• YAKHAK HOEJI
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• v.52 no.1
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• pp.85-91
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• 2008

8-Acyl and 8-sulfonylamidowogonin analogues were synthesized as potential anti-inflammatory agents. Nitration of 5,7-dihydroxyflavone (chrysin) followed by methylation of phenol groups and reduction of nitro group yielded 8-aminowogonin analogues. Acylation and sufonylation of 8-aminowogonin followed by demethylation reactions gave the title compunds. The synthesized wogonin analogues showed much reduced inhibitory activity on prostaglandin $E_2\;(PGE_2)$ production.

• The Korean Journal of Pain
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• v.7 no.2
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• pp.299-302
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• 1994

Prostaglandin E1(PGE1) is a potent vasodilator and is a useful drug for the treatment of occlusive peripheral vascular disease. It has been used systemically via intravenous route or regionally via intraarterial route. We tried intravenous regional administration of PGE1 for the treatment of a patient with occlusive arterial disease involving left fingers. During the 13th injection, the patient complained of severe pain at the injection site during the drug administration. Thereafter, the patient developed painful and severe swelling with blebs on his left hand. Systemic antibiotics were given together with stellate ganglion block of the affected left side. PGE1 was substituted to reserpine, which is subcutaneously injectable, for the second term treatment.

• Journal of Periodontal and Implant Science
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• v.13 no.1
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• pp.61.2-61.2
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• 1983

• Development and Reproduction
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• v.2 no.2
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• pp.179-187
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• 1998

The effects of prostaglandins in hatching and implantation have been studied but the results were various, and those are not well known by the embryonic stage. The present study examined the effects of prostaglandin $E_2$(PG $E_2$) and prostaglandin $F_2$$_{\alpha}$ (PG $F_2$$_{\alpha}$) on the expansion and hatching of mouse embryos by embryonic stage. Also we tried to measure the concentration of prostaglandins of morula, expanded, and hatching embryos. In early morula stage embryos, high concentration of PG $E_2$(>100$\mu$M) showed cytotoxicity but PG $F_2$$_{\alpha}$ did not. The hatching was inhibited all groups but not gave negative effects on expansion. In 84 hr and 96 hr stage embryos, the hatching rate was decreased at all treatment groups but not inhibited the expansion. When combine prostaglandin with indomethacin, the hatching rate was increased significantly compared to the prostaglandin-treated groups, and as lower and lower the PG $E_2$ concentration, the hatching rate increased to the control level. The embryonic synthesis of PG $E_2$ increased dramatically but that of PG $F_2$$_{\alpha}$ increased gradually. PG $E_2$ showed cytotoxicity at early stage embryos much than late stage embryos, but PG $F_2$$_{\alpha}$ did not. Hatching was inhibited by the high PG $F_2$$_{\alpha}$ concentration. It is suggested that the inhibition of hatching might be at resulted from cytotoxicity of PG $E_2$ on embryo. However, it is thought that the mechanisms of inhibition of hatching are different between PG $E_2$ and PG $F_2$$_{\alpha}$. In conclusion, it can be suggested that PG $E_2$ and PG $F_2$$_{\alpha}$ concerned with the expansion and hatching, and their effects on hatching were different by the embryonic stage.$/ concerned with the expansion and hatching, and their effects on hatching were different by the embryonic stage.

• 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 $10\;{\mu}g/ml$.

• Journal of Pharmaceutical Investigation
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• v.35 no.5
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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.

• The Korean Journal of Pharmacology
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• v.11 no.2
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• pp.41-46
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• 1975

The isolated strips of tortoise intestine are evaluated as a test organ for bioassay of prostaglandin $E_1$. This preparation responded highly sensitively to $PGE_1$ and $PGE_2$ in picogram concentration range. The mean slope and the value of precision index among the doses of 0.1, 0.3 and 0.5ng/ml in final concentration were 37.7 and 0.143, respectively. And this was relatively insensitive to different prostaglandins; $E_1/E_2{\gtrsim}1$, $E_1/A_2{\sim}50$ and $E_1/F_{2\alpha}{\sim}100$, and showed the dual responses to 5-hydroxytryptamine and histamine; initial contraction followed by relaxation. The dose-ratio inducing the relative equal contraction height for $PGE_1$, acetylcholine, caerulein, angiotensin and barium chloride was 0.4 : 50 : 25 : 10 : 100 in this order. These results suggest that the intestinal strips of the tortoise are suitable for bioassay of prostaglandin $E_1$ and $E_2$ between the doses of 0.1 and 1.0 ng/ml level in the tissue extracts.

• Journal of Periodontal and Implant Science
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• v.27 no.4
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• pp.909-922
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• 1997

The purpose of this study was to evaluate the effect of high glucose on prostaglandin E2 production in human gingival fibroblasts and periodontal ligament cells in vitro. In control group, the cells($5{\times}10^4\;cells/ml$) were cultured with Dulbecco's Modified Eagle's Medium contained with 10% fetal bovine serum, 45mg/dl glucose. In experimental groups, glucose was added to the above culture condition at the final glucose concentrations of 100mg/dl(Test group 1), 200mg/dl (Test group 2) and 400mg/dl (Test group 3). Then each group was tested for the cell proliferation rate, protein levels, and prostaglandin E2 production at $\frac{1}{2}$, 1, 2, 5 days. The results were as follows : 1. As glucose concentration increased, cell proliferation rate decreased significantly at 1, 2, 5 days in human gingival fibroblasts and periodontal ligament cells(P<0.01). 2. In human gingival fibroblasts, test group 2 and 3 showed significantly decreased protein levels as compared to control group at 5 days (P<0.01). 3. In human periodontal ligament cells, as glucose concentration increased, protein levels decreased significantly at 2 days and 5 days(P<0.01). 4. Prostaglandin $E_2$ production in human gingival fibroblasts and human periodontal ligament cells significantly increased as glucose concentration increased(P<0.01). results at 5 days showed obvious difference as compared to those at 2 days. From the above results, high glucose appeared to affect cellular activities including cell proliferation rate, protein levels and enhance prostaglandin $E_2$ production. It was assumed that prostaglandin E2 production by high glucose enhances inflammatory reaction and has a toxic effect on human gingival fibroblasts and human periodontal ligament cells. This study suggests that periodontal disease in diabetic patient is related to prostaglandin $E_2$ production.

• Journal of Life Science
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• v.10 no.5
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• pp.529-532
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• 2000

Prostaglandin $E_2$(PG$E_2$) is an abundant eicosanoid in bone that has been implicated in a number of pathological states associated with bone loss, and is also known to stimulate matric metalloproteinase-1 systhesis and secretion in rat and human osteoblast cells, although the intracellular reaction remain unclear. Interleukin-1$\beta$ (IL-1$\beta$) is a cytokine that plays a critical role in bone remodelling and appears to act as a downstream effector of most bone-resorbing agents. However, it is still interesting to examine whether PG$E_2$ regulates IL-1$\beta$ expression by mouse osteoblasts or not. Here we demonstrate that PG$E_2$is a potent inducer of IL-1$\beta$ production by fetal osteoblasts.

• BMB Reports
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• v.38 no.6
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• pp.633-638
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• 2005

Biosynthesis of prostanoids is regulated by three sequential enzymatic steps, namely phospholipase $A_2$ enzymes, cyclooxygenase (COX) enzymes, and various lineage-specific terminal prostanoid synthases. Prostaglandin E synthase (PGES), which isomerizes COX-derived $PGH_2$ specifically to $PGE_2$, occurs in multiple forms with distinct enzymatic properties, expressions, localizations and functions. Two of them are membrane-bound enzymes and have been designated as mPGES-1 and mPGES-2. mPGES-1 is a perinuclear protein that is markedly induced by proinflammatory stimuli, is down-regulated by anti inflammatory glucocorticoids, and is functionally coupled with COX-2 in marked preference to COX-1. Recent gene targeting studies of mPGES-1 have revealed that this enzyme represents a novel target for anti-inflammatory and anti-cancer drugs. mPGES-2 is synthesized as a Golgi membrane-associated protein, and the proteolytic removal of the N-terminal hydrophobic domain leads to the formation of a mature cytosolic enzyme. This enzyme is rather constitutively expressed in various cells and tissues and is functionally coupled with both COX-1 and COX-2. Cytosolic PGES (cPGES) is constitutively expressed in a wide variety of cells and is functionally linked to COX-1 to promote immediate $PGE_2$ production. This review highlights the latest understanding of the expression, regulation and functions of these three PGES enzymes.