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

2019 Fiscal Year Final Research Report

• Project/Area Number: 17K08348
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Natural medicines
• Research Institution: Toho 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
• Keywords: ジンチョウゲ科 / トウダイグサ科 / ジテルペノイド / 抗HIV

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.

Free Research Field

天然物化学

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。