Doi Hisashi, Sato Kengo, Shindou Hideo, Sumi Kengo, Koyama Hiroko, Hosoya Takamitsu, Watanabe Yasuyoshi, Ishii Satoshi, Tsukada Hideo, Nakanishi Koji, Suzuki Masaaki
Division of Bio-Function Dynamics Imaging, RIKEN Center for Life Science Technologies (CLST), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe 650-0047, Japan.
PET Medical Application Group, Central Research Laboratory, Hamamatsu Photonics K.K., 5000 Hirakuchi, Hamakita-ku, Hamamatsu 434-8601, Japan.
Bioorg Med Chem. 2016 Nov 1;24(21):5148-5157. doi: 10.1016/j.bmc.2016.08.032. Epub 2016 Aug 23.
The blood-brain barrier permeability of ginkgolide B was examined using positron emission tomography (PET) probes of a F-incorporated ginkgolide B ([F]-2) and a C-incorporated methylbenzyl-substituted ginkgolide B ([C]-3). PET studies in monkeys showed low uptake of [F]-2 into the brain, but small amounts of [C]-3 were accumulated in the parenchyma. Furthermore, when cyclosporine A was preadministered to rats, the accumulation of [F]-2 in the rat brain did not significantly change, however, the accumulation of [C]-3 was five times higher than that in the control rat. These results provide effective approaches for investigating the drug potential of ginkgolides.
使用含氟银杏内酯B（[F]-2）和含碳甲基苄基取代银杏内酯B（[C]-3）的正电子发射断层扫描（PET）探针检测了银杏内酯B的血脑屏障通透性。对猴子进行的PET研究显示，[F]-2在脑中的摄取量较低，但少量的[C]-3在脑实质中蓄积。此外，当预先给大鼠施用环孢素A时，[F]-2在大鼠脑中的蓄积没有显著变化，然而，[C]-3的蓄积量比对照大鼠高五倍。这些结果为研究银杏内酯的药物潜力提供了有效的方法。
