Venegas W, Lasne C, Lowy R, Buisson J P, Chouroulinkov I
Mutat Res. 1985 Jul;157(1):53-62. doi: 10.1016/0165-1218(85)90049-7.
The mutagenic activities of 5 newly synthesized naphthofurans were analysed in two in vitro cytogenetic assays: the metaphase chromosomal aberration assay and the anaphase telophase bridge-fragment assay. Both assays were conducted using V79 Chinese hamster cells. The compounds included: 2-nitro-7-methoxynaphtho[2,1-b]furan (A), 2-nitro-8-methoxynaphtho[2,1-b]furan (B), 2-nitro-naphtho[2,1-b]furan (C), 2-nitro-7-bromonaphtho[2,1-b]furan (D) and 7-methoxynaphtho[2,1-b]furan (E). The cells were treated with 3 concentrations (0.1, 0.2 and 0.4 microgram/ml) of each compound, in the dose range already tested in studies on the mutagenic properties of the same compounds realised with other systems. The highest concentration, only, was used in the anaphase-telophase assay. In the first approach, compounds A, B and C were active while compounds D and E did not increase significantly the aberration frequency above that of the DMSO controls. The results were confirmed in the second approach. They demonstrated that the two studies were complementary. Based on their genotoxic activities, the 5 compounds were ranked in the following decreasing order of potency: A congruent to B much greater than C greater than D congruent to E congruent to DMSO; which is comparable to the ranking order obtained in different in vitro mutagenic and carcinogenic assays. All these activities are closely related to the highly specific molecular structure of each compound, particularly to the nature and position of the different substituents introduced on the skeleton.
在两项体外细胞遗传学试验中分析了5种新合成的萘并呋喃的诱变活性:中期染色体畸变试验和后期 - 末期桥 - 片段试验。两项试验均使用V79中国仓鼠细胞进行。这些化合物包括:2 - 硝基 - 7 - 甲氧基萘并[2,1 - b]呋喃(A)、2 - 硝基 - 8 - 甲氧基萘并[2,1 - b]呋喃(B)、2 - 硝基萘并[2,1 - b]呋喃(C)、2 - 硝基 - 7 - 溴萘并[2,1 - b]呋喃(D)和7 - 甲氧基萘并[2,1 - b]呋喃(E)。用每种化合物的3种浓度(0.1、0.2和0.4微克/毫升)处理细胞,该剂量范围已在使用其他系统对相同化合物的诱变性研究中进行过测试。仅在后期 - 末期试验中使用了最高浓度。在第一种方法中,化合物A、B和C具有活性,而化合物D和E未使畸变频率显著高于二甲基亚砜(DMSO)对照。这些结果在第二种方法中得到了证实。它们表明这两项研究是互补的。基于它们的遗传毒性活性,这5种化合物按效力从高到低排序如下:A等同于B远大于C大于D等同于E等同于DMSO;这与在不同的体外诱变和致癌试验中获得的排序顺序相当。所有这些活性都与每种化合物的高度特异性分子结构密切相关,特别是与引入骨架上的不同取代基的性质和位置有关。