Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 24, Issue 21, Pages 5148-5157Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.08.032
Keywords
Ginkgolide B; Platelet-activating factor; Blood-brain barrier; PET; C-[C-11]methylation
Funding
- JSPS [13NP0401, 25242070]
- Ministry of Education, Culture, Sports, Science and Technology (MEXT) of Japan
- Grants-in-Aid for Scientific Research [13NP0401, 16H05136, 25242070] Funding Source: KAKEN
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The blood-brain barrier permeability of ginkgolide B was examined using positron emission tomography (PET) probes of a F-18-incorporated ginkgolide B ([F-18]-2) and a C-11-incorporated methylbenzyl-substituted ginkgolide B ([C-11]-3). PET studies in monkeys showed low uptake of [F-18]-2 into the brain, but small amounts of [C-11]-3 were accumulated in the parenchyma. Furthermore, when cyclosporine A was preadministered to rats, the accumulation of [F-18]-2 in the rat brain did not significantly change, however, the accumulation of [C-11]-3 was five times higher than that in the control rat. These results provide effective approaches for investigating the drug potential of ginkgolides. (C) 2016 Elsevier Ltd. All rights reserved.
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