Blood-brain barrier-permeable fluorone-labeled dieckols acting as neuronal ER stress signaling inhibitors

Jong Hwan Kwak, Zhigang Yang, Byungkwon Yoon, Yanxia He, Soojin Uhm, Hyeon Cheol Shin, Bong Ho Lee, Yung Choon Yoo, Kyung Bok Lee, Seung Yun Han, Jong Seung Kim

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)


We studied the blood-brain barrier (BBB) permeability and intracellular localization of a fluorescein isothiocyanate (FITC)-labeled dieckol (1) and a rhodamine B-labeled dieckol (7), for exploring the possible therapeutic application of fluorone-labeled dieckols in neurodegenerative diseases. Both compounds (1 & 7) were synthesized through a click reaction and were found to be localized in the endoplasmic reticulum (ER) of the two types of brain cell lines (SH-SY5Y and BV-2 cells) tested; they also reduced ER stress in the SH-SY5Y human neuroblastoma cells. In addition, 1 and 7 were shown to pass the BBB in rats upon intravenous administration. Altogether, our study demonstrates, for the first time, that targeted ER-stress reduction in brain cells can be achieved by introducing fluorone-dieckol conjugates into systemic circulation. Therefore, 1 and 7 provide a novel and promising ER-targeting therapeutic strategy for neurodegenerative diseases.

Original languageEnglish
Pages (from-to)52-60
Number of pages9
Publication statusPublished - 2015 Aug 1

Bibliographical note

Publisher Copyright:
© 2015 Elsevier Ltd.


  • Blood-brain barrier
  • Click reaction
  • ER localization
  • Endoplasmic reticulum (ER) stress
  • Fluorone-labeled dieckols

ASJC Scopus subject areas

  • Mechanics of Materials
  • Ceramics and Composites
  • Bioengineering
  • Biophysics
  • Biomaterials


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