• Title/Summary/Keyword: 선택적 COX-2 억제제

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Piceatannol-Induced G1 Arrest of the Cell Cycle is Associated with Inhibition of Prostaglandin E2 Production in Human Gastric Cancer AGS Cells (Piceatannol에 의한 AGS 인체 위암세포의 G1 Arrest 및 Prostaglandin E2 생성의 억제)

  • Choi, Yung-Hyun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.7
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    • pp.907-913
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    • 2012
  • Piceatannol (trans-3,4,3',5'-tetrahydroxystilbene) is a polyphenol detected in grapes, rhubarb, and sugarcane. Although recent experimental data revealed that this compound is known to exhibit immunosuppressive and antitumorigenic activities in several cell lines, the molecular mechanisms underlying anticancer activity are poorly understood. In the present study, we investigated possible further mechanisms by which piceatannol exerts its anti-proliferative action in cultured human gastric cancer AGS cells. Piceatannol treatment resulted in the inhibition of growth and G1 arrest of the cell cycle in a concentration-dependent manner, as determined by MTT assay and flow cytometry analysis. The induction of G1 arrest by piceatannol was associated with the modulation of cyclin-dependent kinases (Cdks) and cyclins, up-regulation of the expression of Cdk inhibitor p21 (WAF1/CIP1) in both transcriptional and translational levels, and the inhibition of phosphorylation of retinoblastoma proteins and E2F1 expression. In addition, piceatannol treatment caused a progressive decrease in the expression levels of cyclooxygenase (COX)-2 without significant changes in the levels of COX-1, which was correlated with a decrease in prostaglandin $E_2$ synthesis.

Antioxidative and Antiallergic Effect of Persimmon Leaf Extracts (감잎(Diospyros kaki Thunb) 추출물의 항산화 및 항알레르기 효과)

  • Yoo, Ki-Hwan;Jeong, Jong-Moon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.12
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    • pp.1691-1698
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    • 2009
  • The purpose of this study was to investigate the antioxidative and antiallergic effects of persimmon leaf extract. Antioxidative and anti-inflammatory effects of the crude persimmon leaf extract (PLE) and the partially purified persimmon leaf extract (PPLE) were determined in in vitro assays by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and superoxide anion radicals, and 5-lipoxygenase (5-LO) and cyclooxygenase (COX). Total phenols and total flavonoid levels of PLE and PPLE were $230.0{\pm}19.6$ mg/g and $475.5{\pm}38.7$ mg/g, and $34.8{\pm}6.5$ mg/g and $78.8{\pm}3.6$ mg/g, respectively. DPPH and superoxide radical-scavenging activities ($SC_{50}$) of the PLE and PPLE were $23.8{\pm}3.2$ ppm and $10.0{\pm}1.3$ ppm, and $47.6{\pm}3.4$ ppm and $22.4{\pm}3.3$ ppm, respectively. Inhibitory activities ($IC_{50}$) of PLE and PPLE against 5-LO, COX-1 and COX-2 were $77.1{\pm}11.7$, $38.6{\pm}7.0$ ppm, $47.4{\pm}7.7$, $25.3{\pm}6.3$ ppm, and $129.5{\pm}5.5$, $84.5{\pm}2.3$ ppm, respectively. Moreover, two extracts inhibited dose-dependently NO production in LPS-stimulated RAW 264.7 cells, and also effectively inhibited the cutaneous anaphylaxis reaction activated by anti-dinitrophenyl IgE antibody in mice. These results suggest that PLE and PPLE may be useful for phytochemical materials for prevention and treatment of radical-mediated pathological and allergy diseases.

Effect of Celecoxib, a Cyclooxygenase-2-specific Inhibitor, has no Effect on Chronically Maintained Neuropathic Pain in Rats (장기간 유지된 신경병증성 통증 흰쥐에서 선택적 COX2 억제제인 Celecoxib의 진통효과)

  • Park, Eun-Sung;Kim, Hyun-Jeong;Lee, Min-Ju;Lee, Ji-Yoon;Shin, Teo-Jeon;Seo, Kwang-Suk;Yum, Kwang-Won
    • Journal of The Korean Dental Society of Anesthesiology
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    • v.8 no.1
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    • pp.29-34
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    • 2008
  • 배경: 신경병증성 통증은 스테로이드, 아편유사제 등의 진통제에 잘 반응하지 않는다. 하지만 염증성 매개물질들이 신경병증성 통증의 발생에 관여한다는 보고가 있다. 특히 선택적 COX2 억제제인 celecoxib의 신경병증성 통증에 대한 효과에 관해서 상반된 연구결과가 존재한다. 본 연구는 신경병증성 통증 모델인 척추신경 결찰모델을 이용 기계적, 냉각 이질통 및 온도감각 과민현상의 발현에 celecoxib이 미치는 영향을 관찰하여 celecoxib의 항통각효과를 확인하고자 하였다. 방법: 30마리의 쥐를 이용 척추신경을 결찰하여 신경병증성 통증을 유도하였다 celecoxib (1, 10, 100, and 300 mg/kg)을 경구 투여하였고 총 30마리 중 12마리의 쥐에서 열, 기계적자극에 대해서 통각과민, 냉각자극에 의해 이질통이 발생하였다. 약물 투여 후 30, 60, 120, 180분 후 von Frey, 냉각자극검사, Hargreaves검사를 시행하여 쥐의 행동변화를 관찰하였다. 결과: 신경결찰 후 5일 후에 celecoxib의 용량에 관계없이 열, 기계적 자극에 의한 통각과민, 냉각 자극에 대한 이질통을 감소시키지 않았다(P > 0.05). 또한 celecoxib투여에 의한 장기간의 항 통각효과는 관찰되지 않았다(P > 0.05). 결론: celecoxib을 경구로 투여하였을 때 장기간 유지된 신경병증성 통증 흰쥐에서 약의 투여용량, 투여기간에 따른 항 통각작용은 관찰되지 않았다. 따라서 조직 손상후 발생된 장기간의 신경병증성 통증에 있어서 celecoxib은 효과가 없는 것으로 사료된다.

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Antioxidative and Antiallergic Effects of Aronia (Aronia melanocarpa) Extract (아로니아(Aronia melanocarpa)로부터 유래한 추출물의 항산화 및 항알레르기 효능)

  • Jeong, Jong-Moon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.9
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    • pp.1109-1113
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    • 2008
  • The purpose of this study was to investigate the antioxidative and antiallergic effects of aronia extract. The aronia extract was tested for various antioxidative potentials (scavenging activity of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and superoxide anion radical) and inhibitory effect of 5-lipoxygenase (5-LO) and cyclooxygenase (COX). In aronia extract, polyphenol content was $81.6{\pm}3.3\;mg/g$ and flavonoid content was $5.15{\pm}0.16\;mg/g$. DPPH radical-scavenging activity ($SC_{50}$) of aronia extract was $6.15{\pm}0.343\;ppm$. $SC_{50}$ value of aronia extract against superoxide anion radical was $6.99{\pm}1.28\;ppm$. In addition, $IC\_{50}$ values of aronia extract against 5-LO, COX-1, and COX-2 were $42.07{\pm}0.15\;ppm$, $24{\pm}4.29\;ppm$, and $24.3{\pm}3.5\;ppm$, respectively. These results suggest that aronia extract may be useful for the prevention or treatment of allergic disease.

Deep Vein Thrombosis in Advanced Cervical Cancer Patient after Taking Cyclooxygenase-2 Selective Inhibitors (Cyclooxygenase-2 선택적 억제제를 복용 중 자궁암 환자에 발생한 심부정맥혈전증 1예)

  • Ko, Byung-Joon;Kim, Su-Hyun;Kim, Jeong-A;Hong, Jeong-Ik;Yoon, Do-Kyoung;Kim, Jung-Hwan;Sohn, Keun-Ju;Choi, Youn-Seon
    • Journal of Hospice and Palliative Care
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    • v.8 no.1
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    • pp.57-64
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    • 2005
  • Cyclooxygenase-2 (COX-2) selective inhibitors were specifically developed to reduce the risks of gastrointestinal bleeding associated with other NSAID drugs. However, the APPROVe (Adenomatous Polyp Prevention on VIOXX) trials revealed that rofecoxib sometimes exerts prothrombotic effects. Meanwhile, cancer patients, who also carry a risk of thrombosis due to a variety of mechanisms, are often treated with COX-2 selective inhibitors, due to their relative gastrointestinal safety. This report concerns the case of a 46-year old woman with advanced cervical cancer, who had been treated with opioids and a COX-2 selective inhibitor (celecoxib) for 2 months, for the relief of pain associated with her cancer. The patient was admitted due to swelling of the left leg, which was also accompanied by pain. A computerized tomography scan revealed deep vein thrombosis occurring in multiple veins of both legs. After the administration of low-molecular weight heparin and oral warfarin, the patient's symptoms were relieved initially. However, her prothrombin time was found to be prolonged, necessitating the discontinuation of anticoagulation therapy. The patient's dyspnea worsened, ultimately resulting in her death. In conclusion, the administration of cox-2 selective inhibitors should be carefully considered in patients with a number of different risk factors, and assessed on a case-by-case basis.

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Effectiveness of Multimodal Pain Control in Early Phase After Arthroscopic Rotator Cuff Repair (관절경하 회전근 개 봉합술 후 다중 통증 조절법을 이용한 초기 통증 조절의 유용성)

  • Park, Chang-Min;Kim, Jong-Hae;Kim, Suk-Jun;Choi, Chang-Hyuk
    • Clinics in Shoulder and Elbow
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    • v.15 no.1
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    • pp.1-7
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    • 2012
  • Purpose: The purpose of this study was to identify the effectiveness of multimodal pain control method in an early phase after arthroscopic rotator cuff repair, under interscalene brachial plexus block, this study was performed. Materials and Methods: The study was progressed with the 80 cases of arthroscopic rotator cuff repair. Interscalene brachial plexus block was used to all of the 80 cases and patients were divided into 2 groups. Group A consisted of patients injected with bupivacaine, through subacromial space catheter after surgery, and group B consisted of patients with additional method of multimodal pain control using oral opioids, acetaminophen-tramadol complex and selective COX2 inhibitor. Subacromial cathter was removed after injection in both groups. The pain during the day time and night time was compared on the operation day, postoperative 1st, 2nd, 3rd day and 2nd weeks, and it was measured with VAS (visual analogue scale) score. Additionally, the number of ketolorac injection and side-effect related to analgesics was compared between the 2 groups. Results : The mean VAS score of night time on the operation day and day/night time pain of the 1st, 2nd, 3rd day and 2nd weeks was 7.4, 7.0/6.8, 4.5/5.2, 4.8/5.0, 2.2/2.7 on group A and 6.5, 4.3/5.4, 3.2/4.3, 3.0/4.1, 2.4/2.5 on group B, respectively. Significant difference was observed in the night pain on the operation day, 1st, 2nd, 3rd day time and 1st night time pain (p<.05). The average number of ketololac injection was 1.1 and 0.5 in each group, and there was no difference in the frequency of side effects. Conclusion: Multimodal pain control method, after arthroscopic rotator cuff repair, showed an effective early pain control and improved patients' satisfaction.