Munday R, Smith B L, Munday C M
AgResearch, Ruakura Agricultural Research Centre, Hamilton, New Zealand.
Chem Biol Interact. 1995 Nov 17;98(2):185-92. doi: 10.1016/0009-2797(95)03645-8.
2-Hydroxy-1,4-naphthoquinone has previously been shown to cause severe haemolytic anaemia and renal tubular necrosis in animals. In order to establish if such toxic effects are common to other 2-hydroxynaphthoquinone derivatives, the short-term toxicity of a number of 2-hydroxy-3-alkyl-1,4-naphthoquinones has been compared in rats. 2-Hydroxy-3-methyl, 2-hydroxy-3-ethyl- and 2-hydroxy-3-propyl-1,4-naphthoquinone were found to cause both haemolysis and renal damage, although the severity of the changes provoked by these substances was much lower than those induced by the parent compound at an equivalent dose-level. Furthermore, the toxicity of the hydroxy-alkylnaphthoquinones decreased with increasing size of the alkyl substituent and no toxic changes were recorded in animals dosed with 2-hydroxy-3-butyl- or 2-hydroxy-3-pentyl-1,4-naphthoquinone. The relationship between the in vivo effects of these substances and previously reported data on their in vitro cytotoxicity is discussed in relation to the mechanism of toxicity of these and other naphthoquinone derivatives.
2-羟基-1,4-萘醌先前已被证明可在动物体内引起严重的溶血性贫血和肾小管坏死。为了确定其他2-羟基萘醌衍生物是否也有此类毒性作用，研究人员比较了多种2-羟基-3-烷基-1,4-萘醌在大鼠体内的短期毒性。结果发现，2-羟基-3-甲基、2-羟基-3-乙基和2-羟基-3-丙基-1,4-萘醌均可导致溶血和肾脏损伤，不过在同等剂量水平下，这些物质引发的变化严重程度远低于母体化合物。此外，羟基烷基萘醌的毒性随烷基取代基尺寸的增大而降低，给动物注射2-羟基-3-丁基或2-羟基-3-戊基-1,4-萘醌后未记录到毒性变化。本文结合这些及其他萘醌衍生物的毒性机制，讨论了这些物质的体内效应与先前报道的体外细胞毒性数据之间的关系。
