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Study of novel anti-leishmanial drug

Research Project

Project/Area Number 23659212
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Parasitology (including Sanitary zoology)
Research InstitutionOkayama University

Principal Investigator

WATAYA Yusuke  岡山大学, 大学院・医歯薬学総合研究科, 名誉教授 (90127598)

Co-Investigator(Kenkyū-buntansha) KIM Hye-sook  岡山大学, 大学院・医歯薬学総合研究科, 准教授 (70314664)
SATO Akira  岡山大学, 大学院・医歯薬学総合研究科, 助教 (40530663)
Project Period (FY) 2011 – 2012
Project Status Completed (Fiscal Year 2012)
Budget Amount *help
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2012: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2011: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Keywordsリーシュマニア原虫 / アンチモン製剤 / 抗リーシュマニア活性評価 / Geldanamycin / Hsp90 / Leishmania major / Leishmania donovani / 天然生薬資源 / 感染症 / リーシュマニア / 創薬 / 難治性疾患 / 核酸誘導体
Research Abstract

I performed to new drug discovery research for 68 compounds from organic compounds and natural product using promastigotes of Leishmania major. The EC50values among 2 of them for L. majorwere 42 nM and 27 nM. In contrast, Amphotericin B as a positive control was show 63 nM of EC50value for L. majorand selective toxicity of 46-fold compare tomammalian cells of it. The structure-activity relationship study will be need more. I established the mechanism analysis of HSP90 and complex relationship in L. major and also we found the high anti-leishmanial effect for HSP90 inhibitor and it’s analogs include small molecules (EC50values; 30-40 nM) against L. major promastigotes.

Report

(3 results)
  • 2012 Annual Research Report   Final Research Report ( PDF )
  • 2011 Research-status Report
  • Research Products

    (21 results)

All 2013 2012 2011 Other

All Journal Article (10 results) (of which Peer Reviewed: 10 results) Presentation (9 results) Book (1 results) Remarks (1 results)

  • [Journal Article] Plasmodium falciparumendoplasmic reticulum-resident calcium binding protein is a possible target of synthetic antimalarial endoperoxides, N-89 and N-2512012

    • Author(s)
      Morita, M., Sanai, H., Hiramoto, A., Sato, A., Hiraoka, O., Sakura, T., Kaneko, O., Masuyama, A., Nojima, M., Wataya, Y. and Kim, H.-S.
    • Journal Title

      J Proteome Res.

      Volume: 11 Pages: 5704-11

    • URL

      http://pubs.acs.org/doi/pdf/10.1021/pr3005315

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Andirolides HeP from the flower of andiroba (Carapa guianensis, Meliaceae)2012

    • Author(s)
      Tanaka Y, Sakamoto A, Inoue T, Yamada T, Kikuchi T, Kajimoto T, Muraoka O, Sato A, Wataya Y, Kim H.-S, and Tanaka R.
    • Journal Title

      Tetrahedron

      Volume: 68 Pages: 3669-77

    • URL

      http://www.sciencedirect.com/science/article/pii/S0040402011019727

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Plasmodium falciparum endoplasmic reticulum-resident calcium binding protein is a possible target of synthetic antimalarial endoperoxides, N-89 and N-2512012

    • Author(s)
      Morita M., Sanai H., Hiramoto A., Sato A., Hiraoka O., Sakura T., Kaneko O., Masuyama A., Nojima M., Wataya Y., Kim H.-S.
    • Journal Title

      Journal of Proteome Research

      Volume: 11 Issue: 12 Pages: 5704-5711

    • DOI

      10.1021/pr3005315

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Andirolides H-P from the flower of andiroba (Carapa guianensis, Meliaceae)2012

    • Author(s)
      Tanaka Y., Sakamoto A., Inoue T., Yamada T., Kikuchi T., Kajimoto T., Muraoka O., Sato A., Wataya Y., Kim H.-S., Tanaka R.
    • Journal Title

      Tetrahedron

      Volume: 68 Issue: 18 Pages: 3669-3677

    • DOI

      10.1016/j.tet.2011.12.076

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Antimalarial Activity of Endoperoxide Compound 6-(1,2,6,7- Tetraoxaspiro[7.11] nonadec-4-yl)hexan-1-ol.2011

    • Author(s)
      Sato A., Hiramoto A., Morita M., Matsumoto M., Komich Y., Nakase Y., Tanigawa N., Hiraoka O., Hiramoto K., Hayatsu H., Higaki K., Kawai S., Masuyama A., Nojima M., Wataya Y., Kim H.-S.
    • Journal Title

      Parasitology International

      Volume: 60 Pages: 270-3

    • URL

      http://dx.doi.org/10.1016/j.parint.2011.04.001

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Schistosomicidal and antifecundity effects of oral treatment of synthetic endo-peroxide N-892011

    • Author(s)
      Taniguchi T., Kumagai T., Shimogawara R., Ichinose S., Hiramoto A., Sato A., Morita M., Nojima M., Kim H.-S., Wataya Y., Ohta N.
    • Journal Title

      Parasitology International

      Volume: 60 Pages: 231-6

    • URL

      http://dx.doi.org/10.1016/j.parint.2011.02.007

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Antimalarial activity of 6-(1,2,6,7-tetraoxaspiro [7.11]nonadec-4-yl)hexan- 1-ol (N-251) and its carboxylic acid derivatives.2011

    • Author(s)
      Sato A, Kawai S, Hiramoto A, Morita M, Tanigawa N, Nakase Y, Komichi Y, Matsumoto M, Hiraoka O, Hiramoto K, Tokuhara H, Masuyama A, Nojima M, Higaki K, Hayatsu H, Wataya Y, Kim HS.
    • Journal Title

      Parasitol. Int.

      Volume: 60(4) Pages: 488-92

    • URL

      http://www.sciencedirect.com/science/article/pii/S138357691100136X

    • Related Report
      2012 Final Research Report
    • Peer Reviewed
  • [Journal Article] Antimalarial Activity of 6-(1,2,6,7-Tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251) and Its Carboxylic Acid Derivatives.2011

    • Author(s)
      Sato A., Kawai S., Hiramoto A., Morita M., Tanigawa N., Nakase Y., Komichi Y., Matsumoto M., Hiraoka O., Hiramoto K., Tokuhara H., Masuyama A., Nojima M., Higaki K., Hayatsu H., et al.
    • Journal Title

      Parasitology International

      Volume: 60 Pages: 488-492

    • Related Report
      2011 Research-status Report
    • Peer Reviewed
  • [Journal Article] Antimalarial Activity of Endoperoxide Compound 6-(1,2,6,7-Tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol.2011

    • Author(s)
      Sato A., Hiramoto A., Morita M., Matsumoto M., Komichi Y., Nakase Y., Tanigawa N., Hiraoka O., Hiramoto K., Hayatsu H., Higaki K., Kawai S., Masuyama A., Nojima M., Wataya Y., Kim H.-S.
    • Journal Title

      Parasitology International

      Volume: 60 Pages: 270-273

    • Related Report
      2011 Research-status Report
    • Peer Reviewed
  • [Journal Article] Schistosomicidal and antifecundity effects of oral treatment of synthetic endoperoxide N-89.2011

    • Author(s)
      Taniguchi T., Kumagai T., Shimogawara R., Ichinose S., Hiramoto A., Sato A., Morita M., Nojima M., Kim H.-S., Wataya Y., Ohta N.
    • Journal Title

      Parasitology International

      Volume: 60 Pages: 231-236

    • Related Report
      2011 Research-status Report
    • Peer Reviewed
  • [Presentation] 難治性感染症治療薬の開発研究2013

    • Author(s)
      金 惠淑、佐藤 聡、森田将之、綿矢有佑、熊谷貴、下河原理江子、太田伸生
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      横浜、神奈川
    • Related Report
      2012 Annual Research Report 2012 Final Research Report
  • [Presentation] In vivoにおける抗マラリア活性評価システムの開発2013

    • Author(s)
      大里泰規、片本 茜、中村由香、佐藤 聡、金 惠淑
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      横浜、神奈川
    • Related Report
      2012 Annual Research Report 2012 Final Research Report
  • [Presentation] 経皮吸収型抗マラリア薬の開発研究2013

    • Author(s)
      中村由香、片本 茜、佐藤 聡、檜垣和孝、綿矢有佑、金 惠淑
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      横浜、神奈川
    • Related Report
      2012 Annual Research Report
  • [Presentation] The antimalarial activity of cyclic peroxides. Forum Cheju 15;2012

    • Author(s)
      Wen Jiang, Akira Sato, Masaki Kamata, Hye-Sook Kim.
    • Organizer
      The 15th Japan-Korea Parasitologists, Seminar
    • Place of Presentation
      Miyazaki, Japan
    • Related Report
      2012 Final Research Report
  • [Presentation] 新規抗マラリア薬・環状過酸化化合物の開発研究2012

    • Author(s)
      森田 将之、平本 晃子、佐藤 聡、岡田 和朗、鎌井 一気、脇本 達也、林 孝輔、片本 茜、渡部 裕紀、高橋 拓真、今田 智加子、平岡 修、野島 正朋、檜垣 和孝、綿矢 有佑,金 惠淑
    • Organizer
      日本薬学会第132 年会
    • Place of Presentation
      札幌
    • Related Report
      2012 Final Research Report
  • [Presentation] 環状過酸化化合物N-251の生物学的利用能向上を目的とする開発研究2012

    • Author(s)
      片本 茜、脇本達也、渡部裕紀、森田将之、林 孝輔、佐藤 聡、綿矢有佑、高橋拓真、今田智加子、檜垣和孝、金 惠淑
    • Organizer
      第72回日本寄生虫学会東日本支部会, 第10回分子寄生虫・マラリアフォーラム
    • Place of Presentation
      前橋、群馬
    • Related Report
      2012 Annual Research Report
  • [Presentation] Drug development research for antimalarial endoperoxide N-2512012

    • Author(s)
      Masayuki Morita, Akiko Hiramoto, Kazuaki Okada, Tatsuya Wakimoto, Akane Katamoto, Hiroki Watanabe, Takuma Takahashi, Chikako Imada, Akira Sato, Kazutaka Higaki, Yusuke Wataya, Hye-Sook Kim
    • Organizer
      Forum Cheju 15; The 15th Japan-Korea Parasitologists’ Seminar
    • Place of Presentation
      Miyazaki, Japan
    • Related Report
      2012 Annual Research Report
  • [Presentation] The antimalarial activity of cyclic peroxides2012

    • Author(s)
      Wen Jiang, Akira Sato, Masaki Kamata, Hye-Sook Kim
    • Organizer
      Forum Cheju 15; The 15th Japan-Korea Parasitologists’ Seminar
    • Place of Presentation
      Miyazaki, Japan
    • Related Report
      2012 Annual Research Report
  • [Presentation] 合成環状過酸化化合物N-89投与によるマンソン住血吸虫体内のヘモゾイン蓄積量に与える影響2011

    • Author(s)
      谷口斎恵、熊谷 貴、下河原理江子、平本晃子、佐藤 聡、金 惠淑、綿矢有佑、太田伸生
    • Organizer
      第80回日本寄生虫学会大会
    • Place of Presentation
      東京
    • Year and Date
      2011-07-18
    • Related Report
      2012 Final Research Report
  • [Book] 最新医学「感染症医薬品開発の現状」薬剤耐性マラリアに対する新規治療薬開発の現状2012

    • Author(s)
      金 惠淑、佐藤 聡、森田将之、綿矢有佑
    • Publisher
      最新医学社
    • Related Report
      2012 Annual Research Report
  • [Remarks]

    • URL

      http://www.pharm.okayama-u.ac.jp/lab/joho/index.html

    • Related Report
      2011 Research-status Report

URL: 

Published: 2011-08-05   Modified: 2019-07-29  

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