Borneol and Α-asarone as adjuvant agents for improving blood-brain barrier permeability of puerarin and tetramethylpyrazine by activating adenosine receptors.

ABSTRACT: Puerarin (PUE) and tetramethylpyrazine (TMP) are central nervous system (CNS) drugs used in cerebrovascular diseases. Poor brain-blood barrier (BBB) permeability limited their clinical application. Borneol and α-asarone have been proposed as an oral brain-targeting enhancer. In this study, we aimed to first evaluate the 'orifice-opening' effect of borneol and α-asarone, both aromatic resuscitation drugs, on improvement of brain delivery of PUE and TMP and second to investigate whether the enhancing effects were associated with adenosine receptors (ARs)-mediated trans-BBB pathway. In vitro BBB model was established and borneol and α-asarone significantly increased the cumulative amount of permeated PUE and TMP and the enhancing effects could be counteracted by AR inhibitors. Borneol and α-a

SUBMITTER: Wu JY 

PROVIDER: S-EPMC6201807 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature