1997
DOI: 10.1124/mol.51.5.842
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Chelation and Mobilization of Cellular Iron by Different Classes of Chelators

Abstract: SUMMARYIron chelators belonging to three distinct chemical families were assessed in terms of their physicochemical properties and the kinetics of iron chelation in solution and in two biological systems. Several hydroxypyridinones, reversed siderophores, and desferrioxamine derivatives were selected to cover agents with different iron-binding stoichiometry and geometry and a wide range of lipophilicity, as determined by the octanol-water partition coefficients. The selection also included highly lipophilic ch… Show more

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Cited by 84 publications
(60 citation statements)
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“…The high membrane permeability of the iron-free form of DFP is well documented, as shown by its capacity to rapidly access and deplete intracellular labile iron pools. 36,37 On the other hand, the ability of DFP-Fe complexes to traverse intracellular and plasma membranes of cells has not been studied in detail. 20,21,36,37 One indication is the capacity of orally administered DFP to increase serum transferrin saturation 12 and labile iron 11 within an hour after intake in thalassemia patients, which is attributable to the rapid exit of DFP-Fe complexes from cells into the circulation.…”
Section: Discussionmentioning
confidence: 99%
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“…The high membrane permeability of the iron-free form of DFP is well documented, as shown by its capacity to rapidly access and deplete intracellular labile iron pools. 36,37 On the other hand, the ability of DFP-Fe complexes to traverse intracellular and plasma membranes of cells has not been studied in detail. 20,21,36,37 One indication is the capacity of orally administered DFP to increase serum transferrin saturation 12 and labile iron 11 within an hour after intake in thalassemia patients, which is attributable to the rapid exit of DFP-Fe complexes from cells into the circulation.…”
Section: Discussionmentioning
confidence: 99%
“…36,37 On the other hand, the ability of DFP-Fe complexes to traverse intracellular and plasma membranes of cells has not been studied in detail. 20,21,36,37 One indication is the capacity of orally administered DFP to increase serum transferrin saturation 12 and labile iron 11 within an hour after intake in thalassemia patients, which is attributable to the rapid exit of DFP-Fe complexes from cells into the circulation. At the intracellular level, it is shown in this work that DFP can facilitate the removal of labile iron from nuclei ( Figure 3 Ability to compete effectively for intracellular labile iron with other intermediate affinity species.…”
Section: Discussionmentioning
confidence: 99%
“…Finally, it should be noted that deferoxamine is a standard clinical treatment for humans suffering from iron overload (Lederman et al, 1984;Zanninelli et al, 1997). It is regarded as relatively safe (Lederman et al, 1984) and it is not lipophilic, so it doesn't penetrate cells (Zanninelli et al, 1997). Thus, it is not absorbed across mucus membranes and must be injected when used therapeutically.…”
Section: Metal Binding By Components Of the Gluementioning
confidence: 99%
“…By contrast, the samples collected in deferoxamine achieved good extractions; these were substantially better than was achieved with heating and vortexing of samples that had been already set. Finally, it should be noted that deferoxamine is a standard clinical treatment for humans suffering from iron overload (Lederman et al, 1984;Zanninelli et al, 1997). It is regarded as relatively safe (Lederman et al, 1984) and it is not lipophilic, so it doesn't penetrate cells (Zanninelli et al, 1997).…”
Section: Metal Binding By Components Of the Gluementioning
confidence: 99%
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