Plummer S M, Faux S P
Centre for Mechanisms of Human Toxicity, Leicester, UK.
Carcinogenesis. 1994 Mar;15(3):449-53. doi: 10.1093/carcin/15.3.449.
The genotoxic/mutagenic mechanism(s) of action of fecapentaene-12 (fec-12) is complex but there is evidence to suggest that the generation of active oxygen species (AOS) may be involved. This has been assessed by measuring the formation of 8-hydroxydeoxyguanosine (8-OHdG) in isolated DNA and HeLa cells exposed in vitro to fec-12. The possibility that fec-12 may form AOS via peroxidative 'activation' by prostaglandin H synthase (PHS) has been investigated by measuring 8-OHdG in HeLa cells exposed to fec-12 in the absence or presence of PHS inhibitors. The role of iron as a catalyst in this pathway has also been investigated. A 4-fold increase in the level of 8-OHdG in isolated DNA was seen after exposure to fec-12 (1 mM) alone. This increase was enhanced synergistically by ferrous iron. Fec-12 exposure of HeLa cells at 50 and 100 microM induced 2- and 3-fold increases (P < 0.001) respectively in the level of 8-OHdG in cellular DNA. No increase was seen at 10 microM fec-12. The PHS inhibitors indomethacin and acetylsalicylate blocked the formation of 8-OHdG induced by fec-12 (50 microM) but did not inhibit the formation of 8-OHdG in these cells after exposure to H2O2 and Fe2+. Addition of the iron chelating agent o-phenanthroline to cells prior to fec-12 exposure blocked the increase in 8-OHdG induced by fec-12 (50 microM). Addition of the radical scavenging agent DMSO (10%) to cells prior to fec-12 exposure reduced the level of 8-OHdG to within 10% of control. Specific inhibition of fec-12 induced 8-OHdG formation in HeLa cells by PHS inhibitors suggests that this enzyme may be involved in 'activating' fec-12 to form AOS in cells. Inhibition of fec-12 induced 8-OHdG formation in cells by o-phenanthroline suggests a role for intracellular iron as a catalyst in this process.
粪卟啉-12(fec-12)的遗传毒性/诱变作用机制复杂,但有证据表明活性氧物种(AOS)的产生可能与之有关。这已通过测量体外暴露于fec-12的分离DNA和HeLa细胞中8-羟基脱氧鸟苷(8-OHdG)的形成来评估。通过测量在不存在或存在前列腺素H合酶(PHS)抑制剂的情况下暴露于fec-12的HeLa细胞中的8-OHdG,研究了fec-12是否可能通过PHS的过氧化“激活”形成AOS的可能性。还研究了铁作为该途径中催化剂的作用。单独暴露于fec-12(1 mM)后,分离DNA中8-OHdG的水平增加了4倍。亚铁协同增强了这种增加。以50和100 microM暴露于fec-12的HeLa细胞分别使细胞DNA中8-OHdG的水平增加了2倍和3倍(P < 0.001)。在10 microM fec-12时未观察到增加。PHS抑制剂吲哚美辛和乙酰水杨酸酯阻断了fec-12(50 microM)诱导的8-OHdG的形成,但在这些细胞暴露于H2O2和Fe2+后并未抑制8-OHdG的形成。在fec-12暴露之前向细胞中添加铁螯合剂邻菲罗啉阻断了fec-12(50 microM)诱导的8-OHdG的增加。在fec-12暴露之前向细胞中添加自由基清除剂二甲基亚砜(10%)将8-OHdG的水平降低至对照的10%以内。PHS抑制剂对HeLa细胞中fec-12诱导的8-OHdG形成的特异性抑制表明该酶可能参与在细胞中“激活”fec-12以形成AOS。邻菲罗啉对细胞中fec-12诱导的8-OHdG形成的抑制表明细胞内铁作为该过程中催化剂的作用。