• Herbal Formula Science
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• v.20 no.2
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• pp.1-11
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• 2012

Objectives : The purpose of this study was to investigate the differences of chemical composition or biological activities between decoction and commercial herbal medicines of Samchulkunbi-tang (Shenzhujianpi-tang, SKT). Methods : The extracts of SKT from decoction (SKT1) and two different commercial extractive granules (SKT2 and SKT3) were prepared. The index components of SKTs were analyzed with HPLC. The antioxidant activities of SKTs were studied by measuring free radical scavenging activities on ABTS and DPPH. The anti-inflammatory effects were determined by measuring NO, $PGE_2$ and IL-6 in LPS-stimulated RAW 264.7 cells. Results : The contents of 7 components were 1.40-6.08 mg/g in SKT1, not detected-4.75 mg/g in SKT2, 0.03-1.46 mg/g in SKT3. The scavenging activities on ABTS and DPPH of herbal formulas were increased in dose-dependent manner (SKT1>SKT2>SKT3). SKT1 significantly inhibited $PGE_2$ and IL-6 production and SKT3 slightly inhibited $PGE_2$ production in LPS-stimulated RAW264.7 cells. SKT2 showed no inhibitory effects on production of inflammatory mediators such as $PGE_2$ and IL-6. Conclusions : These results demonstrate that the decoction of SKT has more strong anti-oxidant and anti-inflammatory effects than that of commercial herbal medicines consistent with the contents of index components.

• The Journal of Korean Medicine
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• v.30 no.6
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• pp.44-52
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• 2009

Objectives: This study was performed to evaluate the influence of different extracting solvents (water, methanol, ethanol, or n-hexane) on the anti-inflammatory efficacy of Scutellaria baicalensis (Lamiaceae), which has been used widely as a traditional herbal medicine for its anti-inflammatory properties. Methods: The ability of each extract to inhibit the production of pro-inflammatory mediators such as NO, TNF-$\alpha$, and $PGE_2$ by lipopolysaccharide (LPS)-stimulated mouse macrophage RAW 264.7 cells was measured. Results: The results showed that extraction solvents (except n-hexane) for S. baicalensis showed significant inhibitory effects on NO, TNF-$\alpha$ and $PGE_2$ production. Especially, methanol was the solvent with the greatest activity against NO and $PGE_2$ production. However, there was no difference between the extracts for inhibitory activity of TNF-$\alpha$. Conclusion: The present study suggests that methanol is a superior extraction solvent than water, ethanol, or n-hexane for maintaining the anti-inflammatory effects of S. baicalensis.

• Journal of Acupuncture Research
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• v.19 no.2
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• pp.177-188
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• 2002

Objective : The purpose of this study is to investigate the immunohistological effect of Buthus martensi Karsch Herbal-acupuncture in treating the arthritis, performed several experimental items : those are paw edema, $IL-1{\beta}$, IL-6, IL-8, $TNF-{\alpha}$ and $PGE_2$. Methods : All the male Sprague Dawley rats used in this study were bred and maintaned in our pathogen-free rat colony and were 8 weeks of age at the start of to experiment. The experimental model of arthritis was induced by injection of $50{\mu}g/{\mu}{\ell}$ adjuvant(mineral oil mixed Mycobacterium butyricum). Buthus martensi Karsch Herbal-acupuncture was injected into ST36(足三里) of rats daily for 21 days. Immunohistological analysis was carried out to assess paw edema, $IL-1{\beta}$, IL-6, IL-8, $TNF-{\alpha}$ and $PGE_2$ expression in synovial membrane and sera Buthus martensi Karsch Herbal-acupuncture injected. Results : Buthus martensi Karsch Herbal-acupuncture group showed a decrease with statistical significance, in paw edema, $IL-1{\beta}$, IL-6, IL-8, $TNF-{\alpha}$ and $PGE_2$ in synovial membrane and sera compared with control group. Conclusion : Buthus martensi Karsch Herbal-acupuncture stimulation inhibited the development of immunity to adjuvant induced arthritis in rats. Thus, Buthus martensi Karsch Herbal-acupuncture may have preventive effects on autoimmune inflammatory joint diseases as arthritis. The effect of Buthus martensi Karsch Herbal-acupuncture on the immune function and the disease activity in patients with arthritis warrants further investigation.

• The korean journal of orthodontics
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• v.20 no.2
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• pp.247-266
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• 1990

The alveolar bone remodeling is essential in tooth movement by orthodontic forces. The collagen and chondroitin sulfate are acting as an important roles in bone remodeling. This study was performed to measure out the quantity of the collagen and chondroitin sulfate in the alveolar bone of rats applied by experimental orthodontic forces. The 150 Sprague-Dawley male rats were divided into the $PGE_2$ treated group, indomethacin treated group and the normal group. A 80gm force rubber band was used as a orthodontic appliance between upper incisors and right upper 1st molar, and left side of experimental rats with no appliance was regarded as a control side. The samples of alveolar bones were obtained from pressure and tension sites in all three groups. respectively, and in control sides, too. The results were as follows. 1. The change in total collagen remains stable in both pressure and tension sites of all three groups, compared with control side by the time consuming. 2. The change in soluble collagen showed the most highest level in tension site, lowest level in pressure site of $PGE_2$ treated group in 5th. experimental day. 3. The change in chondroitin sulfate showed the most highest level in pressure site, lowest level in tension site of $PGE_2$ treated group in 5th. experimental day. 4. In indomethacin treated group, the change of soluble collagen and chondroitin sulfate showed small range of variance compared with $PGE_2$ treated and normal group.

• Advances in Traditional Medicine
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• v.7 no.5
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• pp.509-517
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• 2008

Gyejijakyakjimo-tang is a multi-herbal formula that is composed of nine medicinal herbs. Gyejijakyakjimo-tang has been reported to have antipyretic and analgesic effects. Gyejijakyakjimo-tang has traditionally been used for goat and rheumatoid arthritis. However, analgesic and antiinflammatory effects of Gyejijakyakjimo-tang has not been clarified yet. In this study, we investigated the analgesic and anti-inflammatory effect of the aqueous extract of Gyejijakyakjimo-tang. We evaluated the aqueous extract of Gyejijakyakjimo-tang on Lipopolysaccharide (LPS)-induced inflammation in murine raw 264.7 macrophage cells. For this study, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, reverse transcription-polymerase chain reaction (RT-PCR), prostaglandin $E_2$ ($PGE_2$) immunoassay, and nitric oxide (NO) detection were performed. Gyejijakyakjimo-tang suppressed $PGE_2$ synthesis and NO production by inhibiting the LPS-induced expressions of COX-2 and iNOS mRNA in murine raw 264.7 macrophage cells. These results show that Gyejijakyakjimo-tang has the analgesic and anti-inflammatory effect by mostly suppressing COX-2 and iNOS expressions, and resulting in the inhibition of $PGE_2$ synthesis and NO production.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.3
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• pp.599-607
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• 2009

Prunellae Spica is the spike or whole plant of Prunella vulgaris Linne, which has been used for clearing heat from the liver, brightening the eyes and treating headache in traditional oriental medicines. This study was conducted to evaluate the inhibitory effects of the aqueous extract of Prunellae Spica (PSE; PS extract) on the production of NO and PGE2 in LPS-activated Raw 264.7 cells. Cell viability was determined by MTT assay, and all three doses of PS extract (0.03, 0.1 and 0.3 mg/ml) had no significant cytotoxicity during the entire experimental period. The cells were treated with 1 ${\mu}g/ml$ of LPS 1 h before adding PS extract, and increased NO and PGE2 production were detected in LPS-activated cells compared to control. However, these increases were dose-dependently attenuated by treatment with PS extract. The inhibition of NO by PS extract was due to the suppression of iNOS expression via inhibition of $NF{\kappa}B$ nuclear translocation and proteolytic degradation of $I{\kappa}B{\alpha}$. The decreased level of PGE2 was derived from inhibition of COX-2 activity, but expression of COX-2 protein was not affected by PS extract. Moreover, PS extract reduced the elevated production of IL-${\beta}$ and IL-6 by LPS. These results demonstrate that PS extract has inhibitory effects on the production of NO and PGE2 as a consequence of the reduction of proinflammatory cytokines, especially IL-${\beta}$ and IL-6 in LPS-activated Raw 264.7 cells.

• Biomolecules & Therapeutics
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• v.19 no.1
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• pp.27-32
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• 2011

The activation of microglia induces the overproduction of inflammatory mediators that are responsible for the neurodegenerative disorders including Alzheimer's disease and Parkinson's disease. The large amounts of prostaglandin $E_2$ ($PGE_2$) produced by inducible cyclooxygenase (COX-2) is one of the main inflammatory mediators that can contribute to neurodegeneration. The inhibition of COX-2 thus may provide therapeutic strategy for the treatment of neurodegenerative diseases. From the activity-guided purification of EtOAc soluble fraction of Siegesbeckia glabrescens, four compounds were isolated as inhibitors of $PGE_2$ production in LPS-activated microglia. Their structures were determined as 3, 4'-dimethylquercetin (1), 3, 7-dimethylquercetin (2), 3-methylquercetin (3) and 3, 7, 4'-trimethylquercetin (4) by the mass and NMR spectral data analysis. The compounds 1-4 showed dose-dependent inhibition of $PGE_2$ production in LPS-activated microglia with their $IC_{50}$ values of 7.1, 4.9, 4.4, $12.4\;{\mu}M$ respectively. They reduced the expression of protein and mRNA of COX-2 through the inhibition of I-${\kappa}B{\alpha}$ degradation and NF-$\kappa}B$ activity that were correlated with the inactivation of p38 and ERK. Therefore the active compounds from Siegesbeckia glabrescens may have therapeutic effects on neuro-inflammatory diseases through the inhibition of overproduction of $PGE_2$ and suppression of COX-2 overexpression.

• Journal of Pharmacopuncture
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• v.4 no.1
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• pp.5-21
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• 2001

The influence of electroacupuncture (EA), a traditional Chinese medical treatment, on type Ⅱ collagen-induced arthritis (CIA) was examined in DBA/1J mice in vivo. Mice were immunized intradermally twice at the 3-week interval with bovine type Ⅱ collagen(C Ⅱ). EA stimulation, begun on the 21 simultaneously with the second immunization, was applied at the acupoint equivalent to GV4 three times a week for 3 weeks. The results showed that EA delayed the onset, attenuated the severity of arthritis, and reduced the anti-collagen antibody level. Furthermore, we investigated the impact of EA on the productions of endogenous $interleukin-1{\Beta}$ (IL-1 beta) and prostaglandin E2 (PGE2), and the levels of IL-1 beta mRNA in splenocytes and synovial tissues from C Ⅱ immunized mice on the 45 and cyclooxygenase-2 (COX-2) mRNA in lipopolysaccharide (LPS)-stimulated macrophages of normal mice by using reverse transcriptase-polymerase chain reaction (RT-PCR). EA stimulation significant inhibited the concentrations of splenic endogenous IL-1 beta and serum PGE2. The expression of IL-1 beta mRNA in spleen cells was obviously down-regulated and that in synovial tissues was modestly affected by EA. COX-2 mRNA was highly expressed in cultured peritoneal macrophages when stimulated with LPS. Previous treatment with EA also reduced LPS-stimulated induction of COX-2 mRNA. These data suggest that EA has an inhibitory effect on murine CIA, and the partial mechanism of its therapeutic result may be attributed to inhibiting the productions of IL-1 beta and PGE2 by suppression the IL-1 beta and COX-2 gene activations.

• Journal of Pharmacopuncture
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• v.20 no.3
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• pp.207-212
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• 2017

Objectives: Study of the mechanisms involved in cancer progression suggests that cyclooxygenase enzymes play an important role in the induction of inflammation, tumor formation, and metastasis of cancer cells. Thus, cyclooxygenase enzymes could be considered for cancer chemotherapy. Among these enzymes, cyclooxygenase 2 (COX-2) is associated with liver carcinogenesis. Various COX-2 inhibitors cause growth inhibition of human hepatocellular carcinoma cells, but many of them act in the COX-2 independent mechanism. Thus, the introduction of selective COX-2 inhibitors is necessary to achieve a clear result. The present study was aimed to determine the growth-inhibitory effects of new analogues of chalcone epoxide as selective COX-2 inhibitors on the human hepatocellular carcinoma (HepG2) cell line. Methods: Estimation of both cell growth and the amount of prostaglandin E2 (PGE2) production were used to study the effect of selective COX-2 inhibitors on the hepatocellular carcinoma cell. Cell growth determination has done by MTT assay in 24 h, 48 h and 72 h, and PGE2 production has estimated by using ELYSA kit in 48 h and 72 h. Results: The results showed growth inhibition of the HepG2 cell line in a concentration and time-dependent manner, as well as a reduction in the formation of PGE2 as a product of COX-2 activity. Among the compounds those analogues with methoxy and hydrogen group showed more inhibitory effect than others. Conclusion: The current in-vitro study indicates that the observed significant growth-inhibitory effect of chalcone-epoxide analogues on the HepG2 cell line may involve COX-dependent mechanisms and the PGE2 pathway parallel to the effect of celecoxib. It can be said that these analogues might be efficient compounds in chemotherapy of COX-2 dependent carcinoma specially preventing and treatment of hepatocellular carcinomas.

• Molecules and Cells
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• v.22 no.1
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• pp.44-50
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• 2006

We investigated the possible role of p38 MAPK and $ET_B$ receptors in ET-1 induction of cyclooxygenase-2 (COX-2) and prostaglandin $E_2$ ($PGE_2$) in cultured feline esophageal smooth muscle cells (ESMC). Confluent layers of ESMC were stimulated with 10 nM ET-1 and expression of COX-1 and COX-2, involvement of receptors, and activation of p38 MAPK, were examined by Western blot analysis. Levels of $PGE_2$ induced by ET-1 were measured by Elisa. Using $ET_A$and $ET_B$ antagonists (BQ-123 and BQ-788, respectively), the contribution of the ET receptors to COX-1 and COX-2 expression induced by ET-1 was determined. Western blot analysis revealed that treatment of ESMC with ET-1 resulted in transient expression of COX-2 and activation of p38 MAPK. Activation of p38 MAPK was maximal after 1 h. SB202190, a p38 MAPK inhibitor, reduced expression of COX-2, but not COX-1. ET-1-induced release of $PGE_2$ was also blocked by SB202190. COX-2 expression was upregulated only via the $ET_B$ receptor, and COX-1 expression was not affected by either antagonist. Taken together, our data suggest that ET-1 causes p38 MAPK-dependent expression of COX-2 by interacting with $ET_B$ receptors on ESMC.