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1.
Doses of ten acaricides, ranging from 2.5 to 10 μg, induced about 10-60% mortality and inhibited oviposition in engorged Boophilus microplus as well as preventing larval hatching from the eggs. The effects of the acaricides were dose dependent. The efficacy of acaricides in reducing the reproductive potential (inhibition of oviposition × inhibition of hatching/100) was in the following order: dimethoate > dioxathion > naled > diazinon > chlordimeform > carbaryl > trichlorphon > phosphamidon > gamma-HCH > fenitrothion. Most of the acaricides also retarded the oviposition cycle, delaying the peak activity by 4-8 days. The ovarian development in control ticks reached its peak between the 5th and 7th days before decreasing gradually and ceasing completely between the 16-20th days after engorgement. The protein content of the ovaries and the rate of incorporation of [14C]glycine into the tissues followed a similar pattern. Carbaryl, fenitrothion and naled inhibited these activities. Chlordimeform stimulated [14C]glycine incorporation and increased the ovarian protein content up to the 13th day before resorption of the oocytes. The eggs from treated ticks were mostly non-viable and contained more protein; those from dioxathion, carbaryl and chlordimeform treatments had a higher dry weight than the control.  相似文献   

2.
The present study reports on the insecticidal and acaricidal potentials of dibenzyltrisulfide (DBTS) isolated from the roots of Petiveria alliacea L. using thin layer and high performance liquid chromatography. The 96-h LD50 value (μg per tick) obtained for adult Boophilus microplus (Canestrini) topically treated with DBTS was 0·920. The LD50 values obtained for three commercial acaricides dimethoate, lindane and carbaryl were 4·6, 9·3 and 6·9 μg per tick respectively. The IOD50 and IHD50 (concentrations inhibiting egg laying and hatching by 50% respectively) in μg per tick doses for DBTS were 0·22 and 0·24 respectively. The 24-h LD50 dose (μg per insect) obtained for DBTS on adult Cylas formicarius elegantulus (Summer) was 0·193 μg per insect. The vapour from a stock solution of 5 g litre-1 of DBTS was highly toxic to adult Hypothenemus hampei Ferr. inside coffee berries, inflicting 89% mortality within 24 h. © 1997 SCI.  相似文献   

3.
5-tert-Butyl-2-(4-ethynylphenyl)pyrimidine and the corresponding 2,5-disubstituted-4H-1,3-thiazine block the GABA-gated chloride channel at c.20and c.200 nm , respectively, measured as 50% inhibition of the binding of 1-(4-ethynylphenyl)-4-[3H]propyl-2,6,7-trioxabicyclo[2.2.2]octane (4′-ethynyl-4-n-[3H]propylbicycloorthobenzoate; [3H]EBOB) in house fly and mouse brain membranes, and they are also toxic to topically-treated flies with LD50 values of 6–27 μg g−1 alone and 2–6 μg g−1 with piperonyl butoxide (PB) as synergist. In the pyrimidine series, the general pattern of effectiveness of substituents in the 5-position is tert-butyl>isopropyl≈cyclohexyl≈cyclopropyl>methyl, phenyl and 3- and 4-fluorophenyl, and in the 2-position is 4-ethynylphenyl≪4-bromophenyl. These planar pyrimidines and nearly-planar 4H-1,3-thiazines with 2-ethynylphenyl or 2-bromophenyl and 5-tert-butyl or 5-isopropyl substituents are more effective than the corresponding 6H-1,3-thiazine, 6-oxo-1,3-thiazines and 4,6-dioxo-1,3-thiazine examined, but they are less active than the analogous conformationally flexible trans-1,3-dioxanes and -1,3-dithianes. The heterocyclic moiety confers a region of high electron density and positions the 2- and 5-substituents in a linear or parallel relationship for optimal affinity at the receptor. Two observations indicate that the new pyrimidines and thiazines probably act as chloride channel blockers. First, the poisoning signs are identical to those of EBOB in both mice and house flies. Second, each of the pyrimidines, thiazines and dioxanes falls on the same correlation line for inhibition of [3H]EBOB binding and toxicity to house flies (with PB) as that obtained earlier for EBOB analogs, dithianes and polychlorocycloalkanes, suggesting that they all act at the same or closely coupled binding sites in the GABA-gated chloride channel.  相似文献   

4.
Duplicate field trials were carried out on bulk wheat in commercial silos in Queensland and New South Wales. Laboratory bioassays on samples of treated grain at intervals over 9 months, using malathion-resistant strains of insects, established that treatments were generally effective. Fenitrothion (12 mg kg?1)+ (1R)-phenothrin (2 mg kg?1) was more effective than pirimiphos-methyl (6 mg kg?1) + carbaryl (10 mg kg?1) against Sitophilus oryzae (L.) and Ephestia cautella (Walker); the order of effectiveness was reversed for S. granarius (L.). Against Rhyzopertha dominica (F.), Tribolium castaneum (Herbst), T. confusum Jackquelin du Val and Oryzaephilus surinamensis (L.), both treatments effectively prevented the production of progeny. The order of persistence was pirimiphos-methyl> (1R)-phenothrin>carbaryl or fenitrothion. During processing from wheat to white bread, residues were reduced by 98% for carbaryl, >44% for (1R)-phenothrin, 98% for fenitrothion and 85% for pirimiphosmethyl.  相似文献   

5.
The effects of aldrin, carbaryl, α- and γ-chlordane, dichlorodiphenyldichloroethane (DDD), dichlorodiphenyltrichloroethane (DDT), dieldrin, endrin, heptachlor, lindane, methoxychlor, and nonachlor on the short-circuit current and resistance of the isolated intact frog skin were studied. The short-circuit current is approximately equivalent to the rate of active transport of sodium, while the resistance indicates the summed ionic permeability of the skin. At a concentration of 2 × 10?4M, only carbaryl, DDD, dieldrin, and lindane produced significant (P<0.05, paired t test) changes in the short-circuit current. Nonachlor produced a decrease (P=0.12) in the short-circuit current and also increased the resistance (P=0.07). DDD, dieldrin, and carbaryl caused significant increases in short-circuit current while at the same time the resistance was significantly decreased. Lindane increased both the short-circuit current and the resistance. It was concluded that the frog skin probably contains effective permeability barriers that prevent externally applied insecticides from reaching the site of active sodium transport. It appeared likely that most of the insecticides produced the observed effects on the frog skin by altering the sodium permeability of the outer barrier.  相似文献   

6.
The absorption and metabolism of topical doses of carbaryl by larvae of the gypsy moth, Lymantria dispar (L.), were determined using 14C-ring-labeled material. Carbaryl penetration followed four distinct phases of linear absorption, i.e., 0–5 min, 5–60 min, 1–3 hr, and 3–12 hr; the absorption rates for the four phases were 2.8, 0.57, 0.07, and 0.02% per minute, respectively. Ninety percent of the total metabolism of carbaryl occurred within the first 3 hr; over the next 9 hr, metabolism was exceedingly slow with a linear rate of ca. 0.8% per hour. Carbaryl was always the major radiocarbon in the larvae and the feces, amounting to ca. 16 and 9%, respectively, at 12 hr. At 12 hr the metabolite composition was 5-hydroxy carbaryl >N-hydroxy carbaryl > 1-naphthol > 4-hydroxy carbaryl > 5,6-dihydro-5,6-dihydroxy carbaryl. Small amounts of an additional product were detected but not identified. Much of the excretion of carbaryl and metabolites occurred without conjugation. The amounts of carbaryl metabolized by second, third, fourth, and fifth instars were directly correlated with the insecticide tolerances and mixed-function oxidase activity of the various larval stages. The synergistic action of 2,6-dichlorobenzyl-2-propynyl ether and piperonyl butoxide was also correlated with inhibition of the oxidative pathway.  相似文献   

7.
The metabolism of [14C]asulam (methyl 4-aminophenylsulphonylcarbamate), [14C] aminotriazole (1H-1,2,4-triazol-3-ylamine) and [14C]glyphosate (N-(phosphonomethyl)glycine) were assessed in Equisetum arvense L. (field horsetail). Following application of the test herbicides (4mg?0.3 °Ci herbicide/shoot) to the shoots of 2-year-old pot-grown plants, the total recovery of 14C-label after 1 week and 8 weeks was high for all three herbicides (>80-0% of applied radioactivity). Asulam was persistent (>69-7% of recovered radioactivity) in both shoots and rhizomes. Sulphanilamide, a hydrolysis product of asulam, accounted for the remainder of the recovered radioactivity. Aminotriazole showed evidence of conjugation in shoots and rhizomes. The principal 14C-labelled component in shoots was composed of high proportions of aminotriazole (>76-3%) together with the metabolites: X (ninhydrin positive), β-(3-amino-1,2,4-triazolyl-1-)α-alanine, Y (diazotization positive) and various unidentified compounds. Rhizomes generally contained lower proportions of intact aminotriazole (>59.4%) together with the metabolites X,Y and unidentified compounds. The proportion of aminotriazole did not decrease with time in shoots or rhizomes; however, the ratio of metabolite X: Y moved in favour of Y as the interval after treatment increased. Glyphosate was extensively metabolised in shoots and rhizomes to yield aminomethylphosphonic acid (AMPA) and various unidentified compounds. Differential metabolism appears to be one of the factors which may govern the persistence and toxicity of the test herbicides in E. arvense.  相似文献   

8.
Methacrifos (22.5 g t?1) and the three protectant combinations chlorpyrifos-methyl (10 g t?1) plus bioresmethrin (1 g t?1), fenitrothion (12 g t?1) plus (1R)-phenothrin (2 g t?1) and pirimiphos-methyl (4 g t?1) plus carbaryl (8 g t?1) were each applied to grain that was stored in at least 15 silos. Grain temperature and levels of protectant were regularly monitored, and samples from 12 storages using each treatment were taken for laboratory assays against Rhyzopertha dominica and Tribolium castaneum. Grain condition did not deteriorate during storage. Grain remained free of insects in 60 of the 63 storages treated; partial failure in the other 3 storages was attributed to low or irregular levels of protectant. The mean and range of residue values of all protectants were recorded as a function of time and the mean observed values corresponded to predicted values. In laboratory bioassay, the order of effectiveness against T. castaneum was methacrifos > chlorpyrifos-methyl plus bioresmethrin > fenitrothion plus (1R)-phenothrin = pirimiphos-methyl plus carbaryl. The order of effectiveness against R. dominica was carbaryl plus pirimiphos-methyl = (1R)-phenothrin plus fenitrothion > methacrifos > bioresmethrin plus chlorpyrifos-methyl.  相似文献   

9.
Potent herbicidal ethyl 5-[N-(5,7-dimethoxy2H-1,2,4-thiadiazolo-[2,3-a] pyrimidin-2-ylidene)sulfamoyl]-1,3-dimethylpyrazole-4-carboxylate (I) was hydrolyzed under weakly basic conditions to afford a sulfonylurea (VII) , a 2-pyrimidylcyanamide (IV) and a mercaptopyrazole (VI) . The formation of these products was explained by nucleophilic attack at the 1 and 2-positions of the 1,2,4-thiadiazolo[2,3-alpyrimidine ring. This is believed to mimic the process which occurs on application to the plant. I appears to be a pro-pesticide for the sulfonylurea, VII .  相似文献   

10.
The residues and metabolism of methidathion [S-(2, 3-dihydro-5-methoxy-2-oxo-1, 3, 4-thiadiazol-3-ylmethyl) O, O-dimethyl phosphorodithioate] and its secondary metabolites: demethyl-methidathion [S-(2, 3-dihydro-5-methoxy-2-oxo-1, 3, 4-thiadiazol-3-ylmethyl) O-methyl O-hydrogen phosphorodithioate] ( IV ), the sulphide (2,3-dihydro-5-methoxy-3-methylthiomethyl-1,3,4-thiadiazol-2-one) ( I ), tsulphoxide(2,3-dihydro-5-methoxy-3- methylsulphinylmethyl-1,3,4-thiadiazol-2-one) ( II ) and the sulphone (2,3-dihydro-5-methoxy-3-methylsulphonylmethyl-1,3,4-thiadiazol-2-one ( III ) were studied in laboratory-treated tomato fruit. The metabolites and residues of methidathion were determined for the applied doses of 1, 7 and 14 mg of methidathion kg?1 of fruit. Methidathion was metabolised extensively over a 14-day period. The amount of metabolites formed was a function of both the applied dose as well as the time after application. Major water-soluble metabolites were found to be IV and the cysteine conjugate S-(2,3-dihydro-5-methoxy-2-oxo-1,3,4-thiadiazol-3-ylmethyl)-L-cysteine ( VI ). The chloroform-soluble metabolites were identified as the oxygen analogue of methidathion [S-(2,3-dihydro-5-methoxy-2-oxo-1,3,4-thiadiazol-3-ylmethyl) O, O-dimethyl phosphorothioate] ( V ), the sulphoxide II , and the hydroxy compound 2,3-dihydro-3-hydroxymethyl-5-methoxy-1,3,4-thiadiazol-2-one. The oxygen analogue of methidathion ( V ) was found in small amounts, corresponding to <5% of the added methidathion. Demethyl-methidathion ( IV ) appeared to be a precursor in the formation of the cysteine conjugate VI . The sulphide I seemed to be more reactive in forming the cysteine conjugate than the sulphoxide II or the sulphone III .  相似文献   

11.
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   

12.
Several 2-carboxylbenzofurans and their coumarin precursors, compounds 1 – 6 , and the novel compound 7 were synthesized and their insecticidal activity studied using adult sweet potato weevils (Cylas formicarius elegantulus (Summer)) at 24 μg, 48 μg and 72 μg per insect in 0.5 ml litre?1 piperonyl butoxide (PPB) in acetone. The order of toxicity of the compounds as judged by the percentage mortality at 24 μg per insect at 48 h was 2 (100%) > 6 (95%) > 7 (85%) > 4 (75%)) > 3 (65%) > 1 (60%) > 5 (45%) > piperonyl butoxide (0.0%). Compound 2 was equitoxic to 24 μg of technical grade dimethoate. When administered in acetone alone, however, the compounds were only moderately active (i.e. > 120 μg per insect was required for 60% mortality at 48 h). The test compounds were more active at lower doses (48–72 μg per insect) when dissolved in dimethylsulfoxide or in an oil extract obtained from the fruit of Blighia sapida Koenig.  相似文献   

13.
A series of 5,6-diphenyl-3-substituted-thio-1,2,4-triazines ( II-V ) was prepared by treating 5,6-diphenyl-1,2,4-triazine-3-thiol ( I ) with corresponding electrophiles. Condensation of IV or V with 1,2-phenylenediamines gave 2-[(5,6-diphenyl-1,2,4-triazin-3-yl) thiomethyl-1H-benzimidazoles] ( VI ). IV was converted into its corresponding hydrazide ( VII ) by the action of hydrazine hydrate. N-Benzylidene derivatives ( VIII ) were prepared by the condensation of VII with appropriate aryl or heterocyclic aldehydes. The pesticidal activities of all the compounds thus synthesised were determined.  相似文献   

14.
采用提取、萃取及柱层析等方法,从山蒟Piper hancei Maxim甲醇提取物的石油醚和氯仿萃取相中分离到6个脂肪链酰胺类化合物,通过核磁共振、质谱并结合相关文献比对,其结构被分别鉴定为已知化合物chingchengenamide A( C1 )、N-异丁基-反-2-反-4-癸二烯酰胺( C2 )、假荜拨酰胺A( C3 )、荜茇宁( C4 )、N-p-香豆酰酪胺( C5 )和N-反式-阿魏酰酪胺( C6 ),其中 C1 为首次从山蒟中获得。利用幼虫浸液法测试了各化合物对白纹伊蚊Aedes albopictus和致倦库蚊Culex pipiens quinquefasciatus幼虫的12 h杀虫活性。结果表明:在20 mg/L下,化合物 C1 对白纹伊蚊的杀虫活性较高,其校正死亡率为100%,LC50值为5.37 mg/L;化合物 C1 、 C2 、 C3 和 C4 对致倦库蚊的杀虫活性较高,20 mg/L下的校正死亡率分别为100%、88.5%、100%和100%,LC50值分别为1.03、9.68、3.08和2.87 mg/L。  相似文献   

15.
[14C]Flamprop-methyl administered orally to rats (3-4 mg kg?1 body weight) was excreted mostly via the faeces (78.7 and 61.6% in males and females, respectively). Elimination was rapid and 90% of the dose of 14C was excreted in faeces and urine 0-48 h after dosing. The distribution of 14C between faeces and urine was different in males and females. No expired [14C]carbon dioxide was detected and less than 2% of the dose remained in the animals 4 days after dosing. The predominant metabolic pathway was hydrolysis of the ester bond to afford the carboxylic acid which was excreted unchanged and as its glucuronide conjugate. Aromatic hydroxylation occurred at the para- and meta-positions of the N-benzoyl ring. N-(3)-Chloro- 4-fluorophenyl-N-(3,4-dihydroxybenzoyl)-DL -alaninate was also formed. This hydroxylated form of flamprop-methyl was partially O-methylated at the 3-hydroxy group. Flamprop-methyl was also metabolised and eliminated rapidly by dogs, mice and rabbits. The last of these three species afforded very little aromatic hydroxylation and also differed from the others in that the metabolites were eliminated mostly in the urine. Aromatic hydroxylation lay in the order: male rat = female rat > dog= mouse>rabbit (female).  相似文献   

16.
The effects of selected neurotoxic pesticides on the feeding rate of marine mussels (Mytilus edulis) were determined. Two organochlorine pesticides, lindane and endrin, two acetylcholinesterase-inhibiting compounds, dichlorvos and carbaryl and two pyrethroids, flucythrinate and permethrin, were studied. No evidence was found for any specific neurotoxic effect of the organochlorines and pyrethroids on feeding efficiency. In contrast, dichlorvos and carbaryl inhibited the enzyme acetylcholinesterase in mussel gills and were more toxic to feeding efficiency than could be explained by a narcotic mechanism of toxicity alone. Dichlorvos also caused clear behavioural changes in the mussels. The significance of these observations for the application of mussels to impact assessment in the marine environment is discussed. © 1997 SCI.  相似文献   

17.
1,3,5-Triazapenta-1,4-dienes of formula Ar? N?CH? N(R)? CH?N? Ar′, are a new group of biologically active compounds. Various general methods for their preparation are described and their physical and chemical properties, including stability over range of pHs, are discussed. The unsymmetrical 1,3,5-triaza-penta-1,4-dienes(Ar≠Ar′) are unstable; insolution, particularly, they equilibrate to the corresponding stable symmetrical analogues. Structure-activity relationships in laboratory tests against Boophilus microplus and Tetranychus urticae are discussed. Problems in the synthesis of ring-[14C]-amitraz,b [1,5-di-(2,4-dimethylphenyl)-3-methyl-1,3,5-triazapenta-l,4-diene], an active member of the group, are outlined.  相似文献   

18.
The in vivo release of 14CO2 arising from decarbamoylation of [14C]-carbaryl (1-naphthyl methyl-[14C]-carbamate) injected into male and female Periplaneta americana, Leucophaea maderae, Gromphadorhina portentosa and Schistocerca gregaria was measured up to 50 nmol carbaryl/g body weight. The amount of 14CO2 released was proportional to the dose of [14C]-carbaryl injected and was similar for both sexes of each species. The KD50 values for carbaryl for each species did not correlate with their ability to decarbamoylate carbaryl. The degradation of carbaryl by this pathway is not therefore the limiting factor in determining the overall toxic effect of carbaryl in the four species studied. Decarbamoylation is inhibited by nitrogen in all four species. In P. americana the inhibition is virtually complete, in L. maderae, G. portentosa and S. gregaria the inhibition is 84%, 74% and 51% respectively. The results suggest the involvement of two enzymes, one of which is oxygen dependent. Decarbamoylation studies in air suggest the involvement of two enzymes with differing KM values. The involvement of aliesterases and mixed function oxidases in the decarbamoylation pathway(s) have not been established so far with this series of experiments.  相似文献   

19.
The activity levels of glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT) enzymes were estimated in liver, muscle and brain tissues of the fish, Sarotherodon mossambicus (Peters), which had been exposed to sub-lethal (3 mg litre−1) and lethal (25 mg litre−1) concentrations of the carbamate insecticide carbaryl. Based on the results obtained, the changes in GOT and GPT levels in liver, muscle and brain following different periods of sub-lethal and lethal carbaryl exposures suggested that S mossambicus showed adaptive elevation in the activity levels of the two aminotransferase enzymes in the tissues, thereby probably aiding gluconeogenesis through transamination of glucogenic amino acids to meet the energy demand under carbaryl toxicity. © 1999 Society of Chemical Industry  相似文献   

20.

The two cultivated Luffa species can be severely infected by Tomato leaf curl New Delhi virus (ToLCNDV) with up to 100% yield loss. Here, 52 Luffa genotypes were screened for ToLCNDV resistance after natural field infection. Mean vulnerability index (VI) ranged from 0.00 to 75.33; genotypes IIHR-137 and IIHR-138 had no symptoms (VI 0), 16 genotypes were resistant (VI 0–25), 15 were moderately resistant (VI 26–50), and 19 were moderate to susceptible (VI?>?50). Ten of the most resistant genotypes and five susceptible checks were then challenge-inoculated using whiteflies or sap in an insect-proof net house; only IIHR-137 [L. cylindrica (L.) Roem.] was symptomless (VI 0.00), and 3–5% of plants of IIHR-138 [L. cylindrica (L.) Roem.] and IIHR-Sel-1 [L. acutangula (L.) Roxb.] had only mild symptoms; genotype Arka Prasan was most susceptible (VI 80.96). Asymptomatic plants were confirmed as infected using polymerase chain reaction. Susceptible genotypes rapidly developed leaf curling, then a severe mosaic 10 days post-inoculation. The resistant inbred lines identified are good candidates for a breeding program for ToLCNDV-resistant cultivars.

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