Synthesis of glycosylated derivatives of ginkgolides and in vivo evaluation of those pharmacokinetics

2014 Fiscal Year Final Research Report

• Project/Area Number: 24590156
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: National Institute of Radiological Sciences (2013-2014); The Institute of Physical and Chemical Research (2012)
• Principal Investigator: ISHII Hideki 独立行政法人放射線医学総合研究所, 分子イメージング研究センター, 主任研究員 (80425610)
• Co-Investigator(Kenkyū-buntansha): KOYAMA Hiroko 岐阜大学, 大学院医学系研究科, 助教 (50402160)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: 天然物 / プロドラック / PET / プローブ / ギンコライド

Outline of Final Research Achievements

It is said that the effect to Alzheimer or dementia of the ginkgo biloba is caused by ginkgolides, but an evaluation halves that because of the low lipophilicity of ginkgolides, the dramatic curative effect were not observed in the most of cases. In order to overcome these problems, we planned the synthesis of glicosylated which might promote the uptake of ginkgolides to the brain through glucose transporter. In addition, we planned that the in vivo dynamics of the ginkgolide derivatives which we designed composed a short-life radionuclide-labeled derivative and evaluated it.

Free Research Field

有機化学