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1.
Diazinon toxicity to a susceptible strain of house fly (Musca domestica L.) was synergized by tridiphane [2-(3,5-dichlorophenyl)-2-(2,2,2-trichloroethyl)oxirane], a herbicide synergist. Both diazinon and tridiphane were partially metabolized in the house fly by glutathione (GSH) conjugation. Synergism appeared to be due to inhibition of diazinon metabolism/detoxification. Crude glutathione S-transferase (GST) preparations from the house fly catalyzed GSH conjugation of diazinon, tridiphane, 3,4-dichloronitrobenzene (DCNB), and chloro-2,4-dinitrobenzene (CDNB). Tridiphane and the GSH conjugate of tridiphane appeared to inhibit diazinon GSH conjugation, but diazinon did not inhibit tridiphane GSH conjugation. The enzymatic rate of tridiphane GSH conjugation was 22 times the rate of diazinon GSH conjugation; therefore, attempts to assay tridiphane as an inhibitor of diazinon GSH conjugation were inconclusive because of the high concentration of tridiphane GSH conjugate produced during the assay. CDNB underwent enzymatic GSH conjugation at a rate 240 times faster than that of tridiphane and 5000 times faster than that of diazinon. GSH conjugation of CDNB was not inhibited by tridiphane, but was inhibited by the GSH conjugate of tridiphane. In vivo, the GSH conjugate of tridiphane was produced in sufficient concentration to cause the observed inhibition of diazinon metabolism and synergism of diazinon toxicity. However, the possibility that parent tridiphane caused or contributed to the inhibition of diazinon metabolism and synergism of diazinon toxicity could not be excluded. Inhibition of diazinon metabolism did not appear to be due to depletion of either GSH or GST.  相似文献   

2.
The interactions between six insecticides (indoxacarb, cypermethrin, chlorpyrifos, azinphosmethyl, tebufenozide and chlorfenapyr) and three potential synergists, (piperonyl butoxide (PBO), S,S,S-tributyl phosphorotrithioate (DEF) and diethyl maleate (DEM)) were studied by dietary exposure in a multi-resistant and a susceptible strain of the obliquebanded leafroller, Choristoneura rosaceana (Harris). The synergists did not produce appreciable synergism with most of the insecticides in the susceptible strain. Except for tebufenozide, PBO synergized all the insecticides to varying degrees in the resistant strain. A very high level of synergism by PBO was found with indoxacarb, which reduced the resistance level from 705- to 20-fold when PBO was administered alone and to around 10-fold when used in combination with DEF. DEF also synergized indoxacarb, cypermethrin, chlorpyrifos, azinphosmethyl and tebufenozide in the resistant strain. DEM produced synergism of indoxacarb, chlorpyrifos, azinphos-methyl and chlorfenapyr in the resistant strain. DEM was highly synergistic to cypermethrin, and to some extent to tebufenozide in both the susceptible and resistant strains equally, implying that detoxification by glutathione S-transferases was not a mechanism of resistance for these insecticides. The high level of synergism seen with DEM in the case of cypermethrin may be due to an increase in oxidative stress resulting from the removal of the antioxidant, glutathione. These studies indicate that enhanced detoxification, often mediated by cytochrome P-450 monooxygenases, but with probable esterase and glutathione S-transferase contributions in some cases, is the major mechanism imparting resistance to different insecticides in C. rosaceana.  相似文献   

3.
A genetic analysis revealed that the resistance to diazinon of the bulb mite, Rhizoglyphus robini Claparède. lacked sex linkage, and was based on the operation of a dominant allele. Synergism of diazinon by eight inhibitors of detoxifying enzymes in susceptible and resistant strains of the bulb mite was determined. Esterases were shown to play an important role in detoxification against diazinon. S.S.S-tributyl phosphorotrithioate, an esterase inhibitor, was the only synergist which obviously synergized diazinon. The others, including the inhibitors of glutathione-S-transferases, carboxylesterase and mixed function oxidases, showed obscure or even antagonistic effect.  相似文献   

4.
Existence of diazinon, an organophosphorous pesticide, in river waters of Iran near rice paddy fields has been reported by some authors. The present research aimed to determine the acute toxicity and evaluate the effect of sub-lethal concentrations of diazinon on some biochemical parameters of rainbow trout, Oncorhynchus mykiss after 7, 14 and 28 days. No significant differences were observed in the plasma levels of creatinine among the treatment groups at different sampling intervals. Acetylcholinesterase activity and the levels of total protein, albumin as well as globulin in plasma were significantly reduced at both concentrations tested (p < 0.05). Lactate dehydrogenase activity was only decreased on 7th day in 0.1 mg/L diazinon treatment (p < 0.05). Creatine kinase activity was significantly lower in 0.1 mg/L diazinon group at 14th and 28th sampling periods, whereas its activity significantly increased in fishes exposed to 0.2 mf/L diazinon only on 7th day (p < 0.05). Aspartate aminotransferase, alanine aminotransferase activities and glucose levels in diazinon treated groups were significantly higher than the controlled group at experimental periods (p < 0.05). In conclusion, long-term exposure to diazinon at sub-lethal concentrations induced biochemical alterations in rainbow trout, and offers a simply tool to evaluate toxicity-derived alterations.  相似文献   

5.
The interactions between six insecticides (methiocarb, formetanate, acrinathrin, deltamethrin, methamidophos and endosulfan) and three potential synergists (piperonyl butoxide (PBO), S,S,S-tributyl phosphorotrithioate (DEF) and diethyl maleate (DEM)) were studied by topical exposure in strains selected for resistance to each insecticide, and in a susceptible strain of Frankliniella occidentalis (Pergande). In the susceptible strain PBO produced appreciable synergism only of formetanate, methiocarb and methamidophos. Except for endosulfan, PBO synergized all the insecticides to varying degrees in the resistant strains. A very high level of synergism by PBO was found with acrinathrin, which reduced the resistance level from 3344- to 36-fold. PBO slightly synergized the carbamates formetanate (4.6-fold) and methiocarb (3.3-fold). PBO also produced a high synergism of deltamethrin (12.5-fold) and methamidophos (14.3-fold) and completely restored susceptibility to both insecticides. DEF did not produce synergism with any insecticide in the resistant strains and DEM was slightly synergistic to endosulfan (3-fold). These studies indicate that an enhanced detoxification, mediated by cytochrome P-450 monooxygenases, is the major mechanism imparting resistance to different insecticides in F occidentalis. Implications of different mechanisms in insecticide resistance in F occidentalis are discussed.  相似文献   

6.
Pyrethroid resistance in field populations of Australian Helicoverpa armigera (Hübner) is primarily a consequence of the overproduction of esterase isoenzymes which metabolise and sequester pyrethroid insecticides. Biochemical studies have shown that pyrethroid-resistance-associated esterases in H armigera are inhibited by the insecticide synergist piperonyl butoxide (PBO). Esterase inhibition by PBO did not occur immediately after dosing, but exhibited maximum inhibition 3-4 h after dosage. Esterase activity subsequently recovered until full activity was restored by 24 h. Topical bioassays using a pre-treatment of PBO showed that maximum H armigera mortality was achieved with pre-treatment times corresponding to maximum esterase inhibition. These results demonstrated that, with correct temporal application, PBO can restore pyrethroid efficacy against H armigera. It would also be expected that restoration of efficacy with other conventional insecticides, currently compromised by esterase-based resistance mechanisms, would occur.  相似文献   

7.
The prolonged use of dimethoate, introduced into Denmark to control houseflies (Musca domestica L.) that had become resistant to parathion and diazinon, resulted ultimately in dimethoate resistance. Selection with dimethoate led to the disappearance of the hydrolytic phosphatase, a major mechanism of resistance to parathion and diazinon, and its replacement by the acetylcholinesterase AChER with somewhat decreased sensitivity to inhibition by organophosphorus (OP) insecticides. The hydrolytic phosphatase probably disappeared because low substrate turn-over made it ineffective against dimethoxon (O, O-dimethyl S-methylcarbamoylmethyl phosphorothioate, also known as omethoate). which accumulates at higher concentrations than paraoxon (diethyl4-nitrophenyl phosphate) in the haemolymph. Dimethoate selected AChER preferentially because it improved the chances of houseflies surviving against the relatively poor AChE inhibitor dimethoxon, whereas its relatively small insensitivity to OP insecticides, unimportant against good inhibitors such as paraoxon, prevented its selection by parathion.  相似文献   

8.
The rice stem borer, Chilo suppressalis (Walker), an important insect pest of rice in China, has developed resistances to several classes of insecticides in field. In order to investigate multiple resistance mechanisms, synergistic tests were conducted with the Ruian (RA) population and Lianyungang (LYG) population, two representative populations to different insecticides. Results showed that diethyl maleate (DEM), S,S,S-tributyl phosphorotrithioate (DEF) and piperonyl butoxide (PBO), had no significant synergistic or inhibitory effect on the high level of resistance to monosultap (313.4-fold) and moderate level to chlorpyrifos (36.9-fold) in Ruian field population from the year 2011 (RA11). DEF significantly synergized the activity of triazophos in RA11 population (536.8-fold), with synergism ratio of 1.92. DEF and PBO significantly suppressed 43.3% and 40.4% of resistance to fipronil in RA11 population (48.4-fold), respectively, with the synergistic ratios of 1.76 and 1.69. When pretreated with PBO, the activity of deltamethrin against RA11 population were significantly synergized, with synergism ratio of 9.57, and with reducing resistance levels from 152.5- to 15.9-fold. The results of this study indicated that resistance to several classes of insecticide among the field populations of C. suppressalis might be provided by the combination of the multiple resistance mechanisms. Metabolic resistance mechanism might be the major reason for the evolution for resistance to deltamethrin and fipronil, while resistance to monosultap, triazophos and chlorpyrifos is not associated with metabolic resistance.  相似文献   

9.
Laboratory tests in a fly chamber and field trials in the UK and Australia have shown that permethrin, (3-phenoxybenzyl (1R,1S)-cis,trans-3-(2,2-dichlorovinyl)-2, 2-dime-thylcyclopropanecarboxylate) containing 25: 75 cis: trans isomers, applied as water emulsions to cattle and horses will control biting flies. Satisfactory protection against the stable fly, Stomoxys calcitrans (L.) and excellent control against the horn fly, Haematobia (Lyperosia) irritans (L.) was achieved on cattle. Good control was obtained on horses against the stable fly and the sand fly Culicoides spp. These early results are encouraging and toxicity and residue data suggest that permethrin would be a safe insecticide to use on livestock for the control of biting flies of veterinary importance.  相似文献   

10.
In vitro inhibition of electric eel acetylcholinesterase (AChE) by single and simultaneous exposure to organophosphorus insecticides diazinon and chlorpyrifos, and their transformation products, formed due to photoinduced degradation, was investigated. Increasing concentrations of diazinon, chlorpyrifos and their oxidation products, diazoxon and chlorpyrifos-oxon, inhibited AChE in a concentration-dependent manner. IC50 (20 min) values, obtained from the inhibition curves, were (in mol/l): (5.1 ± 0.3) × 10−8, (4.3 ± 0.2) × 10−6 and (3.0 ± 0.1) × 10−8 for diazoxon, chlorpyrifos and chlorpyrifos-oxon, respectively, while maximal diazinon concentration was lower than its IC50 (20 min). Calculated KI values, in mol/l, of 7.9 × 10−7, 9.6 × 10−6 and 4.3 × 10−7 were obtained for diazoxon, chlorpyrifos and chlorpyrifos-oxon, respectively. However, 2-isopropyl-4-methyl-6-pyrimidinol (IMP) and 3,5,6-trichloro-2-pyridinol, diazinon and chlorpyrifos hydrolysis products, did not noticeably affect the enzyme activity at all investigated concentrations. Additive inhibition effect was achieved for lower concentrations of the inhibitors (diazinon/diazoxon ?1 × 10−4/1 × 10−8 mol/l i.e., chlorpyrifos/chlorpyrifos-oxon ?2 × 10−6/3 × 10−8 mol/l), while an antagonistic effect was obtained for all higher concentrations of the organophosphates. Inhibitory power of 1 × 10−4 mol/l diazinon irradiated samples can be attributed mostly to the formation of diazoxon, while the presence of non-inhibiting photodegradation product IMP did not affect diazinon and diazoxon inhibitory efficiencies.  相似文献   

11.
Factors likely to influence the uniformity of treatment and the stability of the insecticides incorporated into peat blocks were investigated. When an Adelphi horizontal mixer was used, 90% of the blocks contained the mean dose (±10%) after dry-mixing the diazinon granules for 3 min. Treatment was slightly less uniform using a concrete mixer or a spade. Between-block variability was greatest when diazinon was applied to the wet surfaces of prepared blocks; in this process, sprinkling granules by hand was less erratic than spraying a liquid formulation. When granular, wettable powder, or emulsifiable concentrate formulations of diazinon were incorporated using the Adelphi mixer, neither the between-block variability nor the subsequent stability of the insecticide were significantly influenced by the formulation used. Insecticide stability was studied by incorporating chlorfenvinphos, chlorpyrifos, diazinon and phorate at 10 mg a.i. per block in January, March, May and July. The relative order of persistence was chlorfenvinphosChlorpyrifos > phorate≫diazinon. There was little loss of insecticide ( < 10%) from the blocks treated with chlorfenvinphos or chlorpyrifos, and the stability of the insecticides was unaffected by seasonal temperature changes, but the rate of loss of diazinon increased markedly from January to July. The rate of oxidation of phorate to its sulphoxide and sulphone analogues increased gradually from January to May but was much slower than in the field after a bow-wave application. With all insecticides, there was no significant difference in loss rates at 25 and 10 mg a.i. per block. After incorporation into three moss peats and two proprietary blocking composts, there was no consistent difference in the rates of loss of either diazinon or of total phorate residues, although the rates of oxidation of phorate and its sulphoxide were not similar in all the peats and composts. It was concluded that, despite the substantial water content and high insecticide concentrations, the principal factor determining insecticide behaviour in the blocks was the adsorptive capacity of the peat.  相似文献   

12.
The relationship between glutathione S-transferase activity toward 3,4-dichloronitrobenzene and O-alkyl or O-aryl conjugation of diazinon was investigated in eight strains of house flies. No significant difference was found in the amount of O-aryl conjugation. In contrast, house flies which had higher glutathione S-transferase activity toward 3,4-dichloronitrobenzene also had higher O-alkyl conjugating activity toward diazinon. The glutathione S-transferase(s) in phenobarbital-pretreated flies degraded diazinon faster than those in the nontreated ones. The present results showed that the formation of the O-alkyl conjugate was enhanced by phenobarbital pretreatment, while the formation of the O-aryl conjugate was not affected by induction. Based on these findings, it would appear that one of the multiple forms of glutathione S-transferase is specifically induced and responsible for the increase in O-alkyl conjugation.  相似文献   

13.
The toxicity of a promising new insecticide, imidacloprid, was evaluated against several susceptible and resistant strains of German cockroach and house fly. Imidacloprid rapidly immobilized German cockroaches followed by a period of about 72 h during which some cockroaches recovered. After 72 h there was no further recovery. Imidacloprid-treated houseflies were immobilized more slowly than treated cockroaches, with the maximum effect observed after 72 h, and there was no recovery. Based upon 72-h LD50 values imidacloprid was moderately toxic to German cockroaches (LD50 values were 6–8 ng mg-1) and had only low toxicity to house flies (LD50 140 ng mg-1). Piperonyl butoxide (PBO) blocked the observed recovery in German cockroaches. PBO also greatly enhanced the 72-h LD50 of imidacloprid from 43- to 59-fold in cockroaches and 86-fold in house flies. Two strains of German cockroach (Baygon-R and Pyr-R) showed >4-fold cross-resistance to imidacloprid. This cross-resistance could not be suppressed by PBO, suggesting that P450 monooxygenase-mediated detoxication is not responsible for this cross-resistance. Variation in the level of synergism observed with PBO (between strains) suggests the ‘basal’ level of monooxygenase-mediated detoxication of imidacloprid is quite variable between strains of German cockroach. The AVER and LPR strains of house fly showed significant cross-resistance to imidacloprid. PBO reduced the level of cross-resistance in AVER from >4·2-fold to 0·5-fold (i.e. the AVER strain LD50 was half that of the susceptible strain when both were treated with PBO), but PBO did not suppress the cross-resistance in LPR. These data suggest monooxygenases are the mechanism responsible for cross-resistance to imidacloprid in AVER, but not in the LPR strain. © of SCI.  相似文献   

14.
In laboratory experiments, residues of diazinon applied to turfgrass, Poa pratensis L., that could be dislodged by rubbing with cheese-cloth, declined from c. 10% of the total applied when the grass was vigorously rubbed immediately after application to 0.3% after 1 day. Sunlight did not influence the rate of decline in dislodgeable residues or residues remaining on or within the leaf blades. In field experiments where 4.5 kg ha?1 of diazinon was applied in liquid or granular form, about 20 times more diazinon was dislodged from the liquid formulation immediately after application than from the granular. By 1 day after application the percentage of the total applied diazinon that could be dislodged was equal for both formulations. Rainfall had a significant effect on the amount dislodged from grass blades, but mowing did not. Similar rates of decline in the dislodgeable fraction of diazinon, chlorpyrifos and isofenphos were observed in field experiments. Recovery of the dislodgeable fraction declined to 0.25% or less of the total amount of any of these insecticides by 1 day after application. However, residues in the thatch remained sufficiently high for control of insects for up to 7 days after application for diazinon and 14 days for chlorpyrifos and isofenphos.  相似文献   

15.
Pyrethroid resistance in B-type Bemisia tabaci Gennadius and Australian Helicoverpa armigera Hübner field populations is primarily conferred by esterase isoenzymes which metabolise and sequester pyrethroid insecticides. It has been shown previously that pyrethroid resistance-associated esterases in H. armigera are inhibited by the insecticide synergist piperonyl butoxide (PBO) over a 22-h period. It is demonstrated here that similar inhibition can be obtained against B-type B. tabaci. Small-scale field trials showed excellent levels of pyrethroid control when insects were pretreated with PBO and then dosed with pyrethroid during the time of maximum esterase inhibition. These results demonstrate that PBO can restore pyrethroid efficacy in the field against both B-type B. tabaci and resistant H. armigera.  相似文献   

16.
A resistant laboratory strain of the German cockroach, Blattella germanica, was developed from a normal laboratory strain by selection with propoxur. Resistance to all insecticides except chlordane began increasing after 15 generations of selection and reached a plateau for most insecticides by generation 27. The resistant colony, designated B-strain, developed significant resistance to carbamates, organophosphorus compounds, pyrethrins and DDT, developed low resistance to gamma-BHC and no resistance to chlordane. The resistance spectrum, effect of synergists and inheritance of resistance of this propoxur resistant strain are similar to a diazinon resistant strain. Therefore, diazinon and propoxur may select for the same resistance mechanism(s) in this species. The practical implications of this research are discussed.  相似文献   

17.
BACKGROUND: Western flower thrips (WFT), Frankliniella occidentalis (Pergande), is among the most important crop pests in the south‐eastern region of Spain. Its increasing resistance to insecticides constitutes a serious problem, and understanding the mechanisms involved is therefore of great interest. Use of synergists to inhibit the enzymes involved in insecticide detoxification is widely used to determine their responsibility for insecticide resistance. However, they do not always act as intended or expected, and caution must be exercised when interpreting synergist results. RESULTS: Laboratory‐selected strains of WFT were used to analyse the effects of the synergists piperonyl butoxide (PBO), S,S,S‐tributyl phosphorotrithioate (DEF) and methiocarb on total esterase activity. Significant differences were found, indicating esterase activity inhibition by DEF, a lower effect for methiocarb and a small inhibition of the activity by PBO. Esterase isoenzyme inhibition by these compounds showed a similar result; this assay revealed an extreme sensitivity of Triplet A (resistance‐associated esterases) to DEF. In an in vivo assay carried out with these compounds at different incubation times, only DEF caused posterior in vitro esterase activity inhibition, with a maximum effect 1 h after treatment. CONCLUSION: In this work, only DEF shows true synergistic inhibition of WFT esterases. Copyright © 2011 Society of Chemical Industry  相似文献   

18.
Abstract

The systemic activity of four granular insecticides (phorate 10%, Temik 10%, diazinon 5% and Sevidol [8% carbaryl + 8% gamma-BHC]) was evaluated for the control of mustard aphid, Lipaphis erysimi (Kalt). The granules were applied in the soil to one month old mustard plants transplanted in pots. 3rd and 4th instar nymphs were used for the trial. Mortality counts were made 24 hours after release. Of the insecticides tested, phorate and Temik at 1 lb a.i./ac proved most effective. Temik had a quick knockdown effect as compared to phorate, as it gave 100% control within 24 hours, while with phorate 100% kill was obtained only after 72 hours. Diazinon at 4 lb a.i./ac gave 83.3% kill after 72 hours. Sevidol proved ineffective as an aphidicide. Residual toxicity of three of the granular insecticides, namely phorate, Temik and diazinon, was tested. Phorate and Temik at 1 lb a.i./ac exhibited the same residual toxicity up to 4 weeks, i.e. 100% and 76% kill obtained at the end of 2 and 4 weeks respectively. Although the toxicity of both pesticides gradually declined there was no significant difference in percentage kill over a period of 5 weeks. After 6 weeks, however, the mortality recorded with Temik was 37.1% and with phorate was 51.1%. The residual toxicity of phorate was further found to last up to 8 weeks, when the mortality obtained was 40%. The residual toxicity of diazinon sharply declined within 2 weeks.  相似文献   

19.
We investigated the molecular basis of resistance in a strain of house fly (BJD) from Beijing, China. This strain showed 567-fold resistance to commonly used deltamethrin. Flies were 64-fold resistant to deltamethrin synergized by piperonyl butoxide (PBO). The 5′-flanking sequence of the cytochrome P450 gene CYP6D1 in BJD strain had a 15-bp insert as in the LPR strain. Two mutations (kdr, super-kdr) in the voltage sensitive sodium channel (VSSC) were also detected in the BJD strain. Our results showed that a combination of resistance alleles for CYP6D1 and VSSC existed in deltamethrin resistant house flies in China.  相似文献   

20.
Analytical methods are described for the determination of residues of chlorfenvinphos, diazinon, fonofos and phorate in soils and carrots. The insecticides, applied in June 1969 at 2 kg (a.i.)/ha, persisted longer in peaty loam than in sandy loam. After 7 months, the sandy loam contained 1% of the applied diazinon and 20–30% of the applied chlorfenvinphos, fonofos and phorate, the latter as its sulphone; the corresponding figures for the peaty loam were 10, 40–50, 40–50 and 30–40% respectively. None of the residues showed any substantial change from October to January. Although high initial concentrations (up to 50 ppm) of the residues in carrots were diluted by plant growth, it is shown that concentrations >1 ppm could be present in marketable crops 12–14 weeks after application at recommended rates. Carrots harvested 26 weeks after sowing contained <0.2 ppm of all insecticides. In contrast, during the first 15 weeks of crop growth the weights of residues in the carrots increased and remained approximately proportional to the square root of the carrot mean weight. Rates of uptake declined as carrot growth declined and subsequently the amounts of chlorfenvinphos, diazinon and fonofos residues in the carrots changed very little, while phorate sulphone steadily declined.  相似文献   

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