新型二酰胺类杀虫剂对鱼尼丁受体作用的分子机理

最近发现了一类新型二酰胺类杀虫剂——氟虫酰胺和氯虫酰胺,其作用靶标是鱼尼丁受体 (ryanodine receptors, RyRs)。本文对RyR的结构与功能、电压门控钙离子通道和鱼尼丁受体钙离子释放通道对细胞质钙离子内环境稳定的调节以及二酰胺类杀虫剂对RyRs作用的分子机理进行综述。二酰胺类杀虫剂使昆虫RyR通道处于持续的开放状态,引发钙离子从肌质网腔内大量释放,破坏了细胞质钙离子内环境的稳定,从而产生不同的药物学特性。这些变化都是由一个不同于鱼尼丁在RyR上的结合部位介导的。该类杀虫剂的作用对昆虫RyR s是高度专一的,结果产生选择毒性。由于二酰胺类杀虫剂的结构独特,作用方式新颖,对鳞翅目害虫效果好、杀虫谱广,对各种益虫和天敌安全,并对现用的杀虫剂无交互抗性,故它们非常适合于抗性治理和IPM。     

昆虫抗药性和昆虫毒理动力学(英文)

不断地使用一种杀虫药剂防治昆虫,会导致昆虫产生抗药性。对昆虫抗药性资料进行广泛综述时,发现了仅单独的解毒作用不能被解释为家蝇对有机氯杀虫药剂产生高抗性原因。作为一个基因。家蝇可以对有机氯产生比对有机磷杀虫剂更高的抗药性,尽管有机磷杀虫剂一般在虫体内是不太稳定的。考虑到昆虫毒理的动力学,杀虫药剂的穿透作用更显示出其实际的重要性。根据穿透和解毒的速率,慢的穿透作用是解毒作用的一个限制因子。防治敏感和抗性昆虫的观察结果,可以划出物理和生物因子之间关系的几种相关曲线图解。这些相关性不仅能说明家蝇对有机磷和有机氯杀虫剂的抗性程度,而且也助于选择出新的杀虫毒剂。     

INSECT RESISTANCE TO INSECTICIDES AND DYNAMICS OF INSECT TOXICOLOGY

Abstract  In field control of insects with insecticides, insects could develop different degrees of resistance. When resistance data were reviewed more extensively, it was found that detoxication alone cannot explain very high resistance of house flies to OC1 (organochlorine) insecticides. As a group, flies can develop much higher resistance to OC1 than to OP (organophosphorus) insecticides. although OPs are generally less stable in insects. With the consideration of the dynamics of insect toxicology. one can readily realize the importance of penetration. Based on the rates of penetration and detoxication. slow penetration is a limiting factor for detoxication. To further explain the observed results on the control of S (susceptible) 'and R (resistant) insects, several correlation curves were plotted. on the relationship between physical and biological factors. These relationships not only indicate approximate degrees of resistance of flies to OPs and OCls, but also help select new toxicants. For example, fast speed of action index of insecticides can produce lower resistance, and the analysis of the joint action of insecticides helps evaluate the types (same or different) of mode of action for controlling resistant insects.     

Management of insecticides for use in disease vector control: Lessons from six countries in Asia and the Middle East

Interventions to control the vectors of human diseases, notably malaria, leishmaniasis and dengue, have relied mainly on the action of chemical insecticides. However, concerns have been raised regarding the management of insecticides in vector-borne disease-endemic countries. Our study aimed to analyze how vector control insecticides are managed in selected countries to extract lessons learned.A qualitative analysis of the situation of vector control insecticides management was conducted in six countries. Multi-stakeholder meetings and key informer interviews were conducted on aspects covering the pesticide lifecycle. Findings were compared and synthesized to extract lessons learned. Centrally executed guidelines and standards on the management of insecticides offered direction and control in most malaria programs, but were largely lacking from decentralized dengue programs, where practices of procurement, application, safety, storage, and disposal were variable between districts. Decentralized programs were better at facilitating participation of stakeholders and local communities and securing financing from local budgets. However, little coordination existed between malaria, visceral leishmaniasis and dengue programs within countries. Entomological capacity was concentrated in malaria programs at central level, while dengue and visceral leishmaniasis programs were missing out on expertise. Monitoring systems for insecticide resistance in malaria vectors were rarely used for dengue or visceral leishmaniasis vectors. Strategies for insecticide resistance management, where present, did not extend across programs or sectors in most countries. Dengue programs in most countries continued to rely on space spraying which, considering the realities on the ground, call for revision of international guidelines.Vector control programs in the selected countries were confronted with critical shortcomings in the procurement, application, safety measures, storage, and disposal of vector control insecticides, with implications for the efficiency, effectiveness, and safety of vector control. Further international support is needed to assist countries in situation analysis, action planning and development of national guidelines on vector control insecticide management.     

USING FILTER PAPER TEST FOR DETECTING INHIBITORY FREQUENCY OF ORGANOPHOSPHATE TO ESTERASES IN COTTON APHIDS, APHIS GOSSYPII (GLOVER)

Abstract The individual esterase activity which is measured by filter paper test (FPT) method may determine the resistance of cotton aphids Aphis gossypii (Glover) against organophosphorus (OP) insecticides. For testing accurately resistant level caused by different insecticides, we applied FPT method for measuring inhibitory action of methyl-parathion, monocrotophos and omethoate to α-NA esterase of individual cotton aphids, and compared the inhibitory frequencies of these three insecticides to susceptible population (BCA) and resistant population (GCA). Results showed that their inhibitory frequencies of the susceptible population were evidently higher than that of the resistant population. The inhibitory rate of α-NA esterase in F1 generation individual cotton aphids by monocrotophos was low when the cotton aphid population had been treated in advance with monocrotophos, but it got to 75%-90% when the cotton aphid population had been untreated in advance with monocrotophos. Besides, the differences in esterase activity were not obvious between them. In same region when cotton aphids were treated with insecticides the inhibitory frequency of esterases in individual by the insecticides was lower than counterparts in individual cotton aphids which were not treated with insecticides. All these demonstrated that inhibitory frequency of α-NA esterase in individual cotton aphids by OP insecticides could be used as a technique of forecasting pest resistance.     

Genetics and evolution of resistance to insecticides

The evolution of resistance to insecticides has become a serious problem world-wide. It is important to identify patterns of insecticide use whereby insecticides can be used in integrated pest management programmes to help control insect numbers, but in such a manner that the evolution of resistance to insecticides will be retarded. The principal mechanisms of insecticide action and of resistance to these are reviewed. Some generalizations that can be made about the evolution of resistance are examined. In general, to control resistance it appears better to use an intense dose of non-persistent pesticides over a circumscribed area. Some features of the problem where population genetics and evolutionary theory might contribute to controlling resistance are discussed.     

昆虫离子通道及其抗药性研究进展

昆虫细胞膜离子通道是多种杀虫剂的作用靶标,通道功能特性的变异等与害虫抗药性密切相关.电压钳及膜片钳等电生理技术在离子通道功能研究中具有独特优势,在杀虫剂作用机理及害虫抗性机理研究中越来越受到重视.昆虫细胞膜离子通道主要包括配体门控通道和电压门控通道两大类.配体门控通道主要包括乙酰胆碱受体、GABA和谷氨酸受体通道等.电压门控通道主要有钠、钾和钙通道等,其中钠通道研究成果较多,与害虫抗性关系密切.由于钙离子的重要生理功能,随着研究深入,钙通道将成为研究重点.     

Towards the understanding of tetrahydroquinolines action in Aedes aegypti: larvicide or adulticide?

Aedes aegypti is an important vector of arboviruses such as dengue, yellow fever, chikungunya and Zika. Among the various types of insecticides used to combat this vector, the insect growth regulators have been developed and recommended for control of their larvae. In this work compounds with proven regulatory action, tetrahydroquinolines will be studied. These regulators act on the hormones responsible for the insect development. Ecdysone, one of the main hormones involved in this process has a specific receptor (EcR), where tetrahydroquinolines derivatives can bind, disrupting the normal action of this hormone, because they have structure similar to hormone 20-hydroxyecdysone (20E). In addition, studies show that this class of compounds interacts strongly in the potassium channel activated by calcium (BK channel). Thus, the goal is to study the action of compounds (tetrahydroquinolines) as insecticides and evaluate their larvicidal action (action on the ecdysone receptor) or adulticide (action on the BK channel) through homology modelling techniques, molecular docking and molecular dynamics simulations and aiming to propose a compound that presents both actions (larvicide / adulticide).     

Mode of action of triflumezopyrim: A novel mesoionic insecticide which inhibits the nicotinic acetylcholine receptor

Triflumezopyrim, a newly commercialized molecule from DuPont Crop Protection, belongs to the novel class of mesoionic insecticides. This study characterizes the biochemical and physiological action of this novel insecticide. Using membranes from the aphid, Myzus persicae, triflumezopyrim was found to displace ³H-imidacloprid with a K_i value of 43 nM with competitive binding results indicating that triflumezopyrim binds to the orthosteric site of the nicotinic acetylcholine receptor (nAChR). In voltage clamp studies using dissociated Periplaneta americana neurons, triflumezopyrim inhibits nAChR currents with an IC₅₀ of 0.6 nM. Activation of nAChR currents was minimal and required concentrations ≥100 μM. Xenopus oocytes expressing chimeric nAChRs (Drosophila α2/chick β2) showed similar inhibitory effects from triflumezopyrim. In P. americana neurons, co-application experiments with acetylcholine reveal the inhibitory action of triflumezopyrim to be rapid and prolonged in nature. Such physiological action is distinct from other insecticides in IRAC Group 4 in which the toxicological mode of action is attributed to nAChR agonism.Mesoionic insecticides act via inhibition of the orthosteric binding site of the nAChR despite previous beliefs that such action would translate to poor insect control. Triflumezopyrim is the first commercialized insecticide from this class and provides outstanding control of hoppers, including the brown planthopper, Nilaparvata lugens, which is already displaying strong resistance to neonicotinoids such as imidacloprid.     

Bacteriological larvicides of dipteran disease vectors.

The apparent success in vector control observed between 1950 and 1970 was followed by worldwide resistance to organosynthetic insecticides wherever they were used intensively. Insect resistance to one or more categories of insecticides has limited the effectiveness of these compounds, and their non-selective mode of action adversely affects non-target organisms. This scenario highlights the need for selective agents in integrated vector control programs. This article gives an overview of the main fundamental and applied research topics on entomopathogenic bacteria in relation to their role in vector control.     

几种杀虫剂对棉铃虫头部酯酶的联合抑制作用

测定了几种药剂及其组合对棉铃虫Helicoverpa armigera头部酯酶活性的独立与联合抑制作用。结果显示：久效磷、敌百虫、呋喃丹对酯酶活性抑制中浓度分别为:2.4443×10^-6、3.4562×10^-7、2.6302×10^-5mol/L。药代动力学分析结果显示:久效磷与呋喃丹对酯酶抑制方式为竞争性抑制,敌百虫为非竞争性抑制。久效磷+敌百虫与敌百虫+呋喃丹两种药剂组合处理后,对酯酶抑制均增强,抑制中浓度分别为:1.0846×10^-6、5.1786×10^-6mol/L,对酯酶的抑制作用属非竞争性抑制作用。而久效磷+呋喃丹组合对酯酶抑制活性相加,为竞争性抑制作用。结果说明杀虫剂与酯酶的药代动力学互作对混剂的酯酶的抑制作用方式和活性具有重要影响。     

Aryl Hydrocarbon Hydroxylase Induction by Polycyclic Hydrocarbons: Simple Autosomal Dominant Trait in the Mouse

MANY mixed function¹ oxygenases are membrane-bound multicomponent enzyme systems which require NADPH and molecular oxygen for the oxidative metabolism of polycyclic hydrocarbons, drugs and insecticides, as well as numerous lipophilic endogenous substrates^2–4. Any day to day fluctuations in these enzyme activities may therefore influence the intensity and duration of drug action and also the rate of metabolism of chemical carcinogens, insecticides and many normal body substrates.     

Efficacy of mosquito nets treated with a pyrethroid-organophosphorous mixture against Kdr- and Kdr+ malaria vectors (Anopheles gambiae)

In order to prevent the resistance of Anopheles gambiae s.l. to pyrethroids from spreading too quickly and to lengthen the effectiveness of insecticide impregnated mosquito nets, it has recently been suggested to use mixtures of insecticides that have different modes of action. This study presents the results obtained with tulle mosquito nets treated with bifenthrin (a pyrethroid) and chlorpyrifos-methyl (an organophosphorous) both separately and in mixture on two strains of An. gambiae, one sensitive to all insecticides, and the other resistant to pyrethroids. The values of KDt50 and KDt95 and the mortality induced with the mixture of bifenthrin (25 mg/m2) and chlorpyrifos-methyl (4.5 mg/m2) show a significant synergistic effect on the strain of An. gambiae susceptible to insecticides. However, the tested combination does not induce any synergistic effect on the VKPR strain selected with permethrin, but only enhances the effectiveness of the two insecticides taken separately.     

TESTS OF SYNERGISM BETWEEN NICOTINE AND THE PYRETHRINS

Synergism between nicotine and pyrethrum applied by injection to adult Oncopeltus fasciatus Dal. has been reported by Turner (1951).
When these insecticides were applied alone and as a mixture to adult Tribolium castaneum Hbst., using a dipping technique, the data indicated that independent joint action occurred. Similar action could be eliminated because the two insecticides had varying relative potency.
Since the effect of the pyrethrins has been short-lived in some insects, it was postulated that the absence of synergism might be caused by failure of the nicotine to reach a site of action while the pyrethrins were still acting.
Application of nicotine, followed later by treatment with pyrethrins, gave evidence of synergism. A test in which the interval between treatments was varied from ¾ to 6 hr. showed that toxicity was greatest with the shortest interval between applications, and evidence of synergism had practically disappeared after 6 hr. The maximum amount of synergism observed was about twofold.     

Toxicity of thiamethoxam and mixtures of chlorantraniliprole plus acetamiprid, esfenvalerate, or thiamethoxam to neonates of oriental fruit moth (Lepidoptera: Tortricidae)

To assess the toxicity ofthiamethoxam and three mixtures of insecticides to oriental fruit moth, Grapholita molesta (Busck) (Lepidoptera: Tortricidae), we added the insecticides to diet and fed it to neonates of two laboratory colonies; mortality was assessed after 96 h. Thiamethoxam was much less toxic than insecticides previously tested. Five of six analyses of the joint action of chlorantraniliprole plus acetamiprid, esfenvalerate, or thiamethoxam indicated that toxicity was not independent and not correlated. For chlorantraniliprole plus acetamiprid, mortality was slightly lower than expected at low concentrations and greater than expected at high concentrations. For chlorantraniliprole plus esfenvalerate, mortality was less than expected at nearly all concentrations, suggesting antagonism despite the two compounds' different modes of action. For chlorantraniliprole plus thiamethoxam, observed mortality exceeded expected mortality at low concentrations, but this trend did not continue at higher concentrations. Although the null hypothesis of independent and uncorrelated toxicity was rejected for chlorantraniliprole plus acetamiprid and chlorantraniliprole plus thiamethoxam in three of four analyses, differences between observed and expected mortality were minor and inconsistent over the range of concentrations tested. We do not expect these mixtures to exhibit significant synergism or antagonism in the field. Apparent antagonism between chlorantraniliprole and esfenvalerate is particularly relevant because these insecticides (or chlorantraniliprole plus a different pyrethroid) may be used together in apples or peaches for control of oriental fruit moth and hemipteran pests. The effectiveness of each insecticide against oriental fruit moth might be reduced in such applications.     

Interference by DDT and cyclodiene types of insecticides with chloroplast-associated reactions

The effects of DDT, some of its analogs, and selected cyclodiene insecticides on isolated spinach (Spinacea oleracea L.) thylakoids were identified, characterized, and compared to responses induced by selected herbicides. Except for endrin, the insecticides inhibited light-induced electron transport, altered chlorophyll fluorescence transients, and competitively displaced [14C]atrazine [2-chloro-4-(ethylamino)-6-(isopropylamino)-s-triazine], a known photosystem II inhibitor, from the membranes. The insecticides appeared to act at, or near B, the secondary electron acceptor of photo-system II. Binding of DDT and dieldrin was estimated at 900 and 2200 molecules, respectively, per photosynthetic unit (490 chlorophyll molecules). The insecticides also inhibited valinomycin-induced swelling of the thylakoid membrane. Whereas inhibition of electron transport can be attributed to interaction by the insecticides with a proteinaceous component of the thylakoid membrane, interference with the action of valinomycin may involve interaction with lipoidal constituents of the membrane.     

Review of entomopathogenic fungi and nematodes as biological control agents of tephritid fruit flies: current status and a future vision

Several fruit fly species (Diptera: Tephritidae) are invasive pests that damage the quality of fruits in horticultural crops and cause significant value losses worldwide. Management of fruit flies mainly depends on conventional insecticides. Unfortunately, the application of synthetic insecticides has caused environmental pollution, risks for humans and animals, and development of resistance. Furthermore, controlling fruit flies by applying synthetic insecticides is challenging because fruit containing third instars often fall from the tree – subsequently the larvae leave the decaying fruits and pupate in the soil. Consequently, both larvae and pupae are protected from surface-applied insecticides in fruits and soil. So, there is a pressing need for more eco-friendly and selective control measures with new modes of action. Among such measures are entomopathogenic fungi (EPFs) and nematodes (EPNs). I gathered knowledge on past and present research about EPFs and EPNs as biocontrol agents against fruit flies to investigate approaches that may improve their capacities. I also highlighted several recommendations that may help future field studies on the suppression of fruit fly populations by EPFs and EPNs.     

昆虫钠离子通道的研究进展

昆虫只有一个或两个电压门控钠离子通道α亚基基因,但两种转录后修饰(选择性剪切和RNA编辑)实现了昆虫钠离子通道的功能多样性.昆虫β辅助亚基TipE和TEH1-4在钠离子通道表达和调控中也起着重要作用.电压门控钠离子通道在动作电位的产生和传递中至关重要,是多种天然和人工合成神经毒素及杀虫剂的作用靶标,包括广泛使用的拟除虫...