Brown D A, Chidambaram M V, Clarke J J, McAleese D M
Bioinorg Chem. 1978 Sep;9(3):255-75. doi: 10.1016/s0006-3061(00)80045-9.
The design and use of iron(III) chelates in the oral treatment of iron-deficiency anemia is discussed in terms of the following criteria: (1) the ability of a chelate to exist as a monomeric species even at physiological pH values, (2) the rate of transfer of iron from the chelate to the iron-transporting protein-apotransferrin, (3) the rate of depolymerization of ferric citrate polymer by the free ligand, and (4) its nontoxicity and ability to regenerate hemoglobin levels in anemic rats. Detailed species distribution studies, stability constants, and kinetic data for iron(III) acetohydroxamate (criteria 1-3 above) show that it remains monomeric at physiological pH values and undergoes very rapid iron transfer with apotransferrin. Detailed animal studies show a significant increase in regeneration of hemoglobin in rats fed 2 ml of 4 mM Fe(III) acetohydroxamate daily when compared to rats fed similarly with Fe(III) citrate. A strong potential is thus indicated for Fe(III) acetohydroxamate as a source of iron in the anemic animal.
从以下标准出发，探讨了铁（III）螯合物在缺铁性贫血口服治疗中的设计与应用：（1）螯合物即使在生理pH值下也能以单体形式存在的能力；（2）铁从螯合物转移至铁转运蛋白脱铁转铁蛋白的速率；（3）游离配体使柠檬酸铁聚合物解聚的速率；（4）其无毒性以及使贫血大鼠血红蛋白水平恢复的能力。关于乙酰氧肟酸铁（上述标准1 - 3）的详细物种分布研究、稳定常数和动力学数据表明，它在生理pH值下保持单体状态，并与脱铁转铁蛋白进行非常快速的铁转移。详细的动物研究表明，与同样喂食柠檬酸铁的大鼠相比，每天喂食2毫升4 mM乙酰氧肟酸铁的大鼠血红蛋白再生显著增加。因此，乙酰氧肟酸铁作为贫血动物铁源具有很大的潜力。
