Anti-inflammatory activity and enhanced COX-2 selectivity of nitric oxide-donating zinc(ii)–NSAID complexes

2016 ◽  
Vol 45 (36) ◽  
pp. 14053-14057 ◽  
Author(s):  
Triloke Ranjan Lakshman ◽  
Jolly Deb ◽  
Tapan Kanti Paine
Keyword(s):  
Nitric Oxide ◽  
Inflammatory Activity ◽  
Cox 2 ◽  
Anti Inflammatory

Zinc(ii)–NSAID complexes of 1,10-phenanthrolinefuroxan release nitric oxide, and exhibit anti-inflammatory activities via selective COX-2 inhibition.

scholarly journals Anti-inflammatory Activity of Constituents Isolated from Terminalia chebula

2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Min Hye Yang ◽  
Zulfiqar Ali ◽  
Ikhlas A. Khan ◽  
Shabana I. Khan
Keyword(s):  
Nitric Oxide ◽  
Cellular Level ◽  
Inflammatory Activity ◽  
No Production ◽  
Terminalia Chebula ◽  
Arjunolic Acid ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Oxide Synthase ◽  
Inducible Nitric Oxide

This study was aimed at the evaluation of the anti-inflammatory activity of twelve compounds isolated from the methanolic extract of fruits of Terminalia chebula. The activity was determined in terms of their ability to inhibit inducible nitric oxide synthase ( iNOS) and cyclooxygenase-2 (COX-2) in LPS-stimulated macrophages. Two gallotannins [chebulinic acid (1) and 2,3,6-tri- O-galloyl-β-D-glucose (2)] and two triterpenoids [arjunic acid (3) and arjunolic acid (4)] efficiently reduced nitric oxide (NO) production with IC50 values of 53.4, 55.2, 48.8, and 38.0 μM, respectively. The protein expressions of iNOS and COX-2 were decreased in macrophages by treatment with compounds 1–4 (54–69% and 33–37%, respectively) at 50 μM. This is the first report of anti-inflammatory property of 1–4 mediated by inhibition of iNOS and COX-2 activities at the cellular level.

scholarly journals Anti-Inflammatory Effect of 1,3,5,7-Tetrahydroxy-8-isoprenylxanthone Isolated from Twigs ofGarcinia esculentaon Stimulated Macrophage

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
Dan-Dan Zhang ◽  
Hong Zhang ◽  
Yuan-zhi Lao ◽  
Rong Wu ◽  
Jin-wen Xu ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inflammatory Diseases ◽  
Inflammatory Activity ◽  
Drug Candidates ◽  
P38mapk Signaling ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Oxide Synthase ◽  
Inducible Nitric Oxide ◽  
Inflammatory Effect

GarciniaLinn. plants having rich natural xanthones and benzophenones with anti-inflammatory activity attracted a great deal of attention to discover and develop them as potential drug candidates. Through screening targeting nitric oxide accumulation in stimulated macrophage, we found that 1,3,5,7-tetrahydroxy-8-isoprenylxanthone (TIE) had potential anti-inflammatory effect. To understand how TIE elicits its anti-inflammatory activity, we uncovered that it significantly inhibits the production of nitric oxide (NO) and prostaglandin E2 (PGE2) in LPS/IFNγ-stimulated RAW264.7 cells. In further study, we showed that TIE reduced the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), two key molecules responsible for the production of NO and PGE2 during inflammation progress. Additionally, TIE also suppressed the expression of inflammatory cytokines IL-6, IL-12, and TNF-α. TIE-led suppression in iNOS, COX-2, and cytokines production were probably the consequence of TIE’s capability to block ERK and p38MAPK signaling pathway. Moreover, TIE blocked activation of nuclear factor-kappa B (NF-κB) as well as NF-κB regulation of miR155 expression. Our study suggests that TIE may represent as a potential therapeutic agent for the treatment of inflammatory diseases.

scholarly journals In Vitro Anti-Inflammatory Activity of Morus alba L. Stem Extract in LPS-Stimulated RAW 264.7 Cells

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Nattaporn Soonthornsit ◽  
Chetsadaporn Pitaksutheepong ◽  
Warinkarn Hemstapat ◽  
Pongsak Utaisincharoen ◽  
Tasana Pitaksuteepong
Keyword(s):  
Nitric Oxide ◽  
Cell Viability ◽  
Morus Alba ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Nitric Oxide Production ◽  
Oxide Production ◽  
Cox 2 ◽  
Anti Inflammatory

Morus alba L., also known as white mulberry or Mhon, has long been used in traditional medicines. This study was aimed to investigate anti-inflammatory activities of mulberry stem ethanolic extract (MSE) in lipopolysaccharide- (LPS-) stimulated RAW 264.7 macrophage cell line. The MSE was first prepared and then investigated for cell viability using the MTT assay. The anti-inflammatory activities were investigated through the inhibition of inducible nitric oxide synthase (iNOS), cyclooxygenase- (COX-) 2 mRNA expression, and iNOS protein expression using reverse transcription-polymerase chain reaction (RT-PCR) assay and immunoblotting analysis, respectively. The inhibition of nitric oxide production of the MSE was also investigated using the Griess reaction assay. The MSE concentration ranging from 10 to 40 µg/ml yielded cell viability higher than 80%. The MSE at concentrations of 20 and 40 µg/ml demonstrated anti-inflammatory activity through the inhibition of nitric oxide production via suppression of both the iNOS mRNA and protein. It was also found to inhibit the expression of COX-2 mRNA in LPS-induced RAW 264.7 cells. This study is the first to report the anti-inflammatory potential of the extract prepared from the stem of mulberry.

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

2007 ◽  
Vol 35 (03) ◽  
pp. 507-516 ◽  
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.

scholarly journals β-Patchoulene, isolated from patchouli oil, suppresses inflammatory mediators in LPS-stimulated RAW264.7 macrophages

2017 ◽  
Vol 15 (2) ◽  
pp. 136-141 ◽  
Author(s):  
Wen-Hao Yang ◽  
Yu-Hong Liu ◽  
Jia-Li Liang ◽  
Zhi-Xiu Lin ◽  
Qiu-Lin Kong ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inflammatory Cytokines ◽  
Messenger Rna ◽  
Inflammatory Activity ◽  
Prostaglandin E ◽  
Mrna Levels ◽  
Dependent Manner ◽  
Raw264.7 Macrophages ◽  
Cox 2 ◽  
Anti Inflammatory

β-Patchoulene (β-PAE) is a tricyclic sesquiterpene isolated from patchouli oil. According to our previous study, β-PAE has anti-inflammatory activity in vivo; however, its anti-inflammatory response still remains unconfirmed in vitro. Therefore, this study is committed to demonstrate the anti-inflammatory effect of β-PAE on lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. According to our results, pre-treatment with β-PAE significantly decreased the protein and messenger RNA (mRNA) levels of pro-inflammatory cytokines including tumor necrosis factor-α (TNF-α), interleukin (IL)-6, and IL-1β while increased the expressions of anti-inflammatory cytokines like IL-10 in a dose-dependent manner. In addition, real-time polymerase chain reaction (PCR) also revealed that β-PAE could interrupt the mRNA expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and thus decreased the levels of nitric oxide (NO) and prostaglandin E2 (PGE2) in LPS-stimulated RAW264.7 macrophages. In conclusion, these results indicated that β-PAE exerted potent anti-inflammatory activity by maintaining the balance between pro- and anti-inflammatory cytokines as well as suppressing iNOS and COX-2 signaling pathways.

scholarly journals Patchoulene Epoxide Isolated from Patchouli Oil Suppresses Acute Inflammation through Inhibition of NF-κB and Downregulation of COX-2/iNOS

2017 ◽  
Vol 2017 ◽  
pp. 1-14 ◽  
Author(s):  
Jia-Li Liang ◽  
Jia-Zhen Wu ◽  
Yu-Hong Liu ◽  
Zhen-Biao Zhang ◽  
Qi-Duan Wu ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Acetic Acid ◽  
Vascular Permeability ◽  
Inflammatory Activity ◽  
Compositional Variation ◽  
Paw Edema ◽  
Unknown Compound ◽  
Ear Edema ◽  
Cox 2 ◽  
Anti Inflammatory

According to the GC-MS analysis, compositional variation was observed between samples of patchouli oil, of which an unknown compound identified as patchoulene epoxide (PAO) was found only in the long-stored oil, whose biological activity still remains unknown. Therefore, the present study aimed to evaluate the potential anti-inflammatory activity with three in vivo inflammatory models: xylene-induced ear edema, acetic acid-induced vascular permeability, and carrageenan-induced paw edema. Further investigation into its underlying mechanism on carrageenan-induced paw edema was conducted. Results demonstrated that PAO significantly inhibited the ear edema induced by xylene, lowered vascular permeability induced by acetic acid and decreased the paw edema induced by carrageenan. Moreover, PAO markedly decreased levels of tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6), prostaglandin E2 (PGE2), and nitric oxide (NO), but increased levels of interleukin-4 (IL-4) and interleukin-10 (IL-10). PAO was also shown to significantly downregulate the protein and mRNA expressions of cyclooxygenase-2 (COX-2) and inducible nitric-oxide synthase (iNOS). Western blot analysis revealed that PAO remarkably inhibited p50 and p65 translocation from the cytosol to the nucleus by suppressing IKKβ and IκBα phosphorylation. In conclusion, PAO exhibited potent anti-inflammatory activity probably by suppressing the activation of iNOS, COX-2 and NF-κB signaling pathways.

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

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.

scholarly journals Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues

2021 ◽  
Vol 89 (2) ◽  
pp. 22
Author(s):  
Mariia Mishchenko ◽  
Sergiy Shtrygol’ ◽  
Andrii Lozynskyi ◽  
Semen Khomyak ◽  
Volodymyr Novikov ◽  
...  
Keyword(s):  
Drug Design ◽  
Anticonvulsant Activity ◽  
Inflammatory Activity ◽  
Significant Protection ◽  
Protection Level ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Target Agent

Neuroinflammation is an integral part of epilepsy pathogenesis and other convulsive conditions, and non-steroidal anti-inflammatory drugs (NSAIDs) present a potent tool for the contemporary search and design of novel anticonvulsants. In the present paper, evaluation of the anticonvulsant activity of the potential NSAID dual COX-2/5-LOX inhibitor darbufelone methanesulfonate using an scPTZ model in mice in dose 100 mg/kg is reported. Darbufelone possesses anticonvulsant properties in the scPTZ model and presents interest for in-depth studies as a possible anticonvulsant multi-target agent with anti-inflammatory activity. The series of 4-thiazolidinone derivatives have been synthesized following the analogue-based drug design and hybrid-pharmacophore approach using a darbufelone matrix. The synthesized derivatives showed a significant protection level for animals in the scPTZ model and are promising compounds for the design of potential anticonvulsants with satisfactory drug-like parameters.

scholarly journals Protective Effect of Membrane-Free Stem Cells against Lipopolysaccharide and Interferon-Gamma-Stimulated Inflammatory Responses in RAW 264.7 Macrophages

2021 ◽  
Vol 22 (13) ◽  
pp. 6894
Author(s):  
Mei Tong He ◽  
Hye Sook Park ◽  
Young Sil Kim ◽  
Ah Young Lee ◽  
Eun Ju Cho
Keyword(s):  
Nitric Oxide ◽  
Stem Cells ◽  
Interferon Gamma ◽  
Mapk Signaling ◽  
Raw 264.7 ◽  
Raw 264.7 Macrophages ◽  
Protein Expressions ◽  
Ifn Γ ◽  
Cox 2 ◽  
Anti Inflammatory

Recently, adipose-derived stem cells (ADSCs) are considered to be ideal for application in cell therapy or tissue regeneration, mainly due to their wide availability and easy access. In this study, we examined the anti-inflammatory effects of membrane-free stem cell extract (MFSC-Ex) derived from ADSCs against lipopolysaccharide (LPS)/interferon-gamma (IFN-γ) on RAW 264.7 macrophage cells. Exposure of RAW macrophages to LPS and IFN-γ stimuli induced high levels of nitric oxide (NO), cyclooxygenase-2 (COX-2), and prostaglandin E2 (PGE2) production. However, pretreatment with MFSC-Ex inhibited LPS/IFN-γ-induced these pro-inflammatory mediators. To clarify the molecular mechanisms underlying the anti-inflammatory property of MFSC-Ex, we analyzed nuclear factor-kappa B (NF-κB) and mitogen-activated protein kinases (MAPKs) protein expressions by Western blotting. Our study showed that treatment of MFSC-Ex significantly down-regulated inducible nitric oxide synthase (iNOS) and COX-2 protein expressions. Furthermore, phosphorylation of extracellular signal-regulated kinase (ERK) and p38 was also blocked by treatment with MFSC-Ex, indicating that inhibitory effect of MFSC-Ex on MAPK signaling cascade may attribute to inactivation of NF-κB. From these findings, we suggest that MFSC-Ex exert anti-inflammatory activities, which suppressed LPS/IFN-γ-induced production of NO, COX-2 and PGE2 by regulation of NF-κB and MAPK signaling pathway in RAW 264.7 macrophages. In conclusion, MFSC-Ex might provide a new therapeutic opportunity to treatment of inflammatory-related diseases.

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