• Title/Summary/Keyword: $3{\alpha}$

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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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Hyperosmotic Stimulus Down-regulates $1{\alpha}$, 25-dihydroxyvitamin $D_3$-induced Osteoclastogenesis by Suppressing the RANKL Expression in a Co-culture System

  • Tian, Yu-Shun;Jeong, Hyun-Joo;Lee, Sang-Do;Kong, Seok-Heui;Ohk, Seung-Ho;Yoo, Yun-Jung;Seo, Jeong-Taeg;Shin, Dong-Min;Sohn, Byung-Wha;Lee, Syng-Ill
    • The Korean Journal of Physiology and Pharmacology
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    • v.14 no.3
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    • pp.169-176
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    • 2010
  • The hyperosmotic stimulus is regarded as a mechanical factor for bone remodeling. However, whether the hyperosmotic stimulus affects $1{\alpha}$, 25-dihydroxyvitamin $D_3$ ($1{\alpha},25(OH)_2D_3$)-induced osteoclastogenesis is not clear. In the present study, the effect of the hyperosmotic stimulus on $1{\alpha},25(OH)_2D_3$-induced osteoclastogenesis was investigated in an osteoblast-preosteoclast co-culture system. Serial doses of sucrose were applied as a mechanical force. These hyperosmotic stimuli significantly evoked a reduced number of $1{\alpha},25(OH)_2D_3$-induced tartrate-resistant acid phosphatase-positive multinucleated cells and $1{\alpha},25(OH)_2D_3$-induced bone-resorbing pit area in a co-culture system. In osteoblastic cells, receptor activator of nuclear factor ${\kappa}B$ ligand (RANKL) and Runx2 expressions were down-regulated in response to $1{\alpha},25(OH)_2D_3$. Knockdown of Runx2 inhibited $1{\alpha},25(OH)_2D_3$-induced RANKL expression in osteoblastic cells. Finally, the hyperosmotic stimulus induced the overexpression of TonEBP in osteoblastic cells. These results suggest that hyperosmolarity leads to the down-regulation of $1{\alpha},25(OH)_2D_3$-induced osteoclastogenesis, suppressing Runx2 and RANKL expression due to the TonEBP overexpression in osteoblastic cells.

Enhanced Sialylation of Recombinant Erythropoietin in CHO Cells by Human Glycosyltransferase Expression

  • Jeong, Yeon-Tae;Choi, One;Lim, Hye-Rim;Son, Young-Dok;Kim, Hong-Jin;Kim, Jung-Hoe
    • Journal of Microbiology and Biotechnology
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    • v.18 no.12
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    • pp.1945-1952
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    • 2008
  • Sialylation, the attachment of sialic acid residues to a protein, can affect the biological activity and in vivo circulatory half-life of glycoproteins. Human ${\alpha}2$,3-sialyltransferase (${\alpha}2$,3-ST) and ${\beta}1$,4-galactosyltransferase (${\beta}1$,4-GT) are responsible for terminal sialylation and galactosylation, respectively. Enhanced sialylation of human erythropoietin (EPO) by the expression of ${\alpha}2$,3-ST and ${\beta}1$,4-GT was achieved using recombinant Chinese hamster ovary (CHO) cells (EC1). The sialic acid content and sialylation of N-glycans were evaluated by HPLC. When ${\alpha}2$,3-ST was expressed in CHO cells (EC1-ST2), the sialic acid content (moles of sialic acid/mole of EPO) increased from 6.7 to 7.5. In addition, the amount of trisialylated glycans increased from 17.3% to 26.1 %. When ${\alpha}2$,3-ST and ${\beta}1$,4-GT were coexpressed in CHO cells (EC1-GTST15), the degree of sialylation was greater than that in EC1-ST2 cells. In the case of EC1-GTST15 cells, the sialic acid content increased to 8.2 and the proportion of trisialylated glycans was markedly increased from 17.3% to 35.5%. Interestingly, the amount of asialoglycans decreased only in the case of GTST15 cells (21.4% to 14.2%). These results show that coexpression of ${\alpha}2$,3-ST and ${\beta}1$,4-GT is more effective than the expression of ${\alpha}2$,3-ST alone. Coexpression of ${\alpha}2$,3-ST and ${\beta}1$,4-GT did not affect CHO cell growth and metabolism or EPO production. Thus, coexpression of ${\alpha}2$,3-ST and ${\beta}1$,4-GT may be beneficial for producing therapeutic glycoproteins with enhanced sialylation in CHO cells.

SUMO Proteins are not Involved in TGF-${\beta}1$-induced, Smad3/4-mediated Germline ${\alpha}$ Transcription, but PIASy Suppresses it in CH12F3-2A B Cells

  • Lee, Sang-Hoon;Kim, Pyeung-Hyeun;Oh, Sang-Muk;Park, Jung-Hwan;Yoo, Yung-Choon;Lee, Junglim;Park, Seok-Rae
    • IMMUNE NETWORK
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    • v.14 no.6
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    • pp.321-327
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    • 2014
  • TGF-${\beta}$ induces IgA class switching by B cells. We previously reported that Smad3 and Smad4, pivotal TGF-${\beta}$ signal-transducing transcription factors, mediate germline (GL) ${\alpha}$ transcription induced by TGF-${\beta}1$, resulting in IgA switching by mouse B cells. Post-translational sumoylation of Smad3 and Smad4 regulates TGF-${\beta}$-induced transcriptional activation in certain cell types. In the present study, we investigated the effect of sumoylation on TGF-${\beta}1$-induced, Smad3/4-mediated $GL{\alpha}$ transcription and IgA switching by mouse B cell line, CH12F3-2A. Overexpression of small ubiquitin-like modifier (SUMO)-1, SUMO-2 or SUMO-3 did not affect TGF-${\beta}1$-induced, Smad3/4-mediated $GL{\alpha}$ promoter activity, expression of endogenous $GL{\alpha}$ transcripts, surface IgA expression, and IgA production. Next, we tested the effect of the E3 ligase PIASy on TGF-${\beta}1$-induced, Smad3/4-mediated $GL{\alpha}$ promoter activity. We found that PIASy overexpression suppresses the $GL{\alpha}$ promoter activity in cooperation with histone deacetylase 1. Taken together, these results suggest that SUMO itself does not affect regulation of $GL{\alpha}$ transcription and IgA switching induced by TGF-${\beta}1$/Smad3/4, while PIASy acts as a repressor.

Flavonol Glycosides of Maesa Lanceolata Leaves

  • Manguro, Lawrence O. Arot;Lemmen, Peter;Ugi, Ivar;Kraus, Wolfgang
    • Natural Product Sciences
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    • v.8 no.3
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    • pp.77-82
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    • 2002
  • An investigation of the methanolic extract of Maesa lanceolata leaves has led to the isolation of four novel flavonol glycosides characterised as myricetin 3-0-2', 3', 4'-triacetylxylopyranoside (1), quercetin $3-O-{\beta}-3'$, $6'-diacetylglucopyranosyl-(1{\longrightarrow}4)-{\alpha}-2'$, 3'-diacetylrhamnopyranoside (2), myricetin $3-O-xylopyranosyl-(1{\to}3)-{\alpha}-rhamnopyranoside$ (3) and quercetin $3-O-{\beta}-ga1actopyranosyl-(1{\to}4)-{\alpha}-rhamnopyranoside-7-O-{\beta}-galactopyranoside$ (4). Also isolated from the same extract were known flavonols; quercetin (5), myricetin (6), quercetin 3-O-xylopyranoside (7), quercetin $3-O-{\alpha}-rhamnopyranoside$ (8), myricetin $3-O-{\alpha}-rhamnopyranoside$ (9), myricetin $3-O-{\beta}-galactopyranoside$ (10) and quercetin 3-O-rutinoside (11).

Reaction of α-Fe2O3 Red Pigment and Transparent Dielectric Materials (적색안료인 α-Fe2O3와 투명 유전체의 반응)

  • Kim, Bong-Chul;Han, Yong-Soo;Song, Yoon-Ho;Suh, Kyung-Soo;Lee, Jin-Ho;Lee, Nam-Yang;Park, Lee-Soon;Lee, Byung-Kyo
    • Journal of the Korean Ceramic Society
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    • v.39 no.3
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    • pp.226-232
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    • 2002
  • We searched thermal stability of ${\alpha}-Fe_2O_3$ using red color filter for display. In the PDP(Plasma Display Panel), the color filter layer is lied normally between front glass and transparent dielectric materials, so it might be needed to study the reaction of ${\alpha}-Fe_2O_3$ and transparent dielectric materials. The transparent dielectric materials containing ZnO has good transparency. Red colorlayer of ${\alpha}-Fe_2O_3$ contacted with dielectric material layer containing ZnO is changed to colorlessness over 500$^{\circ}$C because ZnO defuse ${\alpha}-Fe_2O_3$, the dielectric materials without ZnO, however, maintain red color at the same condition. We suggest that a layer contacting with ${\alpha}-Fe_2O_3$ red color layer has to lie with transparent dielectric materials without ZnO, then the materials containing ZnO is coated over to get color of ${\alpha}-Fe_2O_3$ for red color filter

Studies on the Constituents of Caltha minor(I) - Saponin from the Leaves - (동이나물의 성분 (I) - 잎의 Saponin-)

  • 윤광로;한덕룡
    • YAKHAK HOEJI
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    • v.35 no.3
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    • pp.236-239
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    • 1991
  • Two triterpenoid saponins were isolated from the methanol extract of Caltha minor leave(Ranunculaceae). The structure of these saponin were elucidated as hederagenin-3-O-$\alpha$-rhamnopyranosyl(1$\rightarrow$2)-$\alpha$-L-arabinopyrano side and 3-O-$\alpha$-L-rhamnopyranosyl(1$\rightarrow$2)-$\alpha$-L-arabinopyranosyl hederagenin 28-O-$\alpha$-L-rhamnopyranosyl(1$\rightarrow$4)-$\beta$-D-glucopyranosyl(1$\rightarrow$6)-$\beta$-D-glucopyranosyl ester.

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The Synthesis and Evaluation of Antihypertensive 4-(${\beta}$-Guanidinoethyl)-17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol (혈압강하제인 4-${\beta}$-Guanidinoethyl)-17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol의 합성 및 평가)

  • Jack C. Kim;Lee Euk-suk;Charles C. Chang;Norman J. Doorenbos
    • Journal of the Korean Chemical Society
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    • v.19 no.3
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    • pp.174-178
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    • 1975
  • The intermediate, 17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(Ⅸ) required for the synthesis of 4-(${\beta}$-guanidinoethyl)-17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(V) was obtained through a reaction of 17${\alpha}$-methyl-3,5-seco-4-norandrostan-17${\beta}$-ol-5-on-3-oic acid(VI) with ammonium hydroxide followed by two reductions(platinum dioxide with hydrogen and lithium aluminium hydride). Condensation of Ⅸ with chloroacetonitrile under anhydrous condition, followed by reduction of the nitrile with lithium aluminium hydride gave 4-(${\beta}$-aminoethyl)-17${\alpha}$-methyl-4-aza-5${\alpha}$-androstan-17${\beta}$-ol(XI). The reaction of XI with 2-methyl-2-thiopseudourea or 3,5-dimethylpyrazole-1-carboxamidine, or cyanamide provided the title compound, V. Relaxation of the nictitating membrane, in the absence of mydriasis, is considered to be evidence of adrenergic neurone blockade. Thus the test compound(V) resembles that of the classical adrenergic neurone blocking agents.

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COMPACT TOEPLITZ OPERATORS

  • Kang, Si Ho
    • Honam Mathematical Journal
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    • v.35 no.3
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    • pp.343-350
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    • 2013
  • In this paper we prove that if Toeplitz operators $T^{\alpha}_u$ with symbols in RW satisfy ${\parallel}uk^{\alpha}_z{\parallel}_{s,{\alpha}{\rightarrow}0$ as $z{\rightarrow}{\partial}\mathbb{D}$ then $T^{\alpha}_u$ is compact and also prove that if $T^{\alpha}_u$ is compact then the Berezin transform of $T^{\alpha}_u$ equals to zero on ${\partial}\mathbb{D}$.