Phytochemical investigation of Daphnane-type diterpenoids aiming to discover next generation anti-HIV drugs
| Project/Area Number |
26460133
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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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| Research Collaborator |
LEE Kuo-Hsiung
CHEN Chin-Ho
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| Project Period (FY) |
2014-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2016: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | HIV感染症 / Gnidimacrin / ダフナン / 抗HIV薬 / gnidimacrin / 抗HIV活性 / 構造活性相関 / ダフナン型 / ジテルペノイド / トウダイグサ科 / ジンチョウゲ科 / 創薬 / 天然物化学 |
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| Outline of Final Research Achievements |
HIV agents which can eliminate latent HIV virus, are expected as the next generation anti-HIV drug. In this study, we established the isolation and purification method of Gnidimacrin, a daphnane-type diterpenoid from Stellera chamaejasme, which shows extremely potent anti-HIV activity against latent HIV virus. In addition, we clarified the effectiveness of Gnidimacrin for the elimination of latent HIV-1 in an ex vivo model using peripheral blood mononuclear cells from patients with HIV infection. Furthermore, the chemically synthesized derivatives of Gnimacrin were evaluated for their in vitro anti-HIV activities. As a result, the acyl group at the 3-position of gnidimacrin is important for the anti-HIV activity, whereas the 2'-position hydroxyl group is an important functional group for further investigation of the mechanism of Gnidimacrin action.
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Report
(4 results)
Research Products
(3 results)
