Pesticide Biochemistry and Physiology最新文献_第3页

Effects of thiacloprid, a neonicotinoid pesticide, on rat reproductive system: Pregnancy hormone disruption and abortion trends 新烟碱类杀虫剂噻虫啉对大鼠生殖系统的影响：妊娠激素紊乱和流产趋势

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-09 DOI: 10.1016/j.pestbp.2024.106166

Thiacloprid (TCL), commonly known as Biscaya, is among the most widely used pesticides in agriculture, designed to eliminate insects by targeting their nicotinic receptors. This study explores the effects of orally administering TCL (at a dose of 50 mg/kg) on the hormone secretion crucial for pregnancy and the factors influencing abortion throughout the early, middle, and late stages of pregnancy in female rats.

Following TCL exposure, there were significant increases in levels of 17β-Estradiol, prostaglandins F_2α and E₂, and serum oxytocin hormone in different stages of pregnancy. In contrast, progesterone and endothelin-1 serum levels notably decreased during the initial and final stages of pregnancy. Additionally, TCL led to a substantial rise in lipid peroxidation levels and a decrease in total thiol molecules and total antioxidant capacity, especially in uterine tissue. Although TCL did not significantly affect the morphological characteristics of the delivered fetuses, it notably increased the number of abortions, especially during the second and third stages of pregnancy.

In summary, our findings suggest that TCL elevates the risk of abortion in pregnant rats by disrupting the secretion of hormones crucial for fertility (such as 17β-Estradiol/progesterone) and by increasing the secretion of abortion-inducing hormones like prostaglandins and oxytocin. Furthermore, these effects may be associated with disruptions in the oxidant/antioxidant balance within the ovaries and uterus.

噻虫啉（TCL），俗称比斯卡亚，是农业中使用最广泛的杀虫剂之一，旨在通过靶向昆虫的烟碱受体来消灭昆虫。本研究探讨了口服 TCL（剂量为 50 毫克/千克）对雌性大鼠妊娠早、中、晚期的妊娠关键激素分泌和流产影响因素的影响。相比之下，孕酮和内皮素-1 血清水平在妊娠初期和末期明显下降。此外，TCL 还导致脂质过氧化水平大幅上升，总硫醇分子和总抗氧化能力下降，尤其是在子宫组织中。总之，我们的研究结果表明，TCL 通过干扰对生育至关重要的激素（如 17β-雌二醇/孕酮）的分泌以及增加前列腺素和催产素等流产诱导激素的分泌，增加了怀孕大鼠的流产风险。此外，这些影响可能与卵巢和子宫内氧化剂/抗氧化剂平衡的破坏有关。

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引用次数: 0

Disruption of exploratory behavior and olfactory memory in cockroaches exposed to sublethal doses of the neonicotinoid Thiamethoxam 暴露于亚致死剂量新烟碱噻虫嗪的蟑螂的探索行为和嗅觉记忆受到破坏

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-09 DOI: 10.1016/j.pestbp.2024.106167

Neonicotinoid insecticides (NNI) are agonists of insect nicotinic acetylcholine receptors (nAChR) that induce non-elucidate mechanisms of abnormal behavior in insects. In this work, we investigated the effects of sublethal doses of the neonicotinoid thiamethoxam (TMX) on neurochemical and physiological parameters in cockroaches. Sublethal doses of TMX (0.01–10 ng.g⁻¹ body mass) caused significant alterations in most of the neurophysiological parameters evaluated. TMX reduced sustained locomotor activity by 19.9–25.8 %, depending on the dose. Leg grooming activity increased by 124.5 ± 3.4 %, 158.7 ± 3.5 %, 168.3 ± 3.4 %, and 160.4 ± 3.4 % (mean ± SEM) with TMX doses of 0.01, 0.1, 1, and 10 ng.g⁻¹, respectively. Exploratory activity was significantly reduced only at the lowest TMX dose (0.01 ng.g⁻¹) – the time spent immobile increased from 30 % to ∼45 %, whereas none of the doses affected the walking speed. Treatment with TMX (0.01 ng.g⁻¹) markedly reduced the olfactory sensitivity of the cockroaches and also reduced the mechanosensory action potential amplitude, rise time and decay time by 61.2 ± 19 %, 50 ± 4 %, and 76.8 ± 9.5 %, respectively. In semi-isolated heart preparations, TMX caused positive chronotropism (increases of 34.7 ± 15.9 %, 26.8 ± 7.8 %, 43.0 ± 16.5 %, and 19.0 ± 13.7 % for 0.01, 0.1, 1, and 10 ng of TMX, respectively). TMX attenuated the activity of glutathione-S-transferase by 35.1 ± 6.4 % at the highest dose tested (10 ng.g⁻¹). TMX caused alterations in the metal ion content of cockroach brains that varied with the dose tested and the ion examined. These findings indicate that sublethal doses of TMX can interfere with normal neurological function in cockroaches and disrupt brain metal ion homeostasis.

新烟碱类杀虫剂（NNI）是昆虫烟碱乙酰胆碱受体（nAChR）的激动剂，可诱发昆虫异常行为的机制尚不清楚。在这项工作中，我们研究了亚致死剂量的新烟碱类杀虫剂噻虫嗪（TMX）对蟑螂神经化学和生理参数的影响。亚致死剂量的噻虫嗪（0.01-10 纳克/克-1 体重）会导致大多数神经生理参数发生显著变化。根据剂量的不同，TMX 可使持续运动活动减少 19.9-25.8%。TMX剂量为0.01、0.1、1和10 ng.g-1时，腿部梳理活动分别增加了124.5 ± 3.4 %、158.7 ± 3.5 %、168.3 ± 3.4 %和160.4 ± 3.4 %（平均值 ± SEM）。只有最低剂量的 TMX（0.01 ng.g-1）才会明显减少探索活动--不动时间从 30% 增加到 45%，而所有剂量都不会影响行走速度。TMX（0.01 ng.g-1）显著降低了蟑螂的嗅觉灵敏度，并使机械感觉动作电位振幅、上升时间和衰减时间分别减少了 61.2 ± 19 %、50 ± 4 % 和 76.8 ± 9.5 %。在半离体心脏制剂中，TMX 可引起正向的时间推移（0.01、0.1、1 和 10 纳克 TMX 分别增加 34.7 ± 15.9 %、26.8 ± 7.8 %、43.0 ± 16.5 % 和 19.0 ± 13.7 %）。在测试的最高剂量（10 纳克/克）下，TMX 可使谷胱甘肽-S-转移酶的活性降低 35.1 ± 6.4%。TMX 会改变蟑螂大脑中的金属离子含量，这种改变随测试剂量和检测离子的不同而变化。这些研究结果表明，亚致死剂量的 TMX 可干扰蟑螂的正常神经功能，并破坏脑金属离子的平衡。

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引用次数: 0

Insecticide binding mode analysis and biological effects of acetylcholinesterase target-site resistance mutations in Spodoptera frugiperda 蛙翅蝶乙酰胆碱酯酶靶位抗性突变的杀虫剂结合模式分析及生物效应

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-09 DOI: 10.1016/j.pestbp.2024.106164

It is urgent to solve insecticide resistance issues for fall armyworm (FAW), Spodoptera frugiperda. Some acetylcholinesterase-1 (Ace-1) mutations (A201S, G227A and F290V) have been identified as a cause of FAW resistance to organophosphates (OPs) and carbamates insecticides (CXs). However, the structural biological mechanisms on the relationship between the Ace-1 mutations and resistance to OPs and CXs still remain elusive. In this study, the A201S and F290V mutaions were found in eight fields populations of FAW except the G227A. Molecular docking revealed that the four Ace-1 proteins (Ace1-WT, Ace1-A201S, Ace1-G227A and Ace1-F290V) had the same binding modes and the same binding energies with acetylcholine (Ach), trichlorfon, chlorpyrifos, methomyl, carbaryl and chlorpyrifos oxide. The structural biological analysis revealed that the A201S mutations can enhance enzyme catalytic efficiency by introducing the hydroxyl group (-OH) from serine which performed the same function as the main-chain -NH and enhanced the interaction with the carboxy oxygen of acetylcholine (Ach), and the F290V mutation can effectively improve FAW resistance to insecticides by increasing the likelihood of Ach to enter the enzyme's active center for phenylalanine replaced by smaller valine under insecticide inhibition conditions. The bioassays and age-stage-specific life table analysis of FAW-SS and FAW-F290V populations revealed that F290V mutation effectively contributed to FAW resistance with a low fitness cost. This study provides a theoretical basis for future pest resistance management.

解决秋绵虫（FAW）（Spodoptera frugiperda）的杀虫剂抗性问题迫在眉睫。一些乙酰胆碱酯酶-1（Ace-1）突变（A201S、G227A 和 F290V）已被确认为导致秋绵虫对有机磷类杀虫剂（OPs）和氨基甲酸酯类杀虫剂（CXs）产生抗性的原因。然而，Ace-1 基因突变与 OPs 和 CXs 抗性之间的结构生物学机制仍未确定。在本研究中，除 G227A 突变外，A201S 和 F290V 突变均出现在 8 个 FAW 田间种群中。分子对接显示，四种 Ace-1 蛋白（Ace1-WT、Ace1-A201S、Ace1-G227A 和 Ace1-F290V）与乙酰胆碱（Ach）、敌百虫、毒死蜱、灭多威、克百威和氧化毒死蜱的结合模式和结合能相同。结构生物学分析表明，A201S突变可通过从丝氨酸中引入羟基（-OH）提高酶的催化效率，该羟基与主链上的-NH具有相同的功能，并增强了与乙酰胆碱（Ach）羧基氧的相互作用；F290V突变可在杀虫剂抑制条件下，通过用较小的缬氨酸取代苯丙氨酸增加Ach进入酶活性中心的可能性，从而有效提高一汽大众对杀虫剂的抗性。对FAW-SS和FAW-F290V种群的生物测定和特定年龄阶段的生命表分析表明，F290V突变以较低的适应性成本有效地提高了FAW的抗性。该研究为未来害虫抗性管理提供了理论依据。

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引用次数: 0

JAK/STAT signaling pathway is involved in antibacterial immunity in the green peach aphid Myzus persicae (Sulzer) JAK/STAT 信号通路参与了桃蚜 Myzus persicae (Sulzer) 的抗菌免疫过程

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-09 DOI: 10.1016/j.pestbp.2024.106168

The Janus kinase/signal transducer and activator of transcription (JAK/STAT) signaling pathway within the innate immune system plays a crucial role in defending insects against bacterial, fungal, and viral pathogens. In this study, we identified and cloned five key genes of this signaling pathway in Myzus persicae: MpDome-1, MpDome-2, MpJak, MpStat92E-1, and MpStat92E-2. Our results illustrated that these genes were highly expressed in first, second and third-instar nymphs. Tissue-specific expression analysis revealed that the five genes were predominantly expressed in the gut. Upon bacterial challenge, particularly with Staphylococcus aureus, the expression levels of all five genes were significantly upregulated. Additionally, Escherichia coli infection significantly upregulated the expression levels of MpDome-1 and MpDome-2, while MpJak, MpStat92E-1 and MpStat92E-2 were weakly upregulated. Functional analysis through RNA interference-mediated knockdown of these target genes revealed a significant increase in mortality following infection with E. coli and S. aureus compared with the control group. These findings suggest that the JAK/STAT signaling pathway is crucial for immune defense against bacterial infections in M. persicae.

先天性免疫系统中的 Janus 激酶/信号转导和转录激活因子（JAK/STAT）信号通路在昆虫抵御细菌、真菌和病毒病原体的过程中发挥着至关重要的作用。在这项研究中，我们发现并克隆了柿小蜂（Myzus persicae）中该信号通路的五个关键基因：MpDome-1、MpDome-2、MpJak、MpStat92E-1 和 MpStat92E-2。我们的研究结果表明，这些基因在一龄、二龄和三龄若虫中的表达量很高。组织特异性表达分析表明，这五个基因主要在肠道中表达。在细菌挑战下，特别是在金黄色葡萄球菌的挑战下，所有五个基因的表达水平都显著上调。此外，大肠杆菌感染会显著上调MpDome-1和MpDome-2的表达水平，而MpJak、MpStat92E-1和MpStat92E-2的上调较弱。通过 RNA 干扰介导的这些靶基因敲除功能分析发现，与对照组相比，感染大肠杆菌和金黄色葡萄球菌后死亡率显著增加。这些研究结果表明，JAK/STAT 信号通路对宿主对细菌感染的免疫防御至关重要。

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引用次数: 0

Mrlac1, an extracellular laccase, is required for conidial morphogenesis as well as the well adaptability in field of Metarhizium rileyi Mrlac1是一种细胞外漆酶，它是分生孢子形态发生以及Metarhizium rileyi野外适应性所必需的。

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-05 DOI: 10.1016/j.pestbp.2024.106161

Acting as an extremely promising fungal pesticide, Metarhizium rileyi exhibits robust insecticidal activity against Lepidoptera pests, particularly the larvae. Though there is a slight delay in efficacy, biopesticides offer salient advantages over traditional chemical pesticide especially in environmental safety, cyclic infection and resistant inhibition. In this study, an exterior T-DNA was randomly inserted into the genome of M. rileyi, resulting in the acquisition of a mutant strain that displayed a colour transition from green to yellow within its conidia. The disruption of Mrlac1, a laccase, has been confirmed to attribute to the epigenetic alterations. Mrlac1 is a secreted protein harboring an N-terminal signaling peptide that undergoes in vivo synthesis and accumulates on the cell wall of M. rileyi. Targeted knock-out mutant exhibited alterations not just in conidia coloration, but significantly diminished capacity to withstand external stressors, particularly non-biological factors such as high humidity, Congo red exposure, and UV radiation. The disruptant suffered a constraint on hyphal polar growth, alteration in conidial surface structure, as well as noticeable increase in adhesion forces between conidia, the core infection factors. There is a remarkable diminution in virulence of Mrlac1 deletion variant against larvae of Spodoptera litura by topical inoculation, but not hemolymph injection. Our findings suggest that Mrlac1 acts as a positive regulator in the normal morphogenesis of fungal conidia, encompassing pigment production, inter-conidia adhesion, and conidial cell wall integrity, while the preservation of these structures holds paramount importance for the survival and infection of M. rileyi in the field.

作为一种极有前途的真菌杀虫剂，Metarhizium rileyi 对鳞翅目害虫，尤其是幼虫，具有很强的杀虫活性。虽然药效稍有延迟，但与传统的化学农药相比，生物农药具有显著的优势，尤其是在环境安全、循环感染和抗药性抑制方面。在这项研究中，一个外部 T-DNA 被随机插入到 M. rileyi 的基因组中，结果获得了一个突变株，其分生孢子的颜色从绿色转变为黄色。经证实，Mrlac1（一种漆酶）的破坏是表观遗传改变的原因。Mrlac1是一种分泌蛋白，含有一个N端信号肽，可在体内合成并积聚在M.rileyi的细胞壁上。靶向敲除突变体不仅表现出分生孢子着色的改变，而且明显降低了抵御外部胁迫的能力，尤其是高湿度、刚果红照射和紫外线辐射等非生物因素。破坏者的分生孢子极性生长受到限制，分生孢子表面结构发生变化，分生孢子之间的粘附力（核心感染因子）明显增加。通过局部接种，Mrlac1缺失变体对斑翅蝶类幼虫的毒力明显减弱，但对血淋巴注射的毒力却没有减弱。我们的研究结果表明，Mrlac1 在真菌分生孢子的正常形态发生过程中起着积极的调节作用，包括色素的产生、分生孢子间的粘附和分生孢子细胞壁的完整性，而这些结构的保护对于 M. rileyi 在野外的生存和感染至关重要。

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引用次数: 0

Co-application of Validamycin A and dsRNAs targeting trehalase genes conferred enhanced insecticidal activity against Laodelphax striatellus 联合应用瓦里达霉素 A 和靶向树胶酶基因的 dsRNA 可增强对 Laodelphax striatellus 的杀虫活性

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-03 DOI: 10.1016/j.pestbp.2024.106160

The small brown planthopper (SBPH), Laodelphax striatellus, poses a significant threat to rice crops, necessitating innovative pest control strategies. This study evaluated the potential of validamycin A (Val A) and RNA interference (RNAi) targeting trehalase genes (LsTre1 and LsTre2) in controlling SBPH. Our results demonstrated that Val A treatment of rice seedlings led to a dose-dependent mortality of SBPH. Concurrently, Val A induced the upregulation of LsTre1 and LsTre2, suggesting a compensatory feedback mechanism. Furthermore, foliar-applied chimeric dsRNA targeting LsTre1 and LsTre2 exhibited higher insecticidal activity than individual dsLsTre1 and dsLsTre2 or mixed dsRNAs. Remarkably, co-application of Val A and chimeric dsRNA increased SBPH mortality due to the suppression of Val A-induced LsTre1 and LsTre2 upregulation by chimeric dsRNA. These results suggest that the co-application of Val A and chimeric dsRNA targeting trehalase genes could be an effective SBPH control strategy.

小褐飞虱（SBPH）（Laodelphax striatellus）对水稻作物构成严重威胁，因此需要创新的害虫控制策略。本研究评估了有效霉素 A（Val A）和针对三卤酶基因（LsTre1 和 LsTre2）的 RNA 干扰（RNAi）在控制 SBPH 方面的潜力。我们的研究结果表明，Val A 处理水稻秧苗会导致 SBPH 出现剂量依赖性死亡。同时，Val A 会诱导 LsTre1 和 LsTre2 的上调，这表明这是一种补偿反馈机制。此外，与单独的 dsLsTre1 和 dsLsTre2 或混合 dsRNA 相比，叶面施用以 LsTre1 和 LsTre2 为靶标的嵌合 dsRNA 表现出更高的杀虫活性。值得注意的是，由于嵌合 dsRNA 抑制了 Val A 诱导的 LsTre1 和 LsTre2 的上调，联合应用 Val A 和嵌合 dsRNA 增加了 SBPH 的死亡率。这些结果表明，联合应用 Val A 和针对树胶酶基因的嵌合 dsRNA 可能是一种有效的 SBPH 控制策略。

引用次数: 0

Baseline sensitivity and resistance risk of Sclerotinia sclerotiorum to glabridin and the possible anti-fungal mechanism 硬菌对格拉菌素的基线敏感性和抗药性风险以及可能的抗真菌机制

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-02 DOI: 10.1016/j.pestbp.2024.106162

Sclerotinia stem rot caused by Sclerotinia sclerotiorum is one of the most serious diseases of oilseed rape. Chemical control is an important method to control this disease, however, development of fungal resistance to commonly used fungicides has led to severe yield losses in recent years. Therefore, development of novel fungicides against S. sclerotiorum is urgently needed. Glabridin is one of the major flavonoids in Glycyrrhiza L. plants, and we previously found that it is very effective against S. sclerotiorum. Nevertheless, the baseline sensitivity and resistance risk of S. sclerotiorum to glabridin as well as the possible anti-fungal mechanism need further elucidation. In this study, we revealed that the EC₅₀ (median effective concentration) values of glabridin against 109 S. sclerotiorum isolates collected from Jiangsu Province of China ranged from 0.51 to 8.03 μg/mL with a mean EC₅₀ value of 3.05 ± 1.27 μg/mL. No cross-resistance was observed between glabridin and carbendazim, and no glabridin-resistant mutants were obtained by chemical induction. RNA profiling result showed that tyrosine metabolism of S. sclerotiorum were evidently affected by glabridin. qRT-PCR, enzyme activity assay, and molecular docking proved that glabridin greatly reduced both the expression level and enzyme activity of tyrosinase in S. sclerotiorum. Furthermore, S. sclerotiorum incurred certain impairment in its membrane integrity after glabridin treatment at 10 μg/mL. This study is the first report on baseline sensitivity and resistance risk of S. sclerotiorum to glabridin, and it is revealed that glabridin may interfere tyrosine metabolism and membrane integrity of S. sclerotiorum.

由硬粒菌（Sclerotinia sclerotiorum）引起的茎腐病是油菜最严重的病害之一。化学防治是控制这种病害的重要方法，但近年来，由于真菌对常用杀菌剂产生抗药性，导致产量严重下降。因此，亟需开发新型杀菌剂来防治 S. sclerotiorum。Glabridin 是甘草中的主要黄酮类化合物之一，我们以前曾发现它对 Sclerotiorum 非常有效。然而，硬皮病菌对草甙的基本敏感性和抗性风险以及可能的抗真菌机制还需要进一步阐明。在这项研究中，我们发现格拉布丁对从中国江苏省收集到的109株S. sclerotiorum分离株的EC50（中位有效浓度）值在0.51至8.03 μg/mL之间，平均EC50值为3.05 ± 1.27 μg/mL。格拉布丁与多菌灵之间未发现交叉抗性，也未通过化学诱导获得格拉布丁抗性突变体。qRT-PCR、酶活性测定和分子对接证明，格拉布丁大大降低了硬皮病菌体内酪氨酸酶的表达水平和酶活性。此外，10 μg/mL的格拉布丁处理后，硬皮病菌的膜完整性受到了一定程度的破坏。该研究首次报道了硬皮菌对草氨嘧啶的基线敏感性和抗性风险，揭示了草氨嘧啶可能会干扰硬皮菌的酪氨酸代谢和膜完整性。

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引用次数: 0

Scaffold hopping approach to the novel hexacyclic pyrazol-3-amide derivatives as potential multi-target insect growth regulators candidates 用支架跳跃方法研究新型六环吡唑-3-酰胺衍生物作为潜在的多靶标昆虫生长调节剂候选物

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-02 DOI: 10.1016/j.pestbp.2024.106163

Ecdysone receptor (EcR) and three insect chitinases (OfChtI, OfChtII, and OfChi-h) are considered as attractive targets for the development of novel insect growth regulators (IGRs) since they are closely related to the insect molting. In this study, to develop potent multi-target IGRs, a series of hexacyclic pyrazol-3-amide derivatives were rationally designed by utilizing the scaffold hopping strategy with the previously reported compound 6j (N-(4-bromobenzyl)-2-phenyl-4,5,6,7-tetrahydro-2H-indazole-5-carboxamide) as a lead compound. The bioassay results indicated that most of the target compounds exhibited obvious insecticidal activity. Especially, compounds a5 and a21 displayed excellent insecticidal activities against P. xylostella with LC₅₀ values of 82.29 and 69.45 mg/L, respectively, exceeding that of 6j (263.78 mg/L). Compounds a5 and a21 also dramatically disturbed the growth and development of O. furnacalis larvae, and their LC₅₀ values were 124.71 and 127.54 mg/L, respectively, superior to the lead 6j (267.33 mg/L). The action mechanism study revealed that the most active compound a21 could act simultaneously on EcR (21.4 % binding activity at 8 mg/L), OfChtI (94.9 % inhibitory at 10 μM), OfChtII (23.1 % inhibitory at 10 μM), and OfChi-h (94.3 % inhibitory at 10 μM), significantly higher than that of the lead compound 6j. The result of molecular docking indicated that transferring the carboxamide group from pyrazole position 5 to 3 enhanced the interactions of a21 with the key amino acid residues of the OfChtI, OfChtII, and OfChi-h, resulting in stronger affinity to the three targets than 6j. The present work offers a useful guidance for the further development of novel multi-target IGRs.

蜕皮激素受体（EcR）和三种昆虫几丁质酶（OfChtI、OfChtII和OfChi-h）被认为是开发新型昆虫生长调节剂（IGRs）的诱人靶标，因为它们与昆虫蜕皮密切相关。本研究以之前报道的化合物 6j（N-(4-溴苄基)-2-苯基-4,5,6,7-四氢-2H-吲唑-5-甲酰胺）为先导化合物，利用支架跳跃策略合理设计了一系列六环吡唑-3-酰胺衍生物，以开发强效多靶点 IGRs。生物测定结果表明，大多数目标化合物具有明显的杀虫活性。尤其是 a5 和 a21 化合物对木虱具有极好的杀虫活性，半数致死浓度分别为 82.29 和 69.45 毫克/升，超过了 6j 的半数致死浓度（263.78 毫克/升）。化合物 a5 和 a21 也极大地干扰了 O. furnacalis 幼虫的生长发育，其 LC50 值分别为 124.71 和 127.54 mg/L，优于铅 6j（267.33 mg/L）。作用机理研究表明，活性最高的化合物 a21 可同时作用于 EcR（8 mg/L 时的结合活性为 21.4%）、OfChtI（10 μM 时的抑制活性为 94.9%）、OfChtII（10 μM 时的抑制活性为 23.1%）和 OfChi-h （10 μM 时的抑制活性为 94.3%），明显高于先导化合物 6j。分子对接结果表明，将羧酰胺基团从吡唑的第 5 位转移到第 3 位增强了 a21 与 OfChtI、OfChtII 和 OfChi-h 的关键氨基酸残基的相互作用，从而使其对这三个靶标的亲和力强于 6j。本研究为进一步开发新型多靶点 IGRs 提供了有益的指导。

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引用次数: 0

Functional analyses of dopamine receptors involved in virus transmission and reproduction in the small brown planthopper Laodelphax striatellus 多巴胺受体参与病毒传播和小褐斑蝶（Laodelphax striatellus）繁殖的功能分析

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-10-01 DOI: 10.1016/j.pestbp.2024.106157

Dopamine (DA) is the most abundant biogenic amine present in the insect central nervous system, and regulates multiple functions in physiology and behaviors through dopamine receptors (DARs). The small brown planthopper Laodelphax striatellus is an important agricultural pest and causes serious damage by transmitting diverse plant viruses, such as rice stripe virus (RSV). However, DARs have not yet been molecularly characterized in planthoppers, and their roles in virus infection and transmission remain largely unknown in insect vectors. In this study, we cloned four LsDARs (LsDOP1, LsDOP2, LsDOP3 and LsDopEcR) from L. striatellus. LsDARs share considerable sequence identity with their orthologous DARs, and cluster nicely with their corresponding receptor groups. The transcript levels of LsDARs varied in different developmental stages and adult tissues, with the highest expressions in the egg stage and in the brain. The expression levels of LsDARs were significantly higher in RSV-viruliferous L. striatellus. Knockdown of LsDOP2 and LsDOP3 significantly downregulated the expressions of viral genes of capsid protein (CP) and RNA3 segment (RNA3), while LsDOP1 knockdown upregulated their expressions. Silencing LsDopEcR upregulated and then downregulated CP and RNA3 expressions. Moreover, LsDOP2 and LsDOP3 knockdown significantly decreased the vertical transmission rates of RSV. Meanwhile, DA injection promoted RSV transmission and accumulation. We further demonstrated that silencing of LsDARs significantly altered the expressions of vitellogenin (LsVg) and Vg receptor (LsVgR). Furthermore, the reproduction performance of L. striatellus was reduced by LsDOP2 and LsDOP3 knockdown, but increased by LsDopEcR knockdown, and not affected by LsDOP1 silencing. These results provide critical information concerning the roles of DARs in virus transmission and reproduction in L. striatellus, and open the way for the development of innovative strategies for planthopper control.

多巴胺（DA）是昆虫中枢神经系统中含量最高的生物胺，通过多巴胺受体（DAR）调节生理和行为的多种功能。小褐斑跳虫（Laodelphax striatellus）是一种重要的农业害虫，通过传播多种植物病毒（如水稻条纹病毒（RSV））造成严重危害。然而，DARs 在跳虫中尚未得到分子鉴定，它们在昆虫载体中病毒感染和传播中的作用在很大程度上仍然未知。在这项研究中，我们从条纹夜蛾中克隆了四个 LsDARs（LsDOP1、LsDOP2、LsDOP3 和 LsDopEcR）。LsDARs 与其直向同源的 DARs 具有相当高的序列同一性，并与相应的受体群很好地聚类。LsDARs在不同发育阶段和成体组织中的转录水平各不相同，在卵期和脑中的表达量最高。在RSV病毒感染的条纹叶蝉中，LsDARs的表达水平明显较高。敲除 LsDOP2 和 LsDOP3 能显著下调病毒基因帽状蛋白（CP）和 RNA3 片段（RNA3）的表达，而敲除 LsDOP1 则能上调它们的表达。沉默 LsDopEcR 会先上调后下调 CP 和 RNA3 的表达。此外，敲除 LsDOP2 和 LsDOP3 能显著降低 RSV 的垂直传播率。同时，DA注射促进了RSV的传播和积累。我们进一步证实，沉默 LsDARs 能显著改变卵黄素（LsVg）和 Vg 受体（LsVgR）的表达。此外，LsDOP2 和 LsDOP3 的敲除会降低条纹叶蝉的繁殖性能，但 LsDopEcR 的敲除会提高其繁殖性能，而 LsDOP1 的沉默则不会影响其繁殖性能。这些结果提供了有关 DARs 在横纹夜蛾病毒传播和繁殖中的作用的重要信息，并为开发创新的花斑叶蝉控制策略开辟了道路。

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引用次数: 0

Biological damage of monocrotaline on the brain and intestinal tissues of Apis mellifera 一缩胺对蜜蜂脑组织和肠组织的生物损伤

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2024-09-30 DOI: 10.1016/j.pestbp.2024.106158

Monocrotaline (MCT) is a toxic alkaloid present in plants, posing a threat to animals in terrestrial ecosystems. However, little is known about its potential impacts on pollinating insects. Here, we report the effects of of MCT on the brains and intestines of foraging honeybees (Apis mellifera). MCT exposure resulted in a reduction in head weight and swelling of the abdomen in honeybees. Additionally, MCT exposure caused morphological damage to the brain, characterized by decreased antioxidant capacity and increased apoptosis, along with intestinal tissue damage that was accompanied by increased antioxidant capacity and apoptosis. Moreover, MCT altered the core gut microbial community structure in honeybees and increased the expression of antimicrobial peptide (AMP) genes in the midgut. These findings indicate that exposure to MCT activates the immune response in the honeybee gut, while the brain does not exhibit an immune response but instead experiences oxidative stress. This study provides a resource for future research exploring interactions between MCT and other insects, and can help deepen our understanding of MCT's potential impacts in ecosystems.

单克隆碱（MCT）是植物中的一种有毒生物碱，对陆地生态系统中的动物构成威胁。然而，人们对其对授粉昆虫的潜在影响知之甚少。在这里，我们报告了 MCT 对觅食蜜蜂（Apis mellifera）大脑和肠道的影响。接触 MCT 会导致蜜蜂头部重量减轻和腹部肿胀。此外，暴露于 MCT 会导致大脑形态损伤，表现为抗氧化能力下降和细胞凋亡增加，同时肠道组织损伤也伴随着抗氧化能力和细胞凋亡的增加。此外，MCT 改变了蜜蜂核心肠道微生物群落结构，增加了中肠抗菌肽基因的表达。这些研究结果表明，暴露于 MCT 会激活蜜蜂肠道的免疫反应，而大脑则不会表现出免疫反应，反而会出现氧化应激。这项研究为今后探索 MCT 与其他昆虫之间相互作用的研究提供了资源，有助于加深我们对 MCT 在生态系统中的潜在影响的理解。

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引用次数: 0