Belhadj-Tahar Hafid, Adamczewski Nicolas, Nassar Bertrand, Coulais Yvon
Poison Control Center and Department of Toxicology, Purpan University Hospital Toulouse, France.
Acta Pharm. 2003 Jun;53(2):111-8.
In vitro toxic effects of sulfonylurea herbicides (thifensulfuron-methyl and metsulfuron-methyl) were evaluated according to a new protocol. Physiological conditions were reproduced in order to boost toxicovigilance. Sulfonylureas and their hydrolysis products were added to biological substrates such as urea, alanine, aspartic acid, alpha-ketoglutarate, oxaloacetate, pyruvate and then incubated with some specific enzymes. Addition of these sulfonylureas and their degradation products did not significantly change the enzymatic activity of the urease, aspartate-aminotransferase, glutamate dehydrogenase, malate dehydrogenase and lactate dehydrogenase. However, the acid hydrolysis products inhibited up to 95% of the activity of the alanine-aminotransferase at low concentrations (0.27 micromol L(-1)). Inhibition did not affect the mitochondrial aspartate-aminotransferase.
根据一项新方案评估了磺酰脲类除草剂(噻吩磺隆和甲磺隆)的体外毒性作用。为提高毒理学监测水平,模拟了生理条件。将磺酰脲类及其水解产物添加到尿素、丙氨酸、天冬氨酸、α-酮戊二酸、草酰乙酸、丙酮酸等生物底物中,然后与某些特定酶一起孵育。添加这些磺酰脲类及其降解产物并未显著改变脲酶、天冬氨酸转氨酶、谷氨酸脱氢酶、苹果酸脱氢酶和乳酸脱氢酶的酶活性。然而,在低浓度(0.27微摩尔/升)时,酸性水解产物对丙氨酸转氨酶活性的抑制率高达95%。这种抑制作用不影响线粒体天冬氨酸转氨酶。