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1.
Partition coefficients of organophosphorus and organochlorine insecticides were determined in several types of membrane. Insecticide partitioning varied among the membranes under study, depending on temperature, cholesterol content and on the physico-chemical profiles of membrane components and the insecticides themselves. The maximal partitions for DDT, lindane, parathion and malathion in egg phosphatidylcholine bilayers over the temperature range from 10 to 37°C (at which the lipid is in the liquid-crystalline state) were about 260000, 2000, 1000 and 120, respectively. Incorporation of 50 mol% cholesterol in egg phosphatidylcholine bilayers dramatically decreased the partition and almost abolished the temperature effect. First-order phase transitions of dimyristoyl-, dipalmitoyl- and distearoylphosphatidylcholines (DMPC, DPPC and DSPC) were accompanied by a sharp increase in insecticide partition. Furthermore, the insecticides under study were more easily accommodated in bilayers of short-aliphatic-chain lipids, since higher values of partition were obtained in DMPC bilayers. Partition values in native membranes depended considerably on the membrane type and composition and were higher in sarcoplasmic reticulum (SR) and mitochondria than in brain microsomes, myelin and erythrocytes. Identical results were obtained in related liposomes of total extracted lipids, although the absolute partitions showed decreased values. In general, the incorporation of insecticides correlated reasonably with the cholesterol content of the membranes. The order of partitioning of the above insecticides did not run parallel with their toxicity to mammals and, both in model and in native membranes, followed the sequence: DDT ? lindane > parathion > malathion.  相似文献   

2.
The organophosphorus insecticides, parathion and azinphos (10?5-10?4M), significantly stimulate the Ca2+-pump activity of sarcoplasmic reticulum, while malathion has a limited effect. The rates of Ca2+ translocation and ATP hydrolysis are both stimulated and, apparently, the Ca2+ATP ratio is improved. Parathion and azinphos maximally increase this ratio by 26 and 14%, respectively. The organochlorine compounds, DDT and aldrin, also stimulate the Ca2+ pump, and lindane has a reduced effect. These effects are smaller than those observed for parathion and azinphos. The order of effectiveness is similar to the toxicity of the compounds to mammals and can be described as follows: parathion > azinphos > DDT ≈ aldrin > malathion ≈ lindane.  相似文献   

3.
Insecticides exert antilytic effects on pig erythrocytes by preventing osmotic disruption of membranes in critical hypotonic saline media. The order of effectiveness is the following: lindane > aldrin ≈ azinphos > parathion ≈ DDT > malathion; empirical protective indexes estimated for K+ leakage, at 0.09 M NaCl, were 5.6, 3.9, 2.9, 2.8, and 2.0, respectively. Erythrocytes swell and hemolyze in solutions containing glycerol below 0.6 M. At higher concentrations and temperatures below 20°C, the extent of cell lysis is very limited and virtually nil in 1 M glycerol. In hypertonic glycerol solutions, cells swell until the initial equilibrium volume is reached and, then, the swelling process ceases. Swelling in 1 M glycerol is related to its permeation through hydrophobic membrane domains. The activation energies of permeation are similar to the dehydration energies of glycerol molecules. As the temperature is increased above 20°C, erythrocytes undergo lysis. The organophosphorus insecticides, parathion and azinphos (10?4M), significantly increase the swelling rates and the extent of cell lysis. Malathion and chlorinated insecticides do not exert apparent effects. However, these compounds are effective in liposomes reconstituted with lipids extracted from erythrocyte membranes.  相似文献   

4.
The insecticidal activity of dimethyl and diethyl forms of parathion, carbophenothion, bromophos and azinphos on glass surfaces and in soil was assessed by bioassay with adult vestigial winged Drosophila melanogaster (Meig.). Both on glass and in soil there were large differences in the initial toxicities of the four different pairs of insecticides, but little difference between diethyl and dimethyl forms of each compound. In soil, toxicity was influenced greatly by soil type and moisture content, decreasing in the order moist sand = dry sand > moist clay-loam > dry clay-loam > dry peat > moist peat. Some of these effects may have been caused by differences in the behaviour of insects confined with moist or dry treated soils. In sterilised or unsterilised moist clay-loam, diethyl forms of three of the four compounds remained toxic longer than their dimethyl counterparts. Possibly such differences could account for the greater effectiveness of certain diethyl compounds in field control of soil insect pests.  相似文献   

5.
BACKGROUND: Codling moth, Cydia pomonella (L.), has been intensely managed with the organophosphate insecticide azinphos‐methyl for 50 years, and populations have developed resistance. New management programs have been developed and implemented that rely more heavily on other classes of insecticides. A prerequisite for developing effective resistance management strategies for these compounds is to establish their current levels of effectiveness. Adult and neonate larval assays were conducted to assess the response of field‐collected codling moth populations from apple in Washington State. RESULTS: Male codling moth populations exhibited a range of responses to a discriminating concentration of azinphos‐methyl in a survey of 20 populations. Populations from certified organic orchards were more susceptible than those from conventional orchards. Mean fecundity was inversely related to azinphos‐methyl tolerance. Male responses to azinphos‐methyl and acetamiprid varied significantly among populations and were correlated. The residual effectiveness of field applications of both insecticides varied significantly against neonate larvae. Neonate bioassays with insecticide‐dipped fruit found significant differences among populations with azinphos‐methyl, acetamiprid, methoxyfenozide and spinosad, but not with esfenvalerate. CONCLUSION: These results support a concern that alternation of insecticides with different modes of action may not be a sufficient strategy to avoid the evolution of broad‐spectrum insecticide resistance by codling moth. Published 2010 by John Wiley & Sons, Ltd.  相似文献   

6.
The effects of DDT (0-100 μM) in pure phospholipid and phospholipid/cholesterol bilayers were investigated by fluorescence polarization of 1,6-diphenyl-1,3,5-hexatriene (DPH), a probe located in the bilayer interior, and by excimer to monomer fluorescence intensity ratio (I′/I) of 1,3-di(l-pyrenyl)propane (Py(3)Py), a probe sitting closer to the polar region. In the gel phase of dimyristoylphosphatidylcholine (DMPC) bilayers, DDT induces concentration-dependent fluidizing effects into the hydrophobic membrane regions, but no effects are observed in the outer regions of the membrane, as evaluated by DPH and Py(3)Py, respectively. Furthermore, in the fluid phase of DMPC and for DDT concentrations higher than 10 μM, I′/I of Py(3)Py decreases, reflecting an order increase of the probe environment and DPH fails to detect any apparent effect. Similar effects were observed in other pure lipid bilayers, namely dipalmitoylphosphatidylcholine (DPPC) and distearoylphosphatidylcholine (DSPC). Unlike DPH, Py(3)Py is very sensitive to DPPC and DSPC pre-transitions which are not abolished by 50 μM DDT. This DDT concentration inhibits to some extent the cholesterol-induced ordering in DMPC bilayers and high cholesterol concentrations (? 30 mol%) do not prevent insecticide interaction, as evaluated by DPH. On the other hand, the effects of DDT reported by Py(3)Py depend on temperature and cholesterol content of DMPC bilayers. Thus, for cholesterol levels ranging from 10 to 50 mol% and for temperatures below the phase transition temperature of DMPC, Py(3)Py fails to detect any significant effect. Nevertheless, above the phase transition temperature of DMPC, Py(3)Py detects either ordering effects of DDT at low cholesterol contents (< 20 mol%) or fluidizing DDT effects at high cholesterol levels (> 20 mol%).  相似文献   

7.
The incorporation of DDT and several analogs into the hydrophobic interior of lecithin bilayers has been monitored by observing the nuclear magnetic resonance spectra of the aromatic ring protons. A fluid bilayer interior was obligatory for the incorporation of the chemicals. The amount of the different compounds which can be taken up into the lipid in aqueous media varies significantly, and this difference is not related to the organic: aqueous partition coefficients of the analogs. The amount of DDT, the most nonpolar of the compounds studied, which could be incorporated into the bilayers was much lower than the levels of other, more water-soluble analogs.  相似文献   

8.
选用辛硫磷、对硫磷、敌敌畏和氧乐果4种有机磷类杀虫剂以及灭多威和甲萘威两种氨基甲酸酯类杀虫剂分别以1∶1、1∶3和3∶1的比例混用,以棉铃虫Helicoverpa armigera为试虫,分别测得单剂和混剂对其乙酰胆碱酯酶(AChE)和羧酸酯酶(CarE)的抑制中浓度(I50),以联合抑制系数作为增效作用的参考指标进行了比较。研究发现,两种药剂不同配比的混剂对同种酯酶的联合抑制作用也往往不同。对AChE和CarE同时具有抑制作用的只有其中的对硫磷＋甲萘威(1∶3)、辛硫磷+对硫磷(1∶3)和灭多威+氧乐果(1∶3),而甲萘威+敌敌畏(1∶3)、甲萘威＋氧乐果(1∶1)、辛硫磷+甲萘威(1∶1)、对硫磷+氧乐果(1∶1)、对硫磷+氧乐果(1∶3)、敌敌畏+氧乐果(1∶3)、灭多威+对硫磷(1∶1) 7种混剂对AChE和CarE都具有拮抗作用。  相似文献   

9.
The ingestion and excretion of sublethal doses of phosfolan, monocrotophos, parathion, and leptophos were studied in larvae of the Egyptian cotton leafworm, Spodoptera littoralis Boisd. Styropor (foamed polystyrene) lamellae treated with insecticide-sucrose mixtures were fed to the larvae and recovery of the undecomposed insecticides from the feces could be estimated by gas-liquid chromatography, without any cleanup of the sample. The insecticidal residues on Styropor were found to be stable for 5 days.As regards the percentage of insecticide recovered from the feces, two groups could be distinguished: (a) leptophos, practically complete; parathion, 59–67%; b) phosfolan, 10–23%; monocrotophos, 4–7%. A tentative hypothesis was advanced that both oral toxicity of the four compounds for S. littoralis larvae and their subsequent recovery in the feces were related to water solubility.  相似文献   

10.
BACKGROUND: Resistance to insecticides has been related to application history, genetic factors of the pest and the dynamic within the treated area. The aim of this study was to assess the geographic variation in azinphos‐methyl response and the role of esterase and cytochrome P450 monooxygenase enzymes in codling moth populations collected within different areas of the Río Negro and Neuquén Valley, Argentina. RESULTS: Diapausing field‐collected populations showed resistance ratios at the LC50 that were 0.7–8.7 times higher than that of the susceptible strain. Mean esterase (EST) and cytochrome P450 monooxygenase activities (expressed as α‐N min?1 mg?1 prot?1 and pg 7‐OHC insect?1 min?1 respectively) were significantly correlated with LD50 values from the field‐collected populations. In addition, azinphos‐methyl response was associated with the geographic area where the insect population was collected: populations from isolated and more recent productive areas presented significantly lower resistance ratios in comparison with populations from older and more intensive productive areas. CONCLUSION: The populations assayed presented different resistance levels to azinphos‐methyl. The response was highly correlated with the orchard's geographic location. EST and ECOD activities were involved in azinphos‐methyl response in the given region. Copyright © 2012 Society of Chemical Industry  相似文献   

11.
Cationic vesicles were produced by incorporating positively-charged stearylamine into the lipid bilayers. The addition of stearylamine has been shown to facilitate targeting of liposomes to the skin-associated bacterium Staphylococcus epidermidis. The adsorption of the liposomes to films of the bacteria immobilized on a solid surface has been studied. The extent of adsorption as a function of liposomal lipid concentration could be described in terms of a Langmuir adsorption isotherm, applicable to situations in which species are adsorbed as monolayers on solid surfaces. Analysis on the basis of the Langmuir model enabled the determination of the maximum theoretical targeting to the bacteria and association/dissociation constants for the interaction. The adsorption was examined under conditions of varying ionic strength. Increasing the ionic strength had the effect of decreasing the extent of targeting and suggested that the interaction between the cationic vesicles and sites on the bacterial surface was mediated by electrical double-layer effects. It follows that electrostatic effects make a major contribution to the interaction between these vesicles and S. epidermidis. The attachment of the vesicles is reversible and ionic strength-induced removal of vesicles from the bacteria could be used as a tool to study the delivery of liposomally encapsulated bactericide to the biofilm.  相似文献   

12.
The adsorption of some plant growth regulating compounds onto lecithin and equimolar lecithin/cholesterol vesicles and the effect of these substances on the rate of chloride/nitrate and sodium/potassium ion exchange across the vesicular membranes have been examined. On comparing the binding of 2,4-D, 2,6-D, 2,4,5-T and IAA to lecithin vesicles in solution at various pH values it is found that the unionised form of these acids is bound very much more strongly than the ionised form. Compounds having relatively low oil/water partition coefficients such as 2,4-D, 2,6-D and 2,4,5-T are adsorbed onto vesicles, from solutions containing equimolar equilibrium concentrations of the unionised molecules, to markedly different extents (depending on the structure of the lipophilic portion of these molecules). Where the oil/water partition coefficient is higher, as for 2,4-dichlorophenol and 2-(2,4-dichlorophenoxy)ethanol, binding to vesicles may also arise due to non-specific solution within the hydrocarbon region of the lipid bilayers. The affinity of these compounds for lecithin has also been assessed by noting the extent to which the inclusion of lecithin in the oil phase increases the oil/water partition coefficient. This has shown that affinity for lecithin depends on the structure of both the lipophilic and hydrophilic portions of the molecule. Only the unionised form of the compounds examined had any large effect on ion flux across the vesicle membranes. Significant increases in the rate of chloride/nitrate exchange were obtained on introducing quite high concentrations (0.015 to 1.5 mM) of the compounds 2,4-D, 2,6-D, 2,4,5-T, IAA, and 2,4-dichlorophenol, but not 2,4-dichlorophenoxyethanol, to suspensions of lecithin vesicles. Similar flux increases were observed with lecithin/cholesterol vesicles except that more pronounced effects on flux were obtained on adding 2,4-dichlorophenol and 2,4-dichlorophenoxyethanol. In contrast 2,4-D, 2,6-D, 2,4-dichlorophenol and IAA had no significant effect on the rate of Na+/K+ ion exchange across lecithin vesicles although increases were observed with equimolar lecithin/cholesterol vesicles. Interpretations of these phenomena are suggested and their relevance to plant growth substance effects at the plasmalemma membrane discussed.  相似文献   

13.
Several glutathione S-transferases which catalyze the conjugation of reduced glutathione with organophosphorus triesters were separated from fat bodies of adult female American cockroaches, Periplaneta americana (L.). Two transferases (I, V) were active on diazinon and three transferases (II, III, IV) were active on methyl parathion. The transferase (I) active on the pyrimidinyl moiety of diazinon was distinguishable from the other transferases on the O-methyl portion of methyl parathion, as shown by chromatographic properties, and additionally it was almost inactive or less active on 3,4-dichloronitrobenzene, methyl iodide, p-nitrobenzyl chloride, trans-cinnamaldehyde, and 1,2-epoxy-3-(p-nitrophenoxy)propane. Transferase II had high activities with “aryl” and “aralkyl” compounds, transferase III with “epoxide” and “alkene,” and transferase IV with “alkyl,” “aryl,” and “aralkyl” compounds. This indicated that the transferases had overlapping substrate specificities. The molecular weight was 35,000–37,000 for both of the enzymes active on methyl parathion and diazinon. The pH optima with methyl parathion and diazinon were about 8.5 and 6.5, respectively. At a glutathione concentration of 5 mM, Michaelis constants were 0.28 and 0.13 mM for methyl parathion and diazinon, respectively.  相似文献   

14.
The toxicity in the brain of several parathion, fenthion, and fensulfothion insecticides and their toxic metabolites was determined by a technique of directly injecting the compounds into the region of the third ventricle of conscious mice, an area rich in cholinesterase activity. The results were compared on a body weight basis to the toxicity of these compounds when given by ip and oral routes. The results show that there is a direct relationship between the relative inhibition of cholinesterase activity in the brain by the organophosphates (e.g., methyl paraoxon, Sumioxon, and some members of the fenthion series) and the toxicity of these compounds in the brain. Methyl paraoxon and Sumioxon were found to be very toxic in the brain, Sumioxon being three to four times less toxic than methyl paraoxon. This is of the same order of effect of these compounds in inhibiting cholinesterases. It is concluded that any selective effects of Sumithion compared with methyl parathion must be due to the greater rate of metabolism of Sumithion to less toxic metabolites as well as to the lower toxicity of the oxon metabolite and not due to the relative rates of penetration of the toxic oxygen metabolites as previously suggested [J. Miyamoto, Agr. Biol. Chem.28, 422 (1964)]. A gas-liquid chromatographic method was employed to assess the distribution in the brain following intracerebral injection of the parathion-type compounds. The results suggest that there may be intracerebral metabolism of thionophosphates in vivo.  相似文献   

15.
Phase transitions in the membrane lipids of chill-sensitive plants at 12°C and below are considered to result in an increase in the activation energy of membrane-bound enzymes and membrane permeability, leading to cell death. In agreement with this hypothesis, chill-hardening at 12°C results in an increase in the degree of unsaturation of the fatty acids associated with the membrane phospholipids of Phaseolus vulgaris and Gossypium hirsutum leaves. However, drought-hardening P. vulgaris leaves at 25°C is as effective in preventing chilling injury as chill-hardening at 12°C but drought-hardening produces no increase in the degree of unsaturation of the membrane fatty acids suggesting that lipid phase changes are not the primary cause of chilling injury. Furthermore, a re-examination of the conditions under which water and electrolytes leak from P. vulgaris leaves indicates that phase changes in the membrane lipids of the plasmalemma and other organelles at 5°C are only of minor importance in determining the extent and speed of chilling injury. The primary cause of chilling injury to P. vulgaris leaves on transfer from 25°C, 85%r.h. to 5°C, 85%r.h. is leaf dehydration due to the opening of the stomata at a time when the permeability of the roots to water is low. The primary factor inducing hardening against chilling injury in P. vulgaris is a water stress and not low temperature per se. Phase transitions in the membrane lipids of a chill-resistant species have now been detected within the same temperature range as those reported for chill-sensitive species. Therefore, the ability of temperate species to withstand chilling injury cannot be explained solely on the maintenance of a high degree of unsaturation of the membrane fatty acids.  相似文献   

16.
The rapid effects of the herbicide EPTC (S-ethyl dipropylthiocarbamate) and the protectant DDCA (N,N-diallyl-2,2-dichloroacetamide) on [2-14C]acetate incorporation into lipids of maize cell cultures were studied in order to determine whether they act at similar sites of lipid synthesis. DDCA, at 0.05 mM and 0.1 mM, increased the incorporation of [2-14C]acetate into neutral lipids of a total lipid extract within 2 h. It had very little effect on the major polar lipid constituents. DDCA altered neither the distribution of label within the major lipid classes, nor turnover of the major lipids within 2 h. EPTC (0.1 mM) inhibited overall uptake of [2-14C]acetate into both neutral and polar lipids by about 30% after a 2-h incubation. The major polar lipid affected was an unidentified glycolipid. In addition to reducing the quantity of lipids synthesized, EPTC changed the lipid profile, altering the distribution of label, mainly within the neutral lipid fraction. A crude membrane fraction from maize cells contained both polar lipids and some neutral lipids. DDCA stimulated [2-14C]acetate incorporation into different lipid species. EPTC inhibited incorporation of [2-14C]acetate into both neutral and polar membrane lipids but altered significantly only its distribution into neutral lipids. DDCA (0.1 mM) given together with EPTC (0.2 mM) partially counteracted the effect of EPTC within the neutral lipid fraction. It is suggested that DDCA has a rapid effect on lipid synthesis, but it is probably not sufficient to account for the entire mode of action of the protectant.  相似文献   

17.
Experiments on the control of wheat bulb fly larvae by seed dressings compared four organophosphorus compounds in standard siliceous earth formulations with special formulations of the same compounds in polyvinyl acetate, polypropylene or wax. The special formulations allowed more insecticide to be placed on the seeds without affecting germination. Counting shoots damaged by wheat bulb fly larvae showed that: siliceous earth formulations of diazinon gave good control which was not improved by special formulations; control with siliceous earth formulations of dimethoate was poor and was improved only little by the special formulations; and control with siliceous earth formulations of parathion and dichlofenthion was moderate and was improved by special formulations, especially polyvinyl acetate and polypropylene. The results suggest that special formulations are of most value with compounds that are moderately effective but where the amount of insecticide in standard seed dressings cannot be increased without damaging the plants.  相似文献   

18.
Perfusion of 14C-(ring)-parathion or 14C-(ring)-paraoxon with blood through isolated, intact rat livers resulted in the rapid degradation of these insecticides. Degradation was negligible in the absence of rat liver (controls), thus demonstrating the capacity of the liver per se to effectively degrade these compounds. Of the total radiocarbon recovered after liver perfusion with [14C]parathion, 33 % could be attributed to unchanged [14C]parathion (similarly distributed between the liver and the blood) while 67.9 % was degraded to water soluble compounds and 2.5% was converted to organic soluble paraoxon and traces of p-nitrophenol. Nearly all of the [14C]paraoxon, however, was degraded by the intact rat liver, resulting in water soluble products that amounted to 98.5% of the total radiocarbon recovered. Unexplained losses of radiocarbon with the perfusion apparatus used were lower in the presence of rat liver which degraded the insecticides to more water soluble compounds. The water soluble degradation products produced from [14C]parathion and [14C]paraoxon were non-toxic to mosquito larvae (Aedes aegypti L.). These ring-labelled products were found to be conjugated p-nito-phenol. Nearly all of the water soluble radiocarbon was located in the perfused blood, while only small amounts (1.8 to 3.0% of recovered) were excreted via the bile or were associated with the liver tissue (1.3 to 1.8 % of recovered).  相似文献   

19.
Chlorpyrifos (Dowco 179) and its dimethyl homologue, chlorpyrifosmethyl (Dowco 214), were used to study the influence of the O,O-dialkyl group of organophosphorus insecticides on toxicity, absorption, and metabolism among larvae of the tobacco budworm [Heliothis virescens (F.)] from strains that were resistant (R) and susceptible (S) to methyl parathion. In toxicity tests, chlorpyrifos and chlorpyrifosmethyl were more toxic than methyl parathion to 3rd-stage R larvae but less toxic to S larvae. Chlorpyrifosmethyl was more toxic (3–4 ×) than chlorpyrifos to both strains of larvae, and the results of absorption studies indicated that the toxicity differential of the homologues may be explained in part by the more rapid absorption of the dimethyl form. Studies of the in vivo metabolism of both Dowco compounds indicated that each was degraded mainly by the cleavage of the pyridylphosphate linkage. In vitro tests demonstrated that the NADPH-dependent microsomal oxidases were of primary importance in detoxification, while glutathione (GSH)-dependent mechanisms (aryl- and alkyltransferases) present in the soluble cell fractions were of lesser importance. O-dealkylation occurred only with chlorpyrifosmethyl. The R larvae demonstrated greater capability in detoxifying both compounds in the comparative in vivo and in vitro studies of metabolism, but the differences were more apparent during the 5th instar than during the 3rd instar.  相似文献   

20.
Twenty-seven insecticides, including organochlorine, organophosphorus compounds and carbamates were tried for potentiation of the toxic effect of malathion. Carbaryl, diazinon, fenthion, gamma-BHC, parathion and tetrachlorvinphos potentiated the action of malathion. Fourteen insecticides gave additive effects while seven proved antagonistic. Insecticides which showed potentiation, were further tested by mixing with malathion in the ratios of 1:9, 3:7, 5:5, 7:3 and 9:1. All the five combinations in the six mixtures gave potentiating effects. Maximum potentiation of 17.6 times was observed in 1:9 combination of malathion and gamma-BHC. The proportions in which the insecticides were mixed had a pronounced effect on the toxic effect of malathion.  相似文献   

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