Studies on molecular targets of new biological compounds having activity against the mutant yeast involving calcium signaling

2011 Fiscal Year Final Research Report

• Project/Area Number: 21580108
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Applied biochemistry
• Research Institution: Iwate University
• Principal Investigator: KIMURA Ken-ichi 岩手大学, 農学部, 教授 (30344625)
• Co-Investigator(Kenkyū-buntansha): SHIONO Yoshihito 山形大学, 農学部, 准教授 (80361278)
• Project Period (FY): 2009 – 2011
• Keywords: Saccharomyces cerevisiae (zds1Δerg3Δpdr1/3Δ) / Ca^<2+>-signaling / bemzophomopsin A / 9-(Methylsulfinyl) hexyl isothocyanate / falcarindiol / pisiferdiol / GSK-3β / calcineurin

Research Abstract

A new compound, bemzophomopsin restored the growth activity of the yeast mutant strain (zds1Δ erg3Δ pdr1/3Δ) at 1.25μg/disc and has no inhibition activity against calcineurin at 100 μM. 9-(Methylsulfinyl) hexyl isothocyanate inhibited GSK-3β with ATP competitive manner on Ki = 10.5μM and falcarindiol inhibited GSK-3β with ATP non-competitive manner on Ki = 86.9μM and the peptide substrate competitive manner on K_i=46.5μM. Pisiferdiol decreased the expression of calcineurin in the mutant yeast.

Research Products

• [Journal Article] Glycogen synthase kinase-3 β inhibition of 6-(methylsulfinyl) hexyl isothiocyanate derived from wasabi (Wasabia Japonica Matsum) (2011)
  • Author(s): Yoshida, J., Nomura, S. Nishizawa, N., Ito, Y. and Kimura, K.
  • Journal Title: Biosci. Biochem. Biotechnol Volume: 75 Pages: 136-139
• [Journal Article] A new benzoxepin metabolite isolated from endophytic fungus Phomopsis sp. (2009)
  • Author(s): Shiono, Y., Nitto, A., Shimanuki, K., Koseki, T., Murayama, T., Miyakawa, T., Yoshida, J. and Kimura, K.
  • Journal Title: J. Antibiot Volume: 62 Pages: 533-535
• [Journal Article] 植物内生糸状菌類から創薬シード分子を探す (2009)
  • Author(s): 塩野義人、木村賢一
  • Journal Title: 化学と生物 Volume: 47 Pages: 390-396
• [Presentation] サワラの球果由来PisiferdiolとCa^<2+>シグナル伝達に関わる遺伝子変異酵母株に対する生育円活性 (2011)
  • Author(s): 油井信弘、宮川都吉、大西素子、木村賢一
  • Organizer: 第55回香料・テルペンおよび精油化学に関する討論会
  • Place of Presentation: つくば
  • Year and Date: 20111119-21
• [Presentation] 山菜のウドとセリ科野菜に含まれるGSK-3β阻害物質falcarindiolの糖尿病に対する効果 (2010)
  • Author(s): 吉田潤、諏訪紗央里、伊藤芳明、宮川都吉、木村賢一
  • Organizer: 第15回日本フードファクター学会
  • Place of Presentation: 仙台
  • Year and Date: 20101004-05
• [Presentation] PP2C活性化物質PisiferdiolのCa^<2+>シグナル伝達に関わる遺伝子変異酵母に対する作用メカニズムの解析 (2010)
  • Author(s): 油井信弘、宮川都吉、大西素子、木村賢一
  • Organizer: 第5回日本ケミカルバイオロジー学会
  • Place of Presentation: 横浜
  • Year and Date: 20100518-19
• [Presentation] Chemical investigation on biological active compounds from endophytic fungi (2010)
  • Author(s): Shiono, Y. and Kimura, K.
  • Organizer: 2010年度日本農芸化学会シンポジウム
  • Place of Presentation: 東京
  • Year and Date: 20100327-30
• [Presentation] Ca^<2+>シグナル伝達に関わる遺伝子変異酵母の阻害剤に対する表現型と標的分子との関連性 (2009)
  • Author(s): 吉田潤、宮川都吉、木村賢一
  • Organizer: 日本ケミカルバイオロジー学会第4回年会
  • Place of Presentation: 神戸
  • Year and Date: 20090518-19
• [Presentation] 遺伝子変異酵母を用いた新たなバイオプローブの探索とその分子標的研究 (2009)
  • Author(s): 木村賢一
  • Organizer: いわて海洋バイオテクノロジ-研究会研究交流技術セミナー
  • Place of Presentation: 釜石
  • Year and Date: 2009-08-06
• [Book] 16 Endophytic microorganisms as a source of bioactive compounds, Bioactive Compounds from Natural sources (2nd Edition), Edited by Corrado Tringali, Edited by Corrado Tringali (2012)
  • Author(s): Shiono, Y. and Kimura, K.
  • Total Pages: 551-577
  • Publisher: Taylor & Francis
• [Remarks] 岩手大学(木村賢一)
  • URL: http://univdb.iwate-u.ac.jp/openmain.jsp
• [Remarks] 山形大学(塩野義人)
  • URL: http://www.tr.yamagata-u.ac.jp/kyouindata.html