• 대한치과교정학회지
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• 제13권2호
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• pp.147-154
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• 1983

This experiment was performed to study the effect of $PGE_2$ on the bone resorption at the tooth movement by orthodontic force. The experimental animals were the Sprague-Dawley strain rats. The orthodontic force was applied by the insertion of separating clamp made of 0.014' (0.356mm) wire to the interproximal site between the 2nd and the 3rd upper right molars. In experiment I, $0.2{\mu}g,\;0.4{\mu}g,\;0.8{\mu}g,\;and\;1.0{\mu}g\;PGE_2$ were locally injected at the submucosa near the 2nd molar of the maxilla each. The effect was detected by the count of the number of osteoclasts appeared at the compressed surface of interradicular bone. In experiment II, 1.0 mg/kg indomethacin (a specificc inhibitor of prostaglandin synthetas.) was subcutaneously injected. The effect was examined by the count of the number of cateoclasts appeared at the compressed surface of interradicular bone. The obtained results were follows; 1. The number of osteoclasts on the compressed surface of the interradicular bone increased in proportion to the increased dosage of $PGE_2$ administered. The number of osteoclasts increased significantly at the administration of $0.8{\mu}g\;and\;1.0{\mu}g\;PGE_2$ in contrast to the control (P<0.05). 2. The administration of 1.0 mg/kg indomethacin decreased the number of osteoclasts at the compressed bony surface significantly (P<0.01).

• IMMUNE NETWORK
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• 제6권3호
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• pp.123-127
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• 2006

Background: Caveolin-1 is a principal component of caveolae membranes in vivo. Although expression of caveolae structure and expression of caveolin family, caveolin-1, -2 and -3, was known in chondrocytes, the functional role of caveolae and caveolins in chondrocytes remains unknown. In this study, we investigated the role of caveolin-1 in articular chondrocytes. Methods: Rabbit articular chondrocytes were prepared from cartilage slices of 2-week-old New Zealand white rabbits by enzymatic digestion. Caveolin-1 cDNA was transfected to articular chondrocytes using LipofectaminePLUS. The cyclooxygenase-2 (COX-2) expression levels were determined by immunoblot analysis, immunostaining, immunohistochemistry, and prostaglandin $E_2\;(PGE_2)$ assay was used to measure the COX-2 activity. Results: Ectopic expression of caveolin-1 induced COX-2 expression and activity, as indicated by immunoblot analysis and $PGE_2$ assay. And also, overexpression of caveolin-1 stimulated activation of p38 kinase and ERK-1/-2. Inhibition of p38 kinase and ERK-1/-2 with SB203580 and PD98059, respectively, led to a dose-dependent decrease COX-2 expression and $PGE_2$ production in caveolin-1-transfected cells. Conclusion: Taken together, our data suggest that ectopic expression of caveolin-1 contributes to the expression and activity of COX-2 in articular chondrocytes through MAP kinase pathway.

• Biomolecules & Therapeutics
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• 제23권5호
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• pp.458-464
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• 2015

Sennoside A (erythro) and sennoside B (threo) are dianthrone glycosides and diastereomers. We investigated their abilities to prevent the gastric lesions associated with diseases, such as, gastritis and gastric ulcer. To elucidate their gastroprotective effects, the inhibitions of $HCl{\cdot}tOH$-induced gastritis and indomethacin-induced gastric ulcers were assessed in rats. It was observed that both sennoside A and sennoside B increased prostaglandin $E_2$ ($PGE_2$) levels and inhibited $H^+/K^+$-ATPase (proton pump). In a rat model, both compounds reduced gastric juice, total acidity and increased pH, indicating that proton pump inhibition reduces gastric acid secretion. Furthermore, sennoside A and B increased $PGE_2$ in a concentration-dependent manner. In a gastric emptying and intestinal transporting rate experiment, both sennoside A and sennoside B accelerated motility. Our results thus suggest that sennoside A and sennoside B possess significant gastroprotective activities and they might be useful for the treatment of gastric disease.

• Journal of Pharmaceutical Investigation
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• 제30권3호
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• pp.173-178
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• 2000

The purpose of this work is to develop a transurethral suppository containing prostaglandin $E_1\;(PGE_1)$, which stabilizes the drug, gives no irritation to physiological body and enhances the erectile response of $PGE_1.\;PGE_1$ transurethral suppositories were prepared with various amounts of compositions such as saturated polyglycolysed glyceride $(Suppocire^{\circledR}\;AP,\;SAP)$, polyoxyethylene hydrogenated castor oil (HCO-50) and ethanol. The melting points, viscosities and $PGE_1$ release of the suppositories were investigated. Ocular irritation test was carried out after application of $PGE_1$ suppository to rabbit's eye. The intracavernous pressure (ICP), penile length and duration of erectile response were determined after transurethral administration of $PGE_1$ suppository and compared with those after intracavernosal injection of $PGE_1$ solution to cats. HCO-50 hardly affected the melting points and viscosities of $PGE_1$ suppositories. Additionally, $PGE_1$ transurethral suppositories, whose melting point ranges was $34-35^{\circ}C$, was speedily melted in physiological body. HCO-50 significantly decreased the dissolution rates of $PGE_1$ from the suppositories. Dissolution mechanism analysis showed the release of $PGE_1$ was proportional to the square root of time, indicating that $PGE_1$ might be released from the suppositories by Fickian diffusion. The release rate of $PGE_1$ from $PGE_1$ suppository [PGE1/SAP/HCO-50/ethanol (1/94.5/2.5/2%)] was about 80% within 2 h. This $PGE_1$ suppository gave no significant irritation to the ocular tissue, expecting that it gave no irritation to the urethral tissue less sensive than ocular tissue. Furthermore, $PGE_1$ in this suppository was stable at $4^{\circ}C$ for 2 years. This suppository increased the ICP and penile erection similar to those of injectable $PGE_1$ solution. However, it gave 2.5-fold increased duration of erectile response than injectable $PGE_1$ solution. Our results suggested that it gave more effective erectile response than injectable $PGE_1$ solution in cats. It is concluded that this $PGE_1$ suppository with good safety, excellent stability and enhanced erectile response, could be a more effective and convenient transurethal delivery system of $PGE_1$.

• The Korean Journal of Physiology and Pharmacology
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• 제2권3호
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• pp.361-368
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• 1998

The spontaneous contractions of gastric smooth muscles are regulated by slow waves, which are modulated by both nervous system and humoral agents. This study was designed to examine the effects of prostaglandin $E_2$ ($PGE_2$) on the contractile and electrical activities of antral smooth muscles in guinea-pig stomach, using an intracellular recording technique. To elucidate the underlying mechanism for its effect on contractility, ionic currents were also measured using a whole-cell patch clamp method. The basal tone by $PGE_2$ was variable, whereas the magnitude of phasic contractions was reduced ($19.0{\pm}2.1%$, n=19). The resting membrane potentials were hyperpolarized ($-4.4{\pm}0.5%$ mV, n=10), and plateau potentials were lowered ($-2.9{\pm}0.5%$ mV, n=10). In most cases, however, the initial peak potentials of slow waves were depolarized more by $PGE_2$ than those of control. The frequency of the slows wave was increased from $5.7{\pm}0.2$ cycles/min to $6.5{\pm}0.2$ (n=22). Voltage-operated $Ca^{2+}$ currents were decreased by $PGE_2$ (n=5). Voltage-operated $K^+$ currents, both Ca-dependent and Ca-independent, were increased (n=5). These results suggest that $PGE_2$ plays an important role in the modulation of gastric smooth muscle activities, and its inhibitory effects on the contractility and activities of slow waves are resulted from both decrease of $Ca^{2+}$ currents and increase of $K^+$ currents.

• Journal of Acupuncture Research
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• 제22권2호
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• pp.155-162
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• 2005

Anemarrhenae Rhizoma (AR) has been widely used for the treatment of various diseases in Oriental medicine. To investigate whether AR possesses anti-inflammatory effects against lipopolysaccharide (LPS)-induced inflammation in the BV2 microglial cells, MTT (3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide) assay. reverse transcription -polymerase chain reaction (RT-PCR), and prostaglandin E2 (PGE2) assay, and nitric oxide (NO) detection assay were performed. From the present results, AR was shown to suppress PGE2 synthesis and NO production by inhibiting the LPS-stimulated enhancement of cyclooxygenase-2 and inducible nitric oxide synthase expression in BV2 microglial cells. These results suggest that AR may offer a valuable means of therapy in the treatment of inflammatory diseases by attenuating LPS-induced PGE2 synthesis and NO production.

• Archives of Pharmacal Research
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• 제27권3호
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• pp.314-318
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• 2004

Microglia are the major inflammatory cells in the central nervous system and become activated in response to brain injuries such as ischemia, trauma, and neurodegenerative diseases including Alzheimer's disease (AD). Moreover, activated microglia are known to release a variety of proinflammatory cytokines and oxidants such as nitric oxide (NO). Minocycline is a semi-synthetic second-generation tetracycline that exerts anti-inflammatory effects that are completely distinct form its antimicrobial action. In this study, the inhibitory effects of minocycline on NO and prostaglandin E$_2$ (PGE$_2$) release was examined in lipopolysaccharides (LPS)-challenged BV2 murine microglial cells. Further, effects of minocycline on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression levels were also determined. The results showed that minocycline significantly inhibited NO and PGE$_2$ production and iNOS and COX-2 expression in BV2 microglial cells. These findings suggest that minocycline should be evaluated as potential therapeutic agent for various pathological conditions due to the excessive activation of microglia.

• 약학회지
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• 제60권3호
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• pp.107-111
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• 2016

Inhibitory activities of 1,5-diarylimidazole analogs with methylthiophenyl group on prostaglandin $E_2$ ($PGE_2$) production from LPS-treated RAW 264.7 cells, were evaluated and compared with those of the corresponding analogs with 4-methanesulfonylphenyl group. Among the tested nineteen analogs with methylthiophenyl group, fourteen analogs showed strong inhibitory activities (>88%) when compared with the reference compound NS-398, and fifteen analogs have similar inhibitory activities with those of parent analogs with 4-methanesulfonylphenyl group. Those results suggest that most of 1,5-diarylimidazole analogs with methanesulfonylphenyl group can be also active even after they are metabolized by reduction.

• 한방안이비인후피부과학회지
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• 제29권4호
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• pp.24-33
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• 2016

Objectives : This study is to investigate the anti-inflammatory and anti-oxidant effects of Tongbi-san extract (TS) on RAW264.7 macrophages using by cell cytotoxicity, Nitric Oxide (NO) and Prostaglandin $E_2$ ($PGE_2$) production and 1,1-diphenyl-2-picryl ghdrazyl (DPPH) free radical scavenging capability. Methods : Cell cytotoxicity was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The production of NO was measured by Griess assay. The production of $PGE_2$ was measured by immunoassay. And the anti-oxidant activity was measured by the DPPH method. Results : TS did not increased significantly compared to the TS untreated group in the cell cytotoxicity. TS inhibited NO and $PGE_2$ production in lipopolysaccharide-stimulated RAW 264.7 cells. TS had the DPPH free radical scavenging capability. Conclusion : The anti-inflammtory and anti-oxidant effects of TS may be use for a treatment of anti-inflammatory diseases.

• Food Science and Biotechnology
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• 제18권1호
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• pp.143-149
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• 2009

The aim of this study was to elucidate the anti-inflammatory activity of safflower (Carthamus tinctorius L.) ethanolic extract fractions (CFEFs). Butanol fraction had the strongest antioxidant activity, and all CFEFs, except for chloroform fraction, partly inhibited lipopolysaccharide (LPS)-induced nitrite production in RAW 264.7 cells. In the cell-free system, hexane and butanol fractions chemically quenched nitric oxide (NO). In addition, the iNOS mRNA transcription was suppressed by ethanol extract and hexane fraction in LPS-stimulated RAW 264.7 cells. Taken together, the inhibitory effect of CFEFs on NO production from LPS-stimulated RAW 264.7 cells, might be due to both the chemical NO quenching activity and the suppression of iNOS mRNA transcription partially. The synthesis of prostaglandin $E_2$ ($PGE_2$) was potently inhibited by ethanol extract to below basal label, and the transcription of cyclooxygenase-2 (COX-2), an enzyme involving in $PGE_2$ synthesis, was partially suppressed by ethanol extract and hexane fraction. Based on these results, CFEFs may be useful as an alternative medicine for the relief and retardation of immunological inflammatory responses through the reduction of inflammatory mediators, including NO and $PGE_2$ production.