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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。
The metabolism of the sulfonylurea herbicides, chlorsulfuron and triasulfuron, was investigated using wheat cytochrome P450 cDNA (CYP71C6v1) heterologously expressed in yeast cells. The results showed that the metabolites 5-hydroxy-chlorsulfuron and 5-hydroxy-ether-tribenuron were able to inhibit the activity of acetolactate synthase (ALSase), and the metabolites and the parent compounds chlorsulfuron and ethametsulfuron- The differences in IC50 values were small, but metabolites did not show activity when stems and leaves sprayed wheat and kidney bean. The IC50 values of chlorpyrifos and its metabolites inhibiting ALS activity in wheat were 7.1 × 10-9 and 7.9 × 10-9mol / L, respectively. The IC50 of ALS activity in wheat was 3.6 × 10-9 and 4.1 × 10- The IC50 of triasulfuron and its metabolites against wheat ALS was 4.6 × 10-9 and 5.3 × 10-9mol / L, respectively, and the IC50 of inhibition of ALSase activity in L. vulgaris was 4.7 × 10-9 and 4.9 × 10-9mol / L. The results show that in the sulfonylurea molecular structure of the benzene ring 5, it is possible to obtain highly active compounds.