Quillardet P, Jenek J, Demerseman P, Royer R, Hofnung M
Mutat Res. 1986 Dec;172(3):223-30. doi: 10.1016/0165-1218(86)90059-5.
We measured the genotoxic activities in two bacterial tests, the Salmonella/histidine assay (a reverse mutation assay) and the SOS Chromotest (an assay for SOS induction in E. coli), of two pairs of isomeric furan analogues of benzo[a]pyrene: pyreno[1,2-b]furan (R7490) and pyreno[2,1-b]furan (R7692) and their 2-nitro derivatives, 8-nitro-pyreno[1,2-b]furan (R7489) and 8-nitro-pyreno[2,1-b]furan (R7691). We found that: For all 4 compounds, the responses were correlated in the two tests. For the 2-nitro derivatives, R7489 and R7691, the responses were extremely high, reaching SOS-inducing potencies of 5.2 X 10(3) and 10(5)/nmole in the SOS Chromotest and mutagenic potencies of 6.3 X 10(4) and 3.7 X 10(7) revertants/nmole in the Salmonella/histidine assay (strain TA98), respectively; the responses were only slightly decreased in nitroreductase-deficient strains. The responses to the two pyrenofurans were increased in the presence of an "activating mixture" but were still lower than that to benzo[a]pyrene. In contrast to benzo[a]pyrene and pyreno[2,1-b]furan (R7692), pyreno[1,2-b]furan (R7490) also gave a response in the absence of an "activating mixture". (5) Compounds with the oxygen heteroatom within the "bay region" gave lower responses than their isomers with the oxygen heteroatom outside the "bay region".
我们在两种细菌试验中测定了两对苯并[a]芘的异构呋喃类似物的遗传毒性活性，即沙门氏菌/组氨酸试验（一种回复突变试验）和SOS色变试验（一种检测大肠杆菌中SOS诱导的试验）：芘并[1,2 - b]呋喃（R7490）和芘并[2,1 - b]呋喃（R7692）及其2 - 硝基衍生物，8 - 硝基 - 芘并[1,2 - b]呋喃（R7489）和8 - 硝基 - 芘并[2,1 - b]呋喃（R7691）。我们发现：对于所有4种化合物，两种试验中的反应具有相关性。对于2 - 硝基衍生物R7489和R7691，反应极高，在SOS色变试验中诱导SOS的效力分别达到5.2×10³和10⁵/纳摩尔，在沙门氏菌/组氨酸试验（菌株TA98）中的诱变效力分别达到6.3×10⁴和3.7×10⁷回复体/纳摩尔；在缺乏硝基还原酶的菌株中，反应仅略有降低。在存在“活化混合物”的情况下，对两种芘并呋喃的反应有所增加，但仍低于对苯并[a]芘的反应。与苯并[a]芘和芘并[2,1 - b]呋喃（R7692）不同，芘并[1,2 - b]呋喃（R7490）在没有“活化混合物”的情况下也有反应。（5）在“湾区”内含有氧杂原子的化合物的反应比其在“湾区”外含有氧杂原子的异构体的反应低。
