Respiratory Inhibition of Acaricide AKD-2023 and Its Deacetyl Metabolite
Respiratory Inhibition of Acaricide AKD-2023 and Its Deacetyl Metabolite
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DOI：
10.1584/jpestics.23.18
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发表时间：
1998
影响因子：
2.4
通讯作者：
Y. Koura;S. Kinoshita;K. Takasuka;S. Koura;Osaki Norio;S. Matsumoto;H. Miyoshi
中科院分区：
文献类型：
--
作者：
Y. Koura;S. Kinoshita;K. Takasuka;S. Koura;Osaki Norio;S. Matsumoto;H. Miyoshi
为确定新型杀螨剂AKD - 2023（2 - 乙酰氧基 - 3 - 正十二烷基 - 1,4 - 萘醌）及其代谢产物DHN（2 - 羟基 - 3 - 正十二烷基 - 1,4 - 萘醌）的杀螨机制，研究了这些化合物对从家蝇中分离出的飞行肌线粒体呼吸的影响。AKD - 2023对琥珀酸和丙酮酸氧化活性的抑制效力远低于DHN。这一结果表明，水解代谢产物DHN实际上具有生物活性，可抑制线粒体呼吸。还证实抑制作用发生在线粒体电子传递链的复合物III处。根据细胞色素b和c1的还原动力学，结合位点显示为复合物III的泛醇氧化位点（Q0中心），这与近期开发的其他杀螨剂不同。
To define acaricidal mechanism of a new acaricidal AKD-2023 (2-acetoxy-3-n-dodecyl-1,4-naphthoquinone) and its metabolite, DHN (2-hydroxy-3-n-dodecyl-1,4-naphthoquinone), the effects of these compounds on the respiration of flight-muscle mitochondria isolated from house flies were investigated. The inhibitory potency of AKD-2023 for succinate and pyruvate oxidation activity was much less than that of DHN. This result suggested that the hydrolyzed metabolite, DHN is virtually biologically active and inhibits the respiration of mitochondria. It was also proved that the inhibition occurs at the complex III in mitochondrial electron transfer chain. On the basis of reduction kinetics of cytochromes b and c 1 , the binding site was shown to be ubiquinol oxidation site (Q 0 center) of complex III, being different from that of other acaricides developed recently.