• Search Research Projects
  • Search Researchers
  • How to Use
  1. Back to previous page

Study on bioactive diterpenoids from medicinal plants of Thymelaeaceae and Euphorbiaceae families

Research Project

Project/Area Number 17K08348
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Natural medicines
Research InstitutionToho University

Principal Investigator

LI Wei  東邦大学, 薬学部, 准教授 (90328633)

Project Period (FY) 2017-04-01 – 2020-03-31
Project Status Completed (Fiscal Year 2019)
Budget Amount *help
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2017: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywordsジンチョウゲ科 / トウダイグサ科 / ジテルペノイド / 抗HIV / HIV / ダフナン / チグリアン / ジンチョウゲ / ミツマタ / 甘遂 / 瑞香狼毒 / 抗HIV活性 / 薬学 / 天然物化学 / 創薬シーズ探索
Outline of Final Research Achievements

The diterpenoids distributed in the plants of Thymelaeaceae and Euphorbiaceae families are rich in the chemical and biological diversity. In the present study, we collected plants belonging to Thymelaeaceae and Euphorbiaceae families from Japan and China, and constructed a plant extract library. Further chemical investigations were carried out. As a result, a number of novel diterpenoids with potent anti-HIV activities were isolated. Their structures were established by extensive physicochemical and spectroscopic analyses. Furthermore, semisynthesis of the derivatives of the natural diterpenoids disclosed the structure-activity relationship and provided optimized lead compounds towards novel anti-HIV drug discovery.

Academic Significance and Societal Importance of the Research Achievements

抗HIV薬による多剤併用療法はHIV増殖を抑制するが根絶することはできず、新規抗HIV薬創製は社会から求められている。本研究は、多様性に富む化学構造と生物活性を有する、ジンチョウゲ科およびトウダイグサ科由来のジテルペノイドを着目して、新規生物活性成分の探索、構造活性相関の解析と構造最適化により、新しい天然由来創薬シーズの発見を通じた革新的な難治疾患治療薬創製に貢献できたと考える。

Report

(4 results)
  • 2019 Annual Research Report   Final Research Report ( PDF )
  • 2018 Research-status Report
  • 2017 Research-status Report
  • Research Products

    (20 results)

All 2020 2019 2018 Other

All Int'l Joint Research (4 results) Journal Article (3 results) (of which Int'l Joint Research: 3 results,  Peer Reviewed: 3 results) Presentation (13 results) (of which Int'l Joint Research: 4 results,  Invited: 3 results)

  • [Int'l Joint Research] Duke University/University of North Carolina(米国)

    • Related Report
      2019 Annual Research Report
  • [Int'l Joint Research] 瀋陽薬科大学(中国)

    • Related Report
      2019 Annual Research Report
  • [Int'l Joint Research] Duke University/University of North Carolina(米国)

    • Related Report
      2018 Research-status Report
  • [Int'l Joint Research] Duke University/University of North Carolina(米国)

    • Related Report
      2017 Research-status Report
  • [Journal Article] Synthesis and Structure?Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents2019

    • Author(s)
      Liu Qingbo、Cheng Yung-Yi、Li Wei、Huang Li、Asada Yoshihisa、Hsieh Min-Tsang、Morris-Natschke Susan L.、Chen Chin-Ho、Koike Kazuo、Lee Kuo-Hsiung
    • Journal Title

      Journal of Medicinal Chemistry

      Volume: 62 Issue: 15 Pages: 6958-6971

    • DOI

      10.1021/acs.jmedchem.9b00339

    • Related Report
      2019 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Daphneodorins A-C, Anti-HIV Gnidimacrin Related Macrocyclic Daphnane Orthoesters from Daphne odora2019

    • Author(s)
      Otsuki Kouharu、Li Wei、Asada Yoshihisa、Chen Chin-Ho、Lee Kuo-Hsiung、Koike Kazuo
    • Journal Title

      Organic Letters

      Volume: 22 Issue: 1 Pages: 11-15

    • DOI

      10.1021/acs.orglett.9b03539

    • Related Report
      2019 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Identification, structural modification, and dichotomous effects on human immunodeficiency virus type 1 (HIV-1) replication of ingenane esters from Euphorbia kansui2018

    • Author(s)
      Liu Qingbo、Li Wei、Huang Li、Asada Yoshihisa、Morris-Natschke Susan L.、Chen Chin-Ho、Lee Kuo-Hsiung、Koike Kazuo
    • Journal Title

      European Journal of Medicinal Chemistry

      Volume: 156 Pages: 618-627

    • DOI

      10.1016/j.ejmech.2018.07.020

    • Related Report
      2018 Research-status Report
    • Peer Reviewed / Int'l Joint Research
  • [Presentation] Gnidimacrin and its derivatives against HIV-1 latency2020

    • Author(s)
      Wei Li
    • Organizer
      22nd International Conference on Emerging Infectious Diseases in the Pacific Rim
    • Related Report
      2019 Annual Research Report
    • Int'l Joint Research / Invited
  • [Presentation] ジンチョウゲ科植物Wikstroemia scytophyllaの化学成分研究2020

    • Author(s)
      山本 明日香、大月 興春、李 寧、李 巍、小池 一男
    • Organizer
      日本薬学会第140年会
    • Related Report
      2019 Annual Research Report
  • [Presentation] Discovery of anti-HIV diterpenoids from medicinal plants of Thymelaeaceae and Euphorbiaceae families2019

    • Author(s)
      Wei Li
    • Organizer
      11th Joint Seminar on Biomedical Sciences
    • Related Report
      2019 Annual Research Report
    • Int'l Joint Research / Invited
  • [Presentation] Tigliane diterpenoids from Wikstroemia scytophylla2019

    • Author(s)
      Mi Zhang、Asuka Yamamoto、Kouharu Otsuki、Wei Li、Kazuo Koike
    • Organizer
      11th Joint Seminar on Biomedical Sciences
    • Related Report
      2019 Annual Research Report
    • Int'l Joint Research
  • [Presentation] 沈丁花由来の抗HIV活性を有する大環状daphnane型ジテルペノイドに関する研究2019

    • Author(s)
      大月 興春、李 巍、浅田 善久、Chen Chin-Ho、Lee Kuo-Hsiung、小池 一男
    • Organizer
      第56回植物化学シンポジウム
    • Related Report
      2019 Annual Research Report
  • [Presentation] ジンチョウゲ科薬用植物ジンチョウゲのダフナン型ジテルペンに関する成分研究2019

    • Author(s)
      大月 興春、三浦 香純、李 巍、浅田 善久、小池 一男
    • Organizer
      日本薬学会第139年会(千葉)
    • Related Report
      2018 Research-status Report
  • [Presentation] ジンチョウゲ科薬用植物ミツマタのダフナン型ジテルペンに関する成分研究2019

    • Author(s)
      師岡 美喜、大月 興春、李 巍、浅田 善久、小池 一男
    • Organizer
      日本薬学会第139年会(千葉)
    • Related Report
      2018 Research-status Report
  • [Presentation] ジンチョウゲ科薬用植物ジンチョウゲの成分研究2018

    • Author(s)
      大月 興春、三浦 香純、李 巍、竹元 裕明、 浅田 善久、小池 一男
    • Organizer
      日本生薬学会第65回年会(広島)
    • Related Report
      2018 Research-status Report
  • [Presentation] トウダイグサ科およびジンチョウゲ科薬用植物由来の潜伏HIVを活性化する抗HIV活性天然物の探索研究2018

    • Author(s)
      李 巍、劉 慶博、浅田善久、Chen Chin-Ho、Lee Kuo-Hsiung、小池 一男
    • Organizer
      第20回応用薬理シンポジウム
    • Related Report
      2018 Research-status Report
  • [Presentation] ジンチョウゲ科およびトウダイクサ科薬用植物 から抗HIVジテルペノイドの探索研究2018

    • Author(s)
      李 巍、劉 慶博、浅田 善久、小池 一男
    • Organizer
      第22回天然薬物の応用と開発シンポジウム
    • Related Report
      2018 Research-status Report
  • [Presentation] Discovery of anti-HIV diterpenoids from medicinal plants of Thymelaeaceae and Euphorbiaceae2018

    • Author(s)
      Wei Li
    • Organizer
      The Fifth World Education Congress of Chinese Medicine
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research / Invited
  • [Presentation] 抗HIV天然物gnidimacrinの化学誘導体合成と構造活性相関2018

    • Author(s)
      劉 慶博、李 巍、Chen Chin-Ho、Lee Kuo-Hsiung、小池 一男
    • Organizer
      日本薬学会第138年会(金沢)
    • Related Report
      2017 Research-status Report
  • [Presentation] 生薬甘遂由来の抗HIV活性成分の探索研究2018

    • Author(s)
      李 巍、劉 慶博、Chen Chin-Ho、Lee Kuo-Hsiung、小池 一男
    • Organizer
      日本薬学会第138年会(金沢)
    • Related Report
      2017 Research-status Report

URL: 

Published: 2017-04-28   Modified: 2022-02-21  

Information User Guide FAQ News Terms of Use Attribution of KAKENHI

Powered by NII kakenhi