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1.
When seeds of winter wheat were carefully dressed in the laboratory with combinations of fungicides (organomercury alone or organomercury plus the systemic fungicide carboxin) and insecticides (aldrin, carbophenothion or chlorfenvinphos as liquid formulations, or a γ-BHC powder formulation) so as to ensure that nearly all the recommended amounts of the active ingredients stuck to them, the insecticides gave good insect control, but γ-BHC with organomercury fungicide decreased the number of plants that germinated, and γ-BHC with carboxin and organomercury was even more damaging. Commercially dressed seeds had only about 30 to 60% of the target dose of fungicides, but more than 80% of the target doses of the liquid insecticides aldrin, carbophenothion and chlorfenvinphos. With combinations of powder fungicide and liquid insecticide, greater amounts of pesticide on the seed were obtained if the insecticide was put on first. Because of unusually late sowings and little fungal infestation, neither laboratory nor commercially treated seeds provided good tests for control of smut.  相似文献   

2.
The acute oral toxicity of chlorfenvinphos [2-chloro-1-(2′, 4′-dichlorophenyl)vinyl diethyl phosphate] was measured in pigeon (Columba livia), pheasant (Phasianus colchicus), and quail (Coturnix coturnix japonica) and the compound was shown to be particularly toxic to pigeons. Additionally, all three species were fed chlorfenvinphos at 100 ppm in their diet for two or four weeks and esterase measurements were made by conventional and electrophoretic methods on extracts of liver, kidney and brain. The conventionally measured esterase inhibition correlated well with the acute oral toxicity figures. A more detailed study of the histochemically stained electrophoregams showed some discrepancies compared with conventional methods but offered a possible explanation of the inter-species toxicity difference in that it revealed differential inhibition of some brain iso-esterases in pigeon but not in pheasant or quail.  相似文献   

3.
The acute single dose oral toxicity of carbophenothion (S-4-chlorophenylthiomethyl OO-diethyl phosphorodithioate) has been determined in Canada geese (Branta canadensis), pigeons (Columba livia) and Japanese quail (Coturnix coturnix japonica). At post mortem examination gross pathological changes were observed in Canada geese and pigeons and esterase levels were determined by conventional and electrophoretic methods on extracts of liver and brain from these two species. Carbophenothion residue levels were determined in liver, brain and gizzard contents from the geese and pigeons. The overall pattern of results suggests that esterase inhibition may not be the dominant factor in carbophenothion poisoning in geese. It is suggested that a brain carbophenothion residue level of 1 part/106 is indicative of death by poisoning in geese.  相似文献   

4.
A series of incidents involving greylag goose (Anser anser) casualties in Angus and Perthshire and a single incident involving pink-footed goose (Anser brachyrhynchus) casualties on Humberside occurred during the winter of 1974/75. The results of post-mortem examinations and brain esterase studies were consistent with the deaths having resulted from organophosphorus poisoning. Chemical analysis revealed the presence of carbophenothion (S-4-chlorophenylthiomethyl OO-diethyl phosphoro-dithioate) residues in the gut contents and internal tissues of the casualties. It was concluded that the geese had died from carbophenothion poisoning following the ingestion of treated winter wheat seed and the factors that led to the incidents are discussed.  相似文献   

5.
An attempt was made to survey systems which carry out reduction of four pesticidal chemicals, heptachlor, parathion, 4,4-dichlorobenzophenone, and carbophenothion sulfoxide, in rat liver microsomes and in the supernatant in vitro. On the basis of the stimulatory effects of nicotinamide cofactors (NADPH and NADH), a flavin cofactor (FAD), localization of the systems, and their sensitivities to heat-inactivation treatment, four different reductive systems were recognized. They are (a) the mixed-function oxidase-coupled reductive systems, (b) an independent NADH-stimulated (instead of NADPH as above) microsomal system for parathion reduction, (c) FAD-stimulated system for reduction of carbophenothion sulfoxide and parathion, present specifically in the supernatant, and (d) a heat stable, nonenzymatic reduction system in the microsomes operated by flavoproteins and a flavin cofactor.  相似文献   

6.
Separate esterase activities of rat and mouse liver microsomes hydrolyzing malathion, trans-permethrin, and cis-permethrin were differentiated on the basis of their sensitivities to inhibition by paraoxon and α-naphthyl N-propylcarbamate (NPC). In rat liver microsomes, the malathionhydrolyzing activity was more sensitive to both inhibitors and showed a different time course of NPC inhibition than the activities hydrolyzing the permethrin isomers. Paraoxon completely inhibited trans-permethrin hydrolysis, but only partially inhibited that of cis-permethrin. The paraoxonsensitive trans- and cis-permethrin-hydrolyzing activities were not differentially inhibited, but separate inhibition curves were obtained for the inhibition of trans- and cis-permethrin hydrolysis by NPC. The mouse liver esterase activity hydrolyzing trans-permethrin showed a similar paraoxon sensitivity to that of rat liver, but that the paraoxon-sensitive portion of the cis-permethrinhydrolyzing activity was 5.5-fold less sensitive to paraoxon than the corresponding rat liver activity and was clearly differentiated from the mouse liver trans-permethrin-hydrolyzing activity. The mouse liver malathion-hydrolyzing activity was 100-fold less sensitive to paraoxon and 14-fold less sensitive to NPC than the corresponding rat liver activity. Rat and mouse liver esterase activities hydrolyzed trans- and cis-permethrin at similar rates under standard assay conditions, but mouse liver esterases were 10-fold less active in hydrolyzing malathion. The higher specific activity of rat liver malathion-hydrolyzing esterases resulted from the greater apparent affinity and maximum velocity for malathion hydrolysis. These results demonstrate that the hydrolysis of malathion, trans-permethrin, and cis-permethrin by rat and mouse liver microsomal preparations involves several esterases with differing substrate specificities and inhibitor sensitivities.  相似文献   

7.
双氟磺草胺的除草活性及对不同小麦品种的安全性评价   总被引：9，自引：4，他引：5  
双氟磺草胺为三唑并嘧啶磺酰胺类除草剂,为了明确其在我国北方麦田的应用前景,采用室内生测法研究双氟磺草胺的杀草谱、除草活性及对不同小麦品种安全性。双氟磺草胺对麦田常见阔叶杂草活性较高,对麦田恶性杂草播娘蒿、麦瓶草、麦家公、猪殃殃和荠菜的除草活性均高于常用除草剂苯磺隆,毒力倍数分别为1.56、6.26、1.65、18.27和22.75。济南17和山优2号2种小麦对双氟磺草胺的耐药性分别为苯磺隆的2.57倍和11.66倍。双氟磺草胺在小麦与5种杂草之间的选择性指数(11.16～49.32)远优于苯磺隆。该除草剂对小麦苗期的株高及鲜重有抑制作用,且对不同小麦品种的影响差异显著,其中对临麦2号、济宁13及济南17的株高和鲜重抑制率相对较高,对潍麦8号、山农6号及泰山9818等相对较低。研究表明双氟磺草胺具有很好的应用前景。  相似文献   

8.
An esterase or esterases in acetone powder preparations of mouse liver microsomes hydrolyze the cyclopropanecarboxylate ester linkage of pyrethroid insecticide chemicals derived from primary alcohols. The rate of cleavage of (+)-trans-chrysanthemates with various alcohol moieties decreases in the following order: 5-propargyl-2-furylmethyl; 5-benzyl-3-furylmethyl (bioresmethrin); 3-phenoxybenzyl; tetrahydrophthalimidomethyl esters. The hydrolysis rate of benzylfurylmethyl esters with various acid moieties decreases in the order: (+)- or (?)-trans-chrysanthemate; (+)-trans-ethanochrysanthemate; tetramethylcyclopropanecarboxylate; (+)- or (?)-cis-chrysanthemate or (+)-cis-ethanochrysanthemate. The trans-isomers of chrysanthemates and ethanochrysanthemates are hydrolyzed from 2.6- to more than 50-fold more rapidly than the corresponding cis-isomers. This enzyme system does not hydrolyze secondary alcohol esters, i.e., allethronyl (+)-trans- and (+)-cis-chrysanthemates.On intraperitoneal administration to mice, the (+)-trans-chrysanthemate and -ethanochrysanthemate of benzylfurylmethanol are of very low toxicity relative to the corresponding (+)-cis-isomers and the tetramethylcyclopropanecarboxylate. S,S,S-tributyl phosphorotrithioate (DEF) pretreatment increases the toxicity of these five compounds by 2.6- to more than 188-fold, with the exception of bioresmethrin whose toxicity is not altered. When the toxicity is increased, it is probably the result of esterase inhibition since DEF strongly inhibits the esterase activity of fresh liver microsomes while the mixed-function oxidase system remains active. The oxidase system metabolizes the chrysanthemates more rapidly than the ethanochrysanthemates of benzylfuryl-methanol. Depending upon the pyrethroid involved, the esterase or the mixed-function oxidase system, or both may be responsible for limiting the toxicity of these pyrethroids to mice.  相似文献   

9.
The effects of methamidophos and tri-o-cresyl phosphate (TOCP) on the endogenous phosphorylation of specific brain proteins were studied in Beijing white laying hens during the early stage of delayed neurotoxicity. Phosphorylation of mitochondrial and synaptosomal proteins was assayed in vitro by using [γ-32P]ATP as phosphate donor. Tri-o-cresyl phosphate (TOCP) administration enhanced the phosphorylation of synaptosomal proteins with molecular weight of 40 and 55 kDa by as much as 36% and 65%, respectively, and decreased the phosphorylation of mitochondrial protein (35 kDa) by 33%. A single dose of methamidophos enhanced the phosphorylation of 32-kDa synaptosomal protein by 44%; however, it had no effect on brain mitochondrial proteins. The activity of neuropathy target esterase (NTE) in dosed hens’ brain and spinal cord was assayed for the effects of methamidophos and TOCP. These results showed that methamidophos inhibited brain NTE by 41% compared with that of control after 7-day exposure, while TOCP inhibited brain NTE by 66%. Moreover, NTE activity from spinal cord in treated hens also exhibited a similar trend of activity inhibition. Together, these results suggested that methamidophos and TOCP induced changes of protein phosphorylation level from hen brain and resulted in different kinds of neurotoxicity.  相似文献   

10.
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   

11.
Inhibition of chicken brain neurotoxic esterase (NTE) by a series of O-halogenated-phenyl-O-alkyl phenylphosphonates was studied in vitro. The “apparent” activity was found to consist of “true” NTE (sensitive to mipafox) plus a minor mipafox-resistant component. The pI50 of O-(2,6-dichlorophenyl) O-methyl phenylphosphonate for “true” NTE was 6.65, whereas it was about 3 for mipafox-resistant hydrolysis of phenyl valerate. This compound is suitable as an alternative to mipafox in the assay of “true” NTE, whereas the use of leptophos oxon gives a less accurate measure. The ethoxy analogs are about as potent in vitro as the corresponding methoxy compounds. Leptophosoxon and ethoxyleptophosoxon are more potent in vitro inhibitors than desbromoleptophosoxon. Within a like group of chlorinated phenylphosphonates, a reasonable correlation between in vitro neurotoxic esterase inhibition of the oxon and in vivo delayed neurotoxic potential by the corresponding phosphonothionate exists. In vivo inhibition of “apparent” NTE from chicken brain, studied 24 hr after an oral dose, is dose dependent for leptophos, ethoxyleptophos, and desbromoleptophos, the latter one being a very potent in vivo inhibitor. Ethoxyleptophos and leptophos have about equal in vivo esterase inhibitory properties. For desbromoleptophos and leptophos there is good agreement between the minimum dose causing delayed neurotoxicity and the dose leading to substantial inhibition of “apparent” NTE; ethoxyleptophos, on the other hand, inhibits the esterase at a dose much lower than the one which is neurotoxic. Several possible explanations for this discrepancy are considered.  相似文献   

12.
Captan, folpet, and perchloromethylmercaptan were effective inhibitors of Penicillium duponti p-nitrophenylpropionate esterase activity (I50 = 0.5 – 2 μM) whereas α-naphthyl acetate esterase activity was not affected by the presence of these compounds. Captan and folpet are both equally effective at pH 7.3 and 8.3. The ionic composition of the medium had strong effects on the degree of inhibition produced by all inhibitors but did not alter esterase activity. Neither succinamide nor phthalimide caused inhibition of the p-nitrophenylpropionate esterase activity: The trichloromethylmercaptan portion of these fungicides appears to be responsible for the observed inhibition. The rapidity of captan and folpet inhibition of esterase activity (complete in < 1 min) compared to the rates of spontaneous decomposition (t12 > 1 min) and the insensitivity of captan and folpet inhibition to hydrogen ion concentration suggest that generation of spontaneous decomposition products is not required for inhibition. The results are consistent with a mechanism in which the entire fungicide molecule binds to the protein followed by enzyme-promoted reactions of captan and folpet which result in loss of esterase activity.  相似文献   

13.
The effect of the thiophosphoroorganic insecticide ronnel and its oxygen analog on oxygen consumption by homogenates, and on succinate dehydrogenase and cytochrome oxidase activities in the mitochrondrial fractions of rat brain and liver, was investigated. A marked inhibition of blood plasma cholinesterase activity by the oxygen analog was demonstrated, but acetylcholinesterase activity was not affected. In contrast to its thiophosphoroorganic precursor, the oxygen analog caused a significant decrease in oxygen consumption by rat brain and liver homogenates and a decrease in cytochrome oxidase activity in both solubilized mitochondrial fractions. The succinate dehydrogenase activity was reduced only slightly by the oxygen analog in the brain fraction, but was marked in the liver fractions. The results suggest that the toxic activity of ronnel in vivo may be ascribed to its oxygen analog which appears as a metabolite of the former.  相似文献   

14.
A new herbicide, epyrifenacil (S-3100), inhibits protoporphyrinogen oxidase (PPO) in plants. Repeated administration of epyrifenacil in laboratory animals led to some toxicological changes related to PPO inhibition, e.g., hepatotoxicity caused by porphyrin accumulation and anemia caused by the inhibition of heme biosynthesis. In vitro studies revealed that an ester-cleaved metabolite, S-3100-CA, is predominant in mammals, exhibits PPO-inhibitory activity, and thus is the cause of epyrifenacil-induced toxicity. To assess the human risk, the effects of species differences on the dynamics (PPO inhibition) and kinetics (liver uptake) of epyrifenacil were evaluated separately. The results of in vitro assays revealed an approximately tenfold weaker inhibition of PPO by S-3100-CA in humans than in rodents and six- to thirteen-fold less hepatic uptake of S-3100-CA in humans than in mice. Finally, it was suggested that humans are less sensitive to the toxicity of epyrifenacil than are rodents, although further mechanistic research is highly anticipated.  相似文献   

15.
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   

16.
Genotoxic effects of Chlorfenvinphos and fenbuconazole were examined by using mitotic index, mitotic phase, chromosomal abnormalities, 2C DNA content and Comet assay on the root meristem cells of Allium cepa. The roots were treated with 10, 20, 40, 60, 80, and 100 ppm concentrations for 24 and 48 h. The results indicated that Chlorfenvinphos and fenbuconazole significantly decreased the mitotic index in all treatments when compared with their controls. The percentages of mitotic phases have changed. Chlorfenvinphos and fenbuconazole significantly increased the abnormal cell frequency at all concentrations and treatment periods when compared with their controls. Different abnormal mitotic figures were observed in all mitotic phases. Among these abnormalities were stickiness, anaphase bridges, c-mitosis, laggards, and micronucleus. These pesticides remarkably depressed the 2C DNA content in the root meristems of A. cepa. The genotoxicity of chlorfenvinphos and fenbuconazole in A. cepa root cells was analyzed using comet assay, which allows the detection of single strand breaks. In all concentrations, chlorfenvinphos and fenbuconazole induced a significant increase in DNA damage. Additionally, it was also researched to determine if there is a relation between the amount of DNA and the DNA damage and a regression analyses was conducted. When the data that was accumulated via comet analysis from A. cepa root tip cells that are treated with type chlorfenvinphos and fenbuconazole, was compared to the data that was acquired as the result of the measurement of 2C DNA amount, a relation with negative correlation was found, (respectively, r = −0.80 and r = −0.82). This relation factor is statistically important and strong (p < 0.05).  相似文献   

17.
The sensitivity of brain acetylcholinesterase and neurotoxic esterase to inhibition by several organophosphorus compounds was studied in selected ectothermic vertebrates. These enzymes are associated with organophosphorus compound acute and delayed toxicity, respectively. In addition, the susceptibility of several of these species to delayed neurotoxicity induced by organophosphorus compounds was studied. Larvae of the gray treefrog, Southern leopard frog, and narrow-mouthed toad were exposed dermally to tri-o-tolyl phosphate or phenyl saliginen cyclic phosphate (PSCP); no symptoms of delayed neurotoxicity were observed in any of these animals up to 2 weeks after metamorphosis. No symptoms of delayed neurotoxicity were seen in juvenile bullfrogs exposed to multiple ip doses of PSCP. The specific activity of neurotoxic esterase was highest in the larval bullfrog, with juvenile channel catfish and adult mosquitofish demonstrating intermediate levels. The larval Southern leopard frog, adult Northern leopard frog, juvenile green treefrog, and adult marine toad exhibited extremely low activities. The specific activity of acetylcholinesterase was highest in the juvenile channel catfish. Neurotoxic esterase in the larval bullfrog was more sensitive to organophosphate inhibition than that in either fish. PSCP was a more potent neurotoxic esterase inhibitor than leptophos-oxon. The juvenile channel catfish had the acetylcholinesterase most sensitive to organophosphate inhibition. Under the conditions tested, no evidence of in vivo sensitivity to the organophosphate-induced delayed neurotoxicity phenomenon was observed.  相似文献   

18.
Carbaryl, chlorfenvinphos, diazinon, disulfoton, parathion, phorate, fenitrothion, thionazin and trichlorphon were tested for their effectiveness in killing wireworms by broadcast treatments. Each insecticide was tested once or more in two field trials cropped with wheat and two cropped with potatoes. Phorate and parathion were very lethal to wireworms at 4 Ib active ingredient per acre (4–48 kg/ha). Thionazin and diazinon were intermediate in effectiveness and the other insecticides ineffective.  相似文献   

19.
0.02% a.i. dicrotophos and dimethoate, 0.025% a.i. demeton-S-methyl, thiometon, chlorfenvinphos and methomyl, and 0.03% a.i. phosphamidon were evaluated in the field for control of aphids (Myzus persicae Sulzer) infesting tobacco. All the insecticides were effective but chlorfenvinphos and methomyl were inferior to the rest. 0.03% and 0.06% a.i. endosulfan and trichlorfon, 0.05% and 0.1% a.i. carbaryl, and 0.025% and 0.05% a.i. methomyl were evaluated in the field for control of caterpillars ofSpodoptera litura (F.) defoliating tobacco. Nearly all the insecticides were effective and carbaryl and trichlorfon gave satisfactory control even at the lower concentrations tested.  相似文献   

20.
Acute intraperitoneal toxicity of mipafox, paraoxon, and soman was highest in chicken, followed by rat, and lowest in frog. Species differences in organophosphorus toxicity were not related to differences in the specific activities of either acetylcholinesterase or carboxylesterase in brain. The sensitivity to inhibition of brain acetylcholinesterase in vitro by the organophosphorus compounds was closely related to the susceptibility of the species to acute organophosphorus poisoning. Both the acute toxicity and the sensitivity of brain acetylcholinesterase to inhibition in vitro by organophosphorus compounds in all the species were in the following order of increasing activity: mipafox < paraoxon < soman. The sensitivity of brain carboxylesterase to inhibition by the organophosphorus compounds were less than that of acetylcholinesterase and it could not be related to species susceptibility to acute organophosphorus toxicity. Paraoxon-insensitive phenyl valerate hydrolase in chicken brain was more sensitive to inhibition by mipafox and soman compared to rat; in chicken the sensitivity of paraoxon-insensitive phenyl valerate hydrolase to inhibition by soman was 9000 times more than that by mipafox, while in rat it was 100 times more. Frog brain had no paraoxon-insensitive phenyl valerate hydrolase activity. No evidence of age dependence was noticed in the specific activities of brain acetylcholinesterase, carboxylesterase, neurotoxic esterase, and paraoxon-insensitive phenyl valerate hydrolase or in the sensitivity of these enzymes to in vitro inhibition by organophosphorus compounds in both rats and chickens.  相似文献   

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