• Journal of Pharmaceutical Investigation
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• 제35권5호
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• pp.375-381
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• 2005

A rapid and specific high-performance liquid chromatographic method was developed and validated for the simultaneous determination of prostaglandin $E_{1}\;(PGE_{1})$ and prostaglandin $E_{1}$ ethyl ester $(PGE_{1}-EE)$ in hairless mouse skin homogenate. The sample treatment procedure involved deproteination and precipitation by acetonitrile. $PGE_{1}$ and $PGE_{1}-EE$ in supernatant were separated in a reversed-phase C18 column without being interfered by other components present in hairless mouse skin homogenate. 9-Anthracenecarboxylic acid was used as an internal standard. The retention times of $PGE_{1}$, 9-anthracenecarboxylic acid and $PGE_{1}-EE$ were, 4.5, 9.5 and 18.0 min, respectively. The assay showed linearity from 1 to $40\;{\mu}g/ml$ for both $PGE_{1}$ and $PGE_{1}-EE$. Precision expressed as RSD ranged from 2.3 to 14.1 % for $PGE_{1}$ and 1.6 to 11.0% for $PGE_{1}-EE$. Accuracy ranged from 100.5 to 119.6 % for $PGE_{1}$ and from 98.0 to 103.7% for $PGE_{1}-EE$. This method was employed successfully to follow the time course of concentrations of $PGE_{1}$ and $PGE_{1}-EE$ in hairless mouse skin homogenate for stability study.

• 예술인문사회 융합 멀티미디어 논문지
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• 제9권6호
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• pp.443-450
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• 2019

본 연구에서는 갈퀴나물(Vicia amoena) 전초를 이용한 에탄올 추출물의 세포독성과 항염증 활성 효과를 평가하였다. RAW264.7 cell(대식세포)에서 염증 매개 물질인 lipopolysaccharide(LPS)로 염증을 유발시켜 nitric oxide (NO) 및 prostaglandin E₂ (PGE₂)같은 염증 유발 인자들의 생성 저해효과를 확인하였다. 갈퀴나물 에탄올 추출물의 염증 유발 인자 억제 시 저해효과를 측정하였을 때 nitric oxide 및 prostaglandin E₂ 생성을 농도 의존적으로 현저하게 저해하는 농도인 40 ㎍/㎖의 농도에서 LPS에 의해 유도된 NO를 36.0 ± 0.5 % 저해하였으며, 특히 PGE₂에서는 88.0 ± 0.8 % 만큼 유의성 있는 저해효과를 나타내었다. 따라서 본 연구결과는 갈퀴나물의 에탄올 추출물이 유의성 있는 항염증 효과를 나타내며, 이러한 효능은 예방의학적 가능성을 충분히 가지고 있기에 염증성 질환의 예방을 위한 항염증 소재로의 개발 가능성을 제시할 수 있을 것으로 기대된다. 차후 에탄올 추출물의 보다 다양한 농도 및 유기용매 분획물에서 염증반응을 매개하는 iNOS·COX-2 등 의 다양한 효소의 발현과 Iκ-Bα의 분해 등 염증반응의 신호전달물질의 변화에 대한 추가적인 연구가 필요할 것으로 판단된다.

• 약학회지
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• 제36권6호
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• pp.570-576
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• 1992

The treatment with gentamicin in the presence of pretreatment with bismuth nitrate significantly reduced blood urea nitrogen compared with given gentamicin alone. But the amelioration of gentamicin-induced nephrotoxicity by bismuth nitrate was abolished by pretreatment with indomethacin that is cyclooxygenase inhibitor, which significantly decreased renal glutathione S-transferase activity and thiobarbituric acid reactive substance compared with mice of given gentamicin and bismuth nitrate. On the other hand, treatment with bismuth nitrate significantly increased prostaglandin $E_2$ production in rat kidney slice. These results suggest that bismuth nitrate might ameliorate the nephrotoxicity of gentamicin via prostaglandin $E_2$ production.

• Biomolecules & Therapeutics
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• 제3권1호
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• pp.72-79
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• 1995

The antiulcer effects of newly synthesized prostaglandin derivatives were investigated in various experimental ulcer models and on gastric secretion in rats. HK-3 and HK-4, PG $E_2$derivatives, prevented the formation of acute gastric ulcer induced by ethanol or aspirin in pylorus-ligated rats. The ulcer formation was moderately inhibited by HK-1 and HK-2, PG $F_{2{\alpha}}$ derivatives, and aggravated by SK-1, SK-2 and SK-3, PG $F_{2{\alpha}}$ derivatives. HK-3 and HK-4 reduced the volume, acid output and pepsin output of gastric juice in pylorus-ligated rats. The gastric perfusion with physiologic saline(pH 6.0) showed relatively constant acid secretion and indomethacin increased the acid secretion. The acid secretion was markedly decreased by PG $E_2$but PG $F_{2{\alpha}}$ caused little change. Prostaglandin derivatives, especially HK-3 arid HK-4, significantly inhibited the acid secretion induced by indomethacin. The results show that, PG $E_2$ derivatives, HK-3 and HK-4, inhibit acid secretion and also have protective effects on gastric ulceration induced by ethanol or aspirin.

• 대한약침학회지
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• 제5권2호
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• pp.40-51
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• 2002

Objectives : The purpose of this study was to investigate the effect of Bee Venom on the lipopolysaccharide-induced expression phospholipase $A_2$, cyclooxygenase-2 and inducible nitrogen oxide synthase, and the generation of arachidonic acid, prostaglandin D2 and E2 in RAW 264.7 cells, a murine macrophage cell line. Methods : The expression of phospholipase $A_2$, cyclooxygenase and inducible nitrogen oxide synthase was determined by western blotting with corresponding antibodies, and the generation of arachidonic acid, prostaglandin $D_2$ and $E_2$ was assayed by ELISA method in RAW 264.7 cells. The non-toxic concentrations (0.1 to $5\;{\mu}g/ml$) of bee venom determined by MTT assay, were used in this study. Results : 1. Bee venom inhibited lipopolysaccharide-induced expression of phospholipase $A_2$ in a dose dependent manner after 48 hours treatment. 2. Bee venom inhibited lipopolysaccharide-induced expression of cyclooxygenase-2 in a dose dependent manner after 24 and 48 hours treatment. 3. Bee venom inhibited lipopolysaccharide-induced expression of inducible nitrogen oxidesynthase in a dose dependent manner after 48 hours treatment. 4. The generation of arachidonic acid, prostaglandin $D_2$ and $E_2$ was not much affected by the treatment of bee venom on the lipopolysaccharide-induced generation of arachidonic acid, prostaglandin $D_2$ and $E_2$ in RAW 264.7 cells.

• 동의생리병리학회지
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• 제20권2호
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• pp.455-459
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• 2006

The inhibitors of prostaglandin $E_2\;(PGE_2)$ production and cyclooxygenase-2 (COX-2) activity have been considered as potential anti-inflammatory agents. In this study, we evaluated 9 compounds isolated from 5 Korean phytomedicinal plants (Spirea prunifolia, Paeonia suffruticosa, Salvia miltiorrhiza, Scutellaria baicalensis, and Artemisia capillaris) for the inhibition of $PGE_2$production and COX-2 expession in lipopolysaccharide (LPS)-stimulated human macrophages U937 cells. As a result, several compound such as prunioside A, penta-O-galloyl-beta-D-glucose, tanshinone IIA, baicalin, baicalein, wogonin, scopolatin, scoparone and decursinol showed potent inhibition of $PGE_2$production (50-70% inhibition at the test concentration of $10\;{\mu}M$). In addition, these compounds were also considered as potential inhibitors of COX-2 activity (45-73% inhibition at the test concentration of $10\;{\mu}M$). These active compound mediating COX-2 inhibitory activities are warranted for further elucidation of active principles for development of anti-inflammatory agents and these properties may contribute to the anti-atopic dermatitis activity.

• Archives of Reconstructive Microsurgery
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• 제9권2호
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• pp.190-198
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• 2000

본 연구는 백서 복직근피판에 있어 허혈-재혈류 손상에 미치는 prostaglandin E1(PGE-1)의 예방효과를 분석 실험하였으며, 그 기전으로 내피세포의 intercellular adhesion molecule-1(ICAM-1)이 down regulation 됨을 확인하였다. 기존의 PGE-1은 혈관 확장 및 혈소판 응고 저하 등의 기전으로 피판 이식술 후 주로 사용하였으나, 허혈-재혈류 손상 시에 PGE-1 역할에 대한 연구는 잘 알려진바 없다. 허혈-재혈류 손상에 대한 기전은 현재 여러 가설로 설명되고 있으나, 최근 내피 세포와 백혈구의 역할이 주목을 받고 있다. 장시간 허혈 상태의 피판은 재혈류시 백혈구가 내피세포에 접착함으로써 직간접적인 경로로 독소를 생성하며, 결국 내피세포 및 주변조직의 괴사로 이어진다. 본 연구는 면역조직학 염색을 통한 내피세포의 ICAM-1 발현 억제와 그로 인한 백혈구의 내피세포 접착 억제를 그 기전으로 볼 수 있었으며, PGE-1을 술 중 투여함으로써 피판의 생존율을 향상시킬 수 있었다.

• The Korean Journal of Pain
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• 제19권1호
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• pp.101-103
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• 2006

Oral prostaglandin E1 (PGE1) is a medicine that is clinically applied during a treatment of patients suffering with vascular disease with chronic arterial obstruction because it has vasodilation and anti-platelet effects. The mechanisms of lumbosacral symptoms associated with spinal stenosis probably include vascular insufficiency with hypoxic injury to the cauda equina and the nerve roots. Thus, increasing the blood supply would be beneficial to improve the pathophysiologic condition. Several studies on the improvement of clinical symptoms of spinal stenosis by PGE1 treatment have been reported on. In this case, 47-year old female underwent posterior compression and posterolateral fusion with a cage at L2-4 due to L3 compression fracture, and she did not show improvement of the radiating pain of her right leg after the operation. Therefore, she received repetitive epidural catheterization and adhesiolysis, epidural block and physical therapy, but her symptoms deteriorated after temporary improvement. Finally, she was given PGE1 and the radiculopathy was completely improved, although some muscle weakness still remained.

• BMB Reports
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• 제41권11호
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• pp.808-813
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• 2008

Human microsomal prostaglandin E synthase-1 (mPGES-1) is a membrane associated protein that catalyzes the conversion of prostaglandin $H_2$ ($PGH_2$) into prostaglandin $E_2$ ($PGE_2$). In this study, the expression of human mPGES-1 in E. coli was significantly enhanced by modifying the utility of specific codons and the recombinant mPGES-1 was efficiently purified to homogeneity. The $K_m$ and $V_{max}$ of the purified enzyme were determined and the trimeric state characterized by chemical cross-linking with glutaraldehyde. The purified mPGES-1 was used for the screening of a chemical library of bioactive or drug compounds to identify novel inhibitors, and oxacillin and dyphylline were identified as moderately inhibiting mPGES-1 with $I_{C50}$ values of 100 and 200 ${\mu}M$, respectively. As these compounds competitively inhibited the catalysis of $PGH_2$, their binding sites appeared to be located near the $PGH_2$ binding pocket.

• The Korean Journal of Physiology
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• 제17권1호
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• pp.63-69
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• 1983

This study was conducted to investigate the effect of prostaglandin $E_2(PGE_2)$ and indomethacin upon the electrical activity of the isolated cat stomach muscle strips$(1.5{\times}7.0\;cm)$. Fifty-seven muscle strips, obtained from 57 cat stomachs(including corpus and antrum) were studied in a muscle chamber filled with Krebs solution(pH 7.4, temperature $36{\pm}0.5^{\circ}C$) aerated with 5% $CO_2$ in $O_2$. The electrical activity was recorded by five capillary electrodes (Ag-AgCl), of which two were placed on the corpus and three on the antrum. After recording of the electrical activity in normal Krebs solution, $PGE_2$ in concentrations of 0.25(N=7), 0.5(=7), 1(N=7) and $2{\times}10^{-7}\;M(N=6)$ were administered to 27 muscle strips, while indomethacin was applied in concentretions of 0.25(N=9), 0.5(N=10), 1(N=6) and $2{\times}10^{-3}\;M(N=5)$ to the remaining 30 strips. The mean frequency were minutely measured from each electrogastrogram. 1) By adding $PGE_2$ in all doses, gastric slow wave frequency increased significantly compared with that in resting state. 2) Following $PGE_2$ administration, peak slow wave frequency increased dose-dependently. 3) After indomethacin addition in all doses, the slow wave frequency decreased significantly compared with that in resting state. 4) Following indomethacin administration, incidence of complete abolition of slow wave increased dose-dependently, and its latent period decreased also in a dose-dependent manner. It is inferred from the above results that prostaglandin $E_2$ has a facilitatory role in the development of gastric slow wave in cat.