Kayukawa Takumi, Furuta Kenjiro, Yonesu Kiyoaki, Okabe Takayoshi
Institute of Agrobiological Sciences National Agriculture and Food Research Organization, Ohwashi 1-2, Tsukuba, Ibaraki 305-8634, Japan.
Drug Discovery Initiative, The University of Tokyo, Hongo 7-3-1, Bunkyo-ku, Tokyo 113-0033, Japan.
J Pestic Sci. 2021 Feb 20;46(1):53-59. doi: 10.1584/jpestics.D20-070.
Juvenile hormone (JH) is an insect-specific hormone that regulates molting and metamorphosis. Hence, JH signaling inhibitors (JHSIs) and activators (JHSAs) can be used as effective insect growth regulators (IGRs) for pest management. In our previous study, we established a high-throughput screening (HTS) system for exploration of novel JHSIs and JHSAs using a cell line (BmN_JF&AR cells) and succeeded in identifying novel JHSIs from a chemical library. Here, we searched for novel JHSAs using this system. The four-step HTS yielded 10 compounds as candidate JHSAs; some of these compounds showed novel basic structures, whereas the others were composed of a 4-phenoxyphenoxymethyl skeleton, the basic structure of several existing JH analogs (pyriproxyfen and fenoxycarb). Topical application of seven compounds to larvae significantly prolonged the larval period, suggesting that the identified JHSAs may be promising IGRs targeting the JH signaling pathway.
保幼激素（JH）是一种昆虫特有的激素，可调节蜕皮和变态。因此，保幼激素信号抑制剂（JHSIs）和激活剂（JHSAs）可作为有效的昆虫生长调节剂（IGRs）用于害虫治理。在我们之前的研究中，我们建立了一种高通量筛选（HTS）系统，用于利用细胞系（BmN_JF&AR细胞）探索新型JHSIs和JHSAs，并成功从化学文库中鉴定出新型JHSIs。在此，我们使用该系统寻找新型JHSAs。四步高通量筛选产生了10种化合物作为候选JHSAs；其中一些化合物具有新颖的基本结构，而其他化合物则由4-苯氧基苯氧基甲基骨架组成，这是几种现有保幼激素类似物（吡丙醚和苯氧威）的基本结构。将7种化合物局部应用于幼虫显著延长了幼虫期，表明所鉴定的JHSAs可能是靶向保幼激素信号通路的有前景的昆虫生长调节剂。
