Schubert J
Environ Health Perspect. 1981 Aug;40:227-32. doi: 10.1289/ehp.8140227.
Chelation enables metals to be transported to or from vulnerable target sites, and to hinder or facilitate their carcinogenic potential. In the reverse sense, metals are capable of ligand scavenging via complexation or mixed complex formation--the latter being the result of interaction with binary complexes. Consequently, metal complexes can be utilized for the transport of selected organic chemotherapeutic drugs to target organs, or for the decorporation of those toxic organic compounds which are able, before or after metabolic activation, of reacting with metals or 1:1 metal complexes. It is emphasized that the degree to which metal ions interact in vivo should employ the conditional constants which take into account competition from other ions, especially Ca2+, H+, and OH-. The genotoxic consequences of the various chemical factors involved in chelation, along with examples: kinetics, stabilization of oxoidation states, lipophilicity, and mixed ligand formation, are discussed.
螯合作用可使金属往返于易受影响的靶位点，并阻碍或促进其致癌潜力。反过来，金属能够通过络合或形成混合络合物来清除配体，后者是与二元络合物相互作用的结果。因此，金属络合物可用于将选定的有机化疗药物转运至靶器官，或用于去除那些在代谢活化前后能够与金属或1:1金属络合物反应的有毒有机化合物。需要强调的是，金属离子在体内的相互作用程度应采用考虑其他离子（尤其是Ca2+、H+和OH-）竞争的条件常数。本文讨论了螯合过程中涉及的各种化学因素的遗传毒性后果，并举例说明了动力学、氧化态稳定、亲脂性和混合配体形成等方面。
