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1.
Detoxification by cytochrome P450 monooxygenases is an important mechanism involved in pesticide resistance in insects and mites. The activity of these enzymes can be induced by a variety of chemicals. The aim of this study was to evaluate the effect of six P450 inducers (phenobarbital, barbital, 3-methylcholanthrene, geraniol, isosafrole, pentamethylbenzene), known to have an inducing activity in insects and mammals, on the O-deethylation activity in the two-spotted spider mite Tetranychus urticae. Treatment with barbital, phenobarbital and geraniol resulted in a dose-dependent increase in activity. Neither 3-methylcholanthrene, isosafrole nor pentamethylbenzene were effective inducers. Time course studies showed that induction by geraniol and barbital started rapidly within a period of 1-4 h after initiation of the treatment, while maximal activity was reached within 4 and 48 h, respectively. In addition, it was shown that induction with xenobiotic compounds can alter the monooxygenase-mediated acaricide tolerance in a susceptible strain of T. urticae. Although barbital induced higher levels of P450 activity, geraniol proved to be a better compound to decrease toxicity of the tested acaricides.  相似文献   

2.
ABC转运蛋白及其相关的多药抗性研究现状   总被引:1,自引:0,他引:1  
ABC(ATP-binding cassette)转运蛋白是一类家族庞大、功能多样的跨膜转运蛋白,其广泛存在于原核和真核生物的各类细胞器中,负责多种物质的跨膜转运,从而调节生物体的一系列生命活动。近年来,越来越多ABC转运蛋白的种类及功能被报道,但是ABC蛋白家族的潜在成员以及功能仍然值得进一步探究和挖掘。该文对不同物种中ABC转运蛋白数量、结构域、功能、研究方法以及其参与调控病原菌多药抗性的研究现状进行综述,并对植物病原菌多药抗性的治理等进行展望。  相似文献   

3.
Transgenic Bt cotton expressing Cry1Ac is important in controlling various agricultural pests, including Helicoverpa armigera. Especially for transgenic crops that are cultivated in large expanses, avoiding resistance development is a key for ensuring sustainability of Bt technologies. Integrated pest management, in which transgenic crops are strategically combined with rational pesticide use, may help to prevent H. armigera resistance acquisition in Bt cotton. In this study, we evaluated the toxicity of a novel insecticide (chlorantraniliprole) on Cry1Ac-susceptible and resistant individuals of H. armigera. More specifically, we assessed the effect of chlorantraniliprole on the activity of two enzymes and conducted laboratory bioassays to determine its toxicity on H. armigera larvae. Chlorantraniliprole increased esterase and glutathione-S-transferase activities in Cry1Ac susceptible and resistant populations of H. armigera. Cry1Ac resistant populations XJ-F (Cry1Ac resistance ratio 21.8-fold), XJ-10.0 (95.8-fold) and BTR (3536.5-fold) did not show cross-resistance to chlorantraniliprole, with LC50 values of 0.0733 (μg/mL) in XJ-F, 0.0545 (μg/ml) in XJ-10.0 and 0.0731 (μg/mL) in BTR, which were close to that in the susceptible strain 96S (0.0954 μg/mL). Our work shows that chlorantraniliprole could be considered to be integrated in Bt cotton management schemes to delay the H. armigera resistance development.  相似文献   

4.
稻田常用农药对四地区二化螟盘绒茧蜂雌成蜂的触杀毒性   总被引:2,自引:1,他引:1  
为明确稻田常用农药对二化螟幼虫期优势寄生性天敌二化螟盘绒茧蜂Cotesia chilonis(Mat-sumura)的毒性,采用药膜法在室内测定了7种杀虫剂原药以及18种常用农药制剂对扬州、安吉、金华和乐清4个地区二化螟盘绒茧蜂雌成蜂的触杀毒性。结果表明,7种杀虫剂原药中氟虫腈、毒死蜱和三唑磷对该蜂毒性较高,杀虫单、吡虫啉和阿维菌素次之,氯虫苯甲酰胺则最低。12种杀虫剂制剂中20%氯虫苯甲酰胺悬浮剂和3种阿维菌素相关制剂对该蜂毒性相对较低,其余均具高毒性;4种杀菌剂中的异稻.三环唑对该蜂高毒,苯甲.丙环唑次之,井岗.蜡芽菌(井冈霉素)和盐酸吗啉胍.三氮唑核苷则毒性最低;2种除草剂中苄嘧.丙草胺毒性高于苄.二氯。此外,同一种药剂对不同地区雌蜂的毒性也有所不同。  相似文献   

5.
In Botrytis cinerea, multidrug resistant (MDR) strains collected in French and German vineyards were tested in vitro, at the germ-tube elongation stage, towards a wide range of fungicides. Whatever the MDR phenotype, resistance was recorded to anilinopyrimidines, diethofencarb, iprodione, fludioxonil, tolnaftate and several respiratory inhibitors (e.g., penthiopyrad, pyraclostrobin). In MDR1 strains, overproducing the ABC transporter BcatrB, resistance extended to carbendazim and the uncouplers fluazinam and malonoben. In MDR2 strains, overproducing the MFS transporter BcmfsM2, resistance extended to cycloheximide, fenhexamid and sterol 14α-demethylation inhibitors (DMIs). MDR3 strains combined the overexpression of both transporters and exhibited the widest spectrum of cross resistance and the highest resistance levels. The four transport modulators, amitriptyline, chlorpromazine, diethylstilbestrol, and verapamil, known to affect some ABC transporters, were tested in B. cinerea. In our experimental conditions, the activity of several fungicides was only enhanced by verapamil. Interestingly, synergism was only recorded in MDR2 and/or MDR3 isolates treated with tolnaftate, fenhexamid, fludioxonil or pyrimethanil, suggesting that verapamil may inhibit the MFS transporter BcmfsM2. This is the first report indicating that a known modulator of ABC transporters could also block MFS transporters.  相似文献   

6.
Insect resistance to the pyrethroid toxins has been examined previously using a number of traditional biochemical and molecular techniques. In this study, a proteomic approach involving two-dimensional polyacrylamide gel electrophoresis (2D-PAGE), matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) and tandem mass spectrometry (MS/MS) were applied to examine changes in resistant stains larvae of Bactracera dorsalis Hendel induced by pyrethroid treatment over a 3 h, 6 h and 12 h time period, and a number of proteins changes were observed to change in the level of regulation. Out of total 15 proteins, 9 proteins were observed only after pyrethroid treatment; 6 proteins showed different expression. After MALDI-TOF analyses and peptide mapping method, the data was compared with those of the known proteins available in public databases. Sequence analyses revealed that resistance response correlates with up-regulation (glycerol-3-phosphate dehydrogenase) and down-regulation (ATP-ADP antiporter) of energy-related proteins. It indicated that increased metabolism and energy-indeed as a resistance response to pyrethroid toxins. The regulation of cytoskeleton proteins were possibly a B. dorsalis tissue repair response or in cell division. Up-regulation of protein synthesis would results in substantial bioenergetic enhancement, suggesting a trade-off insect resistance to pyrethroid. Down regulation of neural protein indicated that neural system was physically injured after pyrethroid stress. Some remaining proteins were not identifiable, suggesting these may be novel proteins. Oriental fruit fly proteomes of pesticide induced provide an integrative basis for consolidating our knowledge of insect resistance. The results pave the way for future investigation of the alteration of the insect resistance to chemical pesticides.  相似文献   

7.
为筛选出高效安全的韭蛆防治药剂,室内采用胃毒触杀联合毒力法比较了吡虫啉、啶虫脒、噻虫嗪、噻虫胺、呋虫胺、烯啶虫胺、噻虫啉与毒死蜱和高效氯氟氰菊酯等6种对照药剂对韭菜迟眼蕈蚊幼虫的毒力,同时用人工土壤法测定了13种药剂对蚯蚓的急性毒性,并通过盆栽试验验证了其对韭蛆和蚯蚓的选择毒力。结果表明,吡虫啉、噻虫胺、呋虫胺、噻虫啉、噻虫嗪对韭菜迟眼蕈蚊4龄幼虫的毒力明显高于6种对照药剂,对虫酰肼的相对毒力倍数分别为101.6、55.0、32.9、27.2、13.6;13种供试药剂中,除吡虫啉、啶虫脒、噻虫胺、呋虫胺对蚯蚓中等毒性外,其余均为低毒;盆栽试验中,吡虫啉、噻虫嗪、毒死蜱、噻唑膦、高效氯氟氰菊酯的防虫效果和保苗效果均分别高于其它药剂,但其中只有噻虫嗪对蚯蚓没有明显致死作用。  相似文献   

8.
Drug transporters are membrane proteins that provide protection for organisms against natural toxic products and fungicides. In plant pathogens, drug transporters function in baseline sensitivity to fungicides, multidrug resistance (MDR) and virulence on host plants. This paper describes drug transporters of the filamentous fungi Aspergillus nidulans (Eidam) Winter, Botrytis cinerea Pers and Mycosphaerella graminicola (Fückel) Schroter that function in fungicide sensitivity and resistance. The fungi possess ATP-binding cassette (ABC) drug transporters that mediate MDR to fungicides in laboratory mutants. Similar mutants are not pronounced in field resistance to most classes of fungicide but may play a role in resistance to azoles. MDR may also explain historical cases of resistance to aromatic hydrocarbon fungicides and dodine. In clinical situations, MDR development in Candida albicans (Robin) Berkhout mediated by ABC transporters in patients suffering from candidiasis is common after prolonged treatment with azoles. Factors that can explain this striking difference between agricultural and clinical situations are discussed. Attention is also paid to the risk of MDR development in plant pathogens in the future. Finally, the paper describes the impact of fungal drug transporters on drug discovery.  相似文献   

9.
害虫抗药性是导致杀虫剂防效降低的一个重要因素,而抗性机制的阐明是害虫抗药性综合治理的基础。研究表明,代谢能力增强是害虫抗药性产生的重要原因,害虫对杀虫剂等外源物质的代谢需要细胞色素P450酶系(P450s)、羧酸酯酶(CarEs)、谷胱甘肽S-转移酶(GSTs)、UDP-葡萄糖醛酸转移酶(UGTs)和ATP结合盒转运蛋白(简称ABC转运蛋白)等解毒酶和转运蛋白的参与。结合近年来对害虫抗药性分子机制的研究进展,本文综述了上述解毒酶和转运蛋白参与杀虫剂抗药性的分子机制,并对害虫抗药性治理的新方法进行了展望。  相似文献   

10.
Glutathione S-transferases (GSTs) are known to catalyze conjugations by facilitating the nucleophilic attack of the sulfhydryl group of endogenous reduced glutathione on electrophilic centers of a vast range of xenobiotic compounds, including insecticides and acaricides. Elevated levels of GSTs in the two-spotted spider mite, Tetranychus urticae Koch, have recently been associated with resistance to acaricides such as abamectin [Pestic. Biochem. Physiol. 72 (2002) 111]. GSTs from acaricide susceptible and resistant strains of T. urticae were purified by glutathione-agarose affinity chromatography and characterized by their Michaelis-Menten kinetics towards artificial substrates, i.e., 1-chloro-2,4-dinitrobenzene and monochlorobimane. The inhibitory potential of azocyclotin, dicumarol, and plumbagin was low (IC50 values > 100 μM), whereas ethacrynic acid was much more effective, exhibiting an IC50 value of 4.5 μM. GST activity is highest in 2-4-day-old female adults and dropped considerably with progressing age. Furthermore, molecular characteristics were determined for the first time of a GST from T. urticae, such as molecular weight (SDS-PAGE) and N-terminal amino acid sequencing (Edman degradation). Glutathione-agarose affinity purified GST from T. urticae strain WI has a molecular weight of 22.1 kDa. N-terminal amino acid sequencing revealed a homogeneity of ≈50% to insect GSTs closely related to insect class I GSTs (similar to mammalian Delta class GSTs).  相似文献   

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The oriental tobacco budworm, Helicoverpa assulta, is one of the most destructive pests for numerous commercial crops, and these organisms are responsible for enormous economic losses in Chinese agriculture. Insect larvae often feed within host plant fruits, providing protection from many currently used insecticides and making field control of H. assulta very difficult. Owing to its novel mode of action, high insecticidal activity, and low mammalian toxicity, the nonsystemic insecticide indoxacarb has been considered a promising alternative for the control of lepidopterous pests of agricultural significance. Indoxacarb evidences an elevated insecticidal activity against H. assulta. After 13 generations of selection with indoxacarb and bifenthrin insecticides under laboratory conditions, the LC50 of these compounds for H. assulta increased by 4.19-fold and 10.67-fold, respectively. The synergists diethyl maleate (DEM) and triphenyl phosphate (TPP) increased indoxacarb toxicity by 2.76-fold and 4.10-fold in resistant strains and, comparatively, 1.58-fold and 1.75-fold in susceptible strains, suggesting that carboxylesterase (CarE) and glutathione-S-transferases (GSTs) may be involved in the development of indoxacarb resistance in H. assulta. Activity and kinetic parameters observed in detoxification enzymes further demonstrated that the enhanced activity of CarE and GSTs may be critical in development of indoxacarb resistance in H. assulta. The data provides a foundation for further study of the indoxacarb resistance mechanism observed in H. assulta and the rational use of indoxacarb as a rotation insecticide with other insecticide classes for the control of H. assulta.  相似文献   

13.
This study has determined the uptake of three pesticides, applied as commercial or model formulations in the presence of a wide range of surfactants, into the leaves of three plant species (bentazone into Chenopodium album L. and Sinapis alba L., epoxiconazole and pyraclostrobin into Triticum aestivum L.). The results have confirmed previous findings that the initial dose (nmol mm(-2)) of xenobiotic applied to plant foliage is a strong, positive determinant of uptake. This held true for all the pesticide formulations studied, although surfactant concentration was found to have an effect. The lower surfactant concentrations studied showed an inferior relationship between the amount of xenobiotic applied and uptake. High molecular mass surfactants also produced much lower uptake than expected from the dose uptake equations in specific situations.  相似文献   

14.
Human membrane drug transporters are recognized as major actors of pharmacokinetics. Pesticides also interact with human drug transporters, which may have consequences for pesticide toxicokinetics and toxicity. The present review summarizes key findings about this topic. In vitro assays have demonstrated that some pesticides, belonging to various chemical classes, modulate drug transporter activity, regulate transporter expression and/or are substrates, thus bringing the proof of concept for pesticide‐transporter relationships. The expected low human concentration of pesticides in response to environmental exposure constitutes a key‐parameter to be kept in mind for judging the in vivo relevance of such pesticide‐transporter interactions and their consequences for human health. Existing data about interactions of pesticides with drug transporters remain, however, rather sparse; more extensive and systematic characterization of pesticide‐transporter relationships, through the use of high throughput in vitro assays and/or in silico methods, is, therefore, required. In addition, consideration of transporter polymorphisms, pesticide mixture effects and physiological and pathological factors governing drug transporter expression may help to better define the in vivo relevance of pesticide‐transporter interactions in terms of toxicokinetics and toxicity for humans. © 2019 Society of Chemical Industry  相似文献   

15.
Bacillus thuringiensis (Bt) has been used as sprayable pesticides for many decades. Bt strains utilized in these products produce multiple insecticidal proteins to complement a narrow insect specificity of each protein. In the late 1990s, genes encoding Bt insecticidal proteins were expressed in crop plants such as cotton and corn to protect these crops from insect damage. The first Bt protein used in transgenic cotton was Cry1Ac to control Heliothis virescens (tobacco budworm). Cry1Ab was applied to corn to control Ostrinia nubilalis (European corn borer). Since these insects have developed resistance to Cry1Ac and Cry1Ab, new Bt proteins are required to overcome the resistance. In order to protect corn furthermore, it is desired to control Diabrotica virgifera (Western corn rootworm), Helicoverpa zea (corn earworm) and Spodoptera frugiperda (fall armyworm). Recently, many new Bt insecticidal proteins have been discovered, but most of them require protein engineering to meet the high activity standard for commercialization. The engineering process for higher activity necessary for Bt crops is called optimization. The seed industry has been optimizing Bt insecticidal proteins to improve their insecticidal activity. In this review, several optimization projects, which have led to substantial activity increases of Bt insecticidal proteins, are described.  相似文献   

16.
为筛选防治暗黑鳃金龟Holotrichia parallela的有效药剂,用浸虫法测定了7种药剂对暗黑鳃金龟幼虫的毒力,分别采用浸虫法、浸叶法、药膜法测定了7种药剂对其成虫的毒力,并通过大田试验作了进一步验证。浸虫法测得高效氯氟氰菊酯对成虫的毒力最高,LC50值为1.38 mg/L;浸叶法测得辛硫磷毒力最高,为42.05 mg/L;药膜法测得毒死蜱毒力最高,为18.51 mg/L。其中,高效氯氟氰菊酯毒力值变化最大,浸虫法毒力是浸叶法毒力的61.86倍;氯虫苯甲酰胺、氟虫腈在3种生测方法中毒力相当,但均较低。丁硫克百威对暗黑鳃金龟幼虫的毒力最高,LC50值为7.29 mg/L。田间试验结果显示,35%辛硫磷微囊悬浮剂4 500 g/hm2(有效成分,余同)防效达80.66%,对花生的保果、增产幅度分别为77.90%、17.56%;30%毒死蜱微囊悬浮剂2 250 g/hm2、20%丁硫克百威乳油3 000 g/hm2与辛硫磷防效相当,且显著高于其它药剂。因此,选用以上药剂于7月中下旬花生封垄前田间灌墩可以有效减轻暗黑鳃金龟为害。  相似文献   

17.
Indoxacarb (DPX-MP062) is a recently introduced oxadiazine insecticide with activity against a wide range of pests, including house flies. It is metabolically decarbomethoxylated to DCJW. Selection of field collected house flies with indoxacarb produced a New York indoxacarb-resistant (NYINDR) strain with >118-fold resistance after three generations. Resistance in NYINDR could be partially overcome with the P450 inhibitor piperonyl butoxide (PBO), but the synergists diethyl maleate and S,S,S-tributyl phosphorothioate did not alter expression of the resistance, suggesting P450 monooxygenases, but not esterases or glutathione S-transferases are involved in the indoxacarb resistance. Conversely, the NYINDR strain showed only 3.2-fold resistance to DCJW, and this resistance could be suppressed with PBO. Only limited levels of cross-resistance were detected to pyrethroid, organophosphate, carbamate or chlorinated hydrocarbon insecticides in NYINDR. Indoxacarb resistance in the NYINDR strain was inherited primarily as a completely recessive trait. Analysis of the phenotypes vs. mortality data revealed that the major factor for indoxacarb resistance is located on autosome 4 with a minor factor on autosome 3. It appears these genes have not previously been associated with insecticide resistance.  相似文献   

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20.
The brown planthopper (BPH), Nilaparvata lugens (Stål) is a serious threat to the rice production throughout Asia. The indiscriminate application of various xenobiotics in rice ecosystem is perceived as one of the factors for the frequent outbreak of BPH. The present study has critically analysed the secondary effects of some xenobiotics used in rice field on certain plant and insect parameters that subsequently favour BPH outbreak. Application of 2,4-D, carbendazim, deltamethrin and urea reduced the innate BPH resistance of PTB 33 rice variety due to favourable alterations in rice free amino acid and sucrose content. Similarly, these chemicals also induced hormesis and enhanced feeding in BPH. Alternatively, soil amendment with neem seed powder and Calotropis gigantea leaves improved plant innate resistance and showed no sign of hormesis or enhanced feeding in BPH. In addition, deltamethrin has the ability to stimulate BPH carboxylesterase titre. Native PAGE analysis of esterases from whole body homogenate of BPH revealed at least five esterase isozyme bands, prominent being E1 and E2. However, no difference in BPH esterase banding pattern was observed between different xenobiotic treatments. All these esterase bands are classified under carboxylesterase based on their inhibition by class specific esterase inhibitors.  相似文献   

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