• Title/Summary/Keyword: Potency

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Isolation and Antimicrobial Activity of a Naphthoquinone from Impatiens balsamina (봉선화의 항균활성성분(抗菌活性成分)과 항균력(抗菌力)에 관(關)한 연구(硏究))

  • Kang, Soo-Chul;Moon, Young-Hee
    • Korean Journal of Pharmacognosy
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    • v.23 no.4
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    • pp.240-247
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    • 1992
  • Impatiens balsamina Linne(Balsaminaceae) known as 'BONG SUN HWA' in Korea and has been used for the treatment of scrofulosis, carbunculus and dysenteria etc. Bioassay-guided fractionation of MeOH extract from the whole plants of Impatiens balsamina has afforded a simple naphthoquinone derivative, 2-methoxy-1,4-naphthoquinone. The structure of this compound was established by spectroscopic methods. This compound possessed strong antifungal activity against Candida albicans, AspergiIlus niger, Crytococcus neoformans and Epidermophyton floccusum. The activity of 2-methoxy-1,4-naphthoquinone on E. floccusum $(MIC{\;}:{\;}5.0{\;}{\mu}g/ml)$ was the same potency as that of nystatin. It showed also strong antibacterial activity against gram-positive bacteria Bacillus subtilis as well as gram-negative bacteria Salmonella typhimurium. Although the activity of this compound on gram-negative bacteria was lower than that of gram-positive bacteria.

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Potential Pests of Ginseng in Scarabaeids (풍뎅이류에 있어서의 인삼의 잠재 해충)

  • 김기황
    • Journal of Ginseng Research
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    • v.15 no.3
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    • pp.200-204
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    • 1991
  • Densities and larval food habits of Holotrichia titanis belonging to Melolonthinae, and of Anomala corpulenta and A. mfocuprea belonging to Rutelinae, collected from surroundings of ginseng fields, were investigated to determine potentia]s as ginseng pests in scarabaeids. H. titanis had similar food habit to the ginseng pests, H. morosa and H. diomphalia, although the density of H. titanis was relatively low during the period of survey, which indicates that the scarabaeid may have potentials to be a major pest with build-up or the population in the fields. However, A. corpulenta and A. rufacuprea with higher populations than H. morose and H. dicmphalia had no or low potency as ginseng pests since they had little preference to ginseng roots or did not feed on these. The latter two species in Rutelinae showed different food habits in relation to dead organic matter.

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Free Radical Scavenging Activity and Protective Ability of Methanolic Extract from Duchesnea indica Against Protein Oxidation and DNA Damage

  • Hu, Weicheng;Shen, Wei;Wang, Myeong-Hyeon
    • Preventive Nutrition and Food Science
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    • v.14 no.4
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    • pp.277-282
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    • 2009
  • The antioxidant potency of methanolic extract of Duchesnea indica (MDI; Indian strawberry) was investigated by employing various established in vitro systems, such as total phenolic content, 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, reducing power assay, metal chelating assay, superoxide radical scavenging activity and protective ability of DNA damage and protein oxidation. MDI inhibited metal chelating by 75.57% at 2 mg/mL, scavenged 50% DPPH free radical at 29.13 ${\mu}$g/mL, and eliminated approximately 46.21% superoxide radical at the concentration of 1 mg/mL. In addition, MDI showed strong ability on reducing power, DNA damage protection and protein oxidation protection. Overall, results suggested that MDI might be beneficial as a potent antioxidant and effectively employed as an ingredient in food applications.

Design and Synthesis of an Anticancer Diarylurea Derivative with Multiple-Kinase Inhibitory Effect

  • El-Gamal, Mohammed I.;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.33 no.5
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    • pp.1571-1576
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    • 2012
  • A diarylurea compound 1 possessing pyrrolo[3,2-$c$]pyridine nucleus was designed and synthesized with structure similarity to Sorafenib. Compound 1 was tested over 60-cancer cell line panel at a single dose concentration of 10 ${\mu}M$ and showed high activity. It was further tested in a five-dose mode to determine its $IC_{50}$, TGI, and $LC_{50}$ values over the 60 cell lines. Compound 1 showed high potency and good efficacy, and was accordingly tested at a single dose concentration of 10 ${\mu}M$ over a panel of 40 kinases. At this concentration, it completely inhibited the enzymatic activities of a number of oncogenic kinases, including ABL, ALK, c-RAF, FLT3, KDR, and TrkB. The target compound was subsequently tested over these 6 kinases in 10-dose testing mode in order to determine its $IC_{50}$ values.

Strategy to Overcome Drug Resistance That Develops during Treatment of Chronic Hepatitis B in Children

  • Hong, Suk Jin;Choe, Byung-Ho
    • Pediatric Gastroenterology, Hepatology & Nutrition
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    • v.15 no.2
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    • pp.63-73
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    • 2012
  • Development of antiviral resistance to lamivudine is the most important factor for the treatment failure. It is necessary to establish proper guidelines to overcome drug resistance for children with chronic hepatitis B. Primary treatment with lamivudine should be considered if patients are in immune-clearance phase and have persistently elevated ALT levels more than twice the upper limit of normal value. Before initiating the therapy, careful consideration of the patient's status is required to exclude abnormal liver function tests due to other causes. The treatment option should be carefully decided to suppress the viral replication effectively. To obtain good compliance, clinicians should educate patients and their parents. Appropriate monitoring for virologic breakthrough and genotypic resistance is important in deciding to change the treatment plan. Sequential monotherapy should be avoided and a combination of drugs in other categories is recommended. New antiviral agents, such as entecavir and tenofovir, which have high potency and high genetic barrier, are soon expected to be available for use with children.

Involutive Micanorm Logics with the n-potency axiom (N-멱등 공리를 갖는 누승적 미카놈 논리)

  • Yang, Eunsuk
    • Korean Journal of Logic
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    • v.20 no.2
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    • pp.273-292
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    • 2017
  • In this paper, we deal with some axiomatic extensions of the involutive micanorm logic IMICAL. More precisely, first, the two involutive micanorm-based logics $P_nIMICAL$ and $FP_nIMICAL$ are introduced. Their algebraic structures are then defined, and their corresponding algebraic completeness is established. Next, standard completeness is established for $FP_nIMICAL$ using construction in the style of Jenei-Montagna.

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Some of the Food Color Additives Are Potent Inhibitors of Human Protein Tyrosine Phosphatases

  • Shrestha, Suja;Bhattarai, Bharat Raj;Lee, Keun-Hyeung;Cho, Hyeong-Jin
    • Bulletin of the Korean Chemical Society
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    • v.27 no.10
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    • pp.1567-1571
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    • 2006
  • Synthetic color additives approved for general food use are sixteen in European Union, seven in U. S. A. and twelve in Japan. Twelve food dyes were examined for their inhibitory potency against human protein tyrosine phosphatases (PTPases). Half of the food colorants inhibited PTPases significantly and three of them were potent inhibitors with low micromolar IC50 values. Also examined were the synthetic dyes structurally similar but not allowed in food. Some of them were potent inhibitors of PTPases. Considering the importance of PTPases in cellular signal transduction, inhibition of PTPases by food colorants might cause harmful effects in human health.

Computational Study of Mutagen X

  • Cho, Seung-Joo
    • Bulletin of the Korean Chemical Society
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    • v.24 no.6
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    • pp.731-732
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    • 2003
  • Mutagen X (MX), 3-chloro-4-(dichloromethyl)-5-hydroxy-2(5H)-furanone is one of the most potent directing acting mutagen ever tested in SAL TA100 assay. Although MX analogues have been synthesized, tested for mutagenicity and modeled by structure-activity relationship (SAR) methods, the mechanism of interaction of these compounds with DNA to produce their remarkable mutagenic potency remains unresolved. MX exists as an equilibrium mixture of both ring and open form in water. This equilibrium is very fast for Ames test. Because the mixture is not separable by experimental methods, it is not clear which one is really responsible for the observed mutagenicity. There have been many debates that which one is really responsible for the observed mutagenicity. We used ab initio methods for the MX analogues. It seems both ring and open form could react with DNA bases as electrophiles. However, every open form has consistently lower LUMO energy than corresponding ring form. It is reasonable to assume that the major reaction will go through via open form for MX analogues. This suggest that the open form is more likely really mutagenic.

Histopathological Study on Inhibition of Oogenesis by Quercetin in Japanese medaka (Oryzias latipes) (Japanese medaka에 있어 Quercetin의 난자성숙 저해에 대한 조직병리학적 연구)

  • 황갑수
    • Environmental Analysis Health and Toxicology
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    • v.14 no.1_2
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    • pp.55-63
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    • 1999
  • Endocrine disrupting chemicals probably cause the cytological or/and morphological changes of germinal cells in gonad. Accordingly, this study was aimed to make sure that the effect of hormone-mimicking chemicals on gonad morphology such as decrease of germinal cells, inhibition of cellular maturation and change in the ratio of germinal cells in the different developmental phase can be observed by histopathological procedures and can be a useful bio-indicator for the evaluation of endocrine disruption by environmental chemicals. In this experiment, female Japanese medaka were exposured to quercetin, a phytoestrogen, at the concentration of 100 $\mu\textrm{g}$/L. quercetin showed the significant decrease in the number and rate of vitellogenic follicular oocytes in the treated group for 4 and 6 weeks. The weak development of yolk could be also observed. We could conclude that quercetin has anti-estrogenic or androgen-like potency by exerting the inhibition effect on oogenesis in fish female- gonad. From the result of this study, the applied methods and techniques can be evaluated to be a useful biomonitoring means for water pollution, expecting a good result of the subsequent study on apoptosis.

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Tocopherols and Tocotrienols in Cereal Grains (화곡류 종실의 토코페롤과 토코트리에놀 연구현황과 전망)

  • 이동진;이지영
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.48
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    • pp.1-12
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    • 2003
  • Vitamin E is a fat-soluble vitamin that exists in eight different forms, which are $\alpha$, $\beta$, $\gamma$, and $\delta$ tocopherol, and $\alpha$, $\beta$, $\gamma$, and $\delta$ tocotrienol. Tocopherols and tocotrienols are important antioxidant in foods, feeds and their raw materials, where they scavenge lipid radicals. Each form has its own biological activity, the measure of potency or functional use in the body. Antioxidants such as vitamin E act to protect cells against the effects of free radicals, which are potentially damaging by-products of the body's metabolism. Free radicals can cause cell dam-age that may contribute to the development of cardiovascular disease and cancer, The content of tocopherols and tocotrienols vary depending on the environmental condition such as growing regions, temperature, crops and varieties. This report deals with chemical and physical properties and extends to their nutritional and health effect on the tocopherols and tocotrienols in cereal grains.