Anti-inflammatory effects of Centella asiatica ethanolic extracts towards indomethacin-induced gastric ulcer model in rats by altering COX-2 expression

Asiatic acid (AA), a pentacyclic triterpene compound in the medicinal plantCentella asiatica, was evaluated for antinociceptive and anti-inflammatory effects. Treatment of male ICR mice with AA significantly inhibited the numbers of acetic acid-induced writhing responses and the formalin-induced pain in the late phase. In the anti-inflammatory test, AA decreased the paw edema at the 4th and 5th h afterλ-carrageenan (Carr) administration and increased the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) in the liver tissue. AA decreased the nitric oxide (NO), tumor necrosis factor-α(TNF-α), and interleukin-1β(IL-1β) levels on serum level at the 5th h after Carr injection. Western blotting revealed that AA decreased Carr-induced inducible nitric oxide synthase (iNOS), cyclooxygenase (COX-2), and nuclear factor-κB (NF-κB) expressions at the 5th h in the edema paw. An intraperitoneal (i.p.) injection treatment with AA also diminished neutrophil infiltration into sites of inflammation as did indomethacin (Indo). The anti-inflammatory mechanisms of AA might be related to the decrease in the level of MDA, iNOS, COX-2, and NF-κB in the edema paw via increasing the activities of CAT, SOD, and GPx in the liver.

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Efficacy of a chitosan-curcumin mixture in treating indomethacin-induced acute gastric ulcer in rats

Current Pharmaceutical Biotechnology ◽

10.2174/1389201022666210127115427 ◽

2021 ◽

Vol 22 ◽

Author(s):

Sineenat Kuadkaew ◽

Suwipa Ungphaiboon ◽

Narubodee Phdoongsombut ◽

Sireewan Kaewsuwan ◽

Sirima Mahattanadul

Keyword(s):

Gastric Ulcer ◽

Gastric Mucus ◽

Ulcer Index ◽

Antiulcer Agent ◽

Alternative Agent ◽

Anti Oxidant ◽

Potential Alternative ◽

Cox 2 ◽

Anti Inflammatory ◽

Cox 1

Background: Curcumin is claimed as a potent protectant against gastric ulcer (GU) induced by strong necrotizing agents including NSAIDs through its antioxidant, anti-inflammatory and gastroprotective activities. However, it was found to exert opposite effects to either delay ulcer healing or exacerbate ulcer inflammation through some curative mechanisms differently modified by curcumin dosage. Its ability in inhibiting the expression of COX-2 may also delay the healing of NSAIDs-induced GU. Recently, a topical chitosan-curcumin solution has been found to be a safe and potential alternative agent in treating oral ulcer. Therefore, an oral chitosan-curcumin mixture was developed and determined for its efficacy in treating NSAIDs-induced GU in rat. Methods: A chitosan (150 mg)-curcumin (20 mg) mixture with optimal gastric pH was developed. Indomethacin (30 mg/kg) was given orally to the rat and test preparations were administered orally at 5 h later and then every 24 h for two consecutive days. The sum of all gastric ulcerated areas (mm2) for each stomach was used as ulcer index. Gastric pro-inflammatory mediators and cytoprotective factors were determined. Results: An oral administration of a chitosan-curcumin mixture exerted a superior efficacy than curcumin, chitosan or lansoprazole (a standard antiulcer agent) in healing indomethacin-induced GU. It was revealed that the mixture exhibited the highest anti-oxidant, anti-inflammatory and gastric mucus producing activities including the high potency in down-regulating pro-inflammatory COX-2 and iNOS expression but up-regulating cytoprotective COX-1, nNOS and eNOS expression. Conclusion: The present findings indicated the benefit of a chitosan-curcumin mixture as a potential alternative agent in treating NSAIDs-induced gastric ulcer.

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Discovery of a COX-2 selective inhibitor hit with anti-inflammatory activity and gastric ulcer protective effect

Future Medicinal Chemistry ◽

10.4155/fmc-2017-0115 ◽

2017 ◽

Vol 9 (16) ◽

pp. 1899-1912 ◽

Cited By ~ 7

Author(s):

Mohamed A Abdelgawad ◽

Rania B Bakr ◽

Ahmed O El-Gendy ◽

Gehan M Kamel ◽

Amany A Azouz ◽

...

Keyword(s):

Gastric Ulcer ◽

Protective Effect ◽

Selective Inhibitor ◽

Inflammatory Activity ◽

Cox 2 ◽

Anti Inflammatory

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Anti-inflammatory effects of ethanolic extracts from Micromeria species

Planta Medica ◽

10.1055/s-0030-1264885 ◽

2010 ◽

Vol 76 (12) ◽

Author(s):

M Bival Tefan ◽

D Jelic ◽

S Vladimir-Kneevic ◽

M Trzun ◽

K Frka Boric ◽

...

Keyword(s):

Ethanolic Extracts ◽

Anti Inflammatory

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Comparative antiulcer effect of curcumin and tetrahydrocurcumin in a gastric ulcer model system

Planta Medica ◽

10.1055/s-0033-1351972 ◽

2013 ◽

Vol 79 (13) ◽

Author(s):

S Mahattanadul ◽

S Nima ◽

S Tewtrakul ◽

P Tansakul

Keyword(s):

Gastric Ulcer ◽

Model System ◽

Ulcer Model

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Faculty Opinions recommendation of Anti-inflammatory activity of monogalactosyldiacylglycerol in human articular cartilage in vitro: activation of an anti-inflammatory cyclooxygenase-2 (COX-2) pathway.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.13272062.14628172 ◽

2011 ◽

Author(s):

Johanne Martel-Pelletier ◽

Hassan Fahmi

Keyword(s):

Articular Cartilage ◽

Cyclooxygenase 2 ◽

Inflammatory Activity ◽

Human Articular Cartilage ◽

In Vitro Activation ◽

Cox 2 ◽

Anti Inflammatory

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Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

Letters in Organic Chemistry ◽

10.2174/1570178617999201106113114 ◽

2020 ◽

Vol 17 ◽

Author(s):

Deepak Kumar Singh ◽

Mayank Kulshreshtha ◽

Yogesh Kumar ◽

Pooja A Chawla ◽

Akash Ved ◽

...

Keyword(s):

Molecular Docking ◽

Biological Activities ◽

Inflammatory Activity ◽

Standard Drug ◽

Docking Score ◽

Chemical Structures ◽

Cox 2 ◽

Anti Inflammatory ◽

Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

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