title: Iron binding dendrimers: a novel approach for the treatment of haemochromatosis.
abstract: A range of iron binding dendrimers terminated with hexadentate ligands formed from hydroxypyridinone, hydroxypyranone, and catechol moieties have been synthesized in order to investigate their potential as clinically useful iron(III)-selective chelators capable of removing dietary iron from the gastrointestinal tract and preventing the development of iron overload typical of haemochromatosis and thalassaemia intermedia. The iron chelating abilities of these molecules have been characterized by MALDI-TOF mass spectrometry and UV spectrometry. Hydroxypyridinone-terminated dendrimers were found to possess a high affinity and selectivity for iron(III). A hydroxypyridinone-based dendrimer was demonstrated to be highly efficient at reducing the absorption of iron(III) in rat intestine. This family of dendrimers may find an application in the treatment of iron overload.
authors.affiliation: Department of Pharmacy and Drug Control Centre, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK.
authors.forename: Tao
authors.initials: T
authors.lastname: Zhou
authors.forename: Hendrik
authors.initials: H
authors.lastname: Neubert
authors.forename: Ding Yong
authors.initials: DY
authors.lastname: Liu
authors.forename: Zu Dong
authors.initials: ZD
authors.lastname: Liu
authors.forename: Yong Min
authors.initials: YM
authors.lastname: Ma
authors.forename: Xiao Le
authors.initials: XL
authors.lastname: Kong
authors.forename: Wei
authors.initials: W
authors.lastname: Luo
authors.forename: Sykes
authors.initials: S
authors.lastname: Mark
authors.forename: Robert C
authors.initials: RC
authors.lastname: Hider
mesh_terms: D000818:Animals; D050091:Dendrimers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006432:Hemochromatosis / Q000188:drug therapy*; D066298:In Vitro Techniques; D007408:Intestinal Absorption / Q000187:drug effects; D007501:Iron / Q000378:metabolism; D007502:Iron Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship
chemical_list: D050091:Dendrimers; D007502:Iron Chelating Agents; D011728:Pyridones; D007501:Iron