绿磺隆、醚苯磺隆及其体外代谢物对乙酰乳酸合成酶的离体抑制作用
Inhibition of Acetolactate Synthase Activity by Chlorsulfuron, Triasulfuron and Their Metabolites in vitro
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摘要: 利用异源表达于酵母细胞中的小麦细胞色素P450cDNA(CYP71C6v1)研究了磺酰脲类除草剂绿磺隆、醚苯磺隆的代谢作用。结果表明,代谢产物5-羟基绿磺隆和5-羟基醚苯磺隆能够抑制乙酰乳酸合成酶(ALS酶)活性,且代谢产物与母体化合物绿磺隆、醚苯磺隆抑制ALS酶活性的IC50值差异小,但是代谢产物在茎叶喷雾小麦和菜豆时,均未表现出活性。绿磺隆及其代谢产物抑制小麦ALS酶活性的IC50值分别为7.1×10-9和7.9×10-9mol/L,抑制菜豆ALS酶活性的IC50分别为3.6×10-9和4.1×10-9mol/L;醚苯磺隆及其代谢产物抑制小麦ALS酶活性的IC50分别为4.6×10-9和5.3×10-9mol/L,抑制菜豆ALS酶活性的IC50分别为4.7×10-9和4.9×10-9mol/L。结果表明,在磺酰脲类分子苯环5位上进行结构改造,有可能得到高活性的化合物。Abstract: The metabolism of two sulfonylurea herbicides chlorsulfuron and triasulfuron was investigated by using wheat cytochrome P450 cDNA(CYP71C6v1) which expressed in yeast.The results showed that chlorsulfuron and triasulfuron were hydroxylated at 5-position on the phenyl ring.The difference in IC50 of parent compound and 5-hydroxy metabolites to acetolactate synthase(ALS) was small.However,their metabolites injured neither wheat nor bean,when applied as post-emergence treatment.The IC50 of chlorsulfuron and its metabolites to wheat ALS were 7.1×10-9 and 7.9×10-9 mol/L,respectively,and to bean ALS were 3.6×10-9 and 4.1×10-9mol/L,respectively.The IC50of triasulfuron and its metabolites to wheat ALS were 4.6×10-9 and 5.3×10-9 mol/L,respectively,and to bean ALS were 4.7×10-9 and 4.9×10-9 mol/L,respectively.These results suggested that proper groups at 5-position on phenyl ring of sulfonylurea molecule might possess high herbicidal activity.
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