• 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.

• 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.

• 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.

• Korean Journal of Pharmacognosy
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• v.35 no.2 s.137
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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.

• Proceedings of the Korean Society of Developmental Biology Conference
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• 2003.10a
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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.

• 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.

• Archives of Pharmacal Research
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• v.22 no.1
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• pp.18-24
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• 1999

Various flavonoid derivatives were previously reported to possess the inhibitory activity on cyclooxygenase/lipoxygenase. And these properties of flavonoids might contribute to their anti-inflammatory activity in vivo. In this study, several polyhydroxylated/methoxylated flavonoid derivatives such as oroxylin A. wogonin, skullcapflavone II, tectorigenin and iristectorigenin A were isolated from the medicinal plants. these compounds were evaluated fro their inhibitory effects on cyclooxygenase/lipoxygenase from the homogenate of human platelets in vitro. It was found that isoflavones including daidzein and tectorigenin possessed the inhibitory activity on cycloooxygenase, although the potency of inhibition was far less than that of indomethacin. In addition, oroxylin A, baicalein and wogonin inhibited 12-lipoxygenase activity without affecting cyclooxygenase, which suggested that 5,6,7- or 5,7,8-trisubstitutions of A-ring of flavone gave favorable results. The IC50 values of oroxylin A and NDGA against 12-lipoxygenase were found to be 100 and 1.5 uM, respectively.

• Food Science and 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.

• Natural Product Sciences
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• v.5 no.2
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• pp.65-69
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• 1999

By bioassay guided fractionation followed by chromatographic separation of the MeOH extract from the fruit of Evodia rutaecarpa (Juss.) Benth. (Rutaceae), a new cyclooxygenase-2 inhibitor was isolated and identified as an alkaloid, rutaecarpine. Other alkaloids such as evodiamine and dehydroevodiamine together with limonoids were also isolated and characterized.

• Korean Journal of Pharmacognosy
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• v.34 no.1 s.132
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• pp.25-27
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• 2003

In order to clarify the anti-thrombosis activity of rhubarb, we investigated the effect of stilbene derivatives from rhizomes of Rheum undulatun on cyclooxygenase activity. Stilbene derivatives (desoxyrhapontigenin, rhapontigenin, piceatannol) exhibited the inhibitory effects on COX-1, and desoxyrhapontigenin showed inhibitory effect on COX-2. These inhibitory effect may partially contributed to anti-thrombosis activity of rhubarb.