共查询到20条相似文献，搜索用时 45 毫秒
1.
Taiyo Yokoi Taku Nabe Shinri Horoiwa Ken&#x;ichiro Hayashi Sayoko Ito-Harashima Takashi Yagi Yoshiaki Nakagawa Hisashi Miyagawa 《Journal of Pesticide Science》2021,46(1):68
Juvenile hormone (JH) agonists constitute a subclass of insect growth regulators and play important roles in insect pest management. In this work, a multi-step virtual screening program was executed to find novel JH agonists. A database of 5 million purchasable compounds was sequentially processed with three computational filters: (i) shape and chemical similarity as compared to known JH-active compounds; (ii) molecular docking simulations against a Drosophila JH receptor, methoprene-tolerant; and (iii) free energy calculation of ligand–receptor binding using a modified MM/PBSA (molecular mechanics/Poisson–Boltzmann surface area) protocol. The 11 candidates that passed the three filters were evaluated in a luciferase reporter assay, leading to the identification of a hit compound that contains a piperazine ring system (EC50=870 nM). This compound is structurally dissimilar to known JH agonists and synthetically easy to access; therefore, it is a promising starting point for further structure optimization. 相似文献
2.
Shouya Naruse Mayuko Ogino Takao Nakagawa Yoko Yasuno Akiya Jouraku Takahiro Shiotsuki Tetsuro Shinada Ken Miura Chieka Minakuchi 《Journal of Pesticide Science》2021,46(1):60
Insect juvenile hormone (JH) mimics (JHMs) are known to have ovicidal effects if applied to adult females or eggs. Here, we examined the effects of exogenous JHMs on embryonic development of the bean bug, Riptortus pedestris. The expression profiles of JH early response genes and JH biosynthetic enzymes indicated that JH titer was low for the first 3 days of the egg stage and increased thereafter. Application of JH III skipped bisepoxide (JHSB3) or JHM on Day 0 eggs when JH titer was low caused reduced hatchability, and the embryos mainly arrested in mid- or late embryonic stage. Application of JHMs on Day 5 eggs also resulted in an arrest, but this was less effective compared with Day 0 treatment. Interestingly, ovicidal activity of synthetic JHMs was much lower than that of JHSB3. This study will contribute to developing novel insecticides that are selective among insect species. 相似文献
3.
Insect growth regulators (IGRs) have been proposed as agents for the control of insect pests. These compounds disrupt the normal development of insects by mimicking juvenile hormone and the molting hormone, 20-hydroxyecdsyone, or by interfering with chitin synthesis. The effectiveness and selectivity of IGRs provide new tools for integrated pest management. The simultaneous advances in the chemistry of IGRs and the ability to study insect tissues in culture, have led to research on the mode of action of IGRs in vitro. Plodia interpunctella and Spodoptera frugiperda have been used to examine the effects of IGRs on wing imaginal discs in organ culture, as well as in hormonally responsive cell lines established from wing imaginal discs of these species. Our research has focused on the action of ecdysteroid mimics, chitin synthesis inhibitors and juvenile hormone mimics. The effects of the IGRs on chitin synthesis, uptake of amino-sugars, and cellular proliferation were studied in tissue culture. The results demonstrate the effectiveness of using organ cultures and hormonally responsive cell lines for investigating IGRs at the cellular and tissue level. © 1998 Society of Chemical Industry 相似文献
4.
5.
Marek Jindra 《Journal of Pesticide Science》2021,46(1):3
Insect Growth Regulators (IGRs) represent advanced, bio-rational insecticides. This Special Issue reflects progress in IGR development that has been enabled by insight into the molecular principles of biosynthetic or hormone signaling pathways. The unifying principle is aiming at processes and molecular targets that are unique to arthropods and ideally to narrower insect taxa representing pests or disease vectors. While some strategies of obtaining the desired compounds for chemical intervention rely on rational, structure-based design or computational power, others exploit technologies allowing automated, high-throughput screening of large chemical libraries. All avenues leading to selective and environmentally safe pest control are valid as we face the imminent threat of the declining world insect population. 相似文献
6.
保幼激素(juvenile hormone, JH)是由咽侧体分泌的倍半萜类化合物,可以调控昆虫的很多生理过程,如发育、变态、生殖等。作为bHLH-PAS(helix-loop-helix-Per-ARNT-Sim)转录因子家族成员之一的methoprene-tolerant (Met)是JH的受体,在JH的信号传导过程中有非常重要的作用。本研究通过实时荧光定量PCR结合RNAi技术测定了沉默Met基因后黏虫Mythimna separata的Vg基因表达、卵巢发育和生殖行为,旨在探究Met基因在黏虫生殖过程中的功能。结果表明当Met基因沉默后,与卵巢发育密切相关的卵黄原蛋白(vitellogenin, Vg)基因表达量下调了50%,从而显著抑制了卵巢发育,并导致产卵显著延迟、产卵历期显著缩短,产卵量显著下降。结果表明Met基因是黏虫生殖发育过程中的关键受体基因,它通过调节后续Vg的表达和沉积,来达到控制卵巢发育,从而调控生殖作用。 相似文献
7.
BACKGROUND: One of the most studied actions of juvenile hormone (JH) is its ability to modulate ecdysteroid signaling during insect development and metamorphosis. Previous studies in mosquitoes showed that 20‐hydroxyecdysone (20E) regulates vitellogenin synthesis. However, the action of JH and its mimics, e.g. methoprene, on female reproduction of mosquitoes remains unknown. RESULTS: Here, a major malaria vector, Anopheles gambiae Giles, was used as a model insect to study the action of methoprene on female reproduction. Ecdysteroid titers and expression profiles of ecdysone‐regulated genes were determined before and after a blood meal. An ecdysteroid peak was detected at 12 h post blood meal (PBM). The maximum expression of ecdysone‐regulated genes, such as ecdysone receptor (EcR), hormone receptor 3 (HR3) and vitellogenin (Vg) gene, coincided with the ecdysteroid peak. Interestingly, topical application of methoprene at 6 h PBM delayed ovarian development and egg maturation by suppressing the expression of ecdysone‐regulated genes in female mosquitoes. CONCLUSION: The data suggest that ecdysteroid titers are correlated with Vg synthesis, and methoprene affects vitellogenesis by modulating ecdysteroid action in A. gambiae. Copyright © 2010 Society of Chemical Industry 相似文献
8.
The efficacy of juvenile hormone III (JH III) and two JH-mimicking compounds was compared in laboratory experiments with Reticulitermes lucifugus (Rossi), R. santonensis Feytaud and R. virginicus (Banks). Induction of presoldier, soldier and/or soldier-worker intercaste differentiation was taken as positive response to the treatment. The novel juvenogen, a fatty acid ester of a juvenoid alcohol, induced greatest soldier differentiation in all species tested, followed by hydroprene. JH III was less effective. Representatives of three Reticulitermes species showed similar trends in soldier induction rates. Differences in mortality in treatments of termites of the same species from different colonies with the same compound were observed and evidently were caused by differences in the conditions of respective colonies. 相似文献
9.
Arash Zibaee Ali Reza BandaniDavide Malagoli 《Pesticide biochemistry and physiology》2012,102(1):30-37
Effects of the two insect growth regulators (IGRs) methoxyfenozide, 20-hydroxyecdysone (20E) agonist, and pyriproxifen, Juvenile hormone (JH) agonist, were examined on the cellular immune responses of the Sunn pest, Eurygaster integriceps versus the entomopathogenic fungus Beauveria bassiana. The simultaneous treatment with the IGRs and the fungal spores altered haemocyte count (total and differentiate), nodulation response and phenoloxidase (PO) activity in a dose- and time-dependent manner. It was observed that different concentrations of methoxyfenozide increased total and differentiate haemocyte numbers as well as B. bassiana-induced nodulation response. In contrast with the JH agonist, pyriproxifen significantly decreased total and differentiate haemocyte numbers and inhibited nodule formation in E. integriceps adults. The 20E agonist displayed major effects when injected at the doses 2.79 and 5.59 μg/mg adult. In contrast, injecting adults by pyriproxifen significantly impaired their ability to raise an efficacious response against the fungal spores. The ability of the two IGR analogues to interfere with activity of the PO system in haemolymph of E. integriceps adults was also investigated 6 h after injection by fungal spores. Methoxyfenozide had an excitatory effect on PO activity when the 5.59 μg/mg concentration was used against adults. Conversely, pyriproxifen had an inhibitory effect on PO activity when used at 1.49 μg/mg adult concentration. These findings demonstrate that pyriproxifen may interfere with cell-mediated immunity of E. integriceps. So, pyriproxifen could be a good candidate for the integrated control of the Sunn pest. 相似文献
10.
William S. Bowers Gopalan C. Unnithan Jun-Ichi Fukushima Jun Toda Takeyoshi Sugiyama 《Pest management science》1995,43(1):1-11
Twenty-one synthetic compounds, containing one or more furan rings, were demonstrated to possess anti-juvenile hormone (AJH) activity as evidenced by their induction of premature metamorphosis in the milkweed bug, Oncopeltus fasciatus (Dallas) by contact, topical application or fumigation. The ED50 of the four most active analogs required to induce precocious metamorphosis from 3rd-instar nymphs by residue contact in a Petri dish compared favorably with that of precocene II (6,7-dimethoxy-2,2-dimethyl 2H-chromene) a naturally occurring phytochemical AJH. Precocious metamorphosis was fully reversible by co-treatment with juvenile hormone (JH III) or JH analogs, demonstrating that the observed AJH activity resulted from an induced deficiency of juvenile hormone. 相似文献
11.
Kotaro Koiwai Kana Morohashi Kazue Inaba Kana Ebihara Hirotatsu Kojima Takayoshi Okabe Ryunosuke Yoshino Takatsugu Hirokawa Taiki Nampo Yuuta Fujikawa Hideshi Inoue Fumiaki Yumoto Toshiya Senda Ryusuke Niwa 《Journal of Pesticide Science》2021,46(1):75
Insect growth regulators (IGRs) can be developed by elucidating the molecular mechanisms of insect-specific biological events. Because insect molting, and metamorphosis are controlled by ecdysteroids, their biosynthetic pathways can serve as targets for IGR development. The glutathione S-transferase Noppera-bo (Nobo), which is conserved in dipteran and lepidopteran species, plays an essential role in ecdysteroid biosynthesis. Our previous study using 17β-estradiol as a molecular probe revealed that Asp113 of Drosophila melanogaster Nobo (DmNobo) is essential for its biological function. However, to develop IGRs with a greater Nobo inhibitory activity than 17β-estradiol, further structural information is warranted. Here, we report five novel non-steroidal DmNobo inhibitors. Analysis of crystal structures of complexes revealed that DmNobo binds these inhibitors in an Asp113-independent manner. Among amino acid residues at the substrate-recognition site, conformation of conserved Phe39 was dynamically altered upon inhibitor binding. Therefore, these inhibitors can serve as seed compounds for IGR development. 相似文献
12.
Gopalan C. Unnithan John F. Andersen Tomomi Hisano Eiichi Kuwano Ren Feyereisen 《Pest management science》1995,43(1):13-19
Seventeen substituted imidazoles were tested as inhibitors of juvenile hormone (JH) III synthesis by cockroach corpora allata in an in-vitro radio-chemical assay. Most of these 1,5-disubstituted imidazoles were highly potent, with IC50 values of less than 100nM. The compounds differed in their ability to cause an accumulation of the precursor methyl farnesoate in the glands. Four of the imidazoles were tested by topical application to previtellogenic adult females, and all caused a significant inhibition of JH synthesis and an accumulation of intraglandular methyl farnesoate for at least three days after treatment. Methyl farnesoate epoxidase activity of homogenates of corpora allata was inhibited by the compounds TH -14 and TH -27. This P450-dependent epoxidase activity was inhibited at less than 10 nM. The results show that the 1,5-disubstituted imidazoles are powerful inhibitors of the last step of juvenile synthesis in this cockroach. 相似文献
13.
多杀菌素对小菜蛾体内多功能氧化酶和保幼激素酯酶活力的影响 总被引：1，自引：3，他引：1
采用生化分析方法,测定了不同浓度多杀菌素(spinosad)处理后小菜蛾体内多功能氧化酶(mixed-function oxidases/,MFO s)和保幼激素酯酶(juvenile hormone esterase,JHE)的活性,分析了酶活性的变化动态。结果表明,小菜蛾体内MFO s和JHE活性变化趋势受多杀菌素浓度影响。用LC50浓度处理后其保幼激素滴度变化趋势与对照相似,用LC80浓度处理后保幼激素滴度降低,并且滴度高峰出现时间比对照有所提前。不同浓度多杀菌素对氧化酶O-脱甲基活力的影响具有时间效应,用LC20浓度处理后的活力曲线上升拐点出现在24h,LC50浓度处理的则出现在12h。除LC80浓度处理在36h时活力值高于对照外,多杀菌素各处理都能抑制氧化酶N-脱甲基活力。高剂量(LC50、LC80)作用后小菜蛾体内保幼激素降解率与氧化酶N-或O-脱甲基活力有相似的变化趋势。 相似文献
14.
15.
Pesticide-induced hormesis may be an alternative mechanism for pest resurgence which is a serious problem in agriculture. Confirmation of the general phenomenon of hormesis may have significant implications for the design of pest control strategies and pest resistance management practices, although this has proved difficult due to the lack of appropriate methodology and the absence of well-defined mechanisms to support the experimental observations. In this study, a model-based approach to describe a dose-response relationship incorporating the hormetic effect was applied to the detection and estimation of imidacloprid-induced hormesis in the green peach aphid, Myzus persicae (Sulzer). The results indicated that imidacloprid at low concentrations induced stimulation of fecundity, however, high concentrations inhibition. This was reflected in an inverted U-shaped curve and related to the change of juvenile hormone III (JH III) levels in M. persicae. Fitting the data with quadratic and Weibull functions, which included a parameter for hormesis, showed that the magnitude of the hormetic effect was 31.31% for fecundity and 32.21% for JH III levels. The presence of hormesis in fecundity induced by imidacloprid may be related to the change in JH III levels in M. persicae. 相似文献
16.
Bruce D. Hammock Yehia A.I. Abdel-Aal Christopher A. Mullin Terry N. Hanzlik Richard M. Roe 《Pesticide biochemistry and physiology》1984,22(2):209-223
A series of 27 substituted thio-1,1,1-trifluoropropanones was synthesized by reacting the corresponding thiol with 1,1,1-trifluoro-3-bromopropanone. The resulting sulfides were screened as inhibitors of hemolymph juvenile hormone esterase and α-naphthyl acetate esterase activity of the cabbage looper, Trichoplusia ni, electric eel acetylcholinesterase, bovine trypsin, and bovine α-chymotrypsin. The presence of the sulfide bond increased the inhibitory potency on all of the enzymes tested when compared with compounds lacking the sulfide. In general, the compounds proved to be poor inhibitors of chymotrypsin and moderate inhibitors of trypsin. By varying the substituent on the sulfide, good inhibitory activity was obtained on α-naphthyl acetate esterase, acetylcholinesterase, while some of the compounds proved to be extremely powerful inhibitors of juvenile hormone esterase. The most powerful inhibitor tested was 3-octylthio-1,1,1-trifluoro-2-propanone, with an I50 of 2.3 × 10?9M on JH esterase. This compound showed a molar refractivity similar to that of the JH II backbone, was not toxic to T. ni, and was moderately toxic to mice, with a 48-hr LD50 of >750 mg/kg. It effectively delayed pupation when applied to prewandering larvae of T. ni, as expected for a JH esterase inhibitor. Thus, some members of this series are promising for evaluating the role of JH esterase in insect development. The series also indicates that, by varying the substituent on the sulfide moiety, potent “transition-state” inhibitors can be developed for a wide variety of esterases and proteases. 相似文献
17.
保幼激素(juvenile hormone, JH)可以调控昆虫滞育,保幼激素环氧水解酶(juvenile hormone epoxide hydrolase, JHEH)是调节保幼激素代谢的关键酶之一。为探索JHEH在七星瓢虫Coccinella septempunctata L.滞育中的调控作用,利用RT-PCR和RACE技术克隆获得七星瓢虫JHEH全长基因,命名为Csjheh(GenBank登录号:MH932586),该基因cDNA全长2 077 bp,开放阅读框(ORF)1 380 bp,编码459个氨基酸,预测蛋白质分子量为51.39 kD,理论等电点(pI)为8.79。疏水性分析结果显示该基因具有典型环氧水解酶的N末端疏水结构。氨基酸序列比对结果表明,Csjheh与中欧山松大小蠹、赤拟谷盗、丽蝇蛹集金小蜂、内华达古白蚁保幼激素环氧水解酶同源性达到64.24%。利用实时荧光定量PCR技术研究其时空表达模式,结果表明Csjheh基因在七星瓢虫成虫初羽化阶段表达量较高,滞育诱导条件下表达量呈先下降后上升的趋势,滞育60 d时与初羽化阶段接近。本研究结果对揭示JHEH参与JH的调控作用,进而调控昆虫滞育提供了理论参考。 相似文献
18.
The pioneering work of Gerry Brooks on cyclodiene insecticides led to the discovery of a class of enzymes known as epoxide hydrolases. The results from four decades of work confirm Brooks' first observations that the microsomal epoxide hydrolase is important in foreign compound metabolism. Brooks and associates went on to be the first to carry out a systematic study of the inhibition of this enzyme. A second role for this enzyme family was in the degradation of insect juvenile hormone (JH). JH epoxide hydrolases have now been cloned and expressed from several species, and there is interest in developing inhibitors for them. Interestingly, the distantly related mammalian soluble epoxide hydrolase has emerged as a promising pharmacological target for treating hypertension, inflammatory disease and pain. Tight-binding transition-state inhibitors were developed with good ADME (absorption, distribution, metabolism and excretion). These compounds stabilize endogenous epoxides of fatty acids, including arachidonic acid, which have profound therapeutic effects. Now EHs from microorganisms and plants are used in green chemistry. From his seminal work, Dr Brooks opened the field of epoxide hydrolase research in many directions including xenobiotic metabolism, insect physiology and human health, as well as asymmetric organic synthesis. 相似文献
19.
抑咽侧体素 (ASTs) 是一类由昆虫脑神经细胞分泌，通过作用于咽侧体进而抑制保幼激素 (JH) 合成与释放的昆虫神经肽。因其具有调控昆虫生长、发育和生殖等生理过程的功能，被认为是一类潜在的害虫控制剂。本文在简介了昆虫神经肽在害虫防治中的应用基础上，综述了昆虫神经肽抑咽侧体素的发现、类别和功能，并结合本研究组的工作，重点介绍抑咽侧体素及其类似物的结构修饰和优化、活性构象及构效关系研究，同时也介绍了抑咽侧体素及其类似物的受体和作用机制研究进展。最后，展望了该领域的未来发展趋势，期望为新的生态友好型农药的研发提供一定的参考作用。 相似文献
20.
Gerald T. Brooks Grahame E. Pratt David W. Mace John A. Cocks 《Pest management science》1985,16(2):132-142
The spontaneous biosynthesis of methyl (2E,6E)-(10R)-10,11-epoxy-3,7,11-trimethyldodeca-2,6-dienoate (juvenile hormone III; JH III) in excised corpora allata of Periplaneta americana was inhibited by a number of synthetic prop-2-ynyl ethers and 1,3-benzodioxole derivatives. One structurally diverse group of compounds inhibited only the final biosynthetic enzyme methyl farnesoate epoxidase (EC.1.14.14.–) at low to moderate concentrations, but at higher concentrations, also inhibited methyl farnesoate (MF) formation, causing an accumulation of MF in the concentration range 10 to 100 μM. For a second, more limited, group of compounds, there was close congruence between the inhibition of JH III biosynthesis and that of total ester (MF plus JH III) biosynthesis over their effective inhibitory concentration ranges. In contrast to the first group, there was no accumulation of MF and these compounds evidently inhibited JH III biosynthesis, at the level of either farnesoic acid esterification by O-methyl transferase (EC.2.1.1.–), or at an earlier step in the biosynthetic pathway that remains to be elucidated. 相似文献