YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Characterization of the Brain Transport and Brain-to-Blood Efflux of Nitrone Based Antioxidant, PBN

Nitrone계 항산화제 (PBN)의 뇌에서 혈액으로의 배출과 뇌 수송 특성

  • 이나영 (숙명여자대학교 약학대학) ;
  • 강영숙 (숙명여자대학교 약학대학)
  • Published : 2003.08.01
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Abstract

We have investigated the transport characteristics of synthetic antioxidant and free radical scavenger, $\alpha$-phenyl-n-tert-butyl nitrone (PBN) at the blood-brain barrier (BBB) by in vitro uptake study in conditionally immortalized rat brain capillary endothelial cell line (TR-BBB). Also, the efflux of PBN from brain to blood is estimated using the brain efflux index (BEI) method. Choline is a charged organic cation, including nitrogen-methyl group and shows the carrier-mediated distribution to the brain. [$^3$H]Choline uptake by TR-BBB cells was significantly inhibited by PBN with $IC_{50}$/ of 1.2 mM, which appears to be due to similar structures between choline and PBN. And, PBN was microinjected into Par2 of the rat brain by BEI method, and was eliminated from the brain with an apparent elimination half-life of about 2 min. Also, [$^3$H]choline efflux was significantly inhibited by PBN using BEI method. In conclusion, the efflux transport of PBN takes place across the BBB and PBN may be transported into the brain and eliminated from the brain by BBB choline transporter.

Keywords

References

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