• Title/Summary/Keyword: IC_{50}$

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Inhibition of Low Density Lipoprotein-oxidation, ACAT-1, and ACAT-2 by Lignans from the Bark of Machilus thunbergii

  • Shrestha, Sabina;Park, Ji-Hae;Lee, Dae-Young;Cho, Jin-Gyeong;Lee, Do-Gyeong;Cho, Moon-Hee;Jeong, Tae-Sook;Kang, Hee-Cheol;Baek, Nam-In
    • Journal of Applied Biological Chemistry
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    • v.54 no.1
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    • pp.63-66
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    • 2011
  • The bark of Machilus thunbergii was extracted with 80% aqueous methanol (MeOH), and the concentrated extract was partitioned using ethyl acetate (EtOAc), butanol (n-BuOH), and $H_2O$, successively. From the EtOAc fraction, five lignans were isolated through the repeated silica gel, octadecyl silica gel (ODS) and, Sephadex LH-20 column chromatography. Based on nuclear magnetic resonance (NMR), mass spectroscopy (MS), and infrared spectroscopy (IR) spectroscopic data, the chemical structures of the compounds were determined to be machilin A (1), machilin F (2), licarin A (3), nectandrin A (4), and nectandrin B, (5). This study presents comparative account of five lignans from M. thunbergii bark contributing inhibition of low density lipoprotein (LDL), ACAT-1, and ACAT-2. Compounds 2-5 showed varied degree of antioxidant activity on LDL with $IC_{50}$ values of 2.1, 11.8, 15.3, and $4.1{\mu}M$. Compounds 1, 2, and 3 showed inhibition activity on ACAT-1 with values $63.4{\pm}6.9%$ ($IC_{50}=66.8{\mu}M$), $53.7{\pm}0.9%$ ($IC_{50}=109.2{\mu}M$), and $78.7{\pm}0.2%$ ($IC_{50}=40.6{\mu}M$), respectively, at a concentration of 50 mg/mL, and on ACAT-2 with values $47.3{\pm}1.5%$ ($IC_{50}=149.7{\mu}M$), $39.2{\pm}0.2%$ ($IC_{50}=165.2{\mu}M$), and $52.1{\pm}1.0%$ ($IC_{50}=131.0{\mu}M$, respectively, at a concentration of 50 mg/mL.

Screening of Inhibitory Activity of Edible Mushrooms on Dopamine ${\beta}-Hydroxylase$ (식용 버섯류의 도파민 베타 수산화효소에 대한 저해활성 검색)

  • Hwang, Keum-Hee;Kim, Hyun-Ku;Han, Yong-Nam
    • Korean Journal of Food Science and Technology
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    • v.29 no.2
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    • pp.194-197
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    • 1997
  • Dopamine ${\beta}-hydroxylase\;(DBH)$ catalyses the enzymatic reaction of dopamine to norepinephrine. For the purpose of screening DBH inhibitory activity from edible mushrooms, Ganoderma lucidum, Agaricus bisporus and Lentinus edodes were examined by tracing inhibitory activities against bovine adrenal DBH, utilizing tyramine as a substrate. Among the three edible mushrooms tested, Ganoderma lucidum showed potent enzyme inhibitory activilies above 100% against DBH in chloroform fraction. Lentinus edodes and Agaricus bisporus showed inhibitory activities in ethylacetate fraction on 79.7% and 64.7%, respectively. Each solvent fraction of these mushrooms were assessed in the aspects of their inhibitory activities against DBH, and their $IC_{50}$ values were calculated. $IC_{50}$ value of chloroform fraction of Ganoderma lucidum was $1.60{\times}10^{-4}\;g$, and those of ethylacetate fractions of Agaricus bisporus and Lentinus edodes were $5.50{\times}10^{-4}\;g\;and\;2.35{\times}10^{-4}\;g$, respectively.

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Physiological Activities of Thiacremonone Produced in High Temperature and High Pressure Treated Garlic

  • Woo, Koan Sik;Hwang, In Guk;Kim, Hyun Young;Lee, Sang Hoon;Jeong, Heon Sang
    • Preventive Nutrition and Food Science
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    • v.21 no.1
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    • pp.68-72
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    • 2016
  • To examine the possibility of using thiacremonone isolated from high-temperature-high-pressure treated garlic, this study investigated the physiological activities properties. The $IC_{50}$ values of hydroxyl, superoxide, hydrogen peroxide, and nitric oxide radical scavenging activities of thiacremonone were 92.50, 65.05, 12.60, and $81.53{\mu}g/mL$, respectively. On the other hand, the activities of vitamin C were 104.93, 99.43, 42.42, and $122.64{\mu}g/mL$, and the activities of butylated hydroxyanisole were 37.22, 68.45, 22.47, and $40.54{\mu}g/mL$, respectively. The $IC_{50}$ value of ACE inhibition activities of thiacremonone and captoprill were 0.265 and $0.036{\mu}g/mL$, respectively. The $IC_{50}$ value of xanthine oxidase inhibition activities of thiacremonone and allopurinol were 39.430 and $9.346{\mu}g/mL$, respectively. The $IC_{50}$ value of tyrosinase inhibition activities of thiacremonone and kojic acid were 101.931 and $65.648{\mu}g/mL$, respectively.

A PROMISING NEW ANTI-WRINKLE INGREDIENT: Pericarpium castaneae extracts

  • Kim, Beom-Jun;Jo, Byoung-Kee;Kim, Jeong-Ha
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.25 no.4 s.34
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    • pp.57-63
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    • 1999
  • Pericarpium castaneae extracts have variously potent activities, such as anti-oxidative activity and free radical scavenging activity. in vivo and in vitro studies both indicate that pericarpium castaneae extracts acts as a free radical scavenger($IC_{50}:7.6{\mu}g/ml$) stronger than gallic acid($IC_{50}:12.5{\mu}g/ml$) and ellagic acid($IC_{50}:15{\mu}g/ml$) which could prevent cutaneous UV damages and skin aging. The extracts showed a good effect as a anti-oxidant($IC_{50}:50{\mu}g/ml$). It was shown that the appearance of wrinkle in human skin was reduced by topical application of pericarpium castaneae extracts. And the treatment of human skin with the extracts increased the elasticity and moisture of the skin. We investigated the effect of the pericarpium castaneae extracts on production of extracellular matrix using cultured A431 fibroblast cells. The results indicated that the extracts had no detectable effect on collagen synthesis. But synthesis of cell adhesion protein was increased by the extracts. The results suggest that increase of cell adhesion protein synthesis by pericarpium castaneae extracts has closely related to reduction of wrinkle in skin.

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EFFICACY AND BIOLOGICAL ACTIVITIES OF A NEW ANTI-AGING AGENT OBTAINED FROM ARECA CATECHU

  • Lee, Kun-Kook;Lee, Kwang-Sik;Kim, Jeong-Ha;Jo, Byung-Kee;Choi, Jung-Do
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.24 no.3
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    • pp.24-30
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    • 1998
  • Inhibitory effects of the new material obtained from Areca catechu seed (CC-516) according to a special process, and its applicability to the skin as a cosmetic raw material in terms of its efficacy were presented. Areca catechu extract out of 150 medicinal plants, exhibited high inhibitory effect on the porcine pancreatic elastase ($IC_{50}$ : $40.8{\mu}$g/ml). It also had an inhibitory effect on the human leukocyte elastase ($IC_{50}$ : 48.1$\mu$g/ml), hyaluronidase ($IC_{50}$ : $416{\mu}$g/ml), antioxidative activity ($IC_{50}$ : $45.4\mu$g/ml) and free radical scavenging activity ($SC_{50}$ : $10.2{\mu}$g/ml). The cream contained 3% of CC-516 improved skin hydration above 16.5%. Especially, the skin elasticity increases more than 35% and skin wrinkles decreased more than 23%. The CC-516 was designed to be utilized in cosmetology. The cream containing 3% of this product has not only protecting effect on the skin mechanical properties provided by the collagen and the elastin in the derm but also restructuring effect of scarring or aging tissue.

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A PROMISING NEW ANTI-WRINKLE INGREDIENT : Pericarpium castaneae extracts

  • Kim, Beom-Jun;Jo, Byoung-Kee;Kim, Jeong-Ha
    • Proceedings of the SCSK Conference
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    • 1999.10a
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    • pp.57-64
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    • 1999
  • Pericarpium castaneae extracts have variously potent activities, such as anti-oxidative activity and free radical scavenging activity. in vivo and in vivo studies both indicate that pericarpium castaneae extracts acts as a flee radical scavenger ($IC_{50}$/: 7.6$\mu\textrm{g}$/ml) stronger than gallic acid($IC_{50}$/: 12.5$\mu\textrm{g}$/ml) and ellagic acid($IC_{50}$/: 15$\mu\textrm{g}$/ml) which could prevent cutaneous UV damages and skin aging. The extracts showed a good effect as a anti-oxidant ($IC_{50}$/: 50$\mu\textrm{g}$/ml). It was shown that the appearance of wrinkle in human skin was reduced by topical application of pericarpium castaneae extracts. And the treatment of human skin with the extracts increased the elasticity and moisture of the skin. We investigated the effect of tile pericarpium castaneae extracts on production of extracellular matrix using cultured A431 fibroblast cells. The results indicated that the extracts had no detectable effect on collagen synthesis, But synthesis of cell adhesion protein was increased by the extracts. The results suggest that increase of cell adhesion protein synthesis by pericarpium castaneae extracts has closely related to reduction of wrinkle in skin.

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High Speed InP HBT Driver Ie For Laser Modulation

  • Sung Jung Hoon;Burm Jin Wook
    • Proceedings of the IEEK Conference
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    • 2004.08c
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    • pp.883-884
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    • 2004
  • High-speed IC for time-division multiplexing (TDM) optical transmission systems have been designed and fabricated by using InP heterojunction-bipolar-transistor (HBT) technology. The driver IC was developed for driving external modulators, featuring differential outputs and the operation speed up to 10 Gbps with an output voltage swing of 1.3 Vpp at each output which was the limit of the measurement. Because -3 dB frequency was 20GHz, this circuit will be operated up to 20Gbps. 1.3Vpp differential output was achieved by switching 50 mA into a 50 $\Omega$ load. The power dissipation of the driver IC was 1W using a single supply voltage of -3.5Y. Input md output return loss of the IC were better than 10 dB and 15 dB, respectively, from DC to 20GHz. The chip size of fabricated IC was $1.7{\Box}1.2 mm^{2}$.

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Effect of Atrazine, Perfluorooctanoic Acid and Zearalenone on IFNγ, TNFα, and IL-5 mRNA Expression in Jurkat Cells

  • Lee, Sung-Woo;Son, Hwa-Young;Yoon, Won-Kee;Jung, Ju-Young;Park, Bae-Keun;Cho, Eun-Sang;Park, Sang-Joon;Kim, Tae-Hwan;Ryu, Si-Yun
    • Biomolecules & Therapeutics
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    • v.18 no.3
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    • pp.286-293
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    • 2010
  • Cytokine production is a sensitive indicator for monitoring perturbations of the immune system by xenobiotics in animals and humans. In the present study, we evaluated the changes in $IFN{\gamma}$, IL-5 and $TNF{\alpha}$ mRNA expression after atrazine (ATZ), perfluorooctanoic acid (PFOA) or zearalenone (ZEA) exposure in Jurkat cells. The IC50 (concentration for a 50% inhibition of cell proliferation) of PFOA and ZEA after 3 days culture were $226.6\;{\mu}M$ and $52.6\;{\mu}M$, respectively. The effects of ATZ on cytokine expression followed in increasing order of $IFN{\gamma}$>IL-5>$TNF{\alpha}$ at $3\;{\mu}M$ and at the lower concentrations the degree of effects on three cytokines were less clear between the cytokines when compared to control level. PFOA had marked increasing effect in order of $IFN{\gamma}$>$TNF{\alpha}$>IL-5 mRNA expression at IC50, and these patterns were continued at the lower concentrations, IC50/2 and IC50/4. ZEA caused the overexpression of cytokine mRNAs in order of IL-5>$IFN{\gamma}$>$TNF{\alpha}$ at both IC50 and IC50/2, and at IC50/4 the overexpression order was IL-5>$TNF{\alpha}$. On other hand, $IFN{\gamma}$ was less distinct compared to the control. These data indicate that ATZ, PFOA and ZEA caused the overtranscription of $IFN{\gamma}$, IL-5 and $TNF{\alpha}$ mRNA, and the overproduction of these cytokines may eventually lead to immune disorders.

o-Dihydroxyisoflavone Derivatives from Highly Aged Korean Fermented Soybean Paste by Jang Yang Process and Its Biological Activity (장양(藏釀) 기술이 사용된 전통 고숙성 된장에서 유래한 o-Dihydroxyisoflavone 유도체의 생리활성)

  • Kim, Dong-Hyun;Park, Jun-Seong;Park, Nok-Hyun;Moon, Eun-Jeong;Yu, Sun-Hye;Kim, Duck-Hee;Kim, Han-Kon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.35 no.3
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    • pp.203-208
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    • 2009
  • Doenjang (Korean fermented soybean paste) is a unique fermented food in Korea. It has been traditionally manufactured from soybeans, by Jang Yang process. We focused on the newly formed compound in highly aged Doenjang and its biological activity. One new o-dihydroxyisoflavone, 7,3',4'-trihydroxyisoflavone and two known o-dihydroxyisoflavone derivatives were isolated from 5-year-old Doenjang and evaluated as potent antioxidant and whitening effect by comparing with other known isoflavone. 7,8,4'-Trihydroxyisoflavone (compound 1), 7,3',4'-trihydroxyisoflavone (compound 2) and 6,7,4'-trihydroxyisoflavone (compound 3) inhibited DPPH (diphenyl-1-picrylhydrazyl) formation by 50 % at a concentration of $21.5{\pm}0.2$, $28.7{\pm}0.4$ and $32.6{\pm}0.6$ ($IC_{50}$) respectively, whereas daidzein showed weak DPPH radical scavenging activity. In superoxide scavenging effect were measured in one assay. Compound 1 ($IC_{50}=18.10{\pm}0.2{\mu}M$) and 2 ($IC_{50}=10.54{\pm}0.4{\mu}M$) show significant inhibitory activity and greater effect than L-ascorbic acid. But compound 3 and daidzein showed lower inhibition activity. Also, o-dihydroxyisoflavone derivatives evaluated as potent inhibitors on tyrosinase activity and melanin formation in melan-a cells. Compound 1 ($IC_{50}=11.21{\pm}0.2{\mu}M$), compound 2 ($IC_{50}=5.23{\pm}0.6{\mu}M$) exhibited significant inhibitory effect on tyrosinase activity. Furthermore, those compounds are significantly suppressed the cellular melanin formation by 50 % at a concentration of $12.23{\pm}0.7{\mu}M$ (1) and $7.83{\pm}0.7{\mu}M$ (2). This result suggests that 7,3',4'-trihydroxyisoflavone from highly aged Doenjang could be used as an active ingredient for cosmetics.

Cytotoxicity on Cancer cells of the Extract of Sophora flavescens Ait. (고삼 추출물의 암세포에 대한 세포독성)

  • Lee, Hyun-Ok;Chun, Ju-Yeon;Lee, Ji-Youn;Kim, Chang-Hee
    • Journal of dental hygiene science
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    • v.2 no.1
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    • pp.15-19
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    • 2002
  • In this study, we investigated the cytotoxicity of ethyl acetate subfraction of Sophora flavescens Ait.(EASS) on cancer cells using MTT quantitative analysis. The EASS was cytotoxicity from the concentration of 6.25 g/ml to KB, B16, HeLa, and MCF-7 cancer cells and the cytotoxicity was significant, (p < 005) increased as the concentrations of EASS were increased, (12.5, 25, 50, 100 g/ml). The IC for KB, B16, HeLa, and MCF-7 were 56.58, 65.43, 83.95, and 106.65 g/ml, respectively. Conclusively, the EASS inhabited the growth of cancer cells and the order of potency of cytotoxicity was KB > B16 > HeLa > MCF-7.

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