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Chloroquine and hydroxychloroquine binding to melanin : some possible consequences for pathologies

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dc.contributor.authorSchroeder, R.L.
dc.contributor.authorGerber, J.P.
dc.date.issued2014
dc.description.abstractFor 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.
dc.identifier.citationToxicology Reports, 2014; 1:963-968
dc.identifier.doi10.1016/j.toxrep.2014.10.019
dc.identifier.issn2214-7500
dc.identifier.issn2214-7500
dc.identifier.urihttps://hdl.handle.net/1959.8/163223
dc.language.isoen
dc.publisherElsevier
dc.rightsCopyright 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/)
dc.source.urihttp://dx.doi.org/10.1016/j.toxrep.2014.10.019
dc.subjectmelanin
dc.subjectchloroquine
dc.subjecthydroxychloroquine
dc.subjectsepia
dc.subjectadsorption
dc.subjectdesorption
dc.titleChloroquine and hydroxychloroquine binding to melanin : some possible consequences for pathologies
dc.typeJournal article
pubs.publication-statusPublished
ror.fileinfo12143285010001831 13143282800001831 9915910311001831_53108670490001831.pdf
ror.mmsid9915910311001831

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