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Fumio Matsumura 《Pesticide biochemistry and physiology》2010,97(2):133-139
In this review an effort was made to summarize the up to date information on the knowledge on the action mechanism of diflubenzuron (DFB), a prototype chemical for the benzoylurea type insecticides, with respect to its molecular mechanism to inhibit insect chitin synthesis. The key problem in pinpointing the action site of this insecticide has been the lack of in vitro demonstration of its action to inhibit insect chitin synthesis under cell free conditions. This problem was solved when an approach using a intracellular vesicle preparation from the cuticle of newly molted Periplaneta americana was developed. Using this approach it has become possible to identify that DFB indeed inhibits the process of incorporation of N-acetylglucosamine into insect chitin. Recently there has been a breakthrough in this field, when a sulfonylurea receptor (SUR) was identified in Drosophila melanogaster. This information was instrumental in establishing that insect SUR in the above intracellular vesicular preparation from P. americana as well as Blattella germanica is likely the actual target site of DFB to cause inhibition of chitin synthesis. The role of SUR in this case has been determined, by using glibenclamide, a typical SUR specific inhibitor as an aid, to be helping the exocytotic movement of these vesicles as is the case of other members of the group of ABC-transporters to which insect SUR belongs. In this case both DFB and glibenclamide have been shown to cause the depolarization of the vesicle membrane through inhibition of the K+ channel, which leads to their inhibition of chitin synthesis. 相似文献
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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
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Upon pathogen or insect attack, plants respond with production of a specific blend of the alarm signals salicylic acid (SA) and jasmonic acid (JA), which are recognized as key players in the regulation of the signaling pathways involved. SA and JA responsive genes and SA/JA cross talk were well characterized in dicotyledonous species, but little is known in monocotyledonous plants. Using qRT-PCR, the expression profiles of SA and JA responsive genes were investigated after SA and JA treatments in monocots wheat. The results showed that Glu2 and PR-2 responded almost exclusively to SA, PR-3 and LOX2 responded positively to methyljasmonate (MeJA) treatment, while Lipase and PR-1.1 were induced in response to treatment with SA or MeJA. Furthermore, either by pathogen infection or exogenous application of hormones can activate the antagonistic effect between SA and JA in wheat, which has been well elucidated in dicotyledonous species. The outcomes of SA-JA interactions could be affected by the relative concentration of each hormone. This study shed light on marker genes that can represent SA and JA pathways in wheat and provided some clues for better understanding their interactions in monocot. 相似文献
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Christopher Browning Alastair G. McEwen Kotaro Mori Taiyo Yokoi Dino Moras Yoshiaki Nakagawa Isabelle M. L. Billas 《Journal of Pesticide Science》2021,46(1):88
The ecdysone receptor (EcR) possesses the remarkable capacity to adapt structurally to different types of ligands. EcR binds ecdysteroids, including 20-hydroxyecdysone (20E), as well as nonsteroidal synthetic agonists such as insecticidal dibenzoylhydrazines (DBHs). Here, we report the crystal structures of the ligand-binding domains of Heliothis virescens EcR/USP bound to the DBH agonist BYI09181 and to the imidazole-type compound BYI08346. The region delineated by helices H7 and H10 opens up to tightly fit a phenyl ring of the ligands to an extent that depends on the bulkiness of ring substituent. In the structure of 20E-bound EcR, this part of the ligand-binding pocket (LBP) contains a channel filled by water molecules that form an intricate hydrogen bond network between 20E and LBP. The water channel present in the nuclear receptor bound to its natural hormone acts as a critical molecular adaptation spring used to accommodate synthetic agonists inside its binding cavity. 相似文献
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Moisés J. Zotti Ellen De Geyter Luc Swevers Antônio S.K. Braz Luis P.B. Scott Pierre Rougé Josep Coll Anderson D. Grutzmacher Eder J. Lenardão Guy Smagghe 《Pesticide biochemistry and physiology》2013
Ecdysteroid signal transduction is a key process in insect development and therefore an important target for insecticide development. We employed an in vitro cell-based reporter bioassay for the screening of potential ecdysone receptor (EcR) agonistic and antagonistic compounds. Natural ecdysteroids were assayed with ecdysteroid-responsive cell line cultures that were transiently transfected with the reporter plasmid ERE-b.act.luc. We used the dipteran Schneider S2 cells of Drosophila melanogaster and the lepidopteran Bm5 cells of Bombyx mori, representing important pest insects in medicine and agriculture. Measurements showed an EcR agonistic activity only for cyasterone both in S2 (EC50 = 3.3 μM) and Bm5 cells (EC50 = 5.3 μM), which was low compared to that of the commercial dibenzoylhydrazine-based insecticide tebufenozide (EC50 = 0.71 μM and 0.00089 μM, respectively). Interestingly, a strong antagonistic activity was found for castasterone in S2 cells with an IC50 of 0.039 μM; in Bm5 cells this effect only became visible at much higher concentrations (IC50 = 18 μM). To gain more insight in the EcR interaction, three-dimensional modeling of dipteran and lepidopteran EcR-LBD was performed. In conclusion, we showed that the EcR cell-based reporter bioassay tested here is a useful and practical tool for the screening of candidate EcR agonists and antagonists. The docking experiments as well as the normal mode analysis provided evidence that the antagonist activity of castasterone may be through direct binding with the receptor with specific changes in protein flexibility. The search for new ecdysteroid-like compounds may be particularly relevant for dipterans because the activity of dibenzoylhydrazines appears to be correlated with an extension of the EcR-LBD binding pocket that is prominent in lepidopteran receptors but less so in the modeled dipteran structure. 相似文献
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Salvatore Guarino Ezio Peri Paolo Lo Bue Maria Pia Germanà Stefano Colazza Leonid Anshelevich Uzi Ravid Victoria Soroker 《Phytoparasitica》2013,41(1):79-88
The red palm weevil (RPW), Rhynchophorus ferrugineus Olivier (Coleoptera, Curculionidae), is one of the most severe pests of ornamental palm species in urban areas of Mediterranean countries. Aiming to discover inhibitory semiochemicals for RPW population management in urban environments, we conducted electroantennographic (EAG) screenings of 17 commercially available synthetic compounds, representing three groups of plant volatiles (isoprenoids, phenyl propanoid derivatives and fatty acid derivatives) known for their repellent effects toward insects. These tests were followed by trap-based screenings of EAG-active menthone, α-pinene and methyl salicylate, singly and in combination, under urban conditions. In EAG bioassays, RPW antennae of both sexes showed positive dose-dependent responses to 13 of the 17 synthetic chemicals with significant differences among them. In field trapping experiments, conducted in the city of Palermo, Italy, from weeks 31 to 38 in 2010 and 2011, α-pinene, tested singly or in combination with methyl salicylate (2010) or menthone (2011), reduced trap catches by about 30% to 40%. Methyl salicylate and menthone alone were inactive. In conclusion, RPW is significantly affected by α-pinene. This isoprenoid is a promising disruptant for semiochemical-based management of this pest. In addition, identification of a large number of EAG-active chemicals could serve as a database for future design of active repellents or attractants of RPW adults. 相似文献
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Hadi Mosallanejad Luc Swevers Yoshiaki Nakagawa 《Pesticide biochemistry and physiology》2008,92(2):70-76
The activity profile of the most recent commercial non-steroidal ecdysteroid agonist chromafenozide (ANS-118), was evaluated on a comparative basis to methoxyfenozide (RH-2485) that is to date the most potent commercial agonist against Lepidoptera. This was done first at the molecular and cellular level regarding its induction activity of an ecdysteroid-responsive reporter gene and its cell proliferation inhibition activity, and subsequently at the level of larvicidal toxicity. For in vitro experiments three ecdysteroid-responsive insect cell lines were used: Drosophila melanogaster (Diptera) S2 cells, Bombyx mori (Lepidoptera) Bm5 cells and Spodoptera exigua (Lepidoptera) Se4 cells. The in vivo toxicity was scored against two major lepidopteran pests in the world, the beet armyworm S. exigua and the cotton leafworm Spodoptera littoralis. In vitro results revealed that chromafenozide and methoxyfenozide are highly potent against lepidopteran cells compared to dipteran cells, supporting the lepidopteran-specificity of these compounds. Interestingly, in the reporter gene induction experiments and proliferation inhibition experiments, a slightly higher efficacy was observed in S2 compared to Bm5 cells at high concentrations of chromafenozide and methoxyfenozide. Our analysis shows the high potency and efficacy of the chromafenozide compound as an ecdysteroid agonist towards lepidopteran insects at a level that is similar to methoxyfenozide. 相似文献
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以昆虫鱼尼丁受体为靶标的化合物活性筛选方法研究进展 总被引：4，自引：2，他引：2
昆虫鱼尼丁受体(ryanodine receptor,RyR)是目前新型杀虫剂创制中备受关注的靶标之一。在以RyR为靶标的杀虫剂氟虫酰胺和氯虫酰胺商品化后,大量基于该靶标的新型化合物被设计并合成出来。为加速研发和快速准确筛选以昆虫RyR为靶标的药剂,主要以氟虫酰胺和氯虫酰胺的活性筛选研究为例,对作用于RyR化合物的各种活体筛选方法和离体筛选方法进行了综述。其中活体筛选方法主要包括:点滴法、浸叶法、浸卵法、浸虫法、注射法和喷雾法;离体筛选方法主要包括MTT法、膜片钳技术、荧光技术、膜片钳技术与荧光技术结合以及计算机模拟筛选。通过对各种方法的分析比较,认为离体筛选方法快速、准确,在新型RyR杀虫剂活性的筛选研究中将进一步得到应用。 相似文献
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L. Ma Y. Xie Z.Y. Gu B.B. Wang F.C. Li K.Z. Xu W.D. Shen B. Li 《Pesticide biochemistry and physiology》2013
Silkworm (Bombyx mori), a model Lepidoptera insect, is an important economic insect. Its silk gland is the important organ for silk protein synthesis and secretion. Phoxim exposure causes deficient cocooning of silkworm and has become one of the major negative factors for the silk industry. To study the impact of phoxim exposure on silk gland, using gene chip technology, we examined differentially expressed genes in silk gland after silkworms were exposed to phoxim (4.0 μg/mL) for 24 h. Functional annotation, classification and KEGG signaling pathway analysis were performed. The results showed that out of 3206 genes detected in silk gland after phoxim exposure, 270 were differentially expressed significantly, including 249 up-regulated genes and 21 down-regulated genes. These differentially expressed genes related to apoptosis, detoxification and protein degradation were selected. Using qRT-PCR, the expression levels of 9 genes involved in apoptosis, detoxification and protein degradation were validated. In addition, the expression profiles of three related fibroin synthesis genes (Fib-H, Fib-L and P25) were analyzed. Our results showed that phoxim exposure induced apoptosis of silk gland cells and inhibition of fibroin synthesis. This may be the cause of deficient silkworm cocooning. 相似文献
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López CE Acosta IF Jara C Pedraza F Gaitán-Solís E Gallego G Beebe S Tohme J 《Phytopathology》2003,93(1):88-95
ABSTRACT A polymerase chain reaction approach using degenerate primers that targeted the conserved domains of cloned plant disease resistance genes (R genes) was used to isolate a set of 15 resistance gene analogs (RGAs) from common bean (Phaseolus vulgaris). Eight different classes of RGAs were obtained from nucleotide binding site (NBS)-based primers and seven from not previously described Toll/Interleukin-1 receptor-like (TIR)-based primers. Putative amino acid sequences of RGAs were significantly similar to R genes and contained additional conserved motifs. The NBS-type RGAs were classified in two subgroups according to the expected final residue in the kinase-2 motif. Eleven RGAs were mapped at 19 loci on eight linkage groups of the common bean genetic map constructed at Centro Internacional de Agricultura Tropical. Genetic linkage was shown for eight RGAs with partial resistance to anthracnose, angular leaf spot (ALS) and Bean golden yellow mosaic virus (BGYMV). RGA1 and RGA2 were associated with resistance loci to anthracnose and BGYMV and were part of two clusters of R genes previously described. A new major cluster was detected by RGA7 and explained up to 63.9% of resistance to ALS and has a putative contribution to anthracnose resistance. These results show the usefulness of RGAs as candidate genes to detect and eventually isolate numerous R genes in common bean. 相似文献
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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
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B. Li Y.H. Wang Y.X. Xu Z.G. Wei Y.H. Chen W.D. Shen 《Pesticide biochemistry and physiology》2010,98(1):19-25
To investigate the genotyping criteria for the insect acetylcholinesterase gene (ace), we cloned two types of ace genes in domestic (Bombyx mori) and wild silkworm (Bombyxmandarina) through RT-PCR. The cloned genes were named Bm-ace1, Bm-ace2, Bmm-ace1 and Bmm-ace2, respectively. The ORFs of Bm-ace1 and Bmm-ace1 contained 2025 base pairs, encoding 683 amino acid residues (AA’s). The predicted protein has a molecular weight (MW) of 76.955 kDa and an isoelectric point (pI) of 6.36. The Bm-ace2 and Bm-ace2 genes contained 1917 bp nucleotides, encoding 638 AA’s. The predicted protein has a MW of 71.675 kDa and a pI of 5.49. Both ace1 and ace2 contain signature domains of acetylcholinesterases. Homology analysis of 18 NCBI downloaded insect AChEs peptide sequences and the 4 AChEs deducted in this study revealed that type 1 and type 2 insect AChEs had significant differences. Type 2 sequence is more conserved than type 1. Near the active centers of both types of AChEs, 48 strictly conserved AA’s (336-384) are present, and homology of these two peptide fragments was only 54.16%. Meanwhile, at AA positions 280-297, type 1 and type 2 AChEs both have conserved sequences with the similarity of the two being 52.94%. In type 2 AChEs, a uniquely conserved peptide sequence is found at positions 226-239 (QHLRVRHHQDKPL). We propose to use the above mentioned three conserved regions as criteria for insect acetylcholinesterases gene genotyping. This will benefit the genotyping of other acetylcholinesterase genes and the study of their functions. 相似文献
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Recent advances in hormones in insect pest control 总被引：1，自引：0，他引：1
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Diana K. Londoño Haichuan Wang Michael J. Lydy 《Pesticide biochemistry and physiology》2007,89(2):104-110
Previous studies performed in our laboratory have measured the effect of atrazine exposure on cytochrome P450-dependent monooxygenase activity and have found increased activity in midge larvae (Chironomus tentans) as a result of atrazine exposure (1-10 ppm). Here we report the cloning and expression of a specific C. tentans CYP4 gene that is responsive to atrazine induction with an open reading frame of 1678 bp which encodes a putative protein of 559 amino acid residues. Alignments of deduced amino acid sequences with other insect P450 genes and phylogenetic analysis indicated a high degree of similarity to other insect CYP4 genes. Northern blotting analysis employing a fragment of 1200 bp from the CYP4 gene as a probe indicated that the CYP4 gene was expressed in all developmental stages, but was expressed at highest levels in late instar larvae. Additionally, over-expression of CYP4 in C. tentans exposed to atrazine (10 mg/l) confirms the ability of atrazine to induce specific P450 genes and provides insight into potential consequences of atrazine exposure in aquatic organisms. 相似文献
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Ecdysteroids are a class of steroid hormones in arthropods that control molting and metamorphosis through interaction with intracellular nuclear receptors. In contrast to the extensive literature describing their biosynthetic pathways and signaling components, little has been known about how these hormones are traveling into and out of the cells through lipid bilayers of the cell membranes. Recently, a series of studies conducted in the fruit fly Drosophila melanogaster revealed that membrane transporters have critical functions in trafficking ecdysteroids across cell membranes, challenging the classical simple diffusion model of steroid hormone transport. Here we summarize recent advances in our understanding of membrane transporters involved in ecdysteroid signaling in Drosophila, with particular focus on Ecdysone Importer (EcI) that is involved in ecdysteroid uptake in peripheral tissues. We then discuss the potential advantage of EcI blockers as a novel pest management tool as compared to classical insect growth regulators. 相似文献
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胰岛素是一类生物体内在进化上非常保守的具有调控代谢、生长、发育、生殖和寿命等多种功能的肽类激素。在昆虫中,以多基因家族编码的类胰岛素为主,在结构上与脊椎动物胰岛素同源。近年来,有关昆虫类胰岛素及其信号通路等方面已有较多研究,特别是对黑腹果蝇的研究,为人类胰岛素相关疾病诊断与治疗提供了较好的试验模型。本文主要介绍昆虫类胰岛素及其受体、类胰岛素表达与释放、类胰岛素信号通路及其在调控昆虫生殖、寿命、代谢、生长与发育和翅型分化等生理功能的最新研究进展,为促进其在害虫控制或天敌保护利用等方面的应用提供参考。 相似文献