VITAMINS
Online ISSN : 2424-080X
Print ISSN : 0006-386X
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Volume 83, Issue 10
Displaying 1-11 of 11 articles from this issue
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  • Activation of hepatic stellate (vitamin A-storing) cells and retinoic acid receptor function
    Yoshihiro Mezaki, Mayako Morii, Kiwamu Yoshikawa, Noriko Yamaguchi, Mi ...
    Article type: Article
    2009 Volume 83 Issue 10 Pages 559-568
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_559
    JOURNAL FREE ACCESS
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    Hepatic stellate cells (HSCs) store vitamin A and play an important role in liver fibrosis. During fibrogenesis, HSCs are activated and lose vitamin A-containing lipid droplets. However, relevance of retinoid receptor function in liver fibrogenesis is unknown. Here we demonstrate that expression of retinoic acid receptor α (RARα) is up-regulated in activated rat HSCs at a post-transcriptional level. RARα proteins showed a speckled distribution in the cytosol, in spite of their possession of a nuclear localization signal (NLS). Exogenously expressed RARα protein fragments containing an NLS were localized in the nuclei of activated rat HSCs and never colocalized with the endogenous RARα proteins in the cytosol, suggesting that the NLS of endogenous RARα proteins is masked. Biochemical analysis showed that 65% of RARα proteins in activated HSCs were insoluble in a mixture of detergents. This insoluble, speckled cytosolic distribution of RARα proteins may represent a new marker of HSC activation.
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  • Structure-Activity Relationship Study on TEI-9647 and TEI-9648 : Aiming at the Strongest VDR Antagonist with Modification of the 2α and 24 Positions
    Atsushi Kittaka, Nozomi Saito, Kazuya Takenouchi, Seiichi Ishizuka
    Article type: Article
    2009 Volume 83 Issue 10 Pages 569-579
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_569
    JOURNAL FREE ACCESS
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    The unique structures and interesting biological profiles of the first vitamin D receptor (VDR) antagonists TEI-9647 and TEI-9648 prompted us to investigate the structure-activity relationships of these vitamin D_3 lactones and search for more potent anti-vitamin D molecules. Our general approach to develop vitamin D_3 lactones was, 1) to introduce the 2α-substitutions, that is, a methyl, 3-hydroxypropyl or 3-hydroxypropoxy group into TEI-9647 and TEI-9648 to improve their VDR binding affinity, 2) to also introduce a C24-substitution to stabilize the compound, 3) to determine the influence of the modified structures of the lactone moiety, on the stereochemistry, and on both VDR binding affinity and antagonistic activity, and 4) to investigate their biological effects after the C2α and C24-double modification of TEI-9647 and TEI-9648. In this review, we describe our striking results with C2α- and C24-functionalization of these VDR antagonists. The (23S,24S)-2α-(3-hydroxypropoxy)-24-propyl-TEI-9647 was found to have 851-fold improved antagonistic activity (IC_<50>=7.4pM) over the original TEI-9647 (IC_<50>=6.3nM).
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  • Hydrogen sulfide as a biofactor
    Ikuyo Ichi, Tatsuya Matsura, Shosuke Kojo
    Article type: Article
    2009 Volume 83 Issue 10 Pages 581-585
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_581
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  • Targeting of tumor using derivatives of vitamin B_12
    Shoji Yamada, Keiko Yamada
    Article type: Article
    2009 Volume 83 Issue 10 Pages 586-589
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_586
    JOURNAL FREE ACCESS
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  • [title in Japanese]
    [in Japanese], [in Japanese], [in Japanese], [in Japanese], [in Japane ...
    Article type: Article
    2009 Volume 83 Issue 10 Pages 590-591
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_590
    JOURNAL FREE ACCESS
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  • [title in Japanese]
    [in Japanese], [in Japanese], [in Japanese], [in Japanese]
    Article type: Article
    2009 Volume 83 Issue 10 Pages 591-
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_591_1
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  • [title in Japanese]
    [in Japanese], [in Japanese]
    Article type: Article
    2009 Volume 83 Issue 10 Pages 591-592
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_591_2
    JOURNAL FREE ACCESS
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  • [title in Japanese]
    [in Japanese], [in Japanese], [in Japanese], [in Japanese], [in Japane ...
    Article type: Article
    2009 Volume 83 Issue 10 Pages 592-593
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_592
    JOURNAL FREE ACCESS
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  • [title in Japanese]
    [in Japanese], [in Japanese], [in Japanese], [in Japanese], [in Japane ...
    Article type: Article
    2009 Volume 83 Issue 10 Pages 593-
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_593_1
    JOURNAL FREE ACCESS
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  • [title in Japanese]
    [in Japanese], [in Japanese], [in Japanese], [in Japanese]
    Article type: Article
    2009 Volume 83 Issue 10 Pages 593-594
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_593_2
    JOURNAL FREE ACCESS
    Download PDF (361K)
  • [title in Japanese]
    Article type: Bibliography
    2009 Volume 83 Issue 10 Pages 596-600
    Published: October 25, 2009
    Released on J-STAGE: October 10, 2017
    DOIhttps://doi.org/10.20632/vso.83.10_596
    JOURNAL FREE ACCESS
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