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Involvement of a Novel Organic Cation Transporter in Paeonol Transport Across the Blood-Brain Barrier

Authors
Gyawali, AsmitaKrol, SokhoeurnKang, Young-Sook
Issue Date
May-2019
Publisher
KOREAN SOC APPLIED PHARMACOLOGY
Keywords
Blood-brain barrier; Paeonol; Novel organic cationic transporter system; Brain transport; TR-BBB cells
Citation
BIOMOLECULES & THERAPEUTICS, v.27, no.3, pp.290 - 301
Journal Title
BIOMOLECULES & THERAPEUTICS
Volume
27
Number
3
Start Page
290
End Page
301
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/3648
DOI
10.4062/biomolther.2019.007
ISSN
1976-9148
Abstract
Paeonol has neuroprotective function, which could be useful for improving central nervous system disorder. The purpose of this study was to characterize the functional mechanism involved in brain transport of paeonol through blood-brain barrier (BBB). Brain transport of paeonol was characterized by internal carotid artery perfusion (ICAP), carotid artery single injection technique (brain uptake index, BUI) and intravenous (IV) injection technique in vivo. The transport mechanism of paeonol was examined using conditionally immortalized rat brain capillary endothelial cell line (TR-BBB) as an in vitro model of BBB. Brain volume of distribution (VD) of [H-3] paeonol in rat brain was about 6-fold higher than that of [C-14] sucrose, the vascular space marker of BBB. The uptake of [H-3] paeonol was concentration-dependent. Brain volume of distribution of paeonol and BUI as in vivo and inhibition of analog as in vitro studies presented significant reduction effect in the presence of unlabeled lipophilic compounds such as paeonol, imperatorin, diphenhydramine, pyrilamine, tramadol and ALC during the uptake of [H-3] paeonol. In addition, the uptake significantly decreased and increased at the acidic and alkaline pH in both extracellular and intracellular study, respectively. In the presence of metabolic inhibitor, the uptake reduced significantly but not affected by sodium free or membrane potential disruption. Similarly, paeonol uptake was not affected on OCTN2 or rPMAT siRNA transfection BBB cells. Interestingly. Paeonol is actively transported from the blood to brain across the BBB by a carrier mediated transporter system.
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