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Development of new antimalarial trandermal agent

Research Project

Project/Area Number 18K07086
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Review Section Basic Section 49040:Parasitology-related
Research InstitutionOkayama University

Principal Investigator

Kim Hye-Sook  岡山大学, 医歯薬学総合研究科, 准教授 (70314664)

Project Period (FY) 2018-04-01 – 2021-03-31
Project Status Completed (Fiscal Year 2020)
Budget Amount *help
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2020: ¥390,000 (Direct Cost: ¥300,000、Indirect Cost: ¥90,000)
Fiscal Year 2019: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2018: ¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
Keywordsマラリア / 過酸化物 / 外用剤 / 経皮吸収 / 新薬候補 / 非経口剤 / 軟膏製剤 / 製剤 / 抗マラリア / 非経口製剤 / マラリア治療 / マラリア予防
Outline of Final Research Achievements

I found the usefulness for slow-released transdermal agent of new antimalarial endoperoxides (N-89 and N-251) found as our new antimalarial drug research. As a suitable base of ointment of end-peroxide's, polyethylene glycol (PEG) 400 and PEG4000 in a ratio of 8: 1 was selected and pharmacokinetic analysis and antimalarial efficacy evaluation was performed using a ointment preparation containing N-89 under same conditions. As a result, an excellent antimalarial effect and a complete cure effect were obtained by applying an ointment preparation containing 60 mg / kg of N-89 twice a day for 3 days at 4 Cm2 of transdermal area. All mice completely cured until infection rate of 1.5% in malaria group, but in mice with an infection rate of more than 1.5% will be propose to be used in combination with an clinically used antimalarial drugs which long half-life.

Academic Significance and Societal Importance of the Research Achievements

マラリアによる死亡の9割は5歳未満の乳幼児である現状から、経口投与による治療は難しく、注射器等を用いる治療は現地の状況を鑑みて、推奨出来ない。我々は経口投与で優れた抗マラリア薬効と完治効果を示す新規抗マラリア薬候補として見出した有機合成化合物・ N-89, N-251が非侵襲性で乳幼児へのマラリア治療に適用可能であることを見出した。即ち、N-89とN-251の薬効を長期間持続しながら副作用が発現した時に対処しやすい剤形である経皮吸収型製剤が in vivo 実験でマラリアを完治することを明らかにした。この結果は単剤で安価でかつ簡便に重症マラリアで死亡するアフリカの乳幼児の救命に貢献できる。

Report

(4 results)
  • 2020 Annual Research Report   Final Research Report ( PDF )
  • 2019 Research-status Report
  • 2018 Research-status Report
  • Research Products

    (21 results)

All 2020 2019 2018 Other

All Int'l Joint Research (5 results) Journal Article (7 results) (of which Int'l Joint Research: 2 results,  Peer Reviewed: 7 results,  Open Access: 7 results) Presentation (9 results) (of which Int'l Joint Research: 1 results,  Invited: 2 results)

  • [Int'l Joint Research] Catholic University of Pusan/Pusan National University(韓国)

    • Related Report
      2020 Annual Research Report
  • [Int'l Joint Research] 釜山カトリック大学(韓国)

    • Related Report
      2019 Research-status Report
  • [Int'l Joint Research] ハイフォン医科薬科大学(ベトナム)

    • Related Report
      2019 Research-status Report
  • [Int'l Joint Research] Catholic University of Pusan(韓国)

    • Related Report
      2018 Research-status Report
  • [Int'l Joint Research] Haiphong Univ. Medicine and Pharmacy(ベトナム)

    • Related Report
      2018 Research-status Report
  • [Journal Article] Direct interaction analysis of microRNA-351-5p and nuclear scaffold lamin B1 mRNA by the cell-free in vitro mRNA/miRNA binding evaluation system.2020

    • Author(s)
      Akira Sato, Yoko Ogino, Akira Shimotsuma, Akiko Hiramoto, Hye-Sook Kim, Yusuke Wataya.
    • Journal Title

      Nucleosides, Nucleotides and Nucleic Acids

      Volume: 39 Issue: 6 Pages: 799-805

    • DOI

      10.1080/15257770.2019.1702675

    • Related Report
      2019 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Pharmacokinetic analysis of new synthetic antimalarial N-2512019

    • Author(s)
      Okada Kazuaki、Sato Akira、Hiramoto Akiko、Isogawa Rena、Kurosaki Yuji、Higaki Kazutaka、Miyoshi Shin-Ichi、Chang Kyung-Soo、Kim Hye-Sook
    • Journal Title

      Tropical Medicine and Health

      Volume: 47 Issue: 1 Pages: 1-8

    • DOI

      10.1186/s41182-019-0167-4

    • Related Report
      2019 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Genomic and biological features of Plasmodium falciparum resistance against antimalarial endoperoxide N-892019

    • Author(s)
      Morita Masayuki、Hayashi Kosuke、Sato Akira、Hiramoto Akiko、Kaneko Osamu、Isogawa Rena、Kurosaki Yuji、Miyoshi Shin-ichi、Chang Kyung-Soo、Wataya Yusuke、Kim Hye-Sook
    • Journal Title

      Gene

      Volume: 716 Pages: 144016-144016

    • DOI

      10.1016/j.gene.2019.144016

    • Related Report
      2019 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Oral activity of the antimalarial endoperoxide 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251) against Leishmania donovani complex2019

    • Author(s)
      Kwofie Kofi Dadzie、Sato Kai、Sanjoba Chizu、Hino Akina、Shimogawara Rieko、Amoa-Bosompem Michael、Ayi Irene、Boakye Daniel A.、Anang Abraham K.、Chang Kyung-Soo、Ohashi Mitsuko、Kim Hye-Sook、Ohta Nobuo、Matsumoto Yoshitsugu、Iwanaga Shiroh
    • Journal Title

      PLOS Neglected Tropical Diseases

      Volume: 13 Issue: 3 Pages: 7235-7235

    • DOI

      10.1371/journal.pntd.0007235

    • Related Report
      2018 Research-status Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme2018

    • Author(s)
      Yosuke Sakata, Kosuke Yabunaka, Yuko Kobayashi, Hirohisa Omiya, Naoki Umezawa, Hye- Sook Kim, Yusuke Wataya, Yoshimi Tomita, Yosuke Hisamatsu, Nobuki Kato, Hirokazu Yagi, Tadashi Satoh, Koichi Kato, Haruto Ishikawa and Tsunehiko Higuchi
    • Journal Title

      ACS Medicinal Chemistry Letters

      Volume: 9 Issue: 10 Pages: 980-985

    • DOI

      10.1021/acsmedchemlett.8b00222

    • Related Report
      2018 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Insights into the mode of action of 1,2,6,7-tetraoxaspiro [7.11] nonadecane (N-89) against adult Schistosoma mansoni worms2018

    • Author(s)
      Blay Emmanuel Awusah、Kumagai Takashi、Yamabe Masafumi、Hino Akina、Shimogawara Rieko、Kim Hye-Sook、Sato Akira、Ichimura Koichiro、Ayi Irene、Iwanaga Shiroh、Ohta Nobuo
    • Journal Title

      Parasitology International

      Volume: 67 Issue: 4 Pages: 403-412

    • DOI

      10.1016/j.parint.2018.03.006

    • Related Report
      2018 Research-status Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Multiple antiviral activities of the antimalarial and anti-hepatitis C drug candidates N-89 and N-2512018

    • Author(s)
      Ueda Youki、Gu Weilin、Dansako Hiromichi、Kim Hye-Sook、Yoshizaki Sayaka、Okumura Nobuaki、Ishikawa Tomohiro、Nishitsuji Hironori、Kato Fumihiro、Hishiki Takayuki、Satoh Shinya、Ishii Koji、Masuda Michiaki、Shimotohno Kunitada、Ikeda Masanori、Kato Nobuyuki
    • Journal Title

      Biochemistry and Biophysics Reports

      Volume: 15 Pages: 1-6

    • DOI

      10.1016/j.bbrep.2018.05.007

    • Related Report
      2018 Research-status Report
    • Peer Reviewed / Open Access
  • [Presentation] 新しいマラリア治療薬の開発―過酸化物をベースにした軟膏製剤の基礎研究―2020

    • Author(s)
      井黒 香奈子、五十川 怜奈、池田 奈々子、黒崎 勇二、Kyung-Soo Chang、金 惠淑
    • Organizer
      グローバルヘルス合同大会2020
    • Related Report
      2020 Annual Research Report
  • [Presentation] 新しいマラリア治療薬の開発-軟膏製剤としての実用化に向けた基礎研究-2020

    • Author(s)
      井黒 香奈子、五十川 怜奈、池田 奈々子、黒崎 勇二、Chang Kyung-Soo、金 惠淑
    • Organizer
      日本薬学会第141年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] Comparative proteome analysis of Plasmodium falciparum resistance against antimalarial endoperoxide N-892019

    • Author(s)
      Hye-Sook Kim, Akira Sato, Rena Isogawa, Yuji Kurosaki, Kyung-Soo Chang
    • Organizer
      大韓寄生虫・熱帯医学会第60周年記念秋の学術大会および総会
    • Related Report
      2019 Research-status Report
  • [Presentation] Pharmacokinetic study of synthetic antimalarial N-2512019

    • Author(s)
      Rena Isogawa, Kyung-Soo Chang, Akira Sato, Hye-Sook Kim
    • Organizer
      大韓寄生虫・熱帯医学会第60周年記念秋の学術大会および総会
    • Related Report
      2019 Research-status Report
  • [Presentation] 経皮吸収型抗マラリア製剤の開発研究2019

    • Author(s)
      石井涼香、越智彩乃、三次真悠子、五十川怜奈 、 佐藤 聡 、黒崎勇二、Kyung-Soo Chang、○金 惠淑
    • Organizer
      第88回日本寄生虫学会大会
    • Related Report
      2018 Research-status Report
  • [Presentation] マラリアの創薬研究ー過酸化物を用いた抗マラリア薬開発の現況ー2018

    • Author(s)
      金 惠淑
    • Organizer
      第59回日本熱帯医学会大会
    • Related Report
      2018 Research-status Report
    • Invited
  • [Presentation] 過酸化物を用いた非経口マラリア治療剤の開発研究2018

    • Author(s)
      ○石井 涼香、越智 彩乃、三次 真悠子、五十川 怜奈、王野 さくら、佐藤 聡、黒崎 勇二、Kyung-Soo Chang、金 惠淑
    • Organizer
      第74 回 日本寄生虫学会 西日本支部大会
    • Related Report
      2018 Research-status Report
  • [Presentation] Development of transdermal type-antimalarial endoperoxide research2018

    • Author(s)
      ○Hye-Sook Kim, Ayano Ochi, Ryoka Ishii, Mayuko Miyoshi, Yuji Kurosaki, Kyung-Soo Chang
    • Organizer
      The 60th Annual Meeting of the Korean Society for Parasitology and Tropical Medicine
    • Related Report
      2018 Research-status Report
  • [Presentation] Current situation of synthetic endoperoxides: Schistosomiasis, protozoan diseases, malaria and others2018

    • Author(s)
      HYe-Sook Kim
    • Organizer
      14th International Congress of Parasitology
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research / Invited

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Published: 2018-04-23   Modified: 2024-01-30  

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