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昆虫激素激动剂的设计、合成及生物学评价

Design, synthesis, and biological evaluation of insect hormone agonists.

作者信息

Yokoi Taiyo

机构信息

Sagami Chemical Research Institute.

出版信息

J Pestic Sci. 2024 Nov 20;49(4):303-310. doi: 10.1584/jpestics.J24-02.

DOI:10.1584/jpestics.J24-02
PMID:39877879
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11770153/
Abstract

Agonists of insect hormones, namely molting hormone (MH) and juvenile hormone (JH), disrupt the normal growth of insects and can be employed as insecticides that are harmless to vertebrates. In this study, a series of experiments and computational analyses were conducted to rationally design novel insect hormone agonists. Syntheses and quantitative structure-activity relationship (QSAR) analyses of two MH agonist chemotypes, imidazothiadiazoles and tetrahydroquinolines, revealed that the structural factors important for the ligand-receptor interactions are significantly different between these chemotypes. On the other hand, a virtual screening cascade combining ligand- and structure-based methods identified a piperazine derivative as a novel JH agonist. The results obtained in this study will be useful for the future development of novel insect growth regulators.

摘要

昆虫激素的激动剂，即蜕皮激素（MH）和保幼激素（JH），会干扰昆虫的正常生长，并且可以用作对脊椎动物无害的杀虫剂。在本研究中，进行了一系列实验和计算分析，以合理设计新型昆虫激素激动剂。对两种MH激动剂化学类型，即咪唑并噻二唑和四氢喹啉的合成及定量构效关系（QSAR）分析表明，这些化学类型之间对于配体-受体相互作用重要的结构因素存在显著差异。另一方面，结合基于配体和基于结构方法的虚拟筛选级联鉴定出一种哌嗪衍生物作为新型JH激动剂。本研究获得的结果将有助于新型昆虫生长调节剂的未来开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/da054614101b/jps-49-4-J24-02-figure05.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/af93129ba0e1/jps-49-4-J24-02-figure01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/ac9eb05e5d18/jps-49-4-J24-02-figure02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/38972c7c5288/jps-49-4-J24-02-Eg01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/9c554840b6e4/jps-49-4-J24-02-figure03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/dc9f2d967462/jps-49-4-J24-02-Eg02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/9ee61c021722/jps-49-4-J24-02-Eg03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/a46bf1368214/jps-49-4-J24-02-figure04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/da054614101b/jps-49-4-J24-02-figure05.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/af93129ba0e1/jps-49-4-J24-02-figure01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/ac9eb05e5d18/jps-49-4-J24-02-figure02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/38972c7c5288/jps-49-4-J24-02-Eg01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/9c554840b6e4/jps-49-4-J24-02-figure03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/dc9f2d967462/jps-49-4-J24-02-Eg02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/9ee61c021722/jps-49-4-J24-02-Eg03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/a46bf1368214/jps-49-4-J24-02-figure04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45eb/11770153/da054614101b/jps-49-4-J24-02-figure05.jpg

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本文引用的文献

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A luciferase reporter assay for ecdysone agonists using HEK293T cells.使用 HEK293T 细胞的蜕皮激素激动剂荧光素酶报告基因检测法。
Biosci Biotechnol Biochem. 2022 Oct 20;86(11):1490-1496. doi: 10.1093/bbb/zbac139.
2
Detection of juvenile hormone agonists by a new reporter gene assay using yeast expressing Drosophila methoprene-tolerant.利用表达果蝇对保幼激素耐受的酵母的新报告基因检测法检测保幼激素激动剂。
FEBS Open Bio. 2021 Oct;11(10):2774-2783. doi: 10.1002/2211-5463.13277. Epub 2021 Aug 30.
3
A Commercial Extract of Roots as a Source of Unusual Ecdysteroid Derivatives with Insect Hormone Receptor Binding Activity.
一种根的商业提取物，作为具有昆虫激素受体结合活性的不寻常蜕皮甾体衍生物的来源。
J Nat Prod. 2021 Jul 23;84(7):1870-1881. doi: 10.1021/acs.jnatprod.0c01274. Epub 2021 Jun 18.
4
Juvenile hormone III skipped bisepoxide is widespread in true bugs (Hemiptera: Heteroptera).保幼激素III双环氧物在半翅目（异翅亚目）昆虫中广泛存在。
R Soc Open Sci. 2021 Feb 3;8(2):202242. doi: 10.1098/rsos.202242.
5
Receptor-binding affinity and larvicidal activity of tetrahydroquinoline-type ecdysone agonists against .四氢喹啉型蜕皮激素激动剂对……的受体结合亲和力及杀幼虫活性
J Pestic Sci. 2021 Feb 20;46(1):101-108. doi: 10.1584/jpestics.D20-089.
6
Nonsteroidal ecdysone receptor agonists use a water channel for binding to the ecdysone receptor complex EcR/USP.非甾体蜕皮激素受体激动剂利用一个水通道与蜕皮激素受体复合物EcR/USP结合。
J Pestic Sci. 2021 Feb 20;46(1):88-100. doi: 10.1584/jpestics.D20-095.
7
Virtual screening identifies a novel piperazine-based insect juvenile hormone agonist.虚拟筛选鉴定出一种新型的基于哌嗪的昆虫保幼激素激动剂。
J Pestic Sci. 2021 Feb 20;46(1):68-74. doi: 10.1584/jpestics.D20-074.
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Identification of novel juvenile-hormone signaling activators high-throughput screening with a chemical library.利用化学文库进行高通量筛选以鉴定新型保幼激素信号激活剂。
J Pestic Sci. 2021 Feb 20;46(1):53-59. doi: 10.1584/jpestics.D20-070.
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Reporter gene assays for screening and identification of novel molting hormone- and juvenile hormone-like chemicals.用于筛选和鉴定新型蜕皮激素和保幼激素样化学物质的报告基因检测法。
J Pestic Sci. 2021 Feb 20;46(1):29-42. doi: 10.1584/jpestics.D20-079.
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Transcription-inducing activity of natural and synthetic juvenile hormone agonists through the Drosophila Methoprene-tolerant protein.通过果蝇保幼激素耐受蛋白对天然和合成保幼激素激动剂的转录诱导活性。
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