Phytochemical investigation of Daphnane-type diterpenoids aiming to discover next generation anti-HIV drugs

2016 Fiscal Year Final Research Report

• Project/Area Number: 26460133
• 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)
• Research Collaborator: LEE Kuo-Hsiung ; CHEN Chin-Ho
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: HIV感染症 / Gnidimacrin / ダフナン / 抗HIV薬

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.

Free Research Field

天然物化学