scholarly journals Anti-Inflammatory Effects of Protein Kinase Inhibitor Pyrrol Derivate

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Halyna M. Kuznietsova ◽  
Maryna S. Yena ◽  
Iryna P. Kotlyar ◽  
Olexandr V. Ogloblya ◽  
Volodymyr K. Rybalchenko
Keyword(s):  
Kinase Inhibitor ◽  
Malonic Dialdehyde ◽  
Redox Balance ◽  
Redox Status ◽  
Protein Carbonyl ◽  
Rat Colon ◽  
Sod Activity ◽  
Reference Drug ◽  
Grade Scale ◽  
Anti Inflammatory

In our previous studies we showed antitumor and anti-inflammatory activities of protein kinases inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1H-pyrrol-2,5-dione (MI-1) on rat colon cancer model. Therefore anti-inflammatory effect of MI-1 on rat acetic acid induced ulcerative colitis (UC) model was aimed to be discovered. The anti-inflammatory effects of MI-1 (2.7 mg/kg daily) compared to reference drug Prednisolone (0.7 mg/kg daily) after 14-day usage were evaluated on macro- and light microscopy levels and expressed in 21-grade scale. Redox status of bowel mucosa was also estimated. It was shown that in UC group the grade of total injury (GTI) was equal to 9.6 (GTIcontrol=0). Increase of malonic dialdehyde (MDA) by 89% and protein carbonyl groups (PCG) by 60% and decrease of superoxide dismutase (SOD) by 40% were also observed. Prednisolone decreased GTI to 3 and leveled SOD activity, but MDA and PCG remained higher than control ones by 52% and 42%, respectively. MI-1 restored colon mucosa integrity and decreased mucosa inflammation down to GTI = 0.5 and leveled PCG and SOD. Thus, MI-1 possessed anti-inflammatory properties, which were more expressed that Prednisolone ones, as well as normalized mucosa redox balance, and so has a prospect for correction of inflammatory processes.

scholarly journals Oxidative Stress and Its Consequences in the Blood of Rats Irradiated with UV: Protective Effect of Cannabidiol

Antioxidants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 821
Author(s):  
Michał Biernacki ◽  
Małgorzata Michalina Brzóska ◽  
Agnieszka Markowska ◽  
Małgorzata Gałażyn-Sidorczuk ◽  
Bogdan Cylwik ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Uv Radiation ◽  
Thioredoxin Reductase ◽  
Redox Balance ◽  
Receptor Activation ◽  
Protein Carbonyl ◽  
Ros Generation ◽  
Uvb Radiation ◽  
Down Regulation ◽  
Anti Inflammatory

UVA/UVB radiation disturbs the redox balance of skin cells, and metabolic consequences can be transferred into the blood and internal tissues, especially after chronic skin exposure to UV radiation. Therefore, the aim of this study was to evaluate the effect of cannabidiol (CBD), an antioxidant and anti-inflammatory phytocannabinoid, on oxidative stress and its consequences in the blood of nude rats whose skin was exposed to UVA/UVB radiation for 4 weeks. It was shown that CBD penetrated the blood and in UVB-irradiated rats was preferentially located in the membranes of polymorphonuclear leukocytes, which promoted reduction of ROS generation and up-regulation of antioxidant ability by increasing the activity of glutathione reductase and thioredoxin reductase, while the level of reduced glutathione decreased by UV radiation. Consequently, reduction in UV-induced lipid peroxidation, assessed as 4-hydroxynonenal (4-HNE) and 8-isoprostane (8-isoPGF2α) as well as protein modifications, estimated as 4-HNE-protein adducts and protein carbonyl groups, was observed. CBD, by countering the UV-induced down-regulation of 2-arachidonylglycerol, promoted its antioxidant/anti-inflammatory effects by reducing CB1 and increasing PPARγ receptor activation and consequently ROS and TNF-α down-regulation. The results suggest that CBD applied topically to the skin minimizes redox changes not only at the skin level, but also at the systemic level.

N-acetylcysteine a possible protector against indomethacin-induced peptic ulcer: crosstalk between antioxidant, anti-inflammatory, and antiapoptotic mechanisms

2017 ◽  
Vol 95 (4) ◽  
pp. 396-403 ◽  
Author(s):  
Nema Ali Soliman ◽  
Doaa Hussein Zineldeen ◽  
Mohamed Alaa Katary ◽  
Darin Abd Ali
Keyword(s):  
Normal Saline ◽  
Redox Status ◽  
Interferon Γ ◽  
Control Group ◽  
Albino Rats ◽  
Dependent Manner ◽  
Reference Drug ◽  
Pretreated Group ◽  
Anti Inflammatory ◽  
Glucose 6 Phosphate Dehydrogenase

This study investigated the gastroprotective effects of N-acetylcysteine (NAC) against indomethacin-induced gastric ulcer in rats. Ulceration was induced by a single oral administration of indomethacin (30 mg/kg). 50 male albino rats were allocated into 5 equal groups: control group received normal saline orally, indomethacin group rats received normal saline orally for 5 days and indomethacin (50 mg/kg) on the last day, ranitidine group received ranitidine (reference drug) orally for 5 days (50 mg/kg) before receiving indomethacin (50 mg/kg) on the last day, and NAC groups received NAC orally at 300 and 500 mg/kg, respectively, for 5 days before receiving indomethacin (50 mg/kg) on the last day. Gastric tissue interleukin-1β (IL-1β), interferon-γ (IFN-γ), and caspase-3 levels were immunoassayed. Total thiol (T-SH), myeloperoxidase (MPO), and glucose-6-phosphate dehydrogenase (G6PD) were determined by spectrophotometry. Cytokine-induced neutrophil chemoattractant 2α (CINC-2α) gene expression was evaluated in addition to Bcl-2 immunohistochemistry. Pretreatment with NAC improved the inflammatory, apoptotic, and redox status in a dose-dependent manner particularly in NAC 500 mg/kg pretreated group. These results show a role for NAC in improving indomethacin-induced gastric ulceration via antioxidative, antiapoptotic, and anti-inflammatory interactive mechanisms.

scholarly journals Hepatoprotective influence of quercetin and ellagic acid on thioacetamide-induced hepatotoxicity in rats

2018 ◽  
Vol 96 (6) ◽  
pp. 624-629 ◽  
Author(s):  
Nehal A. Afifi ◽  
Marwa A. Ibrahim ◽  
Mona K. Galal
Keyword(s):  
Ellagic Acid ◽  
Liver Toxicity ◽  
Underlying Mechanism ◽  
Redox Status ◽  
Expression Level ◽  
Male Rats ◽  
Reference Drug ◽  
Liver Injuries ◽  
Anti Inflammatory ◽  
New Treatment

Despite all the studies performed to date, therapy choices for liver injuries are very few. Therefore, the search for a new treatment that could safely and effectively block or reverse liver injuries remains a challenge. Quercetin (QR) and ellagic acid (EA) had potent antioxidant and anti-inflammatory activities. The current study aimed at evaluating the potential hepatoprotective influence of QR and EA against thioacetamide (TAA)-induced liver toxicity in rats and the underlying mechanism using silymarin as a reference drug. Fifty mature male rats were orally treated daily with EA and QR in separate groups for 45 consecutive days, and then were injected with TAA twice with 24 h intervals in the last 2 days of the experiment. Administration of TAA resulted in marked elevation of liver indices, alteration in oxidative stress parameters, and significant elevation in expression level of fibrosis-related genes (MMP9 and MMP2). Administration of QR and EA significantly attenuated the hepatic toxicity through reduction of liver biomarkers, improving the redox status of the tissue, as well as hampering the expression level of fibrosis-related genes. In this study, QR and EA were proved to attenuate the hepatotoxicity through their antioxidant, metal-chelating capacity, and anti-inflammatory effects.

scholarly journals Aqueous and Methanol Extracts of Paullinia pinnata (Sapindaceae) Improve Monosodium Urate-Induced Gouty Arthritis in Rat: Analgesic, Anti-Inflammatory, and Antioxidant Effects

2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Pius Pum Tseuguem ◽  
Télesphore Benoît Nguelefack ◽  
Basile Ngnanmegne Piégang ◽  
Sorelle Mbankou Ngassam
Keyword(s):  
Antioxidant Activities ◽  
Gouty Arthritis ◽  
Antioxidant Properties ◽  
Monosodium Urate ◽  
Leaf Extracts ◽  
Sod Activity ◽  
Reference Drug ◽  
Anti Inflammatory ◽  
The Brain

The profound modification of lifestyle and food habits has led to an important increase in the prevalence of gout. Unfortunately, there are current unmet needs for the treatment of this disease, prompting the search for new alternatives. Paullinia pinnata is a plant used to treat various diseases including arthritis. The present work aimed to investigate the antigouty activities of the aqueous (AEPP) and methanolic (MEPP) extracts of P. pinnata as well as their in vivo antioxidant properties. The gouty arthritis was induced by injecting 50 μl of monosodium urate (MSU, 100 mg/ml) in the left hind ankle of rats. P. pinnata extracts were administered orally at the doses of 100 and 200 mg/kg/day for 6 days, starting 24 h after MSU injection. Allopurinol 5 mg/kg/day was used as reference drug. Inflammation and hyperalgesia were daily monitored from 24 hours after treatment initiation and for the 6 consecutive days. Myeloperoxidase (MPO) quantification was done in collected synovial fluid. Nitrite oxide (NO), malondialdehyde (MDA), and superoxide dismutase (SOD) were evaluated in the spinal cord and the brain. The serum content of SOD was additionally quantified. AEPP and MEPP significantly (p<0.001) reduce MSU-induced inflammation (22.41% to 93.65%) and hyperalgesia (33.33% to 64.44%) in both ankle and paw. AEPP and MEPP significantly (p<0.001) reduce synovial MPO production with the percentage ranging from 76.30% to 85.19%. AEPP and MEPP significantly (p < 0.001) reduce serum, spinal, left and right hemispheres NO, and MDA and increase the SOD activity (p<0.001). P. pinnata leaf extracts possess potent curative effects against MSU-induced gouty arthritis that combines analgesic, anti-inflammatory, and antioxidant activities. These findings support the use of P. pinnata leaves extracts in the treatment of gouty arthritis and further present the plant as a potent source of efficient antigouty medicine.

Reduction of paw edema and liver oxidative stress in carrageenan-induced acute inflammation by Lobaria pulmonaria and Parmelia caperata, lichen species, in mice

2019 ◽  
pp. 1-9
Author(s):  
Samira Salem ◽  
Essaid Leghouchi ◽  
Rachid Soulimani ◽  
Jaouad Bouayed
Keyword(s):  
Time Course ◽  
Acute Inflammation ◽  
Lichen Species ◽  
Paw Edema ◽  
Sod Activity ◽  
Edema Formation ◽  
Lobaria Pulmonaria ◽  
Anti Inflammatory ◽  
Endogenous Antioxidant ◽  
Inflammatory Effect

Abstract. Paw edema volume reduction is a useful marker in determining the anti-inflammatory effect of drugs and plant extracts in carrageenan-induced acute inflammation. In this study, the anti-inflammatory effect of Lobaria pulmonaria (LP) and Parmelia caperata (PC), two lichen species, was examined in carrageenan-induced mouse paw edema test. Compared to the controls in carrageenan-induced inflammation (n = 5/group), our results showed that pretreatment by single oral doses with PC extract (50–500 mg/kg) gives better results than LP extract (50–500 mg/kg) in terms of anti-edematous activity, as after 4 h of carrageenan subplantar injection, paw edema formation was inhibited at 82–99% by PC while at 35–49% by LP. The higher anti-inflammatory effect of PC, at all doses, was also observed on the time-course of carrageenan-induced paw edema, displaying profile closely similar to that obtained with diclofenac (25 mg/kg), an anti-inflammatory drug reference (all p < 0.001). Both LP and PC, at all doses, significantly ameliorated liver catalase (CAT) activity (all p < 0.05). However, superoxide dismutase (SOD) activity, glutathione peroxidase (GPx) activity and glutathione (GSH) levels were found increased in liver of PC- compared to LP-carrageenan-injected mice. Our findings demonstrated on one hand higher preventive effects of PC compared to LP in a mouse carrageenan-induced inflammatory model and suggested, on the other hand, that anti-inflammatory effects elicited by the two lichens were closely associated with the amelioration in the endogenous antioxidant status of liver.

scholarly journals The Anti-Inflammatory Effect of a γ-Lactone Isolated from Ostrich Oil of Struthio camelus (Ratite) and Its Formulated Nano-Emulsion in Formalin-Induced Paw Edema

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3701
Author(s):  
Salah E. M. Eltom ◽  
Ahmed A. H. Abdellatif ◽  
Hamzah Maswadeh ◽  
Mohsen S. Al-Omar ◽  
Atef A. Abdel-Hafez ◽  
...  
Keyword(s):  
Oral Administration ◽  
Standard Procedure ◽  
P Value ◽  
Skin Thickness ◽  
Paw Edema ◽  
Reference Drug ◽  
Struthio Camelus ◽  
Anti Inflammatory ◽  
Nano Emulsion ◽  
Inflammatory Effect

The ostrich oil of Struthio camelus (Ratite) found uses in folk medicine as an anti-inflammatory in eczema and contact dermatitis. The anti-inflammatory effect of a γ-lactone (5-hexyl-3H-furan-2-one) isolated from ostrich oil and its formulated nano-emulsion in formalin-induced paw edema was investigated in this study. Ostrich oil was saponified using a standard procedure; the aqueous residue was fractionated, purified, and characterized as γ-lactone (5-hexyl-3H-furan-2-one) through the interpretation of IR, NMR, and MS analyses. The γ-lactone was formulated as nano-emulsion using methylcellulose (MC) for oral solubilized form. The γ-lactone methylcellulose nanoparticles (γ-lactone-MC-NPs) were characterized for their size, shape, and encapsulation efficiency with a uniform size of 300 nm and 59.9% drug content. The γ-lactone was applied topically, while the formulated nanoparticles (NPs) were administered orally to rats. A non-steroidal anti-inflammatory drug (diclofenac gel) was used as a reference drug for topical use and ibuprofen suspension for oral administration. Edema was measured using the plethysmograph method. Both γ-lactone and γ-lactone-MC-NPs showed reduction of formalin-induced paw edema in rats and proved to be better than the reference drugs; diclofenac gel and ibuprofen emulsion. Histological examination of the skin tissue revealed increased skin thickness with subepidermal edema and mixed inflammatory cellular infiltration, which were significantly reduced by the γ-lactone compared to the positive control (p-value = 0.00013). Diuretic and toxicity studies of oral γ-lactone-MC-NPs were performed. No diuretic activity was observed. However, lethargy, drowsiness, and refusal to feeding observed may limit its oral administration.

Analgesic and anti-inflammatory effects of A-286501, a novel orally active adenosine kinase inhibitor

Pain ◽  
2002 ◽  
Vol 96 (1) ◽  
pp. 107-118 ◽  
Author(s):  
Michael F. Jarvis ◽  
Haixia Yu ◽  
Steve McGaraughty ◽  
Carol T. Wismer ◽  
Joe Mikusa ◽  
...  
Keyword(s):  
Kinase Inhibitor ◽  
Adenosine Kinase ◽  
Anti Inflammatory ◽  
Orally Active

Ozone Therapy Alleviates Monosodium Urate Induced Acute Gouty Arthritis in Rats Through Inhibition of NLRP3 Inflammasome

2021 ◽  
Vol 16 ◽  
Author(s):  
Doaa M. Abdullah ◽  
Soad L. Kabil
Keyword(s):  
Gouty Arthritis ◽  
Antioxidant Defense System ◽  
Albino Rats ◽  
Monosodium Urate ◽  
Ozone Therapy ◽  
Reference Drug ◽  
Acute Gouty Arthritis ◽  
Beneficial Effects ◽  
Anti Inflammatory ◽  
Domain 3

Background: Gout is a metabolic disease strictly related to hyperuricemia. The associated intense inflammation and pain are triggered by the deposited monosodium urate crystals (MSU) in joints. The principal therapeutic strategies of gout involve the control of hyperuricemia and anti-inflammatory medications. Objectives: This study aimed to investigate the possible beneficial effects of ozone therapy, a well-known antioxidant, and an immunomodulation, on gouty arthritis and the underlying mechanisms. Methods : Acute gouty arthritis was induced in male albino rats via MSU crystals intra-articular injection in the ankle joint. The gouty arthritic rats received pre-treatment with ozone, colchicine (as a reference drug), or combination. Results : The obtained results of ozone therapy showed obvious reduction in the degree of ankle edematous swelling, pro-inflammatory cytokines, lipid peroxidation, the nucleotide binding oligomerization domain like receptor containing pyrin domain 3 (NLRP3), procaspase-1, caspase-1, interleukin-1β synovial tissue levels with enhancement of antioxidant defense system. Additionally, ozone therapy significantly attenuated the histological derangements in gouty arthritic rats. Conclusion : This study suggests that ozone is able to treat gouty arthritis and reducing synovial injury through an anti-inflammatory effect as well as antioxidant activity.

Abstract 1727: Apolipoprotein E (ApoE) Induces an Anti-inflammatory Phenotype in Macrophages

Circulation ◽  
2008 ◽  
Vol 118 (suppl_18) ◽  
Author(s):  
Daniel Baitsch ◽  
Ralph Telgmann ◽  
Georg Varga ◽  
Carsten Muller-Tidow ◽  
Martine Bot ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Apolipoprotein E ◽  
Kinase Inhibitor ◽  
Plasma Cholesterol ◽  
Macrophage Phenotype ◽  
Anti Inflammatory ◽  
M2 Phenotype ◽  
Functional Phenotype ◽  
Expression And Activity ◽  
Phenotype Expression

Apolipoprotein E (apoE) exerts anti-atherogenic effects by promoting cholesterol efflux and hepatic lipoprotein clearance. However, apoE retains protective effects even under experimental settings, in which its influence on plasma cholesterol is negligible suggesting that this lipoprotein inhibits atherosclerosis independently from cholesterol transport. To gain further insight into mechanisms underlying apoE-mediated atheroprotection, we investigated its effect on the functional phenotype of RAW 264.7 macrophages overexpressing either of two apoE receptors: ApoER2/LRP8 or VLDL-R. Incubation of ApoER2/LRP8- or VLDL-R-expressing macrophages with apoE downregulated markers of pro-inflammatory M1 functional phenotype (expression and activity of iNOS, production of IL-12), whereas markers of anti-inflammatory M2 phenotype (expression and activity of arginase-I, production of IL-1RA) were upregulated. In addition, macrophage responses typical for M1 phenotype (migration, generation of reactive oxygen species, antibody-dependent cell cytotoxicity) were suppressed in ApoER2/LRP8- or VLDL-R-expressing cells in the presence of apoE. Finally, apoE prevented LPS- and IFN-γ-induced activation of ApoER2/LRP8- or VLDL-R-expressing macrophages as documented by reduced production of IL-12, TNF-α and MCP-1, reduced expression and activity of iNOS and COX2, and reduced activation and/or phosphorylation of NF-κB, IκB and STAT1. The modulatory effects of apoE on macrophage phenotype were inhibited by SB220025, a p38MAP kinase inhibitor, and PP1A, a tyrosine kinase inhibitor. Accordingly, apoE induced tyrosine kinase-dependent activation of p38MAP kinase in ApoER2/LRP8- or VLDL-R-expressing macrophages. Under in vivo conditions, apoE −/− mice transplanted with apoE-producing wild-type bone marrow presented with increased plasma IL-1RA levels. In addition, peritoneal macrophages from transplanted animals demonstrated enhanced M2 phenotype (increased IL-1RA production and CD206 expression). We conclude that apoE signalling over ApoER2/LRP8 or VLDL-R promotes macrophage conversion from pro-inflammatory M1 to anti-inflammatory M2 phenotype. This effect may represent a novel anti-atherogenic activity of apoE.

Inhibition of aberrant crypt growth by non-steroidal anti-inflammatory agents and differentiation agents in the rat colon

1995 ◽  
Vol 60 (4) ◽  
pp. 515-519 ◽  
Author(s):  
Michael J. Wargovich ◽  
Chi Dai Chen ◽  
Charles Harris ◽  
Eileen Yang ◽  
Marco Velasco
Keyword(s):  
Rat Colon ◽  
Anti Inflammatory
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