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In vitro Assessment of Cytochrome P450 Inhibition by Red Ginseng Ginsenosides (홍삼 Ginsenoside의 Cytochrome P450 저해 활성 평가)

  • Ryu, Chang Seon;Shin, Jang Hyun;Shin, Byoung Chan;Sim, Jae Han;Yang, Hyeon Dong;Lee, Sung Woo;Kim, Bong-Hee
    • YAKHAK HOEJI
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    • v.59 no.2
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    • pp.49-54
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    • 2015
  • In the present study we evaluated comparative herb-drug interaction potential of red ginseng total powder, ginsenoside Rg1, and Rb1 by inhibition of CYP isoforms including CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 using pooled human liver microsomes (HLMs). As measured by liquid chromatography-electrospray ionization tandem mass spectrometry, red ginseng total powder inhibited significantly activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and testosterone 6-beta hydroxylation by CYP3A4, but the $IC_{50}$ values were higher than $556{\mu}g/ml$. Activities of CYP2B6, CYP2C9, CYP2D6 and CYP3A4 were inhibited by ginsenoside Rb1. Also, activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6 and testosterone 6-beta hydroxylation by CYP3A4 were inhibited by ginsenoside Rg1. The $IC_{50}$ values of ginsenoside Rb1 and Rg1 were higher than $200{\mu}g/ml$. Based on $IC_{50}$ values against CYP isoforms, ginsenosides-drug interactions by CYP inhibition may be very low in clinical situations.

INVERTIBLE INTERPOLATION ON AX = Y IN A TRIDIAGONAL ALGEBRA ALG𝓛

  • JO, YOUNG SOO;KANG, JOO HO;PARK, DONG WAN
    • Honam Mathematical Journal
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    • v.27 no.2
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    • pp.243-250
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    • 2005
  • Given operators X and Y acting on a separable Hilbert space ${\mathcal{H}}$, an interpolating operator is a bounded operator A such that AX = Y. We show the following: Let ${\mathcal{L}}$ be a subspace lattice acting on a separable complex Hilbert space ${\mathcal{H}}$. and let $X=(x_{ij})$ and $Y=(y_{ij})$ be operators acting on ${\mathcal{H}}$. Then the following are equivalent: (1) There exists an invertible operator $A=(a_{ij})$ in $Alg{\mathcal{L}}$ such that AX = Y. (2) There exist bounded sequences {${\alpha}_n$} and {${\beta}_n$} in ${\mathbb{C}}$ such that $${\alpha}_{2k-1}{\neq}0,\;{\beta}_{2k-1}=\frac{1}{{\alpha}_{2k-1}},\;{\beta}_{2k}=-\frac{{\alpha}_{2k}}{{\alpha}_{2k-1}{\alpha}_{2k+1}}$$ and $$y_{i1}={\alpha}_1x_{i1}+{\alpha}_2x_{i2}$$ $$y_{i\;2k}={\alpha}_{4k-1}x_{i\;2k}$$ $$y_{i\;2k+1}={\alpha}_{4k}x_{i\;2k}+{\alpha}_{4k+1}x_{i\;2k+1}+{\alpha}_{4k+2}x_{i\;2k+2}$$ for $$k{\in}N$$.

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Synthesis of $TiB_2-Al_2O_3$ Composite by Self-Propagating High Temperature Synthesis (SHS) and Its Pressureless Sintering (SHS법에 의한 $TiB_2-Al_2O_3$계 복합물의 합성 및 상압소결에 관한 연구)

  • 최상욱;조동수;김세용;남건태
    • Journal of the Korean Ceramic Society
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    • v.31 no.5
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    • pp.552-560
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    • 1994
  • A composite of TiB2-Al2O3 system was successfully prepared from a mixture of TiO2, B2O3, and Al by self-propagating high temperature synthesis (SHS) with a novel characteristic, utilizing the internal oxidation heat of aluminium metal of the mixture, instead of by a conventional technique, externally heating a mixture of Ti, B and Al2O3. From a mixture with B/Ti molar ratio of =2.0, pure two phases of TiB2 and $\alpha$-Al2O3 with good crystallinity and small, uniform sizes were formed. However, when the B/Ti molar ratio of the mixture goes to a value less than 2.0, in addition to the above main minerals, a small smounts of metastable phases such as TiB and Ti3B4 were formed. It was found that about 60%, the optimum green density of compacts gave their highest reaction rate and temperature during SHS process. TiB2-Al2O3 system composite with B/Ti molar ratio of =2.0 could be pressurelessly sintered even at 190$0^{\circ}C$ under Ar gas flows without any addition of sintering aids, showing their good properties such as 91.2% in relative density, 2750 kgf/$\textrm{mm}^2$ in Vickers hardness and 2620 kgf/$\textrm{cm}^2$ in flexural strength.

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The Action of ATP on Phospholipase $A_2$Activation in C6 Cells (C6세포에서 phospholipase $A_2$활성에 대한 ATP의 작용)

  • 심상수;김명준;윤신희;김창종;조양혁
    • YAKHAK HOEJI
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    • v.45 no.4
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    • pp.413-418
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    • 2001
  • To investigate action of ATP on ischemia-induced brain injury, we measured phospholipase $A_2$activity and nitric oxide (NO) production in C6 cells. ATP alone did not have any influence on phospholipase $A_2$activity but increased NO production. Glutamate (1 mM) significantly increased phospholipase $A_2$activity whereas did not increased NO production. ATP significantly inhibited phospholipase $A_2$activation induced by 0.1 $\mu$M A23187, 1 mM glutamate and 1 mM $H_2O$$_2$, but did not inhibited 1 $\mu$M PMA-induced phospholipase $A_2$activation. From the above results, it is suggested that the action of ATP in C6 cells has dual actions, such as the inhibition of agonist-induced phospholipase $A_2$activation and the increase of NO production.

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A Study on the Synthesis of Antibacterial and Antifungal Naphthoquinoids (항진균, 항박테리아 작용이 있는 나프토퀴논꼴 화합물의 합성에 관한 연구)

  • 박외숙;임재경;장봉석;김주천
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.122-122
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    • 1993
  • 살균, 정균, 살진균, 정진균등의 효능이 있는 나프토퀴논꼴 화합물인 6-oxo-3, 4, 4a, 5-tetrahydro-3-hydroxy-2,2-dimethylnaphtho [1,2] pyran(1)과 그의 유도체인 9-methoxy-6-oxo-3, 4, 4a, 5-tetrahydro-3-hydroxy-2, 2-dimethylnaphtho [1,2] pyran(2), 8,9-dimethoxy-6-oxo-3, 4, 4a, 5-tetrahydro-3-hydroxy-2, 2-dimethylnaph-the [1,2] pyran(3), 9-bromomethyl-6-oxo-3, 4, 4a, 5-tetrahydro-3-hydroxy-2, 2-dimethyl-naphtho [1,2] pyran(4)와 8, 9-methylenedioxy-6-oxo-3, 4, 4a, 5-tetrahydro-3-hydroxy-2, 2-dimethylnaphtho [1,2] pyran(5)을 손쉽게 구할 수 있는 benzene, anisole, 1, 2-di-methoxybenzene, bromomethylbenzene, 1, 3-benzodioxole등을 원료로 하여 합성하는 것이 본 연구의 목적이다.

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Promoter Methylation and Expression of CYP1A2 in Dielhylnitrosamine-induced Mice liver Tumors (Diethylnitrosamine에 의하여 유발된 마우스 간 종양의 CYP1A2 메틸화와 발현)

  • Jin, Bo-Hwan;Oh, Sae-Jin;Ryu, Doug-Young
    • Environmental Mutagens and Carcinogens
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    • v.26 no.3
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    • pp.86-88
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    • 2006
  • Cytochrome P450 1A2 (CYP1A2) is a xenobiotic metabolizing enzyme that is tissue-specifically expressed in the mammalian liver. In this study, the extent of CYP1A2 promoter methylation was analyzed to determine its potential role in the regulation of CYP1A2 in diethylnitrosamine (DEN)-induced mouse liver tumors. CYP1A2 mRNA was under-expressed about three fold in DEN-induced liver tumors compared to age-matched control livers. The CYP1A2 promoter was hypermethylated in DEN-induced liver tumors compared to controls, especially in a promoter domain close to the coding region. These results suggest that promoter methylation is involved in the regulation of CYP1A2 in mouse liver tumors.

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Synthesis and Pharmacological Studies of Some Pyrone and Benzodifuran Derivatives

  • Hishmat, Orchidee H.;El-Diwani, Hoda I.;Bakr, Sherifa M.A.;Mahmoud, Sawsan S.;Nada, Somaya A.
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.168-174
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    • 1993
  • The michael adducts 2a, b were obtained from the reaction of the phenylacelyl derivative 1 with benzadehyde and p-anisaldehyde and p-anisaldehyde respectively. 2a and 2b were subjected to react with cyanoethanoic acid hydrazide, malononitrile, cyanothioacetamide, cyanoacetamide and 1, 1, 3-tricyano-2-amino propene to yield 4a-h and 5a, b respecitively. Hydrogen peroxide oxidation of 2a, b gave the aurone derivative 6a, b. The pyone derivatives 8a, b were obtained from 2a, b by addition of chioroacetyl chioride followed by dehydrochlorination.

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Climate Change Impacts on Paddy Irrigation Requirement in the Nakdong River Basin (기후변화가 낙동강 권역의 논 관개용수 수요량에 미치는 영향)

  • Chung, Sang-Ok
    • Journal of The Korean Society of Agricultural Engineers
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    • v.51 no.2
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    • pp.35-41
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    • 2009
  • The impacts of climate change on paddy irrigation requirements for Nakdong river basin in Korea have been analyzed. The HadCM3 model outputs for SRES A2 and B2 scenarios and International Water Management Institute $10'{\times}10'$ pixels observed data were used with kriging method. Maps showing the predicted spatial variations of changes in climate parameters and paddy irrigation requirements have been produced using the GIS. The results showed that the average growing season temperature was projected to increase by $2.2^{\circ}C$ (2050s A2), $0.0^{\circ}C$ (2050s B2), $3.7^{\circ}C$ (2080s A2) and $2.9^{\circ}C$ (2080s B2) from the baseline (1961-1990) value of $21{\circ}C$. The average growing season rainfall was projected to increase by 15.2% (2050s A2), 24.2% (2050s B2), 41.4% (2080s A2) and 16.7% (2080s B2) from the baseline value of 900 mm. Average volumetric irrigation demands were projected to decrease by 3.7% (2050s A2), 7.0% (2050s B2), 10.2% (2080s A2) and 1.4% (2080s B2) from the baseline value of $1.25{\times}10^9\;m^3$. These results can be used for the agricultural water resources development planning in the Nakdong river basin for the future.

Effect of SiO2/B2O3 ratio on Li ion conductivity of a Li2O-B2O3-SiO2 glass electrolyte

  • Kim, Young Han;Yoon, Mi Young;Lee, Eun Jung;Hwang, Hae Jin
    • Journal of Ceramic Processing Research
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    • v.13 no.spc1
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    • pp.37-41
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    • 2012
  • A lithium ion conducting borosilicate glass was fabricated by a conventional melt quenching technique from a mixture of Li2CO3, B2O3 and SiO2 powders. The Li ion conductivity of the lithium borosilicate glasses was evaluated in terms of the SiO2/B2O3 ratio. In the Li2O-B2O3-SiO2 ternary glass, the glass forming region decreases with an increasing Li2O content. At the same Li2O, the crystallization tendency of the glass samples increases with the SiO2/B2O3 ratio, resulting in a reduced glass forming region in the Li2O-B2O3-SiO2 ternary glass. The electrical conductivity moderately depends on the SiO2/B2O3 ratio in the Li2O-B2O3-SiO2 ternary glass. The conductivity of the glasses slightly increases with the SiO2/B2O3 ratio. The observed phenomenon can be explained by the modification of the glass structure as a function of the SiO2 content.

Solute Carrier SLC41A1 'A MINI REVIEW'

  • Basnet Hom Bahadur
    • Environmental Mutagens and Carcinogens
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    • v.25 no.2
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    • pp.60-65
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    • 2005
  • The human solute carrier, SLC41Al, is a $Mg^{2}+$ transporter that is regulated by extracellular magnesium. Although intracellular magnesium plays a fundamental role in cellular metabolism, little is known about how $Mg^{2}+$ is taken up and controlled by cells. Magnesium plays a fundamental role in cellular metabolism so that its control within the body is critical. Magnesium homeostasis is principally a balance between intestinal absorption of dietary magnesium and renal excretion of urinary magnesium. The kidney, mainly the distal convoluted tubule, controls magnesium reabsorption. Although renal reabsorption is under the influence of many hormones, selective regulation of magnesium transport is due to intrinsic control involving transcriptional processes and synthesis of transport proteins. Using microarray analysis, identification of the genetic elements involved with this transcriptional control has been begun. SLC41A1(GenBank Accession No. AJ514402), comprises 10 putative transmembrane domains, two of which are highly homologous to the integral membrane part of the prokaryote transports $Mg^{2}+$ and other divalent cations $Sr^2+,\;Zn^2+,\;Cu^2+,\;Fe^2+,\;Co^2+,\;Ba^2+,\;and\;Cd^2+,\;but\;not\;Ca^2+,\;Mn^2+,\;and\;Ni^2+.$ Transport of $Mg^{2}+$ by SLC41Al is rheogenic, voltage dependent, and not coupled to Na or Cl. Expressed SLC41Al transports a range of other divalent cations: $Mg^{2+},\;Sr^{2+},\;Zn^{2+},\;Cu^{2+},\;Fe^{2+},\;Co^{2+},\;Ba^{2+},\;and\;Cd^{2+}$. The divalent cations $Ca^{2+},\;Mn^{2+},\;and\;Ni^{2+}$and the trivalent ion $Gd^{3+}$ did not induce currents nor did they inhibit $Mg^{2+}$ transport. The nonselective cation $La^{3+}$ abolishes $Mg^{2+}$ uptake. Computer analysis of the SLC41Al protein structure reveals that it belongs to MgtE protein family & suggested that the human solute carrier, SLC41Al, might be a eukaryotic $Mg^{2+}$ transporter closely related $(60-70\%)$ protein encoded by SLC41A2 is a $Mg^{2}+$ transporter that might be involved in magnesium homeostasis in epithelial cells also transports a range of other divalent cations: $Ba^2,\;Ni^2,\;CO^2,\;Fe^2,\;or\;Mn^2,\;but\;not\;Ca^2,\;Zn^2,\;or\;Cu^{2+}$ that may have related functional properties.

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