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致癌和非致癌性硝基呋喃以及喂食这些化合物的大鼠尿液的致突变活性。

Mutagenic activity of carcinogenic and noncarcinogenic nitrofurans and of urine of rats fed these compounds.

作者信息

Wang C Y, Lee L H

出版信息

Chem Biol Interact. 1976 Sep;15(1):69-75. doi: 10.1016/0009-2797(76)90129-0.

Abstract

The nitrofurans, 2-(2-furyl)-3-(5-nitro-2-furyl)acrylamide (AF-2), N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide (FANFT), nitrofurantoin, 5-nitro-2-furoic acid, 5-nitro-2-furamidoxime, 5-nitrofurfurylidene diacetate and the urine of rats fed these compounds, were assayed for mutagenic activity in Salmonella typhimurium strains TA100 and TA100FR1. All the nitrofurans were mutagenic in the order: AF-2 and FANFT greater than nitrofurantoin greater than 5-nitro-2-furamidoxime greater than 5-nitrofurfurylidene diacetate greater than 5-nitro-2-furoic acid. Strain TA100 was more sensitive than TA100FR1 to the mutagenic influence of these nitrofurans. Only the urine of rats fed AF-2, FANFT and nitrofurantoin had mutagenic activity. Again, TA100 was more sensitive than TA100FR1. The mutagenicity of the urine was not increased by treatment with beta-glucuronidase. AF-2, 2-amino-4-(5-nitro-2-furyl)thiazole (deformylated product of FANFT) and nitrofurantoin were excreted in the urine of rats fed these compounds; whereas the other nitrofurans were not excreted.

摘要

对硝基呋喃类化合物,即2-(2-呋喃基)-3-(5-硝基-2-呋喃基)丙烯酰胺(AF-2)、N-[4-(5-硝基-2-呋喃基)-2-噻唑基]甲酰胺(FANFT)、呋喃妥因、5-硝基-2-呋喃甲酸、5-硝基-2-呋喃甲肟、5-硝基糠叉二乙酸酯以及喂食这些化合物的大鼠尿液,在鼠伤寒沙门氏菌TA100和TA100FR1菌株中检测其致突变活性。所有硝基呋喃类化合物的致突变活性顺序为:AF-2和FANFT>呋喃妥因>5-硝基-2-呋喃甲肟>5-硝基糠叉二乙酸酯>5-硝基-2-呋喃甲酸。TA100菌株比TA100FR1菌株对这些硝基呋喃类化合物的致突变影响更敏感。只有喂食AF-2、FANFT和呋喃妥因的大鼠尿液具有致突变活性。同样,TA100比TA100FR1更敏感。用β-葡萄糖醛酸酶处理后,尿液的致突变性并未增加。AF-2、2-氨基-4-(5-硝基-2-呋喃基)噻唑(FANFT的去甲酰化产物)和呋喃妥因在喂食这些化合物的大鼠尿液中排出;而其他硝基呋喃类化合物未排出。

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