Crataegus orientalis Leaves and Berries: Phenolic Profiles, Antioxidant and Anti-inflammatory Activity

The present study was designed to define the phenolic content, antioxidant and anti-inflammatory activity of Crateagus orientalis Pall. ex M. Bieb., traditionally used by local people in southern parts of F.Y.R. Macedonia. The presence and content of 7 phenolics in ethanolic extracts of leaves and berries were studied using HPLC-DAD, where the most dominant compounds were hyperoside, isoquercitrin and chlorogenic acid. The leaf extract was more effective as a DPPH radical scavenger (IC50 = 29.7 μg/g) than the berry extract, as well as in the relative reducing power on Fe3+. Anti-inflammatory potential was studied by means of cyclooxygenase-1 (COX-1) and 12-lipoxygenase (12-LOX) inhibitory activity; both extracts evinced activity. Furthermore, C. orientalis leaf extract showed a concentration dependent inhibition of COX-1 pathway products 12-HHT and TXB2, reaching IC50 values below the lowest applied concentration (68.9% and 55.2% of 12-HHT and TXB2 production inhibition, respectively, at concentration of 0.4 mg/mL). Although inhibitors such as acetylsalicylic acid and quercetin showed higher activity, this study demonstrates that the investigated extracts are potential anti-inflammatory agents.

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Armillariella mellea Shows Anti-inflammatory Activity by Inhibiting the Expression of NO, iNOS, COX-2 and Cytokines in THP-1 Cells

The American Journal of Chinese Medicine ◽

10.1142/s0192415x07005028 ◽

2007 ◽

Vol 35 (03) ◽

pp. 507-516 ◽

Cited By ~ 18

Author(s):

Shu-Jing Wu ◽

Jenn-Yi Tsai ◽

Min-Nan Lai ◽

Lean-Teik Ng

Keyword(s):

Nitric Oxide ◽

Inflammatory Activity ◽

Medicinal Fungus ◽

Cyclooxygenase 1 ◽

Dependent Inhibition ◽

Cox 2 ◽

Anti Inflammatory ◽

Armillariella Mellea ◽

Oxide Synthase ◽

Cox 1

Armillariella mellea (AM), also known as Mi-Huan-Ku, a popular medicinal fungus used in the traditional Chinese medicine for treating headache, neurasthenia and insomnia. In the present study, our aim was to determine the effects of aqueous (AAM) and ethanol (EAM) extracts of A. mellea on lipopolysaccharide (LPS)-induced inflammatory response by measuring the inducible nitric oxide synthase (iNOS), cyclooxygenase-1 and -2 (COX-1 and COX-2) protein expression, cytokines (TNF-α, IL-4 and IL-8) formation, nitric oxide (NO) release and prostaglandin (PGE2) production in human monocytic (THP-1) cells. At concentration of 100 μg/ml, EAM, but not AAM, effectively protected against LPS-induced cell death in THP-1 cells. At concentrations of 10~100 μg/ml, EAM showed a potent anti-inflammatory activity as demonstrated by a dose-dependent inhibition of LPS (1 μg/ml)-induced release of NO and PGE2, and significantly decreased the transcription of proinflammatory cytokines. EAM at 100 μg/ml significantly blocked the LPS induction of iNOS and COX-2 expression, but not COX-1. Therefore, the protective effect of EAM against LPS-induced inflammatory mediators release could explain, at least in part, its effectiveness in alleviating certain inflammatory related diseases.

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ANTI-INFLAMMATORY ACTIVITY OF BACTERIA ASSOCIATED WITH MARINE SPONGE (HALICLONA AMBOINENSIS) VIA REDUCTING NO PRODUCTION AND INHIBITING CYCLOOXYGENASE-1, CYCLOOXYGENASE-2, AND SECRETORY PHOSPHOLIPASE A2 ACTIVITIES

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i11.20094 ◽

2017 ◽

Vol 10 (11) ◽

pp. 95 ◽

Cited By ~ 1

Author(s):

Yosie Andriani ◽

Leni Marlina ◽

Habsah Mohamad ◽

Hermansyah Amir ◽

Siti Aisha M Radzi ◽

...

Keyword(s):

Methanol Extract ◽

Inflammatory Activity ◽

No Production ◽

Secretory Phospholipase A2 ◽

Phytochemical Screening ◽

Spla2 Activity ◽

Cyclooxygenase 1 ◽

Cox 2 ◽

Anti Inflammatory ◽

Cox 1

Objective: This study aimed to investigate the anti-inflammatory activity of methanol extract and fractions of bacteria associated with sponge (Haliclona amboinensis) and to evaluate their effect in reducing NO production and inhibiting cyclooxygenase-1 (COX-1), cyclooxgenase-2 (COX-2) and secretory phospholipase A2 (sPLA2) activity.Methods: All bacterial isolates were cultured and supernatants were collected for the extraction of secondary metabolites using diaion HP-20 to obtain methanol extracts. Evaluation of cytotoxicity property was carried out on macrophage cell lines (RAW264.7) by 3-(4,5-dimethylthiazol- 2-yl) 2,5-diphenyl tetrazoliumbromide assay. Anti-inflammatory screening was done by inducible nitric oxide assay on RAW264.7 cell lines with lipopolysaccharide (LPS) stimulation. Dianion HP-20 was used to remove salt content. A selected methanol extract was subjected to further fractionations by C-18 reverse phase and their anti-inflammatory potential was evaluated by COX-1 and COX-2, and sPLA2 enzymatic assay.Results: Seven methanol extracts showed no cytotoxic property against RAW 264.7 cell line (inhibitory concentration 50% > 30 μg/ml) and selected for anti-inflammatory screening assay. Result showed methanol extract HM 1.2 reduced NO production >80% and it has been selected for phytochemical screening, further fractionations and assay. Phytochemical screening showed alkaloids and terpenoids present in the HM 1.2. The HM 1.2 and its fractions (F1, F2, F1C1, F1C2, F1C3, and F1C4) were proven to inhibit COX-1, COX-2, and sPLA2 activity in the range of 60.516-116.886%, 20.554- 116.457%, and 70.2667-114.8148%, respectively.Conclusions: This study revealed that bacteria associated with H. amboinensis have produced anti-inflammatory activity via reducing NO production and inhibiting COX-1, COX-2, and sPLA2 activity.

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Differential inhibition of cyclooxygenase-1 (COX-1) and-2 (COX-2) by NSAIDS: Consequences on anti-inflammatory activity versus gastric and renal safety

Inflammopharmacology ◽

10.1007/bf02735560 ◽

1996 ◽

Vol 4 (1) ◽

pp. 61-70 ◽

Cited By ~ 6

Author(s):

M. Pairet ◽

L. Churchill ◽

G. Trummlitz ◽

G. Engelhardt

Keyword(s):

Inflammatory Activity ◽

Differential Inhibition ◽

Cyclooxygenase 1 ◽

Cox 2 ◽

Anti Inflammatory ◽

Cox 1 ◽

Renal Safety

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Differential Inhibition of Cyclooxygenase-1 (COX-1) and -2 (COX-2) by NSAIDs: Consequences on Anti-Inflammatory Activity Versus Gastric and Renal Safety

Side Effects of Anti-Inflammatory Drugs IV ◽

10.1007/978-94-011-5394-2_23 ◽

1997 ◽

pp. 223-232

Author(s):

M. Pairet ◽

L. Churchill ◽

G. Trummlitz ◽

G. Engelhardt

Keyword(s):

Inflammatory Activity ◽

Differential Inhibition ◽

Cyclooxygenase 1 ◽

Cox 2 ◽

Anti Inflammatory ◽

Cox 1 ◽

Renal Safety

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

Medicinal Chemistry ◽

10.2174/1573406416666200930114340 ◽

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.

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Anti-inflammatory activity of leaf extract and fractions of Bursera simaruba (L.) Sarg (Burseraceae)

Journal of Ethnopharmacology ◽

10.1016/j.jep.2004.02.009 ◽

2004 ◽

Vol 92 (1) ◽

pp. 129-133 ◽

Cited By ~ 13

Author(s):

B. Noguera ◽

E. Dı́az ◽

M.V. Garcı́a ◽

A.San Feliciano ◽

J.L. López-Perez ◽

...

Keyword(s):

Leaf Extract ◽

Inflammatory Activity ◽

Bursera Simaruba ◽

Anti Inflammatory

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Anti-Inflammatory Activity of Populus deltoides Leaf Extract via Modulating NF-κB and p38/JNK Pathways

International Journal of Molecular Sciences ◽

10.3390/ijms19123746 ◽

2018 ◽

Vol 19 (12) ◽

pp. 3746 ◽

Cited By ~ 5

Author(s):

Ye Jeong ◽

Mi-Young Lee

Keyword(s):

Nitric Oxide ◽

Protein Kinase ◽

Leaf Extract ◽

Populus Deltoides ◽

Nuclear Translocation ◽

Mapk Signaling ◽

Mitogen Activated Protein Kinase ◽

Inflammatory Activity ◽

No Production ◽

Anti Inflammatory

Populus deltoides, known as eastern cottonwood, has been commonly used as a medicinal plant. The aim of the present study was to investigate the mechanism underlying the anti-inflammatory activity of P. deltoides leaf extract (PLE). PLE effectively inhibited the expression of inducible nitric oxide synthase (iNOS) and nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, but not that of cyclooxygenase-2 (COX-2) and prostaglandin E2. Proinflammatory tumor necrosis factor alpha (TNF-α) levels were also reduced by the extract. PLE inhibited the phosphorylation of nuclear factor-kappa B (NF-κB) and inhibitor of Kappa Bα (IκBα), and blunted LPS-triggered enhanced nuclear translocation of NF-κB p65. In mitogen-activated protein kinase (MAPK) signaling, PLE effectively decreased the phosphorylation of p38 and c-Jun N-terminal protein kinase (JNK), but not of extracellular signal-regulated kinase 1/2 (ERK1/2). Taken together, these results suggest that anti-inflammatory activity of P. deltoides leaf extract might be driven by iNOS and NO inhibition mediated by modulation of the NF-κB and p38/JNK signaling pathways.

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