Chloroquine and hydroxychloroquine binding to melanin : some possible consequences for pathologies
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2014
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Schroeder, R.L.
Gerber, J.P.
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Journal article
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Toxicology Reports, 2014; 1:963-968
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Abstract
For many years chloroquine was used as a prophylactic agent against malaria, and morerecently as a mild immunosuppressive. However, due to lengthy treatment periods, adverseeffects have become apparent, which included retinopathy. The structurally related hydrox-ychloroquine is less toxic, thought to be owing to a lower tissue accumulation in melaninrich areas. This study primarily focused on quantifying melanin binding between chloro-quine and hydroxychloroquine at physiological pH to investigate the potential link betweenbinding and reported toxicity. In addition, for the first time this study quantified the actualextent of adsorption of chloroquine and hydroxychloroquine to melanin and examined thedesorption profile of both drugs from melanin to demonstrate the affinity between the pig-ment and the solutes. The results suggest that there is a difference between the adsorptionaffinities of chloroquine and hydroxychloroquine, potentially explaining the differencesin bioaccumulation in retinal tissue. In addition, both solutes displayed a strong physicalattraction to the absorbent.
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Copyright 2014 The Authors. Published by Elsevier Ireland. This is an open access article under the CC BY-NC-ND 3.0 license. (http://creativecommons.org/licenses/by-nc-nd/3.0/)