title: Inhibitory Effects of Amorphigenin on the Mitochondrial Complex I of Culex pipiens pallens Coquillett (Diptera: Culicidae).
abstract: Previous studies in our laboratory found that the extract from seeds of Amorpha fruticosa in the Leguminosae family had lethal effects against mosquito larvae, and an insecticidal compound amorphigenin was isolated. In this study, the inhibitory effects of amorphigenin against the mitochondrial complex I of Culex pipiens pallens (Diptera: Culicidae) were investigated and compared with that of rotenone. The results showed that amorphigenin and rotenone can decrease the mitochondrial complex I activity both in vivo and in vitro as the in vivo IC50 values (the inhibitor concentrations leading to 50% of the enzyme activity lost) were determined to be 2.4329 and 2.5232 μmol/L, respectively, while the in vitro IC50 values were 2.8592 and 3.1375 μmol/L, respectively. Both amorphigenin and rotenone were shown to be reversible and mixed-I type inhibitors of the mitochondrial complex I of Cx. pipiens pallens, indicating that amorphigenin and rotenone inhibited the enzyme activity not only by binding with the free enzyme but also with the enzyme-substrate complex, and the values of KI and KIS for amorphigenin were determined to be 20.58 and 87.55 μM, respectively, while the values for rotenone were 14.04 and 69.23 μM, respectively.
authors: Department of Pesticide Science, College of Plant Protection, Shenyang Agricultural University, Shenyang 110866, China. jimingshan@syau.edu.cn.
authors: Mingshan
authors: M
authors: Ji
authors: Department of Pesticide Science, College of Plant Protection, Shenyang Agricultural University, Shenyang 110866, China. lyp628@syau.edu.cn.
authors: Yaping
authors: Y
authors: Liang
authors: Department of Pesticide Science, College of Plant Protection, Shenyang Agricultural University, Shenyang 110866, China. guzumin1212@163.com.
authors: Zumin
authors: Z
authors: Gu
authors: Department of Pesticide Science, College of Plant Protection, Shenyang Agricultural University, Shenyang 110866, China. xiuwei001@syau.edu.cn.
authors: Xiuwei
authors: X
authors: Li
mesh_terms: D000818:Animals; D003465:Culex / Q000187:drug effects / Q000201:enzymology*; D042967:Electron Transport Complex I / Q000378:metabolism*; D015971:Gene Expression Regulation, Enzymologic / Q000187:drug effects; D019476:Insect Proteins / Q000378:metabolism; D007306:Insecticides / Q000494:pharmacology*; D007814:Larva / Q000187:drug effects / Q000201:enzymology; D012402:Rotenone / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D019476:Insect Proteins; D007306:Insecticides; D012402:Rotenone; C049148:amorphigenin; D042967:Electron Transport Complex I
keywords: Culex pipiens pallens; amorphigenin; inhibitory mechanism; kinetics; mitochondrial complex I