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丙烯酸酯的生物转化。给大鼠投喂丙烯酸乙酯和丙烯酸丁酯后,其巯基尿酸的排泄及尿中羧酸谱的变化。

Biotransformation of acrylates. Excretion of mercapturic acids and changes in urinary carboxylic acid profile in rat dosed with ethyl and 1-butyl acrylate.

作者信息

Linhart I, Vosmanská M, Smejkal J

机构信息

National Institute of Public Health, Centre of Industrial Hygiene and Occupational Diseases, Prague, Czech Republic.

出版信息

Xenobiotica. 1994 Oct;24(10):1043-52. doi: 10.3109/00498259409043301.

Abstract
  1. The excretion of urinary metabolites was studied in rat dosed intraperitoneally with ethyl acrylate and 1-butyl acrylate. 2. Physiological carboxylic acids, namely, 3-hydroxypropanoic acid, lactic acid and acetic acid were determined by hplc and may be derived from the xenobiotic acrylates. 3. A significant increase in the amounts of 3-hydroxypropanoic acid and acetic acid excreted within 24 h after dosing was found in both the ethyl acrylate and 1-butyl acrylate-exposed rats. 4. A slight increase in the excretion of lactic acid (p < 0.10) was also found in animals exposed to ethyl and 1-butyl acrylates. 5. Two mercapturic acids, N-acetyl-S-(2-carboxyethyl)cysteine and the corresponding N-acetyl-S-[(2-alkoxycarbonyl)ethyl]cysteine were formed from both acrylate esters and were determined by glc. For ethyl acrylate the conversion to mercapturic acids amounted to 11% of the administered dose, whereas for 1-butyl acrylate the corresponding conjugates decreased from 3.6% to 0.5 mmol/kg to 1.6% at 3.0 mmol/kg. 6. Mercapturic acids appear to be potential biological markers of exposure to acrylate esters. However, more sensitive methods would be required for their determination than those available at present.
摘要
  1. 研究了大鼠腹腔注射丙烯酸乙酯和丙烯酸丁酯后尿代谢物的排泄情况。2. 通过高效液相色谱法测定了生理羧酸,即3-羟基丙酸、乳酸和乙酸,它们可能来源于外源性丙烯酸酯。3. 在暴露于丙烯酸乙酯和丙烯酸丁酯的大鼠中,给药后24小时内排泄的3-羟基丙酸和乙酸量均显著增加。4. 在暴露于丙烯酸乙酯和丙烯酸丁酯的动物中,乳酸排泄量也有轻微增加(p<0.10)。5. 两种硫醚氨酸,N-乙酰-S-(2-羧乙基)半胱氨酸和相应的N-乙酰-S-[(2-烷氧羰基)乙基]半胱氨酸由两种丙烯酸酯形成,并通过气相色谱法测定。对于丙烯酸乙酯,转化为硫醚氨酸的量相当于给药剂量的11%,而对于丙烯酸丁酯,相应的共轭物在3.6%至0.5 mmol/kg时从3.6%降至3.0 mmol/kg时的1.6%。6. 硫醚氨酸似乎是暴露于丙烯酸酯的潜在生物标志物。然而,测定它们需要比目前可用的方法更灵敏的方法。

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