Catterall F S, Coombs M M, Ioannides C, Sepiol J J, Wilson J
Molecular Toxicology Group, School of Biological Sciences, University of Surrey, Guildford, GU2 7XH, Surrey, UK.
Mutat Res. 2001 May 31;492(1-2):7-11. doi: 10.1016/s1383-5718(01)00144-9.
The relative mutagenic potentials of 11-amino-16,17-dihydro-15H-cyclopenta[a]phenanthrene, its 17-keto derivative, and 2- and 5-aminochrysene have been compared in Salmonella typhimurium TA98 and TA100 in the presence of a postmitochondrial liver preparation from Aroclor 1254 induced rats. The 11-amino hydrocarbon is a very weak mutagen (0.27 revertants/nmol), whereas the 11-amino-17-ketone is much more active (129 revertants/nmol). 2-Aminochrysene is the most mutagenic arylamine ( approximately 500 revertants/nmol) among these compounds, but its 5-amino isomer is much less active (0.9 revertants/nmol). Possible reasons for these marked differences are suggested. Use of TA98 with over-expressing O-acetyltransferase (YG 1024) and deficient in this enzyme (TA98/l,8-DNP(6)) with the 11-amino-17-ketone and with 5-aminochrysene clearly indicates the importance of this enzyme in their bioactivation, implying oxidation of the amino group to the hydroxylamine in both these compounds.
在存在由Aroclor 1254诱导的大鼠的线粒体后肝匀浆的情况下，已在鼠伤寒沙门氏菌TA98和TA100中比较了11-氨基-16,17-二氢-15H-环戊[a]菲、其17-酮衍生物以及2-氨基和5-氨基 Chrysene的相对诱变潜力。11-氨基烃是一种非常弱的诱变剂（0.27回复突变体/纳摩尔），而11-氨基-17-酮则活性高得多（129回复突变体/纳摩尔）。在这些化合物中，2-氨基 Chrysene是最具诱变活性的芳胺（约500回复突变体/纳摩尔），但其5-氨基异构体的活性则低得多（0.9回复突变体/纳摩尔）。文中提出了这些显著差异的可能原因。将过表达O-乙酰转移酶（YG 1024）且缺乏该酶（TA98/1,8-DNP(6)）的TA98与11-氨基-17-酮和5-氨基 Chrysene一起使用，清楚地表明了该酶在它们生物活化中的重要性，这意味着这两种化合物中的氨基均被氧化为羟胺。
