• Title/Summary/Keyword: potency

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3D-QSAR Study of Melanin Inhibiting (S)-(+)-Decursin and its Analogues by Pharmacophore Mapping

  • Lee, Kyeong;Jung, Sang-Won;Naik, Ravi;Cho, Art E.
    • Bulletin of the Korean Chemical Society
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    • v.33 no.1
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    • pp.149-152
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    • 2012
  • The (S)-(+)-decursin and its analogues are reported as potent inhibitors of melanin production in B16 murine melanoma cells. In order to understand the factors responsible for potency as well as inhibition of potency of (S)-(+)-decursin and its analogues, three-dimensional quantitative structure-activity relationship (3D-QSAR) studies were performed. Since receptor structures are not available, a pharmacophore model was constructed. Using PHASE, we generated 3 different models and selected the seven-site model, which returned excellent statistical values ($r^2$ = 0.9127, $Q^2$ = 0.6878, Pearson-R = 0.9014). Using the generated pharmacophore model, we screened a natural products library and obtained 4'-epi-decursin as the most related compound. 4'-epidecursin is similar to (S)-(+)-decursin, but shows additional interaction possibilities with tyrosinase. The study thus sheds some light on possibility of developing more potent tyrosinase inhibitors.

Synthesis and Antiproliferative Activity of New Aminoisoquinolinylurea Derivatives against Melanoma Cell Line

  • Cho, Hye Jung;El-Gamal, Mohammed I.;Oh, Chang-Hyun;Lee, So Ha;Kim, Garam;Hong, Jun Hee;Choi, Hong Seok;Yoo, Kyung Ho
    • Bulletin of the Korean Chemical Society
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    • v.33 no.11
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    • pp.3635-3639
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    • 2012
  • A series of new diarylureas possessing aminoisoquinoline scaffold was synthesized, and their in vitro antiproliferative activity against A375P human melanoma cell line was tested. Compounds 1d, 1l, 1n, 1p, 1q, and 1t showed superior potency against A375P to Sorafenib. The highest potency was shown by compound 1p possessing 3,5-bis(trifluoromethyl)phenyl terminal ring with $IC_{50}$ value of $0.41{\mu}M$.

The Experimental Study on Anti-bacterial Potency of Jinpi-san on Staphylococcus aureus & Staphylococcus epidermidis. (진피산(秦皮散)이 Staphylococcus aureus와 Staphylococcus epidermidis에 미치는 항균효과에 대한 실험적 연구)

  • Seo, Hyung-Sik
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.20 no.1 s.32
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    • pp.195-200
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    • 2007
  • Objective : This experimental study was performed to investigate the effect of Jinpi-san on Staphylococcus aureus(S. aureus) and Staphylococcus epidermidis(S. epidermidis) that induce keratitis. Methods : Minimal inhibitory concentration(MIC) was measured by dropping to $50{\mu}l$ according to density Jinpi-san(100%, 10%, 1%, 0.1 %). Anti-bacterial potency was measured by the size of inhibition zone with change of volume. Results : 1. MIC on S. aureus in Jinpi-san was $40{\mu}l$ undiluted solution. 2. MIC on S. epidermidis in Jinpi-san was $20{\mu}l$ undiluted solution. Conclusions : These results indicate that Jinpi-san can be used to cure S. aureus, S. epidermidis that induce eye disease(keratitis). If further study is performed, the use of eye drops will be valuable and beneficial in the clinical medicines.

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Inhibitory Activities of Chinese Herbs that Clear Heat on $3{\alpha}-Hydroxysteroid$ dehydrogenase (한방청열제의 $3{\alpha}-Hydroxysteroid$ dehydrogenase에 대한 억제효과)

  • Ahn, Jung-Su;Choi, Seung-Youn;Kwon, Yong-Soo;Kim, Chang-Min
    • Korean Journal of Pharmacognosy
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    • v.29 no.1
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    • pp.8-12
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    • 1998
  • $3{\alpha}-Hydroxysteroid$ dehydrogenase $(3{\alpha}-HSD)$ is one of the main enzymes involved in the metabolism of the active androgen, dihydrotestosterone. The NAD(P)-linked $3{\alpha}-HSD$ of rat liver cytosol is powerfully inhibited by the non-steroidal anti-inflammatory drugs in rank-order of their therapeutic potency. This observation has now been developed into a rapid screen for predicting the potency of products that show anti-inflammatory effect. 52-Chinese Herbs that clear heat were screened by using this method.

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Screening of the Acetylcholinesterase Inhibitors from Medicinal Plants (생약의 아세틸콜린에스터라제 억제활성 검색)

  • Lee, Bong-Ho;Ryu, Geon-Seek;Lee, Eun Seog;Kang, Kye-Jung;Hwang, Dho-Yeun;Hong, Nam-Doo;Choi, Byoung-Wook
    • Korean Journal of Pharmacognosy
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    • v.28 no.4
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    • pp.167-173
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    • 1997
  • We have tested 101 species traditional medicinal plants on Acetylcholinester ase inhibition. Among them. Caesalpina sappan. Cnidium offcinale, Coptis japonica, Ephedra sinica, Eribotrya japonica, Gardenia jasminoides, Liriope platyphylla, Lonicera japonica, Paeonia suffruticosa, Phyllostachys nigra, Polygonum multiflorum, Prunella vulgaris, Rheum undulatum, Salvia miltiorrhiza and Uncaria rhynchophylla showed strong inhibition potency over 88%. In addition, Aconitum carmichaeli, Caesalphina sappan, Cinnamomun japonica, Citrus unshiu, Hordeum vulgare, Glycine max and Rehmannia glutinosa showed relatively good inhibition potency over 80%.

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Market and trend of alternative sweeteners (저칼로리 저감미도 대체감미료 시장 및 동향)

  • Kim, Yang Hee;Kim, Seong-Bo;Kim, Su Jin;Park, Seung-Won
    • Food Science and Industry
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    • v.49 no.3
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    • pp.17-28
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    • 2016
  • The concerns over obesity and obesity-related health problems are increasing as many consumers relate these health problems with sugar. The demand for sugar reduction is also rising and regulatory movement by governments including Korea is driven to reflect such demand. For the past decades, there have been diverse development and marketing of various sweeteners to substitute sucrose and high fructose corn syrup. Low caloric alternative sweeteners can be divided into high intensity sweeteners that have greater sweetness potency compared to sucrose, and low intensity sweeteners such as polyols, oligosaccharides and rare sugars that have less sweetness potency. This paper discusses representative low caloric alternative sweeteners, their market and trend.

1-Methyl Substituent and Stereochemical Effects of 2-Phenylcyclopropylamines on the Inhibition of Rat Brain Mitochondrial Monoamine Oxidase A and B

  • Kang, Gun-Il;Hong, Suk-Kil;Choi, Hee-Kyung
    • Archives of Pharmacal Research
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    • v.10 no.1
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    • pp.50-59
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    • 1987
  • (E)-2-Phenylcyclopropylamine ((E)-TCP), (Z)-2-Phenylacyclopropylamine ((Z)-TCP), (E)-1-methyl-2-phenylcyclopropylamine ((E)-MTCP), and (Z)-1-methyl-2-phenylcyclopropylamine ((Z)-MTCP) were synthesized and used to determine to what extent 1-methylsubstitution and stereochemistry of 2-phenycyclopropylamines affect inhibition of monoamine oxidase (MAO). Inhibition of rat brain mitochondrial MAO-A and B by the compounds were measured using serotonin and benzylamine as the substrate, respectively and $IC_{50}$ values obtianed with 95% confidence limits by the method of computation. For the inhibition of MAO-A, (E)-MTPC ($IC_{50}$ = 6.2 * $10^{-8}$M) was found to be 37 times more potent than (Z)-MTCP ($IC_{50}$ = 7.8 * $10^{-8}$M), was 7 times more potent than (Z)-MTCP($IC_{50}$= 4.7 * $10^{-7}$M) and (E)-TCP($IC_{50}$ =7.8 * $10^{-8}$M),0.6 times as potent as (Z)- TCP ($IC_{50}$ = 4.4 * $10^{-8}$M). The results suggested that while without 1-methyl group, potency of a (Z)-isomer was comparable to that of (E)-isomer, the methyl group in its (Z)-position was very unfavorable to the inhibition of MAO and that in its (E)-position, the methyl group contributed positively to the potency as found by the fact that (E)-MTCP was 1-5 times more potent than (E)-TCP. In view of the selective inhibition of MAO-A- or B over MAO-A and 1-methyl substitution as well as the stereochemical factors did not significantly influence the selectivity.

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Renewable Energy Potentials and Promotion Policies in Indonesia (인도네시아 신재생 에너지 잠재력 및 보급 정책)

  • Yurnaidi, Zulfikar;Kim, Suduk
    • 한국신재생에너지학회:학술대회논문집
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    • 2010.11a
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    • pp.137.1-137.1
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    • 2010
  • For Indonesia, sustainable energy supply is an important factor to preserve the stable economic growth. One important strategy is development of renewable energy, which has not been fully exploited yet. The paper examines the potency of renewable energy in Indonesia. Currently, biomass composes 23% of total primary energy supply, while geothermal and hydropower has a combined share of 3%. But according to the overall potency of renewable energy, hydropower is found to have the highest available resource of 76 GW, followed by biomass and geothermal by 49.81 GW and 28.53 GW, respectively. Although the solar radiation is only at modest level ($4.80kWh/m^2/day$), the tropical all year sunlight can boost the competitiveness of solar photovoltaic and thermal application. As for wind energy, the average speed of 3-6 m/s requires the development of low speed wind turbine. The examination of electricity and petroleum product prices through international comparison for non-OECD countries shows fifth lowest price level for both of petroleum products and electricity for industrial use. As for household electricity price, Indonesia is placed the second among all the countries compared. The energy subsidy and price structure are examined in detail because it could be a source of hindrance to renewable energy promotion. The examination of renewable energy potency in this study could provide insights about recent development of renewable energy in Indonesia. As an outcome of policy examination, the price comparison analysis suggests Indonesia to reduce or even remove the energy subsidies in the long run. These findings can be utilized to formulate effective policies for renewable energy promotion.

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