Study on bioactive diterpenoids from medicinal plants of Thymelaeaceae and Euphorbiaceae families
| Project/Area Number |
17K08348
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Natural medicines
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| Research Institution | Toho University |
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Principal Investigator |
LI Wei 東邦大学, 薬学部, 准教授 (90328633)
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| Project Period (FY) |
2017-04-01 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| 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)
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| 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 |
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| 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.
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| 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。
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Report
(4 results)
Research Products
(20 results)
