• Proceedings of the Korean Society of Applied Pharmacology
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• 2003.11a
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• pp.101-101
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• 2003

Prostaglandins (PGs) and nitric oxide (NO) produced by inducible cyclooygenase (COX-2) and nitric oxide synthase (iNOS), respectively, have been implicated as important mediators in the process of inflammation and carcinogenesis. On this line, the potential COX-2 or iNOS inhibitors have been considered as anti-inflammatory and cancer chemopreventive agents. In our continuing efforts of searching for novel cancer chemopreventive agents from natural products, we isolated natural sesquiterpenoids as potential COX-2 and iNOS inhibitors in cultured lipopolysaccharide (LPS)-activated mouse macrophage RAW 264.7 cells. Alantolactone, a natural eudesmane-type sesquiterpenoid, exhibited a potent inhibition of COX-2 (IC50 = 0.4 $\mu\textrm{g}$/$m\ell$) and iNOS activity (IC50 = 0.08 $\mu\textrm{g}$/$m\ell$) in the assay system determined by PGE2 and NO accumulation, respectively. The inhibitory potential of alantolactone on the PGE2 and NO production was well coincided with the suppression of COX-2 and iNOS protein and mRNA expression in LPS-induced macrophages. Furthermore, alantolactone inhibited NF-kB but not AP-l binding activity on nuclear extracts evoked by LPS-stimulated macrophage cells, suggesting the possible involvement of NF-kB in the regulation of COX-2 and iNOS expression. In further study with COX-2-expressing human colon HT-29 cells, alantolactone inhibited the cell proliferation, down-regulated COX-2, and inhibited the ERK phosphorylation in the early time. These results suggest that a natural sesquiterpenoid alantolactone might be a potential lead candidate for further developing COX-2 or iNOS inhibitor possessing cancer chemopreventive or anti-inflammatory activity

• Food Science and Biotechnology
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• v.15 no.6
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• pp.975-979
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• 2006

The extracts of Oenanthe javanica were evaluated for their effects on the expression of cyclooxygenase-2 (COX-2), which is mediated by the translocation of the p65 subunit into the nucleus. Fractions of ethyl acetate and chloroform from 80% ethanol extracts of O. javanica exhibited inhibitory effects on the secretion of tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) from lipopolysaccharide (LPS)-stimulated peritoneal macrophages; however, the aqueous- and hexane-fractions showed no significant effect. The ethyl acetate- and chloroform-fractions also reduced the COX-2 enzyme levels after 24-hr treatment. RT-PCR showed that the mRNA levels of COX-2 decreased following treatment with these fractions, suggesting that COX-2 expression is transcriptionally regulated by these extracts. We examined the effects of the chloroform- and ethyl acetate-fractions on the cytosolic activation of nuclear factor-${\kappa}B$ ($NF-{\kappa}B$, p65 subunit) and on the degradation of inhibitor-${\kappa}B{\alpha}$ ($I-{\kappa}B{\alpha}$) in order to determine the mechanism of COX-2 regulation. The LPS-stimulated activation of the p65 subunit was significantly blocked upon the addition of $50\;{\mu}g/mL$ of these fractions, and the cytosolic $I-{\kappa}B{\alpha}$ degradation process was simultaneously inhibited. These findings suggest that the inhibition of COX-2 expression by the ethyl acetate-and chloroform-fractions may result from the inhibition of p65 translocation by blocking the degradation of $I-{\kappa}B{\alpha}$; this may be the mechanistic basis for the anti-inflammatory effects of O. javanica.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.9
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• pp.4067-4070
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• 2014

Background: The Chinese Hui ethnic group has diverse origins, including Arab, Persian, Central Asian, and Mongol. The standardized mortality rate of gastric cancer in the Hui population is higher than the overall Chinese population. In this study, we investigated whether COX-2-765G>C polymorphism, an extensively studied polymorphism, contributes to gastric cancer and its precursor lesions (GPL) in the Chinese Hui ethnic group. Materials and Methods: COX-2-765G>C polymorphism was determined by pyrosequencing in 100 gastric cancer cases, 102 gastric cancerand its precursor lesions cases and 105 controls. Data were statistically analyzed using Chi-square tests and logistic regression models. Results: Among the Chinese Hui ethnic group COX-2-765 C allele carriers were at increased risk for gastric cancer (OR=1.977, 95%CI=1.104-3.541). We also found an interaction between COX-2 -765 C carriers and Helicobacter pylori infection and eating pickled vegetables. Conclusions: Our findings suggest a multi-step process of gene-environment interaction contributes to gastric carcinogenesis.

• Korean Journal of Oriental Medicine
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• v.8 no.1
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• pp.65-74
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• 2002

Inflammation is a disease that continues to afflict large numbers of people and may cause other diseases, for example, rheumatoid arthritis, colon cancer, etc. prostaglandins(PGs), one of arachidonic acid metabolites, are major chemical mediators in the process of inflammation. In traditional herbal medicine, many kinds of herbal drugs have been widely used for the treatment of inflammation. So, we analyzed many publications until 2001 which worked on inhibition of $PGE_2$ synthesis by cyclooxygenase-2 (COX-2) with herbs and herb oriented single compounds. And then we tried to make interpretations of herbal traditional prescriptions for inflammation. There are significant correlations between herbal medicine prescribed and inhibitions of COX-2 activity. From our efforts and further researches, we expect to develop new-inflammatory herbal drugs which have more efficacy and fewer side effects.

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.131-131
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• 2001

Prostaglandins and nitric oxide produced by inducible cyclooygenase (COX-2) and nitric oxide synthase (iNOS), respectively, have been implicated as important mediators in the process of inflammation and carcinogenesis. On this line, the potential COX-2 or iNOS inhibitors have been considered as anti-inflammatory and cancer chemopreventive agents.(omitted)

• Bulletin of the Korean Chemical Society
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• v.28 no.5
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• pp.751-757
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• 2007

To develop new COX-2 inhibitors, 1,5-diarylhydantoins and 1,5-diaryl-2-thiohydantoins were synthesized from phenylacetic acids by esterification, bromination, C-N bond formation and cyclization. Esters 1-3 were efficiently synthesized from the starting materials by reflux in absolute methanol for 3 h containing concentrated sulfuric acid as catalyst. Bromination was carried out with N-bromosuccinimide at rt in dichloromethane. Bromides 4-6 were reacted with aniline, p-anisidine, sulfanilamide in ethanol (or N,N-dimethylformamide) to provide the amines 7-15. Hydantoins and 2-thiohydantoins 16-46 were synthesized from amines 7-15 by treating them with potassium isocyanate (or potassium thiocyanate) and triethylamine. The synthetic process from alkyl α-anilinophenylacetate 7-15 to 3-alkylhydantoins was carried out in a one-pot reaction using alkyl isocyanate (alkyl isothiocyanate).

• Journal of the Korea Society of Computer and Information
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• v.15 no.2
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• pp.109-117
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• 2010

Digital watermarking has drawn extensive attention for protecting digital contents from unauthorized copying. This paper proposes a new watermarking scheme in frequency domain for copyright protection of digital audio. In our proposed watermarking system, the original audio is segmented into non-overlapping frames. Watermarks are then embedded into the selected prominent peaks in the magnitude spectrum of each frame. Watermarks are extracted by performing the inverse operation of watermark embedding process. Simulation results indicate that the proposed scheme is robust against various kinds of attacks such as noise addition, cropping, resampling, re-quantization, MP3 compression, and low pass filtering. Our proposed watermarking system outperforms Cox's method in terms of imperceptibility, while keeping comparable robustness with the Cox's method. Our proposed system achieves SNR (signal-to-noise ratio) values ranging from 20 dB to 28 dB. This is in contrast to Cox's method which achieves SNR values ranging from only 14 dB to 23 dB.

• Preventive Nutrition and Food Science
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• v.11 no.1
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• pp.1-5
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• 2006

Conjugated linoleic acid (CLA) is a group of positional and geometric isomers of linoleic acid that have been used to reduce the incidence, growth and metastasis of breast, colon, prostate and gastric cancer in animals. CLA could reduce tumor growth by altering angiogenesis; a process requiring associated angiogenic factors such as vascular endothelial growth factor (VEGF). In this study, we determined whether CLA could modulate the expression of VEGF in murine mammary tumor cells and adipocytes. The c9, t11-CLA isomer reduced VEGF transcripts and protein when mammary tumor cells were stimulated with PMA. That isomer also reduced VEGF expression in un stimulated mouse 3T3-L1 adipocytes. Since VEGF can be regulated by cyclooxygenase-2 (COX-2), we determined whether CLA could alter COX-2 enzyme expression and $PGE_2$ production. The c9, t11-CLA isomer reduced not only COX-2 enzyme expression but also $PGE_2$ production. Thus, c9, t11-CLA could modulate neovascularization by alteration of VEGF expression from mammary tumor cells and adipocytes by reducing COX-2 metabolites.

• Korean Journal of Food Science and Technology
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• v.48 no.4
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• pp.378-383
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• 2016

The glasswort is an edible halophyte demonstrating various physiological effects including anti-inflammatory activity. In the present study, the effects of glasswort extracts on inflammatory events and interactions of THP-1 monocytes with intestinal epithelial cells were investigated. Five solvent fractions, including the ethylether fraction (Fr.E), were prepared from a 70% methanol extract of glasswort. THP-1 monocytes underwent differentiation by phorbol 12-myristate 13-acetate treatment and were then activated by lipopolysaccharide (LPS), which induced cyclooxygenase (COX)-2 expression. None of the glasswort fractions tested alone induced COX-2 in differentiated THP-1 cells. Fr.E, however, enhanced LPS-induced COX-2 expression in differentiated THP-1 cells. Culture media of THP-1 cells treated with each fraction stimulated the growth of normal intestinal INT-407 cells more prominently than that of HT-29 colon cancer cells. COX-2 expression in HT-29 cells was inhibited when the cells were exposed to the THP-1 culture medium treated with Fr.E. Thus, glasswort could modulate the interaction between immune cells and intestinal cells.

• The Journal of Internal Korean Medicine
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• v.29 no.2
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• pp.421-431
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• 2008

Objectives : This study was to investigate the inhibitory effects of Ulmus davidiana on the generation of peroxynitrite $(ONOO^{-})$, nitric oxide (NO) and superoxide anion radicals $(O_{2}^{-})$ in the endothelial cells of rat vessels. The effects of Ulmus davidiana on the expression of inflammation-related proteins, $NF-{\kappa}B$ (p50, p65), COX-2, and iNOS, were examined by western blotting. Methods : For this study, fluorescent probes, namely dihydrorhodamine 123 (DHR 123), 4,5-diaminofluorescein (DAF-2) and 2',7'-dichlorodihydrofluorescein diacetate (DCFDA) were used. Western blotting was performed via using anti-$NF-{\kappa}B$ (p50, p65), anti-COX-2, and anti-iNOS, respectively. Results : Ulmus davidiana inhibited the generation of $ONOO^{-}$, NO and $(O_{2}^{-})$ in the lipopolysaccharide (LPS)-treated endothelial cells of rat vessels in vitro. Ulmus davidiana inhibited the expression of COX-2 and iNOS genes by means of decreasing the $NF-{\kappa}B$ activation. Conclusions : These results suggest Ulmus davidiana is effective on inhibiting the generation of $ONOO^{-}$, NO and $O_{2}^{-}$, and that therefore it might have a potential role as a treatment for the inflammatory process and inflammation-related diseases.