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首页> 外文期刊>Journal of biochemical and molecular toxicology >In vivo antigenotoxic potential and possible mechanism of action of selected 4-hydroxy-2H-chromen-2-one derivatives
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In vivo antigenotoxic potential and possible mechanism of action of selected 4-hydroxy-2H-chromen-2-one derivatives

机译:选定的4-羟基-2H-铬2-2-酮衍生物的体内抗原毒性潜力和可能的作用机理

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The in vivo sex-linked recessive lethal test was carried out in Drosophila melanogaster to investigate whether or not five substituted 4-hydroxy-2H-chromen-2-ones can modulate the genotoxicity of the well-established mutagenic agent ethyl methanesulfonate (EMS). For this purpose, 3 days old Canton S males were treated with the potent mutagen EMS alone in concentration of 0.75 ppm, as well as in combination with one of the five 4-hydroxycoumarins, namely diethyl 2-(1-(4-hydroxy-2-oxo-2H-chromen-3-yl)ethylidene)malonate (2b), 3-(1-(4-hydroxy-2-oxo-2H-chromen-3-yl)ethylidene)pentane-2,4-dione (6b), 4-(4-(4-hydroxy-2-oxo-2H-chromen-3-yl)thiazol-2-ylamino) benzenesulfonic acid (4c), 4-hydroxy-3-(2-(2-nitropheny lamino)thiazol-4-yl)-2H-chromen-2-one (9c), and (E)-4-hydroxy-3-(1-(m-tolylimino)ethyl)-2H-chromen-2-one (5d), in concentration of 70 ppm. The frequency of germinative mutations increased significantly after the treatment with EMS and decreased after treatments with coumarins. The maximum reduction was observed after treatments with 2b, 6b, 4c, and 5d. By the formation of hydrogen bonds or electrostatic interactions with O 6 of DNA guanine, tested coumarins prevent EMS-induced alkylation. The results indicate a protective role of five 4-hydroxycoumarins under the action of a strong mutagen.
机译:在果蝇中进行了体内性相关的隐性致死性试验,以研究五个取代的4-羟基-2H-铬-2-酮是否可以调节成熟的诱变剂甲磺酸乙酯(EMS)的遗传毒性。为此,对3天大的Canton S雄性单独用浓度为0.75 ppm的强力诱变剂EMS处理,并与5种4-羟基香豆素之一,即2-(2-(1-(4-羟基- 2-氧代-2H-铬-3-基)亚乙基)丙二酸酯(2b),3-(1-(4-羟基-2-氧代2H-铬-3-基)亚乙基)戊烷-2,4-二酮(6b),4-(4-(4-羟基-2-氧代-2H-铬-3-基)噻唑-2-基氨基)苯磺酸(4c),4-羟基-3-(2-(2-硝基苯氨基)噻唑-4-基)-2H-铬-2-(9c)和(E)-4-羟基-3-(1-(间甲苯基)乙基)-2H-铬-2- (5d),浓度为70ppm。 EMS处理后,萌发突变的频率显着增加,而香豆素处理后,萌发突变的频率降低。用2b,6b,4c和5d处理后观察到最大减少。通过形成氢键或与DNA鸟嘌呤的O 6发生静电相互作用,经测试的香豆素可防止EMS诱导的烷基化。结果表明五种4-羟基香豆素在强诱变剂的作用下具有保护作用。

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