Search results for: Cyclooxygenase

Authors: M. Hoxha, V. Capra, C. Buccellati, A. Sala, C. Cena, R. Fruttero, M. Bertinaria, G. E. Rovati

Abstract:

Today COXIBs are used in the treatment of arthritis and many other painful conditions in selected patients with high gastrointestinal risk and low cardiovascular (CV) risk. Previously, we have identified an unexpected mechanism of action of a traditional non-steroidal anti-inflammatory drug (NSAID) (diclofenac) and a specific inhibitor of cyclooxygenase-2 (COXIB) (lumiracoxib) demonstrating that they possess weak competitive antagonism at the thromboxane receptor (TP). We hypothesize that modifying the structure of a known COXIB so that it becomes also a more potent TP antagonist will preserve the anti-inflammatory and gastrointestinal safety typical of COXIBs and prevent the CV risk associated with long term therapy.

Keywords: Cyclooxygenase, inflammation, lumiracoxib, thromboxane A2.

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Authors: P. Thongmuang, Y. Sudjaroen

Abstract:

The methanolic extracts from seeds of tamarind (Tamarindus indica) was prepared by Soxhlet apparatus extraction and evaluated for total phenolic content by Folin-Ciocalteu method. Then, methanolic extract was screened biological activities (In vitro) for anti-melanogenic activity by tyrosinase inhibition test, antiinflammation activity by cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2) inhibition test, and cytotoxic screening test with Vero cells. The results showed that total phenolic content, which contained in extract, was contained 27.72 mg of gallic acid equivalent per g of dry weight. The ability to inhibit tyrosinase enzyme, which exerted by Tamarind seed extracts (1 mg/ml) was 52.13 ± 0.42 %. The extract was not possessed inhibitory effect to COX-1 and COX-2 enzymes and cytotoxic effect to Vero cells. The finding is concludes that tested seed extract was possessed antimelanogenic activity with non-toxic effects. However, there was not exhibited anti-inflammatory activity. Further studies include the use of advance biological models to confirm this biological activity, as well as, the isolation and characterization of the purified compounds that it was contained.

Keywords: Tamarindus indica, anti-melanogenic, antiinflammatotion, cytotoxicity, seed, phenolic compounds.

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Authors: Agata Kowalska, Radosław K. Kowalski, Zdzisław Zakęś

Abstract:

Our results showed that treatment with both cyclooxygenase (COX1 or COX2) inhibitors impair reproduction parameters of the medaka. Resveratrol (COX1 inhibitor) caused an decrease in the number of spawning females at the first week of feeding fish with experimental diets. In the group treated with NS- 398 (COX2 inhibitor) we found the lowest sperm velocity parameters and decreased linearity of movement. The ovaries of the medaka fed feed supplemented with Resveratrol or NS-398 were confirmed to have a lower share of matured oocytes however during the experiment (four weeks) the number of eggs spawned by females was similar. Both inhibitors in fish diet (20 mg/kg body weight/day) caused a decrease in the embryo survival. Our results revealed that for the medaka female reproduction, activity of both COX enzymes might be necessary whereas males reproduction competence, as expressed by sperm motility parameters, might be related to COX2 activity.

Keywords: COX innibitors, medaka, reproduction parameters

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Authors: Ali Asghar Saki, Sayed Ali Hosseini Siyar, Abbass Ashoori

Abstract:

This study was conducted to evaluate the effect of Echinacea purpurea on the expression of cyclooxygenase-2 (COX-2), interleukin-17F (IL-17F) in seven-day-old broiler chickens. Four groups were fed with concentration of 0 g/kg, 5 g/kg, 10 g/kg and 20 g/kg from the root of E. purpurea in the basal diet and two other groups were only fed with the basal diet for 21 days. At the 28^th day, lipopolysaccharide (LPS, 2 mg/kg diet) was injected in four groups and the basal diet group was injected by saline as control. The chickens’ spleen RNA expression was measured for the COX-2 and IL-17F genes by Real-Time PCR. The results have shown that chickens which were fed E. purpurea had a lower COX-2 and IL-17F mRNA expression. The chickens who have received LPS only, lymphocyte was lower than other treatments. Vital organ weights were not significantly different, but body weight loss was recovered by dietary herbs inclusion. The results of this study have shown the positive effect of an anti-inflammatory herb to prevent the undesirable effect of inflammation.

Keywords: Echinacea purpurea, broiler chickens, gene expression, lipopolysaccharide.

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Authors: Deepak Mohan, Sushma Sharma

Abstract:

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are a group of widely used drugs for the treatment of rheumatoid diseases and to relieve pain and inflammation due to their analgesic anti-pyretic and anti-inflammatory properties. The therapeutic and many of the toxic effects of NSAIDs result from reversible inhibition of enzymes in the cyclooxygenase (COX) group. In the present investigation the effect of the drug on the concentration of lipids, and on the activity of the enzymes i.e. acid and alkaline phosphatase, GOT, GPT and lipid peroxidase were studied. There was a significant enhancement in the activities of both acid and alkaline phosphatase after 21 days of treatment. Proportionate increase in the MDA contents was observed after different days of diclofenac treatment. Cellular damage in the liver resulted in decrease in the activity of both GOT (Glutamate oxaloacetate transaminase) and GPT (Glutamate pyruvate transaminase) in both low and high dose groups. Significant decrease in the liver contents was also observed in both dose groups.

Keywords: Anti-inflammatory, cyclooxygenase, glutamate oxaloacetate transaminase, malondialdehyde.

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Authors: Amr A. Fouad, Hamed A. Alwadaani, Iyad Jresat

Abstract:

The present study investigated the protective effect of thymoquinone (TQ), against cadmium-induced kidney injury in rats. Cadmium chloride (1.2 mg Cd/kg/day, s.c.), was given for nine weeks. TQ treatment (40 mg/kg/day, p.o.) started on the same day of cadmium administration and continued for nine weeks. TQ significantly decreased serum creatinine, renal malondialdehyde and nitric oxide, and significantly increased renal reduced glutathione in rats received cadmium. Histopathological examination showed that TQ markedly minimized renal tissue damage induced by cadmium. Immunohistochemical analysis revealed that TQ markedly decreased the cadmium-induced expression of inducible nitric oxide synthase, tumor necrosis factor-α, cyclooxygenase-2, and caspase-3 in renal tissue. It was concluded that TQ significantly protected against cadmium nephrotoxicity in rats, through its antioxidant, antiinflammatory, and antiapoptotic actions.

Keywords: Thymoquinone, cadmium, kidney, rats.

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Authors: Amr A. Fouad, Waleed H. Albuali, Iyad Jresat

Abstract:

The protective effect of hesperidin was investigated in rats exposed to liver injury induced by a single intraperitoneal injection of cyclophosphamide (CYP) at a dose of 150 mg kg-1. Hesperidin treatment (100 mg kg-1/day, orally) was applied for seven days, starting five days before CYP administration. Hesperidin significantly decreased the CYP-induced elevations of serum alanine aminotransferase, and hepatic malondialdehyde and myeloperoxidase activity, significantly prevented the depletion of hepatic glutathione peroxidase activity resulted from CYP administration. Also, hesperidin ameliorated the CYP-induced liver tissue injury observed by histopathological examination. In addition, hesperidin decreased the CYP-induced expression of inducible nitric oxide synthase, tumor necrosis factor-α, cyclooxygenase-2, Fas ligand, and caspase-9 in liver tissue. It was concluded that hesperidin may represent a potential candidate to protect against CYP-induced hepatotoxicity.

Keywords: Cyclophosphamide, hesperidin, liver, rats.

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Authors: Rosnani Hasham, Hyun Kyung Choi, Chang Seo Park

Abstract:

Ficus deltoidea from the Moraceae family is a popular medicinal herb in Malaysia. It possesses strong antioxidant and antiinflammatory properties. In the present study, the anti-inflammatory effects of F. deltoidea extract on UVB-irradiated HaCaT Keratinocytes were investigated. HaCaT Keratinocytes were UVBirradiated (12.5 mJ/cm3) and were treated with 0.05, 0.08 or 0.1% of F. deltoidea extract. Cell viability following UVB irradiation was significantly higher in the groups treated with the F. deltoidea extract at doses of 0.05, 0.08 or 0.1% than in control group with UVB irradiation only. Tumor necrosis factor-α (TNF-α), interleukin-1α (IL-1α), interleukin-6 (IL-6) and cyclooxygenase (COX-2) play primary roles in the inflammation process upon UV irradiation and are known to be stimulated by UVB irradiation. Treatment with the F. deltoidea extract dramatically inhibited the UV-induced TNF-α, IL-1α, IL-6, and COX-2 expression. These results suggest that the F. deltoidea extract inhibits the production of pro-inflammatory cytokines and may be an effective protective agent for the treatment of skin diseases.

Keywords: Ficus deltoidea, anti-inflammatory activity, cytokines, COX-2.

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Authors: Horia Păunescu

Abstract:

Purpose: The study aimed to assess the depressant or antidepressant effects of several Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) in mice: the selective cyclooxygenase-2 (COX-2) inhibitor meloxicam, and the non-selective COX-1 and COX-2 inhibitors lornoxicam, sodium metamizole, and ketorolac. The current literature data regarding such effects of these agents are scarce. Materials and methods: The study was carried out on NMRI mice weighing 20-35 g, kept in a standard laboratory environment. The study was approved by the Ethics Committee of the University of Medicine and Pharmacy „Carol Davila”, Bucharest. The study agents were injected intraperitoneally, 10 mL/kg body weight (bw) 1 hour before the assessment of the locomotor activity by cage testing (n=10 mice/ group) and 2 hours before the forced swimming tests (n=15). The study agents were dissolved in normal saline (meloxicam, sodium metamizole), ethanol 11.8% v/v in normal saline (ketorolac), or water (lornoxicam), respectively. Negative and positive control agents were also given (amitryptilline in the forced swimming test). The cage floor used in the locomotor activity assessment was divided into 20 equal 10 cm squares. The forced swimming test involved partial immersion of the mice in cylinders (15/9cm height/diameter) filled with water (10 cm depth at 28C), where they were left for 6 minutes. The cage endpoint used in the locomotor activity assessment was the number of treaded squares. Four endpoints were used in the forced swimming test (immobility latency for the entire 6 minutes, and immobility, swimming, and climbing scores for the final 4 minutes of the swimming session), recorded by an observer that was „blinded” to the experimental design. The statistical analysis used the Levene test for variance homogeneity, ANOVA and post-hoc analysis as appropriate, Tukey or Tamhane tests. Results: No statistically significant increase or decrease in the number of treaded squares was seen in the locomotor activity assessment of any mice group. In the forced swimming test, amitryptilline showed an antidepressant effect in each experiment, at the 10 mg/kg bw dosage. Sodium metamizole was depressant at 100 mg/kg bw (increased the immobility score, p=0.049, Tamhane test), but not in lower dosages as well (25 and 50 mg/kg bw). Ketorolac showed an antidepressant effect at the intermediate dosage of 5 mg/kg bw, but not so in the dosages of 2.5 and 10 mg/kg bw, respectively (increased the swimming score, p=0.012, Tamhane test). Meloxicam and lornoxicam did not alter the forced swimming endpoints at any dosage level. Discussion: 1) Certain NSAIDs caused changes in the forced swimming patterns without interfering with locomotion. 2) Sodium metamizole showed a depressant effect, whereas ketorolac proved antidepressant. Conclusion: NSAID-induced mood changes are not class effects of these agents and apparently are independent of the type of inhibited cyclooxygenase (COX-1 or COX-2). Disclosure: This paper was co-financed from the European Social Fund, through the Sectorial Operational Programme Human Resources Development 2007-2013, project number POSDRU /159 /1.5 /S /138907 "Excellence in scientific interdisciplinary research, doctoral and postdoctoral, in the economic, social and medical fields -EXCELIS", coordinator The Bucharest University of Economic Studies.

Keywords: Antidepressant, depressant, forced swim, NSAIDs.

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