti-inflammatory agents among thiazolo[4,5-b]pyridine-2-ones.

scholarly journals Leguminous Lectins as Tools for Studying the Role of Sugar Residues in Leukocyte Recruitment

1999 ◽  
Vol 8 (2) ◽  
pp. 107-113 ◽  
Author(s):  
N. M. N. Alencar ◽  
E. H. Teixeira ◽  
A. M. S. Assreuy ◽  
B. S. Cavada ◽  
C. A. Flores ◽  
...  
Keyword(s):  
Specific Binding ◽  
Inflammatory Activity ◽  
Carbohydrate Binding ◽  
Binding Affinities ◽  
Paw Oedema ◽  
Carbohydrate Ligands ◽  
Anti Inflammatory ◽  
Inflammatory Effect

The natural physiological ligands for selectins are oligosaccharides found in glycoprotein or glycolipid molecules in cell membranes. In order to study the role of sugar residues in thein vivolectin anti-inflammatory effect, we tested three leguminous lectins with different carbohydrate binding affinities in the peritonitis and paw oedema models induced by carrageenin in rats.L. sericeuslectin was more anti-inflammatory thanD. virgatalectin, the effects being reversed by their specific binding sugars (N-acetylglucosamine and α-methylmannoside, respectively). However,V. macrocarpa, a galactose-specific lectin, was not anti-inflammatory. The proposed anti-inflammatory activity of lectins could be due to a blockage of neutrophil-selectin carbohydrate ligands. Thus, according to the present data, we suggest an important role forN-acetylglucosamine residue as the major ligand for selectins on rat neutrophil membranes.

Sign in / Sign up

Export Citation Format

Share Document