Chelating Compound,Chrysoidine, Is More Effective in Both Antiprion Activity and Brain Endothelial Permeability Than Quinacrine |
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| Authors: | Katsumi Doh-ura Kazuhiko Tamura Yoshiharu Karube Mikihiko Naito Takashi Tsuruo Yasufumi Kataoka |
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| Institution: | (1) Department of Prion Research, Tohoku University Graduate School of Medicine, Sendai, Japan;(2) Department of Pharmaceutical Care and Health Sciences, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan;(3) Department of Drug Design and Drug Delivery, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan;(4) Institute of Molecular and Cellular Biosciences, University of Tokyo, Tokyo, Japan;(5) Department of Prion Research, Tohoku University Graduate School of Medicine, 2-1 Seiryo-cho, Aoba-ku Sendai, 980-8575, Japan |
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| Abstract: | 1. As an extension of our previous study of quinacrine and its derivatives, chelating chemicals were screened to obtain more
effective, better brain-permeable antiprion compounds using either prion-infected neuroblastoma cells or brain capillary endothelial
cells.
2. Eleven chemicals were found to have antiprion activity. Most of them shared a common structure consisting of benzene or
naphthalene at either end of an azo bond. Structure–activity data suggest that chelating activity is not necessary but might
contribute to the antiprion action.
3. Chrysoidine, a representative compound found here, was about 27 times more effective in the antiprion activity and five
times more efficiently permeable through the brain capillary endothelial cells than quinacrine was.
4. These chemicals might be useful as compounds for development of therapeutics for prion diseases. |
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| Keywords: | prion chrysoidine blood– brain barrier aromatic azo compounds therapy chelating agents brain endothelial cells prion-infected neuroblastoma cells |
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