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1.
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   

2.
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   

3.
In vitro studies of the desulfuration of parathion at 37°C by hepatic tissue from males and females of nine mammalian species revealed sex and species variation in initial rates of parathion desulfuration and arylesterase-catalyzed hydrolysis of the oxygen analogue, paraoxon. Double reciprocal plots of initial rates of parathion activation for representative males and females of each species gave Km values ranging from 0.2 × 10?4?1.0 × 10?4M parathion. Guinea pigs and rats were the only animals showing sex differences in activation, males possessing higher desulfurating abilities than the corresponding females. Based upon the sex possessing the higher desulfurating ability, the species pattern of decreasing activity was hamster > guinea pig > mouse > rat > rabbit > bovine > dog > porcine > cat. Studies of paraoxon hydrolysis indicated that only rats showed sex differences in hydrolysis, males possessing higher arylesterase activity than females. The species pattern of decreasing hydrolytic activity was in the order mouse > bovine > rat > guinea pig > rabbit > hamster > cat > dog > porcine.  相似文献   

4.
The organophosphorus insecticides, parathion and azinphos, significantly lower the midpoint temperature of thermotropic phase transitions of lipid bilayers, but malathion has no effect. The effects of parathion and azinphos are more pronounced on bilayers of short-chain lipids. These compounds induce phase separations in binary lipid mixtures containing dimyristoyl and distearoyl phosphatidylcholines, although similar effects could not be noticed in mixtures of dimyristoyl phosphatidylcholine and dimyristoyl phosphatidylethanolamine. Furthermore, the compounds partially restore phase transitions abolished by cholesterol. It is concluded that parathion and azinphos induce molecular disorders in lipid bilayers, either by having fluidizing effects or by promoting phase separations as a consequence of preferential interaction with more fluid lipids. The interaction of the compounds with cholesterol-containing bilayers produces phospholipid-rich lateral domains.  相似文献   

5.
The activities of acetylcholinesterase, diacylglycerol kinase, and phosphatidylinositol phosphodiesterase in rat brain microsomes were measured in the presence and absence of the organophosphorus insecticides, parathion and diazinon, and their respective oxon analogs, paraoxon and diazoxon. Marked inhibition of acetylcholinesterase (by 45–99%) was observed in the presence of paraoxon (10?2–10?6M) and diazoxon (10?2–10?4M). Reduction of acetylcholinesterase activity (by 22–33%) was achieved with the parent insecticides at high concentrations only (10?2M). In most cases, diacylglycerol kinase was insensitive to the pesticides. Marked stimulation of phosphatidylinositol phosphodiesterase (by 10–57%) was observed in the presence of all pesticides (10?2–10?3M). The phosphodiesterase exhibited slightly greater sensitivity to the parent compounds compared to the oxon derivatives. Stimulation of the phosphodiesterase by the insecticides was not correlated with acetylcholinesterase inhibition. Accordingly, the increase in phosphodiesterase activity was judged not to be acetylcholine mediated, but rather represented a direct effect of the pesticides on the enzyme or its microenvironment. Based on the present in vitro observations, it is proposed that certain organophosphorus pesticides may interfere with the normal process of synaptic transmission through both the inhibition of acetylcholinesterase and the stimulation of phosphatidylinositol phosphodiesterase. In view of the high concentrations of pesticides required to elicit the latter effect, interpretation of its physiological significance must await results from further studies performed in vivo.  相似文献   

6.
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   

7.
The rates of penetration of 14C-labeled insecticides (parathion, carbaryl, and dieldrin) through the foregut of the honeybee (Apis mellifera L.) were measured in vitro and in vivo. Uptake of the insecticides from the lumen of the foregut into foregut tissue was directly proportional to insecticide lipophilicity, but penetration through the foregut was not. Of the three insecticides studied, parathion appeared to possess the optimal physicochemical characteristics required for penetration. The uptake of carbaryl and release of dieldrin by the foregut tissues may limit their respective penetration rates. Insecticide penetration was found to be inversely proportional to the sucrose concentration in the lumen of the foregut in both in vitro and in vivo studies. The oral toxicity of carbaryl showed a similar dependence on the sucrose concentration of the solution in which the insecticide was fed. The data presented indicate that the honeybee foregut is permeable to lipophilic compounds and strongly suggest that this permeability may contribute substantially to the toxicity of orally ingested insecticides in this insect.  相似文献   

8.
The action of insecticides on the spontaneous electrical activity of neurohemal tissue in the stick insect, Carausius morosus, has been studied using extracellular electrodes. The pyrethroid, permethrin, causes a massive increase in the frequency of the spontaneously generated action potentials at concentrations between 5 × 10?5 and 5 × 10?8M. Concentrations as low as 5 × 10?11M are still effective in producing bursting activity.DDT, at concentrations between 5 × 10?5M and 5 × 10?6M, produces an overall increase in activity although the bursting activity is less violent than that shown with permethrin. DDT, 5 × 10?7M, is ineffective at altering the resting pattern.Carbaryl and coroxon cause a transitory increase in electrical activity at 1 × 10?4M, but are ineffective at 1 × 10?5M.It is concluded that insecticides could have a direct effect upon the neurohormonal balance in insects.  相似文献   

9.
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   

10.
Dissipation rates of diazinon, endosulfan, leptophos, methamidophos, methomyl, parathion and pirimicarb were studied on five minor vegetable crops, including cos and head lettuce, endive, cauliflower and Chinese cabbage. Residues from foliar treatment generally followed an exponential rate of decline. The number of days for residues to drop to below acceptable tolerances was highly dependent on the magnitude of the initial residue; large variations in initial residues were observed between years, between insecticides, and between crop types. Residues of five insecticides and two fungicides used in furrow treatments for onions intended for pickling were determined in the onions at harvest and after pickling. Fensulfothion and fonofos levels were below the accepted tolerance of 0.1 mg kg?1 at harvest, while chlorfenvinphos, chlorpyrifos and ethion were present above this level; fungicide residues were not detected. Following pickling, only ethion residues were still present in the onions at levels greater than 0.1 mg kg?1.  相似文献   

11.
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   

12.
Perfluidone (1,1,1-trifluoro-N-[2-methyl-4-(phenylsulfonyl)phenyl]methanesulfonamide) was shown to interfere with phosphorylation and electron transport in isolated mung bean (Phaseolus aureus Roxb.) mitochondria. At low molar concentrations (<100 μM), perfluidone acted as an uncoupler of oxidative phosphorylation as evidenced by stimulation of state 4 respiration, induction of ATPase activity, and circumvention of oligomycin-inhibited state 3 respiration. At higher molar concentrations (>100 μM), perfluidone inhibited electron transport by acting on complexes I and II, and on the alternate (cyanide-insensitive) oxidase. In isolated spinach thylakoids (Spinacia oleracea L.), perfluidone also acted as an uncoupler, at low concentrations, as evidenced by stimulation of photoinduced electron transport with water as the reductant and methyl viologen and ferricyanide as oxidants, and from reduced dichlorophenolindophenol to methyl viologen. In addition, perfluidone inhibited the rate and magnitude of valinomycin-induced mitochondrial swelling in isotonic potassium chloride and potassium thiocyanate, and with thylakoids suspended in potassium thiocyanate at concentrations that inhibited ATP generation (<100 μM). Passive swelling in mitochondria was induced at higher concentrations. The permeability of lecithin liposomes to protons was also increased by perfluidone in a manner characteristic of uncouplers. The results obtained suggested that the partitioning of perfluidone perturbs the inner mitochondrial and thylakoid membranes. The perturbations increase the permeability of the membranes to protons and cations (at least potassium) and decrease membrane “fluidity.” As a consequence of the perturbations, the ATP-generating pathway in both mitochondria and chloroplasts is uncoupled and the structural organization of the electron transport components in mitochondria is disrupted, resulting in multisite inhibition of respiration. No evidence was obtained for a direct interaction between perfluidone and redox components of the electron transport pathways.  相似文献   

13.
Homogenates of three strains of Myzus persicae, A, R, and E, with an LD50 for topically applied parathion of 9, 93, and 263 ng per aphid, showed an in vitro hydrolytic degradation of paraoxon of 2.3, 4.7, and 8.6 pmol/mg aphid/h, respectively. These values represent Vmax; Km was <10?7M. The three strains showed a malaoxon degradation of 2.4, 11.9, and 18.8 pmol/mg/h at 10?6M substrate concentration. Vmax for R and E was 21 and 27 pmol, respectively and Km 7 and 4 × 10?7M. Activity in strain A was too low to estimate these entities. The breakdown product of paraoxon was mainly diethyl phosphoric acid, that of malaoxon mainly dimethyl phosphoric acid. No hydrolysis of the carboxylester groups of malaoxon was found. Hydrolysis of paraoxon and malaoxon was inhibited by isopropyl and n-propyl paraoxon and by the salioxon-analog K2. The two latter compounds were shown to act as synergists with parathion when added in amounts that caused little mortality when given alone. The hydrolytic enzyme is soluble and retains its activity during incubations of several hours. It is likely that it is responsible for at least part of the resistance. Resistance was maintained without selection over a period of three years. There was no correlation between degree of resistance and carboxylesterase activity of the strains.  相似文献   

14.
The influence of various host plants on glutathione S-transferase activity was studied in the fall armyworm, Spodoptera frugiperda (J. E. Smith). Fall armyworm larvae were maintained on a semidefined artificial diet until the end of the fifth instar. The newly molted sixth instar larvae were then fed fresh leaves of various host plants for 2 days prior to glutathione S-transferase assays using 3,4-dichloronitrobenzene as substrate. The order of the midgut glutathione S-transferase activity of larvae after the worms fed on these plants was: mustard > turnip > cowpeas > peanuts > cotton > corn > cucumber > potato > Bermudagrass > millet > sorghum > soybeans. The difference in the transferase activity between soybean- and mustard-fed larvae was 10-fold. Kinetic study revealed a quantitative, but no qualitative difference in the glutathione S-transferase between soybean- and cowpea-fed larvae. Monoterpenes, such as α-pinene, β-pinene, menthol, and peppermint oil, had no effect on the enzyme. Cowpea-fed larvae were more tolerant of the insecticides diazinon, methamidophos, and methyl parathion than soybean-fed larvae were. These new observations help explain what has been happening in the field and might be of use in the development of pest management programs.  相似文献   

15.
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   

16.
Deltamethrin and NRDC 157, pyrethroid insecticides that produce different poisoning syndromes in mammals, enhanced veratridine-dependent, sodium channel-mediated 22Na+ uptake in mouse brain synaptosomes. Concentrations producing half-maximal enhancement were 2.5 × 10?8M (deltamethrin) and 2.2 × 10?7M (NRDC 157). This effect was stereospecific: The nontoxic 1S enantiomers had no significant effect on veratridine-dependent activation. At high deltamethrin concentrations, enhancement was maximal at 5 × 10?5?1 × 10?4M veratridine. Pyrethroid enhancement was completely blocked by 5 × 10?6M tetrodotoxin, and neither pyrethroid affected 22Na+ uptake in the absence of veratridine at concentrations up to 1 × 10?5M. The relative potencies of deltamethrin and NRDC 157 in the synaptosomal sodium channel assay agree well with their relative acute toxicities to mice when administered by intracerebral injection. These findings demonstrate that pyrethroids exemplifying both characteristic poisoning syndromes are potent, stereospecific modifiers of sodium channel function in mammalian brain.  相似文献   

17.
The response of plant cell membranes to vinyl organophosphorus insecticides was studied by determining the release of intracellular materials as a measure of membrane permeability and the uptake of [1-14C]-α-aminoisobutyric acid as a measure of active transport. A pretreatment with chlorfenvinphos (2-chloro-1-(2,4-dichlorophenyl)-vinyl diethyl phosphate) at 0.4 mM or higher concentrations increased the leakage of cell contents from the tissues of pea, corn, and beet, but two other vinyl organophosphorus insecticides, tetrachlorvinphos (2-chloro-1-(2,4,5-trichlorophenyl)-vinyl diethyl phosphate) and phosphamidon (2-chloro-2-diethyl carbamoyl-1-methyl vinyl dimethyl phosphate), had no effect. Simultaneous addition of phospholipids, β-sitosterol, or Ca2+ inhibited in varying degrees the chlorfenvinphos-induced permeability, suggesting that the leakage of cell contents might be due to alteration in membrane structure.Chlorfenvinphos or tetrachlorvinphos at 0.1 mM or higher concentrations inhibited the uptake of α-aminoisobutyric acid. The degree of inhibition varied with different plant species. The inhibition was competitive and was not prevented by phospholipids. However, Ca2+ and other divalent cations were stimulatory to the uptake of α-aminoisobutyric acid, either in the presence or absence of chlorfenvinphos. Chlorfenvinphos also inhibited plant growth in tobacco callus and pea stem assays.From the differences in effective concentration, structural requirement, and interaction with phospholipids, it is suggested that chlorfenvinphos affected the membrane permeability and active transport by different mechanisms. These effects probably underlie its inhibitory action on plant growth.  相似文献   

18.
In apterous adults of the spirea aphid, Aphis citricola van der Goot, the optimum conditions for determining acetylcholinesterase (AChE) activity consist of reaction mixture of 0.1 M phosphate buffer (pH 7.5), 10?3M acetylthiocholine (ASCh), and enzyme extract equivalent to 80 ± 3 μg protein incubated for 15 min at 30°C. The Km value for ASCh (6.7 × 10?5M) was much lower than that of butyrylthiocholine (BuSCh) (1.25 × 10?2M). The enzyme activity was almost completely inhibited by 10?6M paraoxon or 10?5M eserine and was 84% inhibited by 10?5M BW284C51 (a specific AChE inhibitor). DTNB was found to inhibit the enzyme activity and was therefore added at the end of the reaction. AChE activity of A. citricola was inhibited in vitro and in vivo by dimethoxon > dimethoate, and aldicarb sulfoxide > aldicarb > aldicarb sulfone. The in vivo effect correlates well with the toxicity level of the various toxicants. A neurotoxicity index which combines both mortality and in vivo inhibition of the aphid AChE activity is suggested as a measure for determining the toxicity of organophosphorus and carbamate compounds toward aphids.  相似文献   

19.
The critical acetylcholinesterase component, that is responsible for the resistance mechanism of decreased sensitivity to the inhibitor in the cattle tick Boophilus microplus (Can.), has been isolated from the organophosphorus-susceptible Yeerongpilly and resistant Biarra and Ridgelands strains. With the substrate acetylthiocholine this enzyme component gave a pH activity profile similar for all strains. Optimal substrate concentration for Ridgelands was 1.73.10?2M compared to 2.70.10?4M for the other strains. Computed Km values were 1.98.10?5M, 3.65.10?5M, and 6.43.10?6M for Yeerongpilly, Biarra, and Ridgelands strains, respectively, while the corresponding Vmax figures were 336, 135, and 21 μmoles acetylthiocholine hydrolyzed per gram of larvae per hour. These results are discussed in relation to the resistance mechanism and compared with similar parameters derived for this enzyme from bovine erythrocytes, the sheep blowfly Lucilia cuprina, and the sheep nematode Trichostrongylus colubtiformis.  相似文献   

20.
Salt gland function and osmoregulation in aquatic birds drinking hyperosmotic water has been suggested to be impaired by organophosphorus insecticides. To test this hypothesis, adult black ducks (Anas rubripes) were provided various regimens of fresh or salt (1.5% NaCl) water before, during, and after ingestion of mash containing 21 ppm fenthion. Ducks were bled by jugular venipuncture after 1, 7, and 12 days of treatment, and were then killed. Brain and salt gland acetylcholinesterase activities were substantially inhibited (44–61% and 14–36%) by fenthion. However, salt gland weight and Na+-K+-ATPase activity, and plasma Na+, Cl?, and osmolality, were uniformly elevated in all groups receiving salt water including those ingesting fenthion. In a second study, salt gland Na+-K+-ATPase activity in mallards (A. platyrhynchos) was not affected after in vitro incubation with either fenthion oxon at concentrations ranging from 0.04 to 400 μM, but was reduced in the presence of 40 and 400 μM DDE (positive control). These findings suggest than environmentally realistic concentrations of organophosphorus insecticides do not markedly affect osmoregulatory function in adult black ducks.  相似文献   

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