Franklin M R
Environ Health Perspect. 1976 Apr;14:29-37. doi: 10.1289/ehp.761429.
The effects of methylenedioxyphenyl insecticide synergists on human health arise, not from their intrinsic toxicity which is relatively low, but from their dual effect on the oxidative detoxication or intoxication processes of the body. They are able to inhibit these reactions by two mechanisms. They are substrates for mixed function oxidation and, thus, compete with other xenobiotics for available enzyme, and an intermediate in their metabolism is able to bind with cytochrome P-450 to form an inactive complex which absorbs maximally at 455 nm. In addition, they are able to activate xenobiotic metabolism by induction (the increased synthesis and retention) of microsomal oxidative enzymes. Evidence for these effects is presented, including spectroscopic and enzyme kinetic data. Correlations with existing in vivo observations are outlined. The inhibition and induction of cytochrome P-450, the central enzyme in the metabolism of xenobiotics, thus provides the focus for consideration of methylenedioxyphenyl synergists as potential hazards.
亚甲二氧基苯基杀虫剂增效剂对人体健康产生的影响，并非源于其本身相对较低的毒性，而是源于它们对人体氧化解毒或中毒过程的双重作用。它们能够通过两种机制抑制这些反应。它们是混合功能氧化的底物，因此与其他异生物质竞争可用的酶，并且其代谢过程中的一种中间体能够与细胞色素P - 450结合形成一种在455nm处有最大吸收的无活性复合物。此外，它们能够通过诱导（微粒体氧化酶的合成和保留增加）来激活异生物质代谢。文中给出了这些作用的证据，包括光谱和酶动力学数据。概述了与现有体内观察结果的相关性。细胞色素P - 450是异生物质代谢的核心酶，其抑制和诱导作用，因此成为将亚甲二氧基苯基增效剂视为潜在危害加以考虑的重点。
