Mode of action of methoprene in affecting female reproduction in the African malaria mosquito,Anopheles gambiae

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     

昆虫神经肽类激素的研究及应用前景

由昆虫脑神经内分泌细胞分泌的神经肽类激素 ,咽侧体活化激素 (allatotropin ,AT)和咽侧体抑制激素 (al latostatin ,AS) ,分别刺激或抑制咽侧体的保幼激素的生物合成 ,从而控制昆虫的生长、发育和变态。利用昆虫神经内分泌的失调 ,使其体内激素水平失调 ,来达到控制害虫的目的。     

喜树碱对小菜蛾体内保幼激素及蜕皮激素滴度的影响

为明确喜树碱对小菜蛾Plutella xylostella生长发育的抑制作用及其机制,设置0.5、1.0、2.0mg/m L剂量处理其3龄幼虫,采用浸叶饲喂法和高效液相色谱法测定了喜树碱对小菜蛾体内蜕皮激素和保幼激素滴度的影响。结果显示,喜树碱各剂量处理均显著抑制了小菜蛾幼虫的生长发育,抑制率最高达到28.42%;各处理小菜蛾化蛹时间均延迟,异常蛹增多,羽化率降低;其中2.0 mg/m L处理后4 d其化蛹率为6.67%,对照组化蛹率为86.60%。0.5、1.0 mg/m L处理下,小菜蛾体内蜕皮激素滴度显著低于对照组,仅为对照组的0.06倍;而保幼激素滴度增加,分别可达到28.74mg/m L和36.29 mg/m L,是对照组的9倍左右。表明喜树碱可影响小菜蛾体内蜕皮激素和保幼激素的平衡,延迟和影响了小菜蛾的正常发育进程,可实现对小菜蛾种群的控制作用。     

Effects of juvenile hormone analog formulations on development and reproduction in the bed bug Cimex lectularius (Hemiptera: Cimicidae)

BACKGROUND: Bed bugs (Cimex lectularius L.) have become a common insect pest in urban areas and are often difficult to manage. Eradication is made more problematic by widespread insecticide resistance, raising interest in alternative control products. Juvenile hormone analogs (JHAs) such as methoprene and hydroprene are relatively harmless to non‐arthropods and have proved to be effective against other urban insect pests. Two JHA products (Gentrol^® and Precor^®, Central Life Sciences, Schaumburg, IL) were tested for efficacy against various bed bug stages as direct spray and as dry residue using three bed bug strains. RESULTS: At 1× and 2× the label rate, Precor^® [active ingredient (S)‐methoprene] had no significant effect on the development or fecundity of bed bugs. At 2× the label rate, confinement to residues of Gentrol^® [active ingredient (S)‐hydroprene] had no significant effect, but residues at 3× and 10× the label rate caused a reduction in fecundity and impaired development. Field strains were more susceptible to the reproductive effects of (S)‐hydroprene than a long‐maintained laboratory strain. CONCLUSIONS: While JHAs are attractive alternatives for pest management because of their inherent safety and distinct mode of action, these JHA formulations would have little impact on bed bug populations without relabeling to allow for higher application rates. Copyright © 2012 Society of Chemical Industry     

Synthesis and juvenile hormone activity of benzimidazolylterpenes possessing a 2,7-dimethyloctane skeleton

Benzimidazolylterpenes, possessing a 2,7-dimethyloctane skeleton showed IGR-activity on pupae of Tenebrio molitor L in laboratory tests: N-(7-methoxy-2,7-dimethyl-2-octenyl)benzimidazole showed the greatest activity.     

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

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。     

七星瓢虫保幼激素环氧水解酶基因克隆及表达分析

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。     

Gerry Brooks and epoxide hydrolases: four decades to a pharmaceutical

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.     

Juvenile hormone III, hydroprene and a juvenogen as soldier caste differentiation regulators in three Reticulitermes species: potential of juvenile hormone analogues in termite control

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.     

Juvenile hormonal activity of mono- and polyenehomobenzenes in Drosophila virilis, Spodoptera frugiperda and Araschnia levana

A series of mono- and polyenehomobenzenes was synthesised by a highly regioselective palladium-catalysed allylic alkylation of substituted and unsubstituted benzylic Grignard reagents employing catalytic amounts of catalyst and tested for juvenile hormone activity on the fruit fly Drosophila virilis Sturtevant (Diptera: Drosophilidae), on an important agricultural pest species, the fall armyworm Spodoptera frugiperda JE Smith (Lepidoptera: Noctuidae), and on the map butterfly Araschnia levana L. (Lepidoptera: Nymphalidae). In D. virilis only polyenehomobenzenes with a geranyl chain and a methyl, methoxy or isopropyl group at the para position of the aromatic ring displayed significant juvenile hormonal activity at low doses. A monoenehomobenzene and polyenehomobenzenes with longer allylic chains or without a substituted aromatic ring were not active. In S. frugiperda and in A. levana, a mono-, a di- and a tetraene displayed juvenile hormonal activity. In the lepidopteran species, a trend for the necessity of a substitution at position 4 of the phenyl group for high juvenile hormonal activity was also found.     

黏虫保幼激素环氧水解酶基因MsJHEH2的克隆与生物学功能

保幼激素环氧水解酶（juvenile hormone epoxide hydrolase,JHEH）是调控保幼激素（juvenile hormone,JH）滴度的重要降解酶。本文在黏虫体内克隆得到一条具有EHN环氧水解酶超家族结构域的保幼激素环氧水解酶MsJHEH2基因cDNA序列（GenBank登录号：MT802192）,长度1533 bp,开放阅读框（ORF）为1389 bp,编码462个氨基酸,推测分子量和等电点分别为52.42 kDa和7.07。表达模式分析发现,MsJHEH2在黏虫各个龄期与组织中均有表达,其中在蛹期和中肠中表达量最高。RNA干扰处理4龄幼虫6 h后的基因沉默效率最高,为64.86%,此时黏虫体内JH滴度上升为对照的1.58倍。该基因沉默后对黏虫无明显致死作用,但导致其蛹历期延长、羽化率降低。本研究表明MsJHEH2可以通过调节JH含量进而影响黏虫生长发育进程。