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抗疟作用中的电荷转移与氧自由基。醌类、氨苯砜代谢物、金属络合物、亚胺离子和过氧化物。

Charge transfer and oxy radicals in antimalarial action. Quinones, dapsone metabolites, metal complexes, iminium ions, and peroxides.

作者信息

Ames J R, Ryan M D, Klayman D L, Kovacic P

出版信息

J Free Radic Biol Med. 1985;1(5-6):353-61. doi: 10.1016/0748-5514(85)90147-3.

DOI:10.1016/0748-5514(85)90147-3
PMID:3837802
Abstract

A mechanism of action is proposed that encompasses almost all of the main categories of antimalarial agents: quinones and precursors, dapsone metabolites, metal complexes of thiosemicarbazones and biguanides, iminium-type ions from acridines and quinolines, and peroxides. The toxic effect of the drugs is believed to result from the generation of reactive oxygen radicals that usually arise via charge transfer. Electrochemical studies (reduction potential and reversibility) were performed on a number of these agents. Reduction potentials range from -0.23 to -1.52 V. It is likely that the in vivo values are appreciably more positive in certain cases.

摘要

提出了一种作用机制,该机制几乎涵盖了抗疟药物的所有主要类别:醌类及其前体、氨苯砜代谢产物、硫代氨基脲和双胍的金属配合物、吖啶和喹啉产生的亚胺型离子以及过氧化物。据信这些药物的毒性作用是由通常通过电荷转移产生的活性氧自由基引起的。对其中一些药物进行了电化学研究(还原电位和可逆性)。还原电位范围为-0.23至-1.52 V。在某些情况下,体内值可能明显更正。

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