• YAKHAK HOEJI
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• v.44 no.3
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• pp.272-278
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• 2000

The antiinflammatory mechanism of NSAIDs is attributed to the reduction of prostaglandin synthesis by the direct inhibition of cyclooxygenase. Inhibition of prostaglandin production in organs such as stomach and kidney can result in gastric lesions, nephrotoxicity and increased bleeding. In this study, newly designed COX-2 inhibitors, synthesized 1,2-benzothiazine derivatives, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. Lead compounds in the structure-activity relationship were studied to synthesize new highly selective COX-2 inhibitors.13 determine inhibitory effect of COX-2, synthesized 1,2-benzothiazine derivatives were screened with accumulation of prostaglandin by lipopolysaccharide (LPS) in aspirin-treated macrophages and murine macropharge cell. Some of synthesized 1,2-benzothiazine derivatives were shown to be effective as selective COX-2 inhibitory activity. Others exhibited a preferential inhibition of COX-2, although some COX-1 inhibitory activity was still present. As a conclusion, simple monomer derivatives were more active than dimer derivatives. Substitution of halogen (Br, C1) on the benzothiazine nucleus slightly enhanced inhibition activity.

• YAKHAK HOEJI
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• v.54 no.6
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• pp.466-473
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• 2010

A series of $3{\beta}$-substituted 5-androstene-$17{\beta}$-carboxamides were synthesized from analogs of $3{\beta}$-hydroxy-5-androstene-$17{\beta}$-carboxylic acid (1) with tert-butylamine, N,N-diethylamine and 3-aminopyridine and some compounds were epoxidized with mCPBA. A rat prostate testosterone $5{\alpha}$-reductase inhibitory activity of synthesized compounds was assessed by radioimmunoassay using [1,2,6,7-3H]-testosterone as substrate. All synthesized compounds showed lower activity than finasteride and the N-(3-pyridino)-$3{\beta}$-carboxycarbonyloxy-5-androstene-$17{\beta}$-carboxamide (12) showed weak inhibitory activity ($IC_{50}$: $2.4{\times}10^{-7}M$).

• Journal of the Korean Applied Science and Technology
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• v.25 no.4
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• pp.533-538
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• 2008

In order to fine antioxidant and whitening agent source from nature, the comparisons of antioxidative activity and tyrosinase inhibitory activity were carried out for various ethanol extract on Polygoni Multiflori Radix, Polygonati Rhizoma and Ephedrae Herba. Comparing for three ethanol extracts, the highest electron donating ability was found at Polygonati Rhizoma (86.6%), but, the highest SOD-like ability, at the Ephedrae Herba (47.8%). Xanthine oxidase experiment exhibited 95.7% of hindrance effect in Ephedrae Herba, and 84.0% in Polygonati Rhizoma. A tyrosinase inhibitory activity assay was conducted to evaluate the whitening effects of the extracts, The tyrosinase inhibitory activity was 6.5% in the Polygoni Multiflori Radix, 32.6% in the Polygonati Rhizoma, 64.0% in the Ephedrae Herba. Based on these results, we suggest that the ethanol extracts of Polygoni Multiflori Radix, Polygonati Rhizoma and Ephedrae Herba can be used as food and cosmetic ingredients.

• Microbiology and Biotechnology Letters
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• v.22 no.6
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• pp.700-706
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• 1994

Lactic acid bacteria in Kimchi fermentation were tested for inhibitory activity against Gram positive bacteria and Gram negative bacteria. The Lactobacillus brevis (KCCM 35464) was found to produce a antimicrobial substance. It showed relatively wide range of inhibition spectrum against gram positive and gram negative bacteria and maintained the inhibitory activity between pH 4.0 and pH 9.0. The antimicrobial substance was obtained in the stationary growth phase and was purified by gel chromatography. The inhibitory effect of the antimicrobial substance on sensitive bacterial strains was determined by filter paper test. The activity of antimicrobial substa- nce was stable at 75$\circ$C. On the basis of its electrophoretic pattern is SDS-PAGE, antimicrobial substance appeared as a single band of 59 KDalton.

• Archives of Pharmacal Research
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• v.22 no.1
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• pp.18-24
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• 1999

Various flavonoid derivatives were previously reported to possess the inhibitory activity on cyclooxygenase/lipoxygenase. And these properties of flavonoids might contribute to their anti-inflammatory activity in vivo. In this study, several polyhydroxylated/methoxylated flavonoid derivatives such as oroxylin A. wogonin, skullcapflavone II, tectorigenin and iristectorigenin A were isolated from the medicinal plants. these compounds were evaluated fro their inhibitory effects on cyclooxygenase/lipoxygenase from the homogenate of human platelets in vitro. It was found that isoflavones including daidzein and tectorigenin possessed the inhibitory activity on cycloooxygenase, although the potency of inhibition was far less than that of indomethacin. In addition, oroxylin A, baicalein and wogonin inhibited 12-lipoxygenase activity without affecting cyclooxygenase, which suggested that 5,6,7- or 5,7,8-trisubstitutions of A-ring of flavone gave favorable results. The IC50 values of oroxylin A and NDGA against 12-lipoxygenase were found to be 100 and 1.5 uM, respectively.

• Korean Journal of Pharmacognosy
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• v.42 no.3
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• pp.218-222
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• 2011

The purpose of this research is to study of inhibitory activity of protostane type triterpens against farnesyl-protein transferase (FPTase). The ingredients of Alismatis Rhizoma, alisol B 23-acetate, C 23-acetate, alisols B and A 24-acetate, and thirteen synthetic analogues from alisol B 23-acetate exhibited inhibition activity against FPTase by scintillation proximity assay method. As a result, alisol C 23-acetate, one of the constituents of Alismatis Rhizoma, the synthetic analogues carboxylated and hydroxylated on branch chain of protostane exhibited a significant inhibitory activity. However, the compounds significantly lowered the inhibitory activity, when there is no 3 position keto on protostane skeletone.

• Journal of the Korean Applied Science and Technology
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• v.25 no.2
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• pp.219-225
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• 2008

In order to fine antioxidant and whitening agent source from nature, the comparisons of antioxidative activity and tyrosinase inhibitory activity were carried out for various ethanol extract on Pueraria Radix, Poria Cocos, and Coptidis Rhizoma. Comparing for three ethanol extracts, the highest electron donating ability was found at Poria Cocos (81.2%), but, the highest SOD-like ability, at the Coptidis Rhizoma(58%). Xanthine oxidase experiment exhibited 23.3% of hindrance effect in Pueraria Radix, and 79.3% in Poria Cocos. To evaluate at the whitening effect, tyrosinase inhibitory activity was conducted. Tyrosinase inhibitory activity was detected at 17.9% in the Puerariae Radix, 5.2% in the Poria Cocos and 83.3% in the Coptidis Rhizoma. From these results, we suggest that the ethanol extracts from Pueraria Radix, Poria Cocos, and Coptidis Rhizoma can be used for cosmetic ingredients.

• Biomedical Science Letters
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• v.29 no.2
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• pp.88-94
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• 2023

In oriental medicine, the fruit of Actinidia polygama has long been used to alleviate the symptoms of gout, arthritis, and inflammation. In this study, it was to designed to analyze the antibacterial activity of A. polygama ethanol extract (APEE) against Streptococcus mutans, one of the major strains for dental caries, and Porphyromonas gingivalis, one of the critical strains for periodontal disease. The antibacterial activity of APEE was analyzed by disk diffusion, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) assays. In addition, it was also analyzed the inhibitory effect of APEE on bacterial growth and biofilm formation against both oral pathogens. APEE exhibited its antibacterial effect through the inhibited bacterial diffusion as well as low concentration of MIC and MBC. In addition, APEE significantly inhibited not only bacterial growth but also biofilm formation in a dose-dependent manner. Consequently, APEE showed potent antibacterial activity against both S. mutans and P. gingivalis, which indicates that APEE might be used as a potential antibacterial material for the improvement of oral healthcare.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.43 no.6
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• pp.648-653
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• 2010

This study was performed to investigate the inhibitory activity of Sargassum thunbergii (ST) against ${\alpha}$-amylase and elucidate the availability of ST extract as a functional food agent. To test the inhibitory activity of ST against ${\alpha}$-amylase, porcine pancreatic ${\alpha}$-amylase and potato starch were used as substrates. It was revealed that ST crude ethanol extracts have high ${\alpha}$-amylase inhibitory activity. Subsequently, ST crude ethanol extract was separated into five partition layers by solvent extraction: n-hexane, chloroform, ethyl acetate, butanol, and water. Chloroform and n-hexane fractions showed higher inhibitory activities than did acarbose (positive control). To confirm the changes in enzyme inhibitory activity by physical treatments, ST crude ethanol extract was subjected to heat, pH, and ${\gamma}$-irradiation treatments. In all heat treatments with the exception of one ($121^{\circ}C$, 15 min), the inhibitory activity was increased compared with the untreated group. With regard to pH stability, ST extract showed no significant changes at pH 4.6, but somewhat decreased inhibitory activity was revealed at pH 2, 8, and 10. On the other hand, ST ethanol extract was stable under ${\gamma}$-irradiation under all conditions (3.20 kGy). In summary, ST ethanol extract can be used in the food industry as a natural ${\alpha}$-amylase inhibitor.

• Journal of Microbiology and Biotechnology
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• v.12 no.4
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• pp.553-556
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• 2002

The inhibitory activity of fifty Bifidobacteria toward the infectivity of a rotavirus, which is the predominant cause of sporadic diarrhea in infants and young children, was investigated, and Bifidobacterium breve K-110 was found to have the most potent inhibitory activity. Accordingly, the rotavirus infection-inhibitory protein was purified, and its molecular weight was determined to be 76 kDa by SDS-PAGE. It was heat-labile and its 50% inhibitory concentration ($IC_{50}$) was 0.045 $\mu g/ml$.