• Title, Summary, Keyword: cyclooxygenase 2

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Docking Mode of 4,5-Diarylpyrroles into Cyclooxygenase-1 and Cyclooxygenase-2 (Cyclooxygenase-1과 Cyclooxygenase-2에 대한 4,5-Diarylpyrroles의 Docking Mode)

  • 이종달;도성탁;구본기
    • YAKHAK HOEJI
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    • v.43 no.6
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    • pp.776-781
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    • 1999
  • Dockings of 4,5-diarylpyrroles into cyclooxygenase-1 and cyclooxygenase-2 were carried out by GOLD program. The sulfonyl groups bonded to 5-phenyl ring of 4,5-diarylpyrroles are directed to Arg513 of COX-2 and Tyr385 of COX-2 docking modes of pyrroles are different from COX-1. Tyr385 and Arg120 of COX-1 and COX-2 have been recognized as important residues. Val523 of COX-2 may be also important. A new COX-2 selective inhibitors could be designed from the docking study.

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Roles of E-cadherin and Cyclooxygenase Enzymes in Predicting Different Survival Patterns of Optimally Cytoreduced Serous Ovarian Cancer Patients

  • Taskin, Salih;Dunder, Ilkkan;Erol, Ebru;Taskin, Elif Aylin;Kiremitci, Saba;Oztuna, Derya;Sertcelik, Ayse
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.11
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    • pp.5715-5719
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    • 2012
  • The relation between cyclooxygenase enzymes and E-cadherin, along with the roles of these markers in the prediction of survival in optimally cytoreduced serous ovarian cancer patients was investigated. Individuals who underwent primary staging surgery and achieved optimal cytoreduction (largest residual tumor volume <1 cm) constituted the study population. Specimens of 32 cases were immunohistochemically examined for cyclooxygenase-1, cyclooxygenase-2, and E-cadherin. Two could not be evaluated for E-cadherin and cyclooxygenase-1. Overall, 14/30, 19/30, and 15/32 cases were positive for E-cadherin, cyclooxygenase-1, and cyclooxygenase-2, respectively. The expressions of E-cadherin and cyclooxygenase-2 were inversely correlated (p:0.02). E-cadherin expression was related with favorable survival (p<0.001). The relation between the expression of cyclooxygenase enzymes and poor survival did not reach statistical significance. On multivariate analysis, E-cadherin appeared as an independent prognostic factor for survival. In conclusion, E-cadherin expression is strongly linked with favorable survival. E-cadherin and cyclooxygenase 2 may interact with each other during the carcinogenesis-invasion process. Further studies clarifying the relation between E-cadherin and cyclooxygenase enzymes may lead to new preventive and therapeutic targets in ovarian cancer.

생쥐의 자궁, 난소, 태아에 있어서 아라키돈산에 특이적인 acyl-CoA synthetase 4 유전자의 발현

  • 박효영;문선정;양정미;이상미;정영희;문승주;강만종
    • Proceedings of the Korean Society of Developmental Biology Conference
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    • pp.96-96
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    • 2003
  • Acyl-CoA synthetase 4는 생쥐에 있어서 거의 모든 조직에서 발현하며 아라키돈산에 특이적인 효소이다. 아라키돈산은 세포막의 인지질로부터 cPLA2에 의하여 유리되고 cyclooxygenase-1, -2에 의하여 eicosanoid로 변환된다. 이렇게 생산된 prostaglandin과 같은 eicosanoid는 배란, 수정, 임신에 있어서 중요한 기능을 수행하고 있다. 그러나 세포막으로부터 유리된 아라키돈산은 acyl-CoA synthetase 4에 의하여 다시 세포막으로 재에스테르화되어 eicosaniod의 생산을 조절하는 것으로 생각되어지고 있다. 또한 acyl-CoA synthetase 4 유전자 한쪽이 knock-out된 heterozygote mouse에서는 사산, 유산과 난소에 있어서 황체 수의 증가 등을 보고하고 있다. 그러므로 본 연구에서는 정상 생쥐 (C57BL/6) 임신 기간 중 acyl-CoA synthetase 4 유전자의 발현을 확인하기 위하여 자궁, 난소, 태아에서 RT-PCR을 수행하였다. 또한 cPLA2, cyclooxygenase-1, cyclooxygenase-2 유전자의 발현 양상을 분석하여 eicosanoid 생산에 관여하는 유전자 상호간의 발현 을 확인하였다. acyl-CoA synthetase 4는 임신 0 day에서부터 19.5 day까지 자궁과 난소에서 모두 발현하고 있었다. 또한 5.5 day에서부터 19.5 day까지의 태아에서도 그 발현이 확인되었다. 그리고 cPLA2와 cyclooxygenase-1은 acyl-CoA synthetase 4와 유사한 양상을 보였으나 cyclooxygenase-2는 임신기간 중의 자궁, 난소, 태아에서 전혀 발현하지 않았다. 그러므로 임신 중 생쥐 자궁, 난소, 태아에 있어서 eicosanoid 생산에는 cPLA2, cyclooxygenase-1, acyl-CoA synthetase 4 유전자가 관여하고 있는 것으로 생각된다.

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Effect of Water Extracts from Thesium chinense Tunczaninov and Prunella vulgaris L. on Aromatase and Cyclooxygenase Activities (하고초 열수추출물이 Aromatase와 Cyclooxygenase 활성에 미치는 영향)

  • Nam, Kyung-Soo;Shon, Yun-Hee
    • Korean Journal of Pharmacognosy
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    • v.35 no.2
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    • pp.147-151
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    • 2004
  • Water extracts from Thesium chinense Tunczaninov (TCTW) and Prunella vulgaris L. (PVW) were tested for aromatase and cyclooxygenase activities. TCTW and PVW were capable of suppressing aromatase in a human placenta microsomal assay. PVW was shown to be more effective than TCTW in the suppression of aromatase activity. TCTW significantly inhibited cyclooxygenase-2 (COX-2) activity at the concentration of 0.25 (p<0.05), 0.5 (p<0.01) and 2.5 mg/ml (p<0.005). PVW also inhibited COX-2 activity in a dose-dependent manner in a concentration range of $0.05{\sim}2.5\;mg/ml$. The expression of COX-2 was inhibitied by TCTW and PVW in western blot analysis. These results suggest that TCTW and PVW may have breast cancer chemopreventive potentials by inhibiting aromatase and cyclooxygenase activities.

Comparison of In Vitro Antioxidant Activity and Cyclooxygenase-2 Promoter Inhibitory Activity in Harmonia axyridis Pallas and Coccinella septempunctata $Linn\dot{e}$ (약용곤충 무당벌레류 추출물의 항산화활성과 Cyclooxygenase-2 Promoter 억제활성 비교)

  • Heo Jin-Chul;Park Ja-Young;Hwang Jae-Sam;Park Hae-Cheol;Kang Seok-Woo;Hwang Seok-Jo;Yun Chi-Young;Kwon Taeg-Kyu;Lee Sang-Han
    • Korean Journal of Food Preservation
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    • v.13 no.4
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    • pp.513-518
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    • 2006
  • Insect resources have been widely recognized that seven millions of insects exhibit it own biological activity by whole body or its metabolic intermediates. In order to investigate antioxidant activity and compare the cyclooxygenase-2 promoter activity from insect extract, we tested in vitro antioxidant assays and cyclooxygenase-2 promoter assay in Coccinella septempunctata Linne and Harmonia axyridis extracts have the anti-oxidant and cyclooxygenase-2 inhibition activities, we examined the anti-oxidant assays including DPPH, FRAP and linoleic acid, ana inhibition of cyclooxygenase-2 expression using a cyclooxygenase-2 promoter-inserted stable cell line. We found that Harmonia axyridis Pallas extract had potentials to anti-oxidant activity and inhibited about 25% of cyclooxygenase-2 transcription activity. These findings indicate that Coccinella septempunctata Linne and Harmonia axyridis Pallas extracts could be an useful insect resource for agrobiotechnological purposes.

In Vitro Inhibition of Cyclooxygenase by Aspalatone (아스파라톤에 의한 사이클로옥시게나제의 저해 - in Vitro)

  • 서대연;한병훈
    • YAKHAK HOEJI
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    • v.39 no.5
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    • pp.565-568
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    • 1995
  • A new antiplatelett agent, aspalatone ([3-(2-methyl-4-pyronyl)]-2-acetyloxybenzoate) was demonstrated to inhibit MDA generation from arachidonic acid catalyzed by partially purified bovine seminal vesicle cyclooxygenase. This inhibition was also observed with acetylsalicylic acid. The results suggest that the mechanism for the antiplatelet effect of aspalatone is, like acetylsalicylic acid, due to its inhibition of cyclooxygenase.

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The Role of Cyclooxygenase Metabolites in the Pathogenetic Mechanism of Endotoxin-Induced Acute Lung Injury in Domestic Pigs (내독소에 의한 돼지의 급성 폐손상에서 Cyclooxygenase 대사물의 역할에 관한 연구)

  • Yoo, Chul-Gyu;Jeong, Ki-Ho;Choi, Hyung-Seok;Lee, Hyuk-Pyo;Kim, Young-Whan;Han, Sung-Koo;Shim, Young-Soo;Kim, Keun-Youl;Han, Yong-Chol
    • Tuberculosis and Respiratory Diseases
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    • v.39 no.1
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    • pp.42-54
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    • 1992
  • Background:It has been suggested that the cyclooxygenase metabolites play an important role in changes of early hemodynamic parameters in the endotoxin-induced acute lung injury. But there have been many debates about their role in the late increase of alveolar-capillary permeability, and it is not known whether they act directly or indirectly through oxygen free radicals which have been known to be produced during the metabolic process of cyclooxygenase pathway. So we performed this study to identify the pathogenetic role of cyclooxygenase metabolites in the endotoxin-induced acute lung injury in domestic pigs. Method: We infused endotoxin into 8 domestic pigs; endotoxin only (n=3), and pretreatment with indomethacin (n=5). We observed the sequential changes in hemodynamic parameters, the concentration of plasma oxidized glutathione (GSSG) in pulmonary arterial and venous blood, and albumin content in bronchoalveolar lavage fluid (BALF). Results: 1) While cardiac output decreased, mean pulmonary arterial pressure, pulmonary vascular resistance, and alveolar-arterial oxygen difference increased over phase 1 (0-2hr) and phase 2 (2-4.5hr) by endotoxin, indomethacin attenuated the decrease in cardiac output during phase 1 and increase in mean pulmonary arterial pressure, pulmonary vascular resistance, and alveolar-arterial oxygen difference during both phases. 2) The increase in plasma GSSG content during phase 2 was not attenuated by indomethacin. 3) The content of BALF albumin was significantly lower in indomethacin groups than that of endotoxin group. Conclusion: These results suggest that it is likely that cyclooxygenase metabolites have an effect on endotoxin-induced acute lung injury during both phases probably through direct action.

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Antiinflammatory Evaluation and Synthesis of Benzothiazine Derivatives as Cyclooxygenase-2 Inhibitor (Cyclooxygenase-2 저해제로서의 benzothiazine 유도체 합성과 항염작용 평가)

  • 신혜순;박명숙;권순경
    • YAKHAK HOEJI
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    • v.44 no.3
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    • pp.272-278
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    • 2000
  • The antiinflammatory mechanism of NSAIDs is attributed to the reduction of prostaglandin synthesis by the direct inhibition of cyclooxygenase. Inhibition of prostaglandin production in organs such as stomach and kidney can result in gastric lesions, nephrotoxicity and increased bleeding. In this study, newly designed COX-2 inhibitors, synthesized 1,2-benzothiazine derivatives, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. Lead compounds in the structure-activity relationship were studied to synthesize new highly selective COX-2 inhibitors.13 determine inhibitory effect of COX-2, synthesized 1,2-benzothiazine derivatives were screened with accumulation of prostaglandin by lipopolysaccharide (LPS) in aspirin-treated macrophages and murine macropharge cell. Some of synthesized 1,2-benzothiazine derivatives were shown to be effective as selective COX-2 inhibitory activity. Others exhibited a preferential inhibition of COX-2, although some COX-1 inhibitory activity was still present. As a conclusion, simple monomer derivatives were more active than dimer derivatives. Substitution of halogen (Br, C1) on the benzothiazine nucleus slightly enhanced inhibition activity.

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Reduction of muscle cyclooxygenase-2 with transcutaneous electrical nerve stimulation and cold therapy in rats of carrageenan-induced inflammatory muscle pain (Carrageenan으로 유도된 염증성 근통증 흰쥐 모델에서 경피신경전기자극과 냉치료에 의한 비복근의 cyclooxygenase-2의 감소)

  • Paek, Yun-Woong;Chae, Yun-Won
    • Journal of Korean Physical Therapy Science
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    • v.9 no.1
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    • pp.89-94
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    • 2002
  • Prostaglandins are generated through two isoforms of the enzyme cyclooxygenase, constitutively expressed cyclooxygenase(COX)-1 and COX-2, which is induced at sites of inflammation. Inhibition of COX-2 is desirable as this may avoid side effects seen with NSAIDs. We examined the effects of transcutaneous electrical nerve stimulation and cold therapy on the levels of muscle cycloooxygenase-2 mRNA in rats of carrageenan-induced inflammatory. The method of behavioral assessment were paw withdrawal latency(PWL) and tail flick test(TFT). The COX-2 mRNA levels were quantified by reverse transcription-polymerase chain reaction (RT-PCR). Following the transcutaneous electrical nerve stimulation and cold therapy, PWL and TFT were increased and COX-2 mRNA expression in gastrocnemius muscles were decreased. These results suggest that a transcutaneous electrical nerve stimulation and cold therapy were good therapy for a muscle pain.

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Protective Effect of Celecoxib, a Selective Cyclooxygenase-2 Inhibitor, Against Beta-Amyloid-Induced Apoptosis: Possible Involvement of Proinflammatory Signals in Beta-Amyloid-Mediated Cell Death

  • Jang, Jung-Hee;Surh, Young-Joon
    • Proceedings of the Korean Society of Toxicology Conference
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    • pp.139-140
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    • 2003
  • Inflammatory as well as oxidative tissue damage has been implicated in pathophysiology of Alzheimer's disease (AD), and non-steroidal anti-inflammatory drugs have been reported to have beneficial effects in the treatment or prevention of AD. In the present study, we investigated the effect of celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, on inflammatory cell death induced by beta-amyloid, a neurotoxic peptide associated with senile plaques formed in the brains of patients with AD.(omitted)

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