• Journal of the Korean Society of Food Science and Nutrition
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• v.40 no.4
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• pp.486-492
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• 2011

This study was designed to evaluate the effect of hot water extract (ESW) and 70% ethanol extract (ESE) from Euphorbia supina Rafin on LPS-stimulated inflammatory response in RAW 264.7 macrophages. Upon investigation at concentrations up to $1000\;{\mu}g$/mL, ESW and ESE did not have any cytotoxic effects on RAW 264.7 macrophages. ESW induced inhibition of 21.6%~54.8% of nitric oxide (NO) production at 100~1000${\mu}g$/mL, and $PGE_2$ production was inhibited up to 25.7%~38.2% at 250~1000${\mu}g$/mL, proportional to the ESW concentrations. ESW induced inhibition of 66.1% and 54.3% of IL-6 production at 250 and $1000\;{\mu}g$/mL, respectively. ESE (100~1000${\mu}g$/mL) induced inhibition of 38.3%~77.5% of NO, 40%~94.7% of $PGE_2$, and 43.9%~89.4% of IL-6 production, proportional to the ESE concentrations. Only 44.1% of IL-10 production was inhibited at a concentration of $500\;{\mu}g$/mL. ESE induced an increase in TNF-${\alpha}$ production at a concentration of 100 and $250\;{\mu}g$/mL, whereas at high concentrations (500 and $1000\;{\mu}g$/mL), ESE induced inhibition of 19.2% and 92.4% of TNF-${\alpha}$ production, respectively. In conclusion, concentrations of more than $500\;{\mu}g$/mL ESE demonstrated effective immune-modulating activity through inhibition of NO, $PGE_2$, IL-6, IL-10, or TNF-${\alpha}$ production, as it relates to the macrophage's immuno-activity; therefore, ESE has potential as a good candidate substance for reduction of inflammatory responses.

• The Korean Journal of Pharmacology
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• v.2 no.1 s.2
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• pp.71-82
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• 1966

The inhibitory effect of 5-hydroxytryptamine (5-HT) on the isolated intestinal strips of the tortoise (Amyda japonica), rat, rabbit and guinea pig was investigated. 1) The strips from the middle or lower part of the tortoise intestine responded with relaxation to 5-HT $(10^{-9}{\sim}10^{-5}g/ml)$, and the magnitude of the relaxation was proportional to the dose of 5-HT. The rectal part of the tortoise intestine, in contrast, showed contraction, the magnitude of which also was proportional to the dose of 5-HT. 2) Various blocking agents such as methysergide, morphine, tetracaine, nethalide, bretylium, hexamethonium, mecamylamine and chlorisondamine, showed no selective blocking activity on the relaxant effect of 5-HT on the tortoise intestine. The inhibitory effect of isoproterenol on the tortoise intestine, however, was selectively blocked by nethalide, and the stimulatory effect of 5-HT on the rectal part of the tortoise was blocked by methysergide. 3) In the presence of 5-HT, the stimulatory effect of DMPP on the tortoise intestine was remarkably attenuated, whereas that of acetylcholine and $BaCl_2$ was little affected. In the presence of isoproterenol, the stimulatory effect of acetylcholine and $BaCl_2$ were affected, but that of DMPP was little affected. 4) Large dose of 5-HT($10^{-4}$g/ml) produced inhibitory effect on the strips from the distal part of the isolated colon of the rat, rabbit and guinea pig, when the strips had been exposed to 5-HT($10^{-4}$g/ml), methysergide or phen`oxybenzamine. 5) Bretylium, as well as nethalide, abolished or remarkably reduced, in a few cases of the experiments, the inhibitory effect of the large dose of 5-HT on the distal part of the colon, whereas morphine did not affect it. 6) The ileal strips of the guinea pig also showed relaxation, as in the colonic strips, having been exposed to the large dose of 5-HT or phenoxybenzamine. This effect, however, was not obsered in the case of the rabbit ileum. 7) The property of the action-site of 5-HT in the tortoise intestine seemd to be different from the 5-HT receptors which have been revealed by several investigators. 8) Adrenergic component seemed to be participated in the inhibitory effect of 5-HT on the colon of the rat and rabbit.

• The Journal of Internal Korean Medicine
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• v.34 no.1
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• pp.31-45
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• 2013

Objectives : Gokgisaeng (Korean mistletoe) is used for the treatment of inflammatory and cancer diseases in traditional Korean medicine and its major component lectins have been reported to induce nitric oxide (NO) in RAW 264.7 macrophages, and also induce apoptosis of various types of cancer cells, although its modulatory effects on cancer cell migration and macrophage activation is poorly understood. The aim of this study is to clarify molecular mechanisms of action responsible for the anti-inflammatory and antitumor migration potentials of Korean mistletoe extract (KME). Methods : We investigated the anti-inflammatory activity of KME on NO production and inducible nitric oxide synthase (iNOS) expression by lipopolysaccharide (LPS) in both RAW 264.7 macrophages and rat C6 glioma cells, and also evaluated inhibitory efficacy on glioma cell growth and migration. For assessment, XTT assay, nitrite assay, RT-PCR, scratch-wound and Boyden chamber assay, and western blot analysis were performed. Results : Previously reported, unlike the efficacy of Gokgisaeng lectin, KME inhibited NO production and iNOS expression, and suppressed pro-inflammatory mediators including IL-$1{\beta}$, IL-6, COX-2, iNOS in LPS-stimulated RAW 264.7 cells. Furthermore, KME suppressed tumor cell growth and migration, and it also inhibited LPS-induced NO release and iNOS activation by down-regulating expression of protein kinase C (PKC) and phosphorylation of ERK in C6 glioma cells. Conclusions : Our research findings provide evidence that KME can play a significant role in blocking pro-inflammatory reaction and malignant progression of tumors through the suppression of NO/iNOS by down-regulating of inflammatory signaling pathways, PKC/ERK.

• Journal of Haehwa Medicine
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• v.7 no.1
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• pp.939-955
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• 1998

Achyranthis Bidentatae Radix(ABR) is important prescriptions that have been used in oriental medicine for stomatitis and wound healing. The study was done to evaluate the inhibitory effects of cytotoxicity, formation of superoxide on the macrophage and neutrophil, prostaglandins($PGE_2$), interleukins($IL-1{\beta}$), collagenase activity and synthesis of collagen and DNA. The results were obtained as follows: 1. ABR was not showed the proliferation difference of human fibroblast and monocyte in 0.01% and 0.001% concentrations to be experimented and in result, it was concluded that they have no cytotoxicity but showed cytotoxicity in 0.1% concentrations. 2. ABR inhibited the formation of superoxide to 48% at the concentration of 0.001% in the mouse monocyte. 3. ABR inhibited the formation of superoxide to 40% at 0.001%, 58% at 0.0001% as compared with control in the human monocyte. 4. ABR inhibited the formation of superoxide to 58% at 0.0001%, 40% at 0.001% in the human neutrophil. 5. ABR was not showed the proliferation difference of human monocyte in all concentrations to be experimented and in result, it was concluded that they inhibited the formation of prostaglandins($PGE_2$) in the human monocyte stimulated with E. coli. 6. ABR showed the all concentration of inhibiting the production of inter1eukins($IL-1{\beta}$) in the human monocyte stimulated with E. coli. 7. ABR didn't influence on collagen synthesis and total protein in fibroblasts. 8. ABR inhibited the collagenase activity to 84% at 0.1%, 69% at 0.2%, 76% at 0.5%, 91% at 0.001% respectively.

• Journal of Microbiology and Biotechnology
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• v.18 no.7
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• pp.1308-1316
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• 2008

Propionibacterium acnes is known to playa pivotal role in the pathogenesis of acne vulgaris. CBT-SL5 is one of the antimicrobial peptides from Enterococcus faecalis SL5, and it has shown antimicrobial activity against P. acnes. The aim of this study was to investigate the anti-inflammatory effect of CBT-SL5 on the inflammation induced by P. acnes in cultured human keratinocyes. Cultured human keratinocytes derived from neonatal foreskin were treated with heat-killed P. acnes to induce inflammation, and then various concentrations of CBT-SL5 were added to the P. acnes-treated keratinocytes. The mRNA expression and protein secretion of interleukin (IL)-8, an inflammation marker, was analyzed by real-time reverse transcription polymerase chain reaction and enzyme-linked immunosorbent assay, respectively. We also analyzed the nuclear factor-kappa B (NF-$\kappaB$) p65 translocation by performing immunofluorescent staining. P. acnes treatment up regulated the IL-8 mRNA expression in the keratinocytes, and this was brought about through both toll-like receptor (TLR)2 and TLR4. At the concentrations of 10, 50, and 100 ng/ml, CBT-SL5 significantly down regulated the P. acnes-induced IL-8 mRNA expression and protein production (p<0.05). At 6 hand 12 h of the treatment, CBT-SL5 significantly suppressed the P. acnes-induced IL-8 mRNA expression. Secretion of IL-8 protein was significantly reduced at 24 h. The functional inhibitory activity of CBT-SL5 was shown by CBT-SL5 suppressing the P. acnes-induced NF-$\kappaB$ translocation from the cytoplasm to the nucleus. These results demonstrated that CBT-SL5 suppressed the P. acnes-induced IL-8 expression in keratinocytes. Therefore, CBT-SL5 may be a novel anti-inflammatory treatment for acne.

• Archives of Pharmacal Research
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• v.20 no.3
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• pp.253-258
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• 1997

Ten, heretofore unreported, $ 5^I-methyl-5^I-[2-(5-substituted uracil-1-yl)ethyl)]-2^I-oxo-3^I$-methylenetetrahydrofurans (H, F, Cl, Br, I, $ CH_3$,$CF_3$,$CH_2CH_3$,$ CH=CH2$, SePh) (7a-j) were synthesized and evaluated against four cell lines (K-562, FM-3A, P-388 and U-937). For the preparation of ${\alpha}$-methylene-${\gamma}$-butyrolactone-linked to 5-substituted uracils (7a-j), the convenient Reformasky type reaction was employed which involves the treatment of ethyl ${\alpha}$-(bromomethyl)acrylate and zinc with the respective 1-(5-substituted uracil-1-yl)-3-butanone (6a-j). The 5-substituted uracil ketones (6a-j) were directly obtained by the respective Michael type reaction of vinyl methyl ketone with the $K_2CO_3$(or NaH)-treated 5-substituted uracils (5a-j) in the presence of acetic acid in the DMF solvent. The .alpha.-methylene-.gamma.-butyrolactone compounds showing the most significant antitumor activity are 7e, 7f, 7h and 7j (inhibitory concentration $(IC_50)$ ranging from 0.69 to $2.9 {\mu}g/ml$), while 7b, 7g and 7i have shown moderate to significant activity. The compounds 7a, 7c and 7d were found to be inactive. The synthetic intermediate compounds 6a-j were also screened and found marginal to moderate activity where compounds 6b and 6g showed significant activity $(IC_50:0.4~2.8 {\mu}g/ml)$.

• Journal of the Korean Chemical Society
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• v.44 no.6
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• pp.533-540
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• 2000

Melanization of B16 melanoma cells was comparatively studied by the aqueous extract of Epimedium koreanum Nakai(EK) and $\alpha$-MSH. In addition, inhibitory effects of RA was investigated. B16 melanoma cells(about 1${\times}10_5$) have been shown an increase in tyrosinase activity and melanin contents in proportion to concentration of $\alpha$-MSH when treated with $\alpha$-MSH and incubated for 72 hrs. They indicated a 350% increase in tyrosinase activity and a 290% increase in melanin contents at 8 ng/mL. In case of EK, they have been shown a 200% increase in tyrosinase activity and a 180% increase in melanin contents at 100 ${\mu}g$/mL. In addition of RA to the above condition, they have been shown an inhibition from 350% to 210% in tyrosinase activity and from 290% to 250% in melanin contents in $\alpha$-MSH, and inhibition from 200% to 100% in tyrosinase activity and from 180% to 120% in melanin contents in EK. From the above results, it is suggested that EK promotes melanization of B16 melanoma cells through cAMP pathway, whereas RA inhibits it.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.32 no.1 s.55
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• pp.59-64
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• 2006

Crinum asiaticum Linne var. japonicum has long been used as a rheumatic remedy, an anti-pyretic, an anti-ulcer treatment, and for the alleviation of local pain and fever in Korea and Malaysia. In order to investigate the possibility of Crinum asiaticum Linne var. japonicum extract as a cosmetic ingredient, we measured its anti-inflammatory effect by inhibition of iNOS (inducible nitric oxide synthase), and the release of PGE2, IL-6, and IL-8. HPLC experiment after extraction with 95% ethanol at pH 3.5 showed that Crinum asiaticum Linne var. japonicum was mainly composed of lycorine (up to 1%), a well-known immunosuppressant. The content of lycorine varied depending on the type of tissue analyzed and the extraction method. In anti-inflammatory assay for inhibition of nitric oxide formation on lipopolysaccharide (LPS)- activated mouse macrophage RAW 264.7 cells, the ethanolic extract of Crinum asiaticum showed inhibitory activity of NO production in dose-dependent manner ($IC_{50} = 83.5 {\mu}g/mL$). Additional study by RT-PCR demonstrated that the extract of Crinum asiaticum significantly suppressed the expression of the iNOS gene. Moreover, the extract of Crinum asiaticum did not show my cytotoxicity, but did show cell proliferation effect against LPS ($10{\sim}60%$ increase of tell viability). In an assay to determine inhibition of the $H_2O_2$-activated release of PGE2, IL-6, and IL-8 in human normal fibroblast cell lines, the release of PGE2 and IL-6 was almost completely inhibited above concentrations of 0.05% and 1%, respectively. Moreover, the release of IL-8 was completely inhibited over the entire range of concentrations (> 0.0025%). The result showed that the extract of Crinum asiaticum Linne var. japonicum has sufficient anti-inflammatory effect. There-fore, Crinum asiaticum Linne var. japonicum extract may be useful as an ingredient of cosmetic products.

• Journal of Physiology & Pathology in Korean Medicine
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• v.22 no.4
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• pp.878-883
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• 2008

Conchiolin is a complex protein which is secreted by the mollusc's outer epithelium to be the organic basis of mollusc shell. This study is to investigate a potential anti-inflammatory activity of conchiolin of oyster shell (COS). We tested the effects of COS on the lipopolysaccharide (LPS)-induced production of nitric oxide (NO) and prostaglandin E2 (PGE 2) in a murine macrophage cell line, RAW 264.7. COS inhibited production of NO and PGE2 in a dose dependent manner and also decreased the expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$) and interleukin-6 (IL-6). These results suggest that COS can inhibit production of pro-inflammatory mediators and might be a useful source to treat inflammation.

• Korean Journal of Veterinary Research
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• v.33 no.4
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• pp.617-622
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• 1993

The preliminary studies on the localization of adrenoceptors were performed on smooth muscle strips of bovine esophageal groove. The mechanical activity of the muscle strip was recorded isometrically in vitro.w In the bottom circular muscle strips. the excitatory ${\alpha}-adrenergic$ responses were not blocked by tetrodotoxin$(2.1{\times}10^{-6}M)$ and denervation which was carried by cold storage of strips for 48 hrs in Tyrode's solution at $5-6{^{\circ}C}$ without oxygen supply. These excitatory ${\alpha}-adrenergic$ responses were partially blocked by atropine. In the lip longitudinal muscle strips, the inhibitory${\beta}-adrenergic$ responses were not blocked by pretreatment of tetrodotoxin and atropine. The results suggest that ${\beta}-adrenergic$ receptors mediating relaxations are located on the postsynaptic smooth muscle cells, whereas ${\beta}-adrenergic$ receptors mediating contractions are located both in the smooth muscle cells and in the cholinergic neurones.