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1.
Bacillus thuringiensis Berliner in combination with 0.1, 0.5, 1.0, 1.5 and 2% boric acid caused 100% mortality of the tobacco caterpillar,Spodoptera litura (F.), irrespective of instar, in a much shorter period (1.77 to 3.61 days) than with boric acid or the pathogen alone. The toxicity ofB. thuringiensis in combination with dicrotophos at 0.02 and 0.04%, with fenitrothion at 0.025 and 0.05%, or with dichlorvos at 0.01 and 0.05%, was enhanced. 相似文献
2.
Treatment of the house cricket Acheta domesticus (L.) with tetraethyl pyrophosphate and dicrotophos causes a depletion of the catecholamine stores of the central nervous system. Fluorescence microscopy of the brain and frontal ganglion 30 min after knock-down revealed a reduction in the catecholamine-specific fluorescence of the corpus centrale and frontal ganglion neuropile. In the corpus centrale the effect was much more pronounced and less variable with dicrotophos than with tetraethyl pyrophosphate, whereas both compounds appeared to have similar effects on the frontal ganglion. The possible relationship of this depletion to symptoms of intoxication requires further investigation. 相似文献
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Conventional film autoradiography was used at the light microscopic level for the localization and quantization of 4-aminobutyric acid (GABA) receptors in the locust brain (Schistocerca americana). Localization of the receptor site was achieved via binding with the receptor-ligand probe [3 H]muscimol. Frozen sections were cut and subsequently incubated either in 40 nM [3H]muscimol or by coincubating sections with [3H]muscimol and one of the following: GABA (50 μM)], a receptor specific agonist [muscimol (1 μM) or isoguvacine (1 μM)], an uptake inhibitor [nipecotic acid (50 μM)], or a noncompetitive channel modulator [avermectin B1a, (1 μM) or aldrin (50 μM)]. Through computer image enhancement and densitometric analysis of the optical density of [3H]muscimol binding sites, the interaction of the above compounds with the putative GABA receptor was determined for various anatomical regions of the locust brain. By comparing the differently treated, but adjacent sections, GABA receptor distribution was quantitated and mapped. Receptor sites were found distributed in the antennal lobes, central body, β-lobe and β-lobe of the corpus pedunculatum, protocerebral bridge, and calyx as well as the optic lobe regions. 相似文献
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Piotr Duchnowicz Piotr Szczepaniak Maria Koter 《Pesticide biochemistry and physiology》2005,82(1):59-65
In the present work, we describe the effect of chlorophenoxyl herbicides 2,4-dichlorophenoxyacetic acid (2,4-D), 4-chloro-2-methylphenoxyacetic acid, and 2,4,5-trichlorophenoxyacetic acid (2,4,5-T), and their metabolites (2,4-dichlorophenol, 4-chloro-2-methylphenol, 2,4-dimethylphenol, and 2,4,5-trichlorophenol) on the activity of ATPase and the corresponding protein damage (measured by loss of -SH group). Basic compounds caused an increase in the activity of the enzyme by 7-9% (at concentration 1 mM). For higher concentrations (2 and 4 mM), a decrease in the ATPase activity was observed for all investigated compounds. The increase of the free -SH group content was observed for all compounds. More profound changes in investigated parameter values were observed for metabolites (when compared to basic compounds) which may suggest their higher toxicity. 相似文献
5.
Daily 75 mg/kg phenobarbital ip injections for 3 days or 25 ppm dieldrin in the diet of mice for 14 days caused an increase in liver cytochrome P-450 and blood B-esterase. Liver A-esterase was not significantly increased. Under in vitro conditions, phenobarbital and dieldrin induced the oxidative as well as hydrolytic metabolism of dicrotophos, dimethoate, and phosphamidon by liver homogenates or combined microsomes plus 105,000g supernatant fractions. The concentration of dimethoxon was increased more than fourfold by the pretreatments after incubation for 4 hr at 37.5°C with NADPH added. The organophosphorus insecticides used in this study were not metabolized as well by the liver microsomes alone or 105,000g supernatant alone, as by the combination of microsomes and 105,000g supernatant. Under in vivo conditions in mice, phenobarbital and dieldrin treatments increased the urinary recovery of metabolites in the initial 6 hr after [14C]carbonyl-dimethoate or [14C]N-ethyl-phosphamidon administration. Analysis of urine showed that the inducers caused a more than sixfold increase in dimethoxon recovered and twofold increase in water-soluble nontoxic metabolites within 6 hr after dimethoate administration. With phosphamidon both inducers increased the rate of metabolism, and the total recovery in aqueous and chloroform fractions was decreased. These results suggest that increased dimethoate toxicity after phenobarbital and dieldrin treatments in whole animals results from stimulation of the activation of dimethoate to dimethoxon, while the increase in hydrolytic products after both pretreatments results in decreased toxicity of the direct acetylcholinesterase inhibitors, dicrotophos and phosphamidon. 相似文献
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A series of known agonists of the mammalian muscarinic receptor were prepared and evaluated for their insecticidal potential. It was discovered that pests such as Nilaparvata lugens (brown planthopper), Nephotettix cincticeps (green leafhopper), Tetranychus urticae (two-spotted spider mite) and Aphis gossypii (cotton aphid) were particularly sensitive to most of these compounds. Several analogs proved to be extremely active, surpassing commercial standards in some of the laboratory bioassays. These compounds exhibited a range of potencies for the insect (Musca) muscarinic receptor. Addition of GTP significantly reduced the affinity of the most potent analog for the Musca mAChR, indicating the compound functions as an agonist in insect tissue. Regression analysis indicated that significant relationships exist between displacement of [3H]QNB at the Musca muscarinic receptor and whole organism toxicity to three insect and one mite species. The results suggested that the insect muscarinic receptor represents a viable target site for insecticidal action. © 1997 SCI. 相似文献
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W. E. Eguagie 《Pest management science》1973,4(3):273-282
Two groups of insecticides were screened against the cacao mirid, S. singularis in small-scale field trials from September 1969 to January 1972. In first group 0.05% promecarb, 0.04% phosphamidon and 0.02% monocrotophos were equally effective and superior to 0.05% mecarbam in the three days after spraying but 0.05% promecarb was most toxic to bugs by the seventh day. In the 0.15 to 0.2% range, all four insecticides showed similar toxicity within 3 days of spraying but only 0.15% mecarbam and 0.2% promecarb maintained control to the seventh day. For mecarbam, phosphamidon and monocrotophos, control at 0.15% was better than at 0.05, 0.04 and 0.02% respectively 7 days after spray whilst 0.2% was superior to 0.05% promecarb 2 days after spray and not afterwards. At either 0.21 or 0.33 lb/acre insecticides in the second group (pirimiphos methyl, HOE 2960, CA 6900 and dicrotophos) gave identical level of control of mirids and control at the latter dosage rate was not better than at the former. There was no significant difference between 3 and 4 oz a.i./10 gal water/200 trees in toxicity to mirids and the insecticides gave equally good control of the bugs at both dosage levels till 35th day after spray. On the basis of efficacy and safety of use, promecarb CA 6900 and pirimiphos methyl were deemed suitable for further (large scale) trials. 相似文献
8.
Michael D. Owen 《Pest management science》1991,32(4):471-478
MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) and MPP+ (1-methyl-4-phenylpyridinium ion) are potent dopaminergic neurotoxins in mammals. The mammalian toxicity of MPTP depends on its conversion, by monoamine oxidase, to MPP+. MPTP is toxic to cockroaches (LD50 720 μg gm?1) and the results suggest that MPTP toxicity depends on monoamine oxidase activity at a site outside the nervous system. MPTP depletes dopamine from cockroach cerebral ganglia and MPP+ inhibits cockroach mitochondrial respiration. While the biochemistry of MPTP toxicity appears to be the same as in mammals it seems that insects are unable to detoxify MPTP before its action has fatal consequences outside the nervous system. 相似文献
9.
Miki Akamatsu Yoshihisa Ozoe Tamio Ueno Toshio Fujita Kazuo Mochida Toshiie Nakamura Fumio Matsumura 《Pest management science》1997,49(4):319-332
Quantitative structure–activity relationships for insecticidal activity (against houseflies) and competitive activity against a specific [35S]tert-butylbicyclophosphorothionate binding (to rat brain membranes) of some picrotoxinin-type 4-aminobutyric acid antagonists, including γ-BHC, endosulfan, bicyclophosphates, dioxatricyclododecenes and related compounds, were examined three-dimensionally using comparative molecular field analysis (CoMFA). The antagonists were classified into two series according to their molecular shapes: i.e. whether their structure was ‘linearly’ extended beyond the ‘mast-head’ position of the ‘boat-like’ skeletons (series 1) or not (series 2). The CoMFA showed that the slopes in steric and electrostatic fields around the molecule were significant for both series in governing the potency variations in insecticidal and binding activities. Hydrophobicity, a possible factor controlling transport behaviour of compounds, was significant in governing variations in insecticidal activity, but not for the case of the rat membrane binding. Assuming that there is a slight topological difference between series 1 and 2 compounds in terms of the mode of binding with the housefly receptor site, the insecticidal activity was analysable with a single equation for the combined set of compounds, but the rat membrane binding was not. The sterically and electrostatically favourable regions surrounding the molecular series indicated by CoMFA were roughly located at positions so as to interact with the binding subsites on the receptors proposed previously. © of SCI. 相似文献
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Cry1Ba3是由本实验室发掘的对小菜蛾有高毒力的杀虫晶体蛋白。为了寻找对杀虫活性有重要影响的氨基酸,为杀虫机理研究和改造杀虫蛋白提供理论依据,本研究利用Ple Bio Informatique Lyonnais数据库对Cry1Ba3的二级结构进行模拟;采用BioEdit软件分析Cry1Ba3的疏水区;将Cry1Ba3与Cry1Aa1、Cry2Aa1、Cry3Aa1以及Cry4Ba1进行多序列比对,从而确定了20个氨基酸突变位点。利用半重叠引物PCR的方法对Cry1Ba3进行定点突变,将突变体在大肠杆菌BL21中进行诱导表达。通过浸叶法对各个突变蛋白杀小菜蛾的生物活性进行测定。获得的20个Cry1Ba3突变体均能在大肠杆菌BL21中表达,并以包涵体形式存在。杀虫活性测定结果表明M6(R192L)、M10(W303A)、M19(H485G)对小菜蛾的活性明显降低,二级结构预测表明活性降低的突变蛋白的构象均发生明显变化,其余17种突变蛋白的活性和二级结构都没有明显变化。说明第192位的精氨酸、第303位的色氨酸和第485位的组氨酸对Cry1Ba3的杀小菜蛾活性有重要影响,上述3个位点氨基酸突变引起的蛋白活性减低可能与毒素的空间结构变化有关。 相似文献
12.
For the purpose of better understanding the molecular mechanism of action of sulfonylurea and sulfonamide herbicides, the quantitative relationship between their structure and herbicidal activity against rape, Brassica campestris L, was analysed using physicochemical parameters and regression analysis and comparative molecular field analysis (CoMFA). The results showed that the structure–activity relationships of the two sets of compounds were identical, which suggested that the two different sets of compounds affect a common region of the receptor site. The CoMFA results were consistent with those derived from traditional QSAR analysis. Combining the traditional QSAR analysis with the CoMFA results, we can conclude that the variations in the herbicidal activity of the two sets of ALS inhibitors were governed dominantly by the three-dimensional steric and electrostatic field parameters of molecules participating in the interaction with the receptor site and there is apparently an optimum electronic property (Σσ or pKa) for the molecules to fit the receptor. © 1999 Society of Chemical Industry 相似文献
13.
Richardson BA Klopfenstein NB Zambino PJ McDonald GI Geils BW Carris LM 《Phytopathology》2008,98(4):413-420
Cronartium ribicola, the causal agent of white pine blister rust, has been devastating to five-needled white pines in North America since its introduction nearly a century ago. However, dynamic and complex interactions occur among C. ribicola, five-needled white pines, and the environment. To examine potential evolutionary influences on genetic structure and diversity of C. ribicola in western United States, population genetic analyses of C. ribicola were conducted using amplified fragment length polymorphism (AFLP) molecular markers. The fungus was sampled at six sites. Collections for two of the six sites were from separate plantings of resistant-selected western white pine and sugar pine. Heterozygosity based on polymorphic loci among populations ranged from 0.28 to 0.40, with resistant-selected plantations at the extremes. Genetic differentiation was also highest between these two populations. Principal coordinates analysis and Bayesian assignment placed most isolates that are putative carriers of virulence to major-gene resistance into a discernable cluster, while other isolates showed no clustering by site or host species. These results indicate that C. ribicola in western North America is not genetically uniform, despite its presumed single site of introduction and relatively brief residence. Moreover, major-gene resistance appears to have imposed strong selection on the rust, resulting in reduced genetic diversity. In contrast, no evidence of selection was observed in C. ribicola from hosts that exhibit only multigenic resistance. 相似文献
14.
Jeffrey R. Bloomquist Holly J. Ferguson Eric D. Cox M. Sreenivasa Reddy James M. Cook 《Pest management science》1997,51(1):1-6
Little information is available on the actions of β-carboline convulsants on insect GABA receptors or their potential as insecticides. Accordingly, two compounds (3-ethoxy-β-carboline, 3-EBC; dimethoxy-β-carboline-3-methyl ester, DMCM) were studied for their effects on Drosophila melanogaster larval neuron discharge and also in lethality bioassays on adult female D. melanogaster and adult male Blattella germanica. Recordings of nerve spiking in the isolated larval central nervous system showed that 3-EBC and DMCM inhibited nerve discharge, and this inhibitory effect was not additive with that of GABA, confirming that the inhibition was expressed through an action on the GABA receptor. Nerve blockage induced by β-carbolines could not be reversed by picrotoxinin, indicating that there may exist some overlap or negative allosteric coupling between the picrotoxinin and β-carboline binding sites. DMCM and 3-EBC effectively antagonized the effects of exogenously applied GABA in nerve preparations from insecticide-susceptible larvae. In contrast, preparations from the rdl strain of D. melanogaster, which possesses a GABA receptor that is highly resistant to cyclodienes and related convulsants, were less sensitive to the GABA antagonist effect of DMCM. Neither of the β-carbolines produced any appreciable mortality in insects, even when synergized with piperonyl butoxide or S,S,S-tributyl phosphorotrithioate, The toxicity of the β-carbolines is probably limited by their relatively weak effects on the GABA receptor and perhaps also by pharmacokinetic factors. These considerations, coupled with the cross-resistance observed in cyclodiene-resistant insects, suggest that the currently available β-carbolines are not viable as lead compounds for insecticide screening efforts. © 1997 SCI. 相似文献
15.
I.N.H. White R.D. Verschoyle M.H. Moradian J.M. Barnes 《Pesticide biochemistry and physiology》1976,6(5):491-500
The oral toxicity of 5-benzyl-3-furylmethyl-(1R, cis)-chrysanthemate (cismethrin) to female rats decreased as their environmental temperature was raised. Acute oral LD50 values increased from 157 mg/kg at 4°C to 197 mg/kg at 20°C and to > 1000 mg/kg at 30°C. Cismethrin was much more toxic given intravenously when the LD50 was 4.5 mg/kg. This value did not change at different environmental temperatures. Irrespective of the environmental temperature, or route of adminstration, following the respective LD50's cismethrin caused tremors in rats when brain levels of 0.5–1.0 μg/g were reached and, at death, brain concentrations were 3.9–5.1 μg/g. These results suggested that the accumulation of cismethrin by the brain could be used as a model for the nervous system as a whole. The isomeric 5-benzyl-3-furylmethyl-(1R, trans)-chrysanthemate (bioresmethrin) was about 50 times less toxic to rats than cismethrin. After an intravenous LD50, tremors started when brain concentrations were 4–5 μg/g. At death, brain levels were 25–35 μg/g. Plasma esterases were about equally active in hydrolysing cismethrin and bioresmethrin, whereas liver microsomal esterases hydrolyzed bioresmethrin over 10 times more rapidly than cismethrin. It is suggested that the lower toxicity of bioresmethrin is not only due to its faster metabolism but to an intrinsically lower toxicity at the critical site of action in the nervous system. 相似文献
16.
Yoshio Katsuda 《Pest management science》1999,55(8):775-782
The pyrethroid group of insecticides consists of natural pyrethrins derived from pyrethrum flowers and synthetic derivatives which are similar in chemical structure to the natural compounds. Pyrethroids have been considered to be ideal insecticides because of their rapid knock-down effect against insects in a minimal dose and low mammalian toxicity. © 1999 Society of Chemical Industry 相似文献
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基于氟虫腈低能构象进行骨架跃迁,设计、合成了25个未见文献报道的苯基吡唑并嘧啶胺和苯基吡唑并嘧啶酮类化合物,所有化合物的结构均通过核磁共振氢谱 (1H NMR)、碳谱 (13C NMR) 及高分辨质谱 (HRMS) 确证。杀虫活性测试表明,目标化合物 A5 、 B1 、 B4 和 B5 在500 mg/L下对小菜蛾的致死率在40%~73%之间,活性弱于氟虫腈。初步分析,其理化性质以及其与昆虫γ-氨基丁酸 (GABA) 受体结合模式方面的差异可能是导致这些化合物活性比氟虫腈低的主要原因。 相似文献
19.
Toxicity and nicotinic acetylcholine receptor interaction of imidacloprid and its metabolites in Apis mellifera (Hymenoptera: Apidae) 总被引：1，自引：0，他引：1
Acute oral and contact toxicity tests of imidacloprid, an insecticide acting agonistically on nicotinic acetylcholine receptors (nAChR), to adult honeybees, Apis mellifera L var carnica, were carried out by seven different European research facilities. Results indicated that the 48-h oral LD50 of imidacloprid is between 41 and > 81 ng per bee, and the contact LD50 between 49 and 102 ng per bee. The ingested amount of imidacloprid-containing sucrose solution decreased with increasing imidacloprid concentrations and may be attributed to dose-related sub-lethal intoxication symptoms or to antifeedant responses. Some previously reported imidacloprid metabolites occurring at low levels in planta after seed dressing, i.e. olefine-, 5-OH- and 4,5-OH-imidacloprid, showed lower oral LD50 values (> 36, > 49 and 159 ng per bee, respectively) compared with the concurrently tested parent molecule (41 ng per bee). The urea metabolite and 6-chloronicotinic acid (6-CNA) exhibited LD50 values of > 99,500 and > 121,500 ng per bee, respectively. The pharmacological profile of the [3H]imidacloprid binding site in honeybee head membrane preparations is consistent with that anticipated for a nAChR. IC50 values for the displacement of [3H]imidacloprid by several metabolites such as olefine, 5-OH-, 4,5-OH-imidacloprid, urea and 6-CNA were 0.45, 24, 6600, > 100,000, and > 100,000 nM, respectively. Displacement of [3H]imidacloprid by imidacloprid revealed an IC50 value of 2.9 nM, thus correlating well with the observed acute oral toxicity of the compounds in honeybees. Neurons isolated from the antennal lobe of A mellifera and subjected to whole-cell voltage clamp electrophysiology responded to the application of 100 microM acetylcholine with a fast inward current of between 30 and 1600 pA at -70 mV clamp potential. Imidacloprid and two of the metabolites (olefine- and 5-OH-imidacloprid) acted agonistically on these neurons, whereas the others did not induce currents at test concentrations up to 3 mM. The electrophysiological data revealed Hill coefficients of approximately 1, indicating a single binding site responsible for an activation of the receptor and no direct cooperativity or allosteric interaction with a second binding site. 相似文献
20.
Johan C. Kapteyn Richard J. Milling Donald J. Simpson Maarten A. De Waard 《Pest management science》1994,40(4):313-319
The sensitivity of cytochrome-P450-dependent sterol 14α-demethylase (P45014DM) to prochloraz and several prochloraz analogues was studied in a cell-free assay of Botrytis cinerea Pers. ex Fr. The EC50 values (concentrations which inhibited radial growth of B. cinerea by 50%) of the compounds tested ranged from 3.3 × 10 ?8 to 1.7 × 10 ?5 M. The IV50 values (concentrations which inhibited cell-free C4-demethyl sterol synthesis by 50%) in cell-free assays of B. cinerea ranged from 2.6 × 10 ?9 to 4.4 × 10 ?7 M. Ranking compounds in terms of their relative inhibitory potencies showed quite similar trends to the order of fungitoxicity, but the IC50 values did not quantitatively reflect the differences in toxicity. Therefore, the differential inhibition of cell-free P45014DM activity by these compounds cannot fully account for their differences in activity towards B. cinerea. Additional mechanisms must be involved. The compounds tested were generally more potent in the B. cinerea assay than in similar assays developed for Penicillium italicum Wehmer and, in particular, Saccharomyces cerevisiae Meyen. This correlated with the relatively higher activity of most test compounds to B. cinerea. Results suggest that the cell-free assay of B. cinerea is more useful to evaluate candidate fungicides as inhibitors of sterol 14α-demethyiase activity than similar assays from model organisms. The present study confirms that the affinity of prochloraz analogues for P45014DM depends on the nature of the N-1 substituent of the imidazole and the azole ring. It was also found that addition of an amino group at C-2 of the imidazole moiety of prochloraz gave a compound (6) which inhibited 4, 4-demethyl sterol biosynthesis in B. cinerea at a different site from the P45014DM. This was confirmed by the observation that laboratory-generated triadimenol-resistant isolates of B. cinerea showed reduced sensitivity to triadimenol and prochloraz, but not to compound 6. 相似文献