Coordination chemistry of metals in medicine: target sites for bismuth

Coordination chemistry of metals in medicine: target sites for bismuth
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DOI:
10.1016/s0010-8545(99)00018-1
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发表时间:
1999-05
影响因子:
20.6
通讯作者:
P. Sadler;Hongyan Li;Hongzhe Sun
P. Sadler;Hongyan Li;Hongzhe Sun
中科院分区:
化学1区
文献类型:
--
作者:
P. Sadler;Hongyan Li;Hongzhe Sun

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铋化合物用于治疗胃肠道疾病,也可用于治疗其他疾病。Bi(III)具有高度可变的配位数(3-10)和不规则的配位数几何。Bi(III)与羧酸盐和氨基羧酸盐的配位化学以分子间相互作用为主,从而形成聚合物结构。Bi(III)与三肽谷胱甘肽的硫酸硫结合强烈,然而这些加合物也具有动力学不稳定性,这使得Bi(III)在细胞内快速易位。Bi(III)的主要生物学靶点似乎是蛋白质和酶。Bi(III)结合蛋白质和酶中的Zn(II)位点(如金属硫蛋白)和Fe(III)位点(如转铁蛋白和乳铁蛋白),抑制细菌的Ni酶脲酶。
Bismuth compounds are used for the treatment of gastrointestinal disorders and may also be useful for the treatment of other diseases. Bi(III) exhibits a highly variable coordination number (3–10) and often an irregular coordination geometry. The coordination chemistry of Bi(III) with carboxylates and aminocarboxylates is dominated by intermolecular interactions which leads to polymeric structures. Bi(III) binds strongly to the thiolate sulfur of the tripeptide glutathione, however these adducts are also kinetically labile which allows rapid translocation of Bi(III) inside cells. The major biological target for Bi(III) appears to be proteins and enzymes. Bi(III) binds to both Zn(II) sites (e.g. metallothionein) and Fe(III) sites (e.g. transferrin and lactoferrin) in proteins and enzymes and inhibits the bacterial Ni enzyme urease.