• Title/Summary/Keyword: prostaglandin E2

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THE CONCENTRATIONS OF PROSTAGLANDIN E2, 6-KETO-PROSTAGLANDIN F1α, AND LEUKOTRIENE B4 IN PULPAL AND PERIAPICAL LESIONS (치수 및 치근단병소에서 Prostaglandin E2, 6-keto-Prostaglandin F1α, Leukotriene B4의 분포에 관한 연구)

  • Shon, Won-Jun;Baek, Seung-Ho;Lim, Sung-Sam
    • Restorative Dentistry and Endodontics
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    • v.25 no.2
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    • pp.193-201
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    • 2000
  • Prostaglandins (PGs) and Leukotrienes (LTs) have been implicated in the genesis of pulpal and periapical inflammation. In this study, the relationships among $PGE_2$, 6-keto-PG $F_1{\alpha}$ (a stable metabolite of $PGI_2$) and $LTB_4$ concentrations in inflamed pulp and periapical lesions were discussed. Pulp tissue were obtained in routine endodontic treatment and periapical lesions in periapical surgery after clinical diagnoses were made. These specimens were divided into four groups as normal pulp group (Control group), acute pulpitis group, chronic pulpitis group, and periapical lesion group. Pulp tissue and periapical lesions were stored in liquid nitrogen. The concentration of $PGE_2$, $PGI_2$ and $LTB_4$ were measured with ELISA. The data were analyzed by one-way ANOVA. Significantly higher levels of $PGE_2$, 6-keto-PG $F_1{\alpha}$ a and $LTB_4$ were found in acute pulpitis group than chronic pulpitis group and periapical lesion group(p<0.05). Periapical lesion group showed significantly higher mean concentrations of $PGE_2$ and $LTB_4$ than chronic pulpitis group. In control and chronic pulpitis group, significant higher levels of $PGI_2$ than $PGE_2$ and $LTB_4$ were found. These results suggested that the high levels of $PGE_2$ and $LTB_4$ in periapical lesions may be due to rich endothelium., fibroblast and lymphocyte known as the main producers of $PGE_2$ and $LTB_4$. $PGI_2$ may be thought to one of the most abundant PGs in normal pulp tissue.

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Inhibitory Effects of of Tacrine Derivatives on Activity of Prostanoids Biosynthesis Prostaglandin Biosynthesis: A Potential Use for Degenerative Brain Disease Treatment (퇴행성 뇌질환 치료제 Tacrine 유도체의 프로스타글란딘 생합성 억제효과)

  • Shin Hea Soon
    • YAKHAK HOEJI
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    • v.49 no.1
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    • pp.103-108
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    • 2005
  • Tacrine analogues for degenerative brain disease treatments have been designed. A series of diazaanthrine derivatives as novel analogues of tacrine has been prepared through the alkyl substitution and the ring expansion. They were expected to retain anti-inflammatory activity by inhibition of prostaglandin production with reduction of side effect as the selective prostaglandin synthase inhibitor. Prostaglandin synthase expression is associated with the deposition of beta-amyloid protein in neuritic plaques in brain inflammation. Therefore selective prostaglandin synthase blockade is important for the prevention and treatment of alzheimer's disease. To evaluate inhibitory effect of prostaglandin synthase, synthetic tacrine derivatives were screened with accumulation of prostaglandin biosynthesis by lipopolysaccharide in aspirin-treated murine macrophage cell. Most of synthetic compounds have shown significant prostaglandin synthase activities in vitro screening with $84.3{\sim}33.6\%$ inhibition of the prostaglandin $E_2$ production at $10\;{\mu}g/ml$.

Antiproliferative Effect of Chungjogupae-tang Treatment was Associated with the Inhibition of Prostaglandin E2 Release in Human Lung Carcinoma Cells (인체폐암세포의 증식 및 prostaglandin E2 생성에 미치는 청조구폐탕의 영향에 관한 연구)

  • Im, Jae-Hyung;Kim, Hoon;Byun, Mi-Kyeon;Kam, Chul-Woo;Park, Dong-Il
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.20 no.4
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    • pp.966-972
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    • 2006
  • The effect of water extract of Chungjogupae-tang (CJGPT) was investigated _on the growth of human lung carcinoma A549 cells. Methods: MTT assay and fluorescent microscope peformed to compare and examine the efficacy of CJGPT treatment on the cytostaticity of lung cancer cells in proportion to time and doses, and DAPI staining and Western blot analysis were used to examine their effect on apoptosis. In addition, the quantitative RT-PCR was used to examine to lung cancer cells growth, and Prostaglandin E2 activity were measured. Results: Exposure of A549 cells to CJGPT respited in the growth inhibition and apoptosis in a dose-dependent manner as measured by MTT assay and fluorescent microscope. The antiproliferative effect by CJGPT treatment in A549 cells was associated with morphological changes such as membrane shrinking and cell rounding up. CJGPT treatment resulted in an up-regulation of cyclin-dependent kinase inhibitor p21 (WAFl/CIPl) in a p53-independent fashion. We found that CJGPT treatment decreased the levels of cyclooxygenase (COX)-2 and inducible nitric oxide synthease (iNOS) expression without significant changes in the expression of COX-1 , which was correlated with a decrease in prostaglandin E2 (PGE2) synthesis. Conclusion: These findings suggested that CJGPT-induced inhibition of human lung carcinoma A549 cell growth was connected with the induction of apoptotic cell death and the results provided important new insights into the possible molecular mechanisms of the anti-cancer activity of CJGPT.

Development of a Coupled Enzyme Assay Method for Microsomal Prostaglandin E Synthase Activity

  • Choi, Kyung-A;Park, Sung-Jun;Yu, Yeon-Gyu
    • Bulletin of the Korean Chemical Society
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    • v.31 no.2
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    • pp.384-388
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    • 2010
  • Human microsomal prostaglandin E synthase-1 (mPGES-1) catalyzes the conversion of prostaglandin $H_2$ ($PGH_2$) into prostaglandin $E_2$ ($PGE_2$). To establish a stable and efficient method to assess the activity of mPGES-1, a coupled enzyme assay system using mPGES-1, 15-hydroxyprostaglandin dehydrogenase (15-PGDH) and phosphomolybdic acid (PMA) was developed. In this assay system, $PGH_2$ was converted to $PGE_2$ by mPGES-1, and then $PGE_2$ was further transformed to the 15-keto-$PGE_2$ by 15-PGDH accompanying the production of NADH, which was easily detected by fluorescence spectrometry in a multi-well plate format. During the reaction, spontaneous oxidation of $PGH_2$ was prevented by PMA. Using this novel assay, the $K_m$ value of mPGES-1 for $PGH_2$ and the $IC_{50}$ value of the previously characterized inhibitor, MK-886, were determined to be 0.150 mM and $2.8\;{\mu}M$, respectively, which were consistent with the previously reported values. In addition, low backgrounds were observed in the multi-wall plate screening of chemical compounds.

Extracellular Prostaglandin $E_2$ Upregulation Effect of the Methanol Extract of Artemisia argyi

  • Lee, Kyoung In;Moon, Young Sook;Pyo, Byoung Sik;Choi, Chul Hee
    • Natural Product Sciences
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    • v.18 no.4
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    • pp.211-214
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    • 2012
  • Since 15-hydroxyprostaglandin dehydrogenase (15-PGDH) is the key metabolic enzyme of prostaglandin $E_2$ ($PGE_2$), inhibition of 15-PGDH is supposed to facilitate various physiological functions by increasing $PGE_2$. Methanol extract of Artemisia argyi (AAME) inhibited 15-PGDH ($IC_{50}$: $13.13{\mu}g/mL$) with relatively low cytotoxicity ($IC_{50}$: $415.00{\mu}g/mL$) and elevated extracellular $PGE_2$ levels in HaCaT cells. Real-time PCR analysis showed that AAME decreased significantly mRNA expression of PG transporter (PGT) in HaCaT cells. These results indicate that AAME could be applicable to functional materials as a 15-PGDH inhibitor and PGT expression inhibitor for the upregulation of extracellular $PGE_2$ level.

Effects of Exogenous Oxytocin on Steroid Hormones and Oxytocin Receptor Concentrations in Pregnant Rats (Oxytocin 투여가 임신 Rat의 Steroid Hormones 및 Oxytocin Receptors 농도에 미치는 영향)

  • 박용수;조현수;변명대
    • Korean Journal of Animal Reproduction
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    • v.26 no.2
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    • pp.183-192
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    • 2002
  • The present studies were carried out to examine the effects of exogenous oxytocin(OT) on plasma, uterine and placenta of estradiol-17$\beta$, progesterone, prostaglandin F$_2$$_{\alpha}$ (PGF$_2$$_{\alpha}$), Prostaglandin E$_2$(PGE$_2$) and OT receptor concentrations in pregnant rats. Pregnant rats received an injection of exogenous OT on days 14, 16, 18, 20, 22 of pregnancy and day 1 of postpartum. Concentrations of plasma estradiol-17 $\beta$ after OT injection started to increase after day 18 and peaked on day 22 of pregnancy but decreased on day 1 of postpartum. Plasma progesterone concentrations declined gradually from day 18 of pregnancy and decreased more rapidly until postpartum 1 day. Concentrations of estradiol-17$\beta$in uterine tissues after OT injection were sharply increased from day 20 to 22 of pregnancy and progestrone concentrations were peaked on day 16 and decreased rapidly from day 16 to 20 and maintained the same level until day 1 of postpartum. Uterine concentrations of PGF$_2$$_{\alpha}$ and PGE$_2$increased gradually until day 20 and peaked on day 22 of pregnancy but showed a marked decrease on day 1 of postpartum. Concentrations of PGF$_2$$_{\alpha}$ in placental tissues increased rapidly from day 14 of pregnancy and decreased sharply on day 1 of postpartum. Concentrations of PGE$_2$increased gradually after day 14 and peaked on day 20 of pregnancy. The concentration of OT receptor in uterus was significantly elevated from day 20 and rose to maximum on day 22 of pregnancy. These findings show that OT suppress the concentration of progestrone and stimulate productions of estradiol-17 $\beta$, PGF$_2$$_{\alpha}$, PGE$_2$ and oxytocin receptor concentrations in pregnant rats.

Harpagophytum Procumbens Suppresses Lipopolysaccharide Induced Expressions of Cyclooxygenase-2 and Inducible Nitric Oxide Synthase in Mouse BV2 Microglial Cells

  • Cho, Hyun-Chol;Song, Yun-Kyung;Lim, Hyung-Ho
    • The Journal of Korean Medicine
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    • v.26 no.4
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    • pp.152-161
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    • 2005
  • The excessive release of proinflammatory products by activated microglia causes neurotoxicity, and this has been implicated in the pathogenesis of neurodegenerative diseases. Harpagophytum procumbens (Pedaliaceae) has been widely used for the treatment of pain and arthritis in the clinical field. In this study, we investigated the effect of Harpagophytum procumbens against lipopolysaccharide-induced inflammation. From the present results, the aqueous extract of Harpagophytum procumbens was shown to suppress prostaglandin-E2 synthesis and nitric oxide production by inhibiting the lipopolysaccharide-stimulated enhancement of cyclooxygenase-2 and inducible nitric oxide synthase expressions in mouse BV2 microglial cells. These results suggest that Harpagophytum procumbens may offer a valuable means of therapy for the treatment of brain inflammatory diseases by attenuating lipopolysaccharide-induced prostaglandin-E2 synthesis and nitric oxide production.

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Prostaglandin E2 Up-regulation and Wound Healing Effect of the Ethanol Extract of Eriobotryae Folium in Human Keratinocyte (피부 각질세포에 대한 비파엽 에탄올 추출물의 PGE2 조절 작용과 상처치료 효과)

  • Im, Do Youn;Lee, Kyoung In
    • Korean Journal of Medicinal Crop Science
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    • v.22 no.6
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    • pp.457-462
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    • 2014
  • Prostaglandin (PG) $E_2$ is an important mediator of skin wound healing without excessive scarring and gastric ulcer healing. However, $PGE_2$ has a short lifetime in vivo because it is metabolized rapidly by 15-hydroxyprostaglandin dehydrogenase (15-PGDH). Ethanol extract of Eriobotryae folium (EFEE) elevated intracellular and extracellular $PGE_2$ levels in HaCaT cells and inhibited 15-PGDH ($ED_{50}$ : $168.4{\mu}g/mL$) with relatively low cytotoxicity ($IC_{50}$ : $250.0{\mu}g/mL$). Real-time PCR analysis showed that mRNA expression of cyclooxygenase (COX)-1 and COX-2 enzymes were increased and prostaglandin transporter (PGT) was decreased in HaCaT cells by EFEE. Moreover, wound healing effect of EFEE ($168.4{\mu}g/mL$) was comparable to that of TGF-${\beta}1$ (300 pg/mL) as a positive control. These results demonstrate that EFEE may be valuable therapeutic materials for the treatment of $PGE_2$ level dependent diseases.

Effects of Yukmijihwangwon on Hypoxia of Neuronal Cells (저산소상태에서 육미지황원의 뇌신경세포 보호효과에 대한 연구)

  • Kang, Bong-Joo;Hong, Seong-Gil;Cho, Dong-Wuk
    • Korean Journal of Oriental Medicine
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    • v.7 no.1
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    • pp.115-124
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    • 2001
  • Yukmijihwangwon (YM) has been known to reinforce the vital essence and have antioxidant activities. This study was designed to examine the inhibitory effects of YM against in vitro hypoxia/reperfusion-induced inflammatory response. We have characterized the production of prostaglandin $E_2$ and arachidonic acid during hypoxia/reperfusion in the human neuroblastoma SK-N-MC and human monocytic macrophage U937 cells and the ingibitory effect of YM on these inflammation-related substance formation has been found out in this study. To investigate inhibition of COX expression by YM during hypoxia in vitro. This result suggested that YM used in this experiment reinforced antiinflammatory potentials and protected cells against hypoxia/reperfusion induced inflammatory response.

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