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IC轴值差异小,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IC铀值分别为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“和4.1×10^-9mot/L;醚苯磺隆及其代谢产物抑制小麦ALS酶活性的IC铀分别为4.6×10^-9和5.3×10^-9mol/L,抑制菜豆ALS酶活性的IC铀分别为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。
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^-9 mol/L, respectively. The IC50 of 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.