昆虫激肽的生理功能及机制

昆虫激肽是一类高度保守的小分子神经活性物质,自其从马德拉蟑螂脑中分离得到至今,人们在多种无脊椎动物体内均发现了这一激肽家族成员。它们具有促进昆虫后肠收缩、马氏管扭动、原尿分泌,调节血淋巴量和水盐平衡,使马氏管跨膜电位去极化,抑制昆虫体内消化酶释放、幼虫体重增长等功能。然而,天然的昆虫激肽很容易被蛋白酶所降解,因此须对其进行结构改造及构效关系研究,以开发出更有潜力的假肽和非肽模拟抗酶解昆虫激肽类似物,对今后实现环境友好型害虫防治策略具有重要意义。     

Synthesis and diuretic activities of pseudoproline‐containing analogues of the insect kinin core pentapeptide

C‐2 dimethylated/unmethylated thiazolidine‐4‐carboxylic acid and C‐2 dimethylated oxazolidine‐4‐carboxylic acid were introduced into the insect kinin core pentapeptide in place of Pro³, yielding three new analogues. NMR analysis revealed that the peptide bond of Phe²‐pseudoproline (ΨPro)³ is practically 100% in cis conformation in the case of dimethylated pseudoproline‐containing analogues, about 50% cis for the thiazolidine‐4‐carboxylic acid analogue and about 33% cis for the parent Pro³ peptide. The diuretic activities are consistent with the population of cis conformation of the Phe²‐ΨPro³/Pro³ peptide bonds, and the results confirm a cis Phe‐Pro bond as bioactive conformation. Copyright © 2011 European Peptide Society and John Wiley & Sons, Ltd.     

An active insect kinin analog with 4-aminopyroglutamate, a novel cis-peptide bond, type VI beta-turn motif

The insect kinins are potent diuretic peptides that preferentially form a cis-Pro, type VI beta-turn. An insect kinin analog containing (2S,4S)-4-aminopyroglutamate, a novel cis-peptide bond, type VI beta-turn motif, demonstrates significant activity in the physiological range in a cricket diuretic assay. This is the first instance of a 4-aminopyroglutamate analog of a peptide with a preference for a type VI turn that demonstrates significant bioactivity. The results provide further confirmatory evidence for the active conformation of the insect kinins, and a new scaffold with which to design biostable, peptidomimetic analogs capable of disrupting critical insect kinin-regulated processes in insects.     

A study of dihydrogen bond interactions through three-centre bond and group indices

We report here an investigation into the correlation between dihydrogen bond energies, three-centre bond indices and group indices in some dihydrogen-bonded dimers. This kind of bond is generated by interaction between proton-donator and proton-acceptor groups, XH^σ+…H′^σ ? M, where X is a more electronegative atom and M a less electronegative atom than hydrogen. The different electronegativities of the X atoms, as well the M atoms, would affect the correlations between H^σ+…H′^σ ?  distances and bond energies of these systems. In this work it will be shown that three-centre bond indices and group indices exhibit a better correlation with bond energies when compared to H^σ+…H′^σ ?  distances for this kind of system.     

Insect kinin mimics act as potential control agents for aphids: Structural modifications of Trp4

Insect kinins are endogenous, biologically active peptides with various physiological functions. The use of insect kinins in plant protection is being evaluated by many groups. Some kinins have been chosen as lead compounds for pest control. We previously reported an insect kinin mimic IV-3 that had insecticidal activity. And by introducing a strong electron withdrawing group (-CF₃) on the benzene ring (Phe²), we discovered a compound, L ₇ , with better activity than lead IV-3 . In this work, taking L ₇ as the lead compound, we designed and synthesized 13 compounds to evaluate the influence of position 4 (Trp⁴) of insect kinin on insecticidal activity, by replacing the H atom on tryptophan with -CH₃ and -Cl or substituting the indole ring of tryptophan with the benzene, naphthalene, pyridine, imidazole, cyclohexane, and alkyl carboxamides. The aphid bioassay results showed that the compounds M ₁ , M ₃ , and M ₅ were more active than the positive control, pymetrozine. Especially, replacing the side chain by an indole ring with 4-Cl substitution ( M ₁ , LC₅₀ = 0.0029 mmol/L) increased the aphicidal activity. The structure–activity relationships (SARs) indicated that the side chain benzene ring at this position may be important to the aphicidal activity. In addition, the toxicity prediction by Toxtree, and the toxicity experiments on Apis mellifera suggested that M ₁ was no toxicity risk on a non-target organism. It could be used as a selective and bee-friendly insecticide to control aphids.     

一种用于昆虫性信息素成分单不饱和双键定位的简便方法

昆虫利用特定的性信息素成分实现种内信息交流和种间生殖隔离,性信息素成分异构体的细微差异都能导致其生物活性的很大改变。本研究利用二甲基二硫醚（DMDS）甲硫基化反应和气相色谱-电子轰击质谱（GC-EI-MS）的方法对脂肪族单不饱和醇、醛和乙酸酯类昆虫性信息素成分双键在碳链中的位置异构进行系统研究。质谱分析结果表明,含有醇和乙酸酯官能团的单不饱和烯烃甲硫基化衍生物的质谱特征碎片分子离子峰（M+）及2个主要的诊断离子m/z 61+14m ［H-（CH₂）_m-CH=S⁺ CH₃］和77+14n［CH₃S⁺ =CH（CH₂）_nOH］（或119+14n,［CH₃S⁺ =CH（CH₂）_nOOCCH₃］）丰度都很强,可以据此直接推断双键在碳链中的位置。尽管单不饱和醛类化合物DMDS衍生物的特征碎片峰也很明显,但是由于羰基的质量数和2个亚甲基的质量数相同,不能由低分辨质谱的特征碎片峰直接推断双键在碳链中的位置。DMDS甲硫基化反应结合GC-EI-MS分析方法鉴定昆虫性信息素成分单不饱和双键在碳链中的位置异构,该方法简单快捷,为昆虫性信息素的结构鉴定工作奠定了坚实的基础。     

Impact of lek mating on the sterile insect technique: A modeling study

Modelling studies are presented which describe the effect of lek mating on the control of a wild population by sterile male release. The mixed leks are assumed to follow a Poisson-binomial distribution and the system includes three parts: territory defense, matings inside a lek and matings outside a lek. The effects of parameters on the hatchability are discussed. Among the parameters, sterile type effect (W_s), female choice (f_s) and mating competitiveness (C_m) are the most important. The application to determining the effects of sterile male release and on the proportion of sterile males required for eradication are also discussed.     

Determination of disulfide bond arrangement in bombyxin-IV, an insulin superfamily peptide from the silkworm,Bombyx mori, by combination of thermolysin digestion of natural peptide and selective synthesis of disulfide bond isomers

The mode of disulfide linkages in bombyxin-IV, an insulin superfamily peptide consisting of A- and B-chains, was determined as A6–A11, A7–B10, and A20–B22. An intermolecular bond of A20–B22 was identified by sequencing and mass spectrometric analysis of the fragments generated by thermolysin digestion of natural bombyxin-IV. The mode of the remaining two bridges was determined by chemical and selective synthesis of three possible disulfide bond isomers of bombyxin-IV. A- and B-chains were synthesized by solid-phase method, and three disulfide bonds were bridged stepwise and in a fully controlled manner. Retention time on reversed-phase high-performance liquid chromatography (HPLC), thermolysin digests, and biological activity of the synthetic [A6–A11, A7–B10, A20–B22-cystine]-bombyxin-IV revealed that it was identical with the natural bombyxin-IV. Two other isomers with respect to disulfide bond arrangement, [A6–A7, A11–B10, A20–B22-cystine]- and [A6–B10, A7–A11, A20–B22-cystine]-bombyxin-IVs, were distinguishable from the natural one by use of HPLC, thermolysin digestion, and bioassay.     

Excitable properties of insect neurones in culture: A developmental study

The passive and excitable electrical properties of cockroach neurones growing in vitro have been investigated using intracellular recording techniques. The resting membrane potentials of the neurones are similar to those of their in vivo counterparts but the input resistances and membrane capacitive properties are more typical of embryonic insect neurones. During the first 12 days of growth in vitro the neurones exhibit delayed rectification in response to the injection of depolarising current steps. After this period “all or none” action potentials can be evoked by depolarising pulses in approximately half of the neurones tested. These spikes are abolised by 1 μM tetrodotoxin but are unaffected by 5 mM Co²⁺. Spontaneous excitatory activity develops in approx 25% of the neurones after 3 weeks in culture.     

Synthetic formyl-methionyl chemoattractants: A conformation-activity study of oxidized tripeptides

The two diastereomeric sulphoxides and the sulphone derived from the formyl-methionyl tripeptide chemoattractant CHO-L-Met-L-Leu-L-Phe-OMe have been synthesized and fully characterized. The diastereomeric sulphoxide tripeptides have been separated at the stage of their N-tert-butyloxycarbonyl synthetic precursors. All of the oxidized sulphur derivatives induce secretion of granule enzymes with ED₅₀s from 1–2×10⁻⁹ M with no significant differences in activity among them. They are also active to the same relative extent in inducing chemotaxis. In parallel, a solution conformational analysis has been performed in solvents of widely different polarities and capabilities of H-bond formation using circular dichroism, infrared absorption and ¹H nuclear magnetic resonance. No significant propensity for formation of intramolecularly (C=O…H-N) H-bonded folded forms has been detected in any of the four tripeptides. Intermolecular S=O…H-N interactions are postulated to tentatively explain the ¹H nuclear magnetic resonance behavior of the Met and, particularly, Leu NH resonances of the two sulphoxide tripeptides in CDCl₃ solution. The biological and conformational data agree with the recently proposed model of the chemotactic peptide receptor of rabbit neurotrophils, which involves the extended backbone of the integrity of the Met side-chain sulphide sulphur atom as a corollary point of ligand interaction.     

风洞技术在昆虫化学通讯研究中的应用

综述了昆虫化学生态学中所使用的风洞技术。内容包括风洞的构造 ,风洞的工作条件 ,风洞操作中的技巧和数据采集 ,昆虫在风洞中表现出的典型行为特征以及一些需要注意的问题     

线粒体DNA序列特点与昆虫系统学研究

昆虫线粒体DNA是昆虫分子系统学研究中应用最为广泛的遗传物质之一。线粒体DNA具有进化速率较核DNA快 ,遗传过程不发生基因重组、倒位、易位等突变 ,并且遵守严格的母系遗传方式等特点。本文概述了mtDNA中的rRNA、tRNA、蛋白编码基因和非编码区的一般属性 ,分析了它们在昆虫分子系统学研究中的应用价值 ,以及应用DNA序列数据来推导分类阶 (单 )元的系统发育关系时 ,基因或DNA片段选择的重要性     

昆虫谷胱甘肽S-转移酶蛋白纯化技术研究

昆虫谷胱甘肽S-转移酶蛋白纯化的主要方法是沉淀法、层析法和电泳法。沉淀法是在进行柱层析前常使用的一种方法,但是其纯化倍数较低。层析法纯化倍数较高,但其费用也较高。电泳通常是作为一种辅助方法来使用。利用这些方法,谷胱甘肽S-转移酶蛋白最高纯化倍数为1138倍(马素永等利用层析法和电泳法对亚洲玉米螟谷胱甘肽S-转移酶蛋白进行纯化)。文章讨论了昆虫谷胱甘肽S-转移酶蛋白纯化研究的应用。     

杭州地区猪尸体上昆虫群落的组成 与演替的初步观察

对杭州地区猪尸体的腐败过程及尸体上昆虫群落的演替规律,进行了初步观察和研究。结果表明,室外地表上猪尸体的腐败过程可以划分为新鲜、肿胀、腐烂、干化和残骸5个连续的阶段;常见昆虫包括3目、19科、33种,其中双翅目的巨尾阿丽蝇、丝光绿蝇、南岭绿蝇、大头金蝇、肥须亚麻蝇等为优势种。尸体上昆虫群落的演替有明显的时间规律可循。许多昆虫类群的出现时间与尸体腐败阶段有明确的对应关系,这种对应关系可以为法医科学中推测死后间隔时间(postmortem interval, PMI)提供依据。     

蔬菜害虫及其天敌昆虫群落多样性和相关性研究

在比较脆弱的菜田生态系统中,蔬菜害虫和天敌如果没有人为防治的干扰,天敌群落和害虫群落在结构上有动态的消长规律。江淮地区蔬菜害虫主要为菜缢管蚜(Brevicoryae brassicae)、瓜绢螟(Diaphania indica)、朱砂叶螨(Tetranychus cinnabarinus)及桃蚜(Myzus persicae)等;昆虫天敌主要为异色瓢虫(Harmonia axyndis)、广赤眼蜂(Trichogramma evanescens)及七星瓢虫(Coccinella septempunctata)等。8月下旬～9月下旬,菜田昆虫种类丰富、个体发生量大,多样性指数及均匀度指数较大。经典型相关分析,蔬菜害虫和天敌群落间典型相关系数达极显著水平,其中载荷较大的指标为多样性指数和均匀度,即两个群落结构间的相关,主要是多样性指数和均匀度的相关。     

昆虫界的“四不象”——一新建“螳目”昆虫简介

该文对 2 0 0 2年 5月建立的昆虫新目———螳目Mantophasmatodea作了简单介绍 ,并建议了该目之中名。该目是昆虫纲中最小的目 ,目前已知 2属 3种 ,分布于非洲     

Comparison of insect kinin analogs with cis-peptide bond, type VI-turn motifs identifies optimal stereochemistry for interaction with a recombinant arthropod kinin receptor from the southern cattle tick Boophilus microplus

The multifunctional 'insect kinins' share the evolutionarily conserved C-terminal pentapeptide motif Phe-X1-X2-Trp-Gly-NH2, where X1=His, Asn, Ser, or Tyr and X2=Ser, Pro, or Ala; and are associated with the regulation of diuresis in a variety of species of insects. We previously reported the functional expression of a southern cattle tick (Boophilus microplus) G protein-coupled receptor that is activated by insect kinins. Four different stereochemical variants of each of the 4-aminopyroglutamic acid (APy) and tetrazole moieties, mimics of a cis-peptide bond, type VI beta-turn in insect kinins were now evaluated on the expressed tick receptor using a calcium bioluminescence plate assay. This study represents the first investigation of the interaction of restricted-conformation analogs incorporating components that mimic specific conformations and/or peptide bond orientations in an expressed arthropod neuropeptide receptor. Analog Ac-RF[APy]WGa (2R,4S) was at least 10-fold more active than the other analogs, thus identifying the optimal stereochemistry for tick receptor interaction. The optimal stereochemistry for the tetrazole insect kinin analogs in the tick receptor assay was identified as (D,L). The APy is superior to the tetrazole as a scaffold for the design of mimetic insect kinin analogs. These biostable analogs provide new tools for arthropod endocrinologists and potential leads in the development of selective, environmentally friendly arthropod pest control agents capable of disrupting insect kinin regulated processes.     

A structure-activity study on the bradykinin B1 antagonist desArg10-HOE 140: The alanine scan

It has recently been shown that the biological activity of the second generation kinin B1 receptor selective antagonist, desArg10 HOE 140, can be improved by specific amino acid substitutions. Starting from this observation, we undertook a systematic structure-activity relationship study of this antagonist, based on the alanine-scan technique, in order to obtain useful information for the rational design of more analogues. Our data indicate that the sequence of desArg10 HOE 140 does not tolerate the replacement by Ala of most of its residues, with the exception of Ser in position 7 and, to a lesser extent, D-Arg in position 1 and Hyp in position 4. The most critical residues appear to be Pro in position 3 and the C-terminal dipeptide DTic-Oic; Ala replacement at these positions resultes in a total loss of activity. Moreover, replacement by Ala of Gly in position 5 reverts the activity of desArg10 HOE 140 to that of an agonist.     

浙江宁波镇海工业园区昆虫多样性研究

于2008年7-11月,对宁波镇海工业园区的昆虫群落多样性进行调查,选取林地、农田、人工苗圃、生态园和工厂区5种具有代表性的生境类型,每月对该地区的昆虫种类及数量进行抽样统计和数据分析.结果表明:该地共有昆虫284种,分属13目108科,其中优势类群为同翅目、直翅目、半翅目、鞘翅目和鳞翅目.在不同功能类群中,从个体数看...