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首页> 外文期刊>Polyhedron: The International Journal for Inorganic and Organometallic Chemistry >Evaluation of 1,2-dimethyl-3-hydroxy-4-pyridinecarboxylic acid and of other 3-hydroxy-4-pyridinecarboxylic acid derivatives for possible application in iron and aluminium chelation therapy
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Evaluation of 1,2-dimethyl-3-hydroxy-4-pyridinecarboxylic acid and of other 3-hydroxy-4-pyridinecarboxylic acid derivatives for possible application in iron and aluminium chelation therapy

机译：评估1,2-二甲基-3-羟基-4-吡啶羧酸和其他3-羟基-4-吡啶羧酸衍生物可能在铁和铝螯合疗法中的应用

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摘要

Four new possible chelating agents for iron and aluminium, 1,2-dimethyl-3-hydroxy-4-pyridinecarboxylic acid (DT712), 3-hydroxy-1,2,6- trimethyl-4-pyridinecarboxylic acid, 2,6-dimethyl-3-hydroxy-4-pyridinecarboxylic acid, and 2-ethyl-3-hydroxy-1-methyl-4-pyridinecarboxylic acid, were synthesized, and their complex formation with Fe(III) and Al(III) was studied by potentiometry, UV-Vis, ~1H NMR, and electrospray mass spectrometry (ESI-MS). Number, stoichiometry, and stability constants of metal-ligand complexes were obtained at 25 C in aqueous (Na)Cl 0.6 m. DT712 is the most promising hydroxypyridinecarboxylic acid considered so far for iron chelation therapy, as it forms the strongest Fe(III) complexes. This compound was further investigated to better clarify its possible behaviour in vivo with particular respect to iron chelation therapy. UV-Vis measurements were performed to determine the kinetics by which DT712 extracts Fe(III) from transferrin. DT712 resulted to have better kinetic properties than existing iron chelators. Ternary metal/DT712/citric acid complexes were studied by ESI-MS to check the competition with a typical low molecular weight ligand in the blood. The formation of only binary Fe(III)/DT712 and Al(III)/DT712 complexes (and ternary complexes in aged solutions), suggests that DT712 effectively compete with citric acid in the metal complexation. Standard reduction potentials of Fe(III)/DT712 complexes, and the kinetic constants of complex formation, were obtained by cyclic voltammetry. Accordingly, no redox cycling is expected to occur at in vivo conditions, and Fe(III)/DT712 complex formation should not be kinetically limited. On the basis of the present results, DT712 is proposed as candidate for iron chelation therapy.
机译：四种可能的铁和铝螯合剂，1,2-二甲基-3-羟基-4-吡啶羧酸（DT712），3-羟基-1,2,6-三甲基-4-吡啶羧酸，2,6-二甲基合成了-3-羟基-4-吡啶羧酸和2-乙基-3-羟基-1-甲基-4-吡啶羧酸，并通过电位法研究了它们与Fe（III）和Al（III）的络合物形成， UV-Vis，〜1H NMR和电喷雾质谱（ESI-MS）。金属-配体配合物的数量，化学计量和稳定性常数是在25°C的0.6 m（Na）Cl水溶液中获得的。 DT712是迄今为止最有希望用于铁螯合疗法的羟基吡啶羧酸，因为它形成最强的Fe（III）配合物。对该化合物进行了进一步研究，以更好地阐明其在体内特别是铁螯合疗法方面的可能行为。进行UV-Vis测量以确定DT712从运铁蛋白中提取Fe（III）的动力学。与现有的铁螯合剂相比，DT712具有更好的动力学性能。通过ESI-MS研究了三元金属/ DT712 /柠檬酸络合物，以检查与血液中典型的低分子量配体的竞争。仅形成二元Fe（III）/ DT712和Al（III）/ DT712配合物（以及老化溶液中的三元配合物），表明DT712在金属配合物中有效地与柠檬酸竞争。 Fe（III）/ DT712配合物的标准还原电位和配合物形成的动力学常数通过循环伏安法获得。因此，预期在体内条件下不会发生氧化还原循环，并且Fe（III）/ DT712复合物的形成不应受到动力学限制。根据目前的结果，建议将DT712用作铁螯合疗法的候选药物。

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