• 대한한방내과학회지
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• 제25권3호
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• pp.398-407
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• 2004

목적 :천축황(天竺黃)이 골대사에 미치는 영향을 검토하고자 생쥐의 골세포를 이용하여 골흡수 억제 효과를 관찰하였다. 방법 :$Interleukin-1{\beta}\;(IL-1{\beta})$는 시험관내에서 osteoblast를 조절하는 것으로 알려져 있는데, 천축황(天竺黃)이 $IL-1{\beta}$ 유발된 $PGE_2$, 생성에 관한 영향을 관찰하였다. 결과 :천축황(天竺黃)는 osteoblast체 독성을 나타내지 않았으며, $PGE_2$ 생성을 억제하였다. 특히, 천축황(天竺黃)을 1시간동안 전처리한 경우 $PGE_2$의 합성을 억제하여 골세포 보호효과가 인정되었으며, 또한 골 흡수인자인 $IL-1{\beta}$에 의해 유발된 alkaline phosphatase의 활성도 억제하였는데, 천축황(天竺黃) 전처리후 16시간째에 훨씬 높은 억제효과를 나타내었다. 유사하게 천축황(天竺黃)을 1시간 동안 전처리한 경우 osteocalcin의 생성이 증가되었다. 또한, calcitonin이 나타내는 osteoclast및 osteoblast 함유세포에서 골 흡수를 억제하였다. 결론 :천축황(天竺黃)은 osteoclast가 매개된 골흡수를 억제하는 효과가 인정되었다.

• 동의생리병리학회지
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• 제34권1호
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• pp.7-13
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• 2020

Sanyeoleumja (SY) is the traditional Korean medicinal prescription for the treatment of inflammatory diseases of eyes. In this study, the anti-inflammatory effects of SY water extract were investigated. To measure the anti-inflammatory effects of SY, we examined the productions of inflammatory factor including nitric oxide (NO), prostaglandin E2 (PGE₂), inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin-6 (IL-6), interleukin-1β (IL-1β) in lipopolysaccharide (LPS)-induced RAW 264.7 cells. SY inhibited NO and PGE₂ production in a dose dependent manner and decreased the protein and mRNA expression of iNOS and COX-2. Also, SY decreased the mRNA expression of interleukin-6 (IL-6) and interleukin-1β (IL-1β). In conclusion, SY downregulated LPS-induced inflammatory factor productions, which could be a clinical basis for inflammatory diseases.

• Journal of Pharmaceutical Investigation
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• 제29권2호
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• pp.111-115
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• 1999

We have studied the transdermal flux of prostaglandin $E_1$ $(PGE_1)$ from a hydrogel patch through hairless mouse skin, to test the possibility of developing a transdermal delivery system. Karaya gum patch containing $PGE_1$ was prepared by casting method. $PGE_1$ was stable in the patch for 10 weeks. The effect of current application, enhancer (propylene glycol monolaurate : PGML), adhesive and patch thickness on the flux was studied using side-by-side diffusion cell. Passive flux of $PGE_1$ was negligible. Cathodal delivery increased the flux about 20 fold. As the concentrations of PGML increased, flux increased. When 5% PGML was used as the enhancer, maximum flux by cathodal iontophoresis was $55\;{\mu}g/cm^2\;hr$. It increased about 2 folds to $100\;{\mu}g/cm^2\;hr$, when the amount of PGML used was 9%. Large increase in flux and the decrease in time to reach maximum flux were observed when the skin was pretreated with neat PGML (maximum flux obtained was about $200\;{\mu}g/cm^2\;hr$). Use of adhesive decreased the flux significantly. To the contrary of our expectation, increase in current density decreased the flux. These flux data together with the stability data indicate that, though the onset of sufficient delivery occur after 1-2 hours of application, therapeutic amount of $PGE_1$ can be delivered through skin using iontophoresis and penetration enhancer.

• 대한약리학회지
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• 제13권1호
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• pp.13-21
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• 1977

The author confirmed the development of the smooth muscle in the oviduct proprius and anterior mesosalpinx in the leghorn, and observed that there was a variation between the action of norepinephrine on albumin-secreting portion of productive oviduct and that of non-productive one, and that $PGE_1$ might play a significant role on the activation of adrenergic ${\alpha}$-receptor in the non-productive oviduct. 1. There were many bundles of smooth muscles with irregular directions, which were identified in the both oviduct proprius and anterior mesosalpinx by Mallory aniline-blue orange G stain. 2. In vitro experiments, the anterior mesosalpinx was always relaxed by norepinephrine. While the albumin-secreting portion of non-productive period of oviduct was relaxed, but that of the productive one contracted by norepinephrine. Both the anterior mesosalpinx and oviduct proprius of chick responsed with relaxation to norepinephrine as shown in the non-productive hen. In vivo experiments, norepinephrine injected through the jugular vein increased the intraoviductal pressure in the productive oviduct, but decreased that in the non-productive one. 3. By treatment with $PGE_1$, in vitro, the relaxation induced not only by norepinephrine, but by periarterial electrical stimulation was converted into contraction, and in the presence of phentolamine, this conversion by $PGE_1$ was not shown. 4. The intra-oviductal pressure of the productive hen treated with indomethacin for 4 days was decreased by norepinephrine, but the increase in pressure by $PGE_1$ or $PGE_{2{\alpha}}$ was supersensitized when these drugs were administered through jugular vein. However, in vivo, the relaxation by norepinephrine was not converted into the stimulation after $PGE_1$ treatment. It might be summarized that the regulation of intra-oviductal pressure was dependent on the summation of the movement of both oviduct and mesosalpinx and intramurally produced prostaglandins contributes to the inherent tone of the prcductive oviduct by activating adrenergic ${\alpha}$-receptor.

• Archives of Plastic Surgery
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• 제32권1호
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• pp.5-11
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• 2005

Prostaglandin $E_1$($PGE_1$) is known to have various physiological action such as vasodilatation, decrease of blood pressure, angiogenesis, inhibition of platelet aggregation and so forth. $PGE_1$ has been developed in many different formulations in order to overcome its chemical instability and deactivation in the lungs when administered parenterally. Lipo-AS013 is a potent drug with higher chemical stability and greater vascular wall targeting than others. The study was done on $3{\times}10cm$ model flap of dorsal skin of Sprague-Dawley rats and the flap perfusion survival were observed and documented. The flap treated with Lipo-AS013 beforehand was given intravenously Sodium fluorescein 10 minutes later, and then Percent Dye Fluorescence Index(% DFI) was calculated. The results were compared to a control group and the group administered locally epinephrine.. In the control group, the % DFI and flap survival rate increased from $54.1{\pm}6.7$ to $65.0{\pm}2.6$(p<0.01) while in Lipo-AS013 group from $55.3{\pm}2.2$ to $67.4{\pm}1.9$(p<0.01), respectively. In the epinephrine group, the % DFI(p<0.05) and flap survival rate(p<0.001) decreased. In the both epinephrine and Lipo-AS013 group Percent DFI and flap survival rate are comparable with the control group.The result indicates that the potent Lipo-AS013 enhances the blood flow and flap survival. This highly potent Lipo-AS013 may have targeting ability and accumulate $PGE_1$ onto the vascular walls. A quantitative analysis of fluorescence on the skin surface is a reliable tool to measure the blood perfusion into an ischemic flap and its viability. Further comparative study with conventional $PGE_1$ and Lipo-$PGE_1$ is needed in order to clarify the action and efficiency of Lipo-AS013.

• Biomolecules & Therapeutics
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• 제17권4호
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• pp.418-421
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• 2009

Structural alterations of wogonin were conducted to observe the role of each functional group at the A-ring of wogonin on the inhibitory activities against COX-2 catalyzed $PGE_2$ production from LPS-induced RAW 264.7 cells. Serial deletion of the functional groups at the A-ring of wogonin exhibited low to comparable bioactivity. The present study validated that all the functional groups at the A-ring of wogonin are important factors to exhibit the optimum inhibitory activities.

• 약학회지
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• 제55권6호
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• pp.462-465
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• 2011

Chrysin analogs with 2-heteroaryl groups were synthesized and evaluated for their inhibitory activities against $PGE_2$ and NO production from LPS-induced RAW 264.7 cells. Chrysin analogs were synthesized from 2-hydroxy-4,6-dimethoxy-acetophenone and heteroaryl aldehydes in 3 steps. The tested chrysin analogs showed decreased inhibitory activity against $PGE_2$ and NO production than those of chrysin.

• 대한약리학회지
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• 제11권2호
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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.

• Archives of Pharmacal Research
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• 제26권5호
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• pp.345-350
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• 2003

5,7-Dihydroxyflavones and their Ο-methylated flavone analogs were prepared and evaluated their anti-inflammatory activity to decipher the structure-activity relationships. Most of the analogs were achieved from 2,4,6-trihydroxyacetophenone in 4 steps. 5,7-Dihydroxy-4 -methoxyflavone (4c) and 7-hydroxy-4 ,5-dimethoxyflavone(6c) were prepared following a different synthetic pathway. Among the synthetic flavones tested, 5-hydroxy-7-methoxyflavone analogs (3a-3e) showed moderate inhibitory activities of $PGE_2$ production from LPS-induced RAW 264.7 cells.

• Archives of Pharmacal Research
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• 제26권8호
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• pp.581-584
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• 2003

Vinylated and allylated chrysin analogues were prepared as congeners of prenylated flavonoids and evaluated their anti-inflammatory activity. 8-Substituted chrysin analogues were prepared from 2 -hydroxy-3 -iodo-4 ,6 -dimethoxyacetophenone in 3 steps. 3-Allylated chrysin analogues were prepared from chrysin in 3 steps. Synthesized chrysin analogues (4, 5 and 8) showed moderate inhibitory activities of $PGE_2$ production from LPS-induced RAW 264.7 cells.