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1.
The ovicidal action of four insecticides and three insect growth regulators, on eggs of various ages of the susceptible (S) strain of Spodoptera littoralis, was investigated. The results revealed that diflubenzuron was the most toxic compound tested on 0-1-day-old eggs, followed by triprene and then methoprene; chlorpyrifos came next in its toxicity, followed by cypermethrin then fenvalerate; methomyl was the least effective. With the progress of embryonic development, 1-2-day-old eggs showed slight tolerance to the action of the pesticides and juvenoids, but apparently resisted the action of diflubenzuron. Eggs 2-3 days old showed increased tolerance to the insecticides and diflubenzuron and, to a lesser extent, to the action of the two juvenoids. A total of 21 insecticide or insect growth regulator-insecticide mixtures, based on their toxicity equivalents (LD25 + LD25), were applied jointly on 0-1-day-old eggs of the S strain. The mixtures which produced high synergism on this stage could be arranged, according to their decreasing order of potentiation, as follows: fenvalerate/diflubenzuron, cypermethrin/triprene, methomyl/methoprene, cypermethrin/methoprene, fenvalerate/ methoprene, cypermethrin/methomyl, cypermethrin/diflubenzuron, fenvalerate/triprene, diflubenzuron/methoprene and methomyl/triprene. The mixtures that produced synergistic effects on 0-1-day-old eggs were also tested against the 1-2 and 2-3-day-oldeggs of the S strain. Theresults indicated that themixtures fenvalerate/diflubenzuron, and cypermethrin with either triprene or diflubenzuron, when tested on 1-2-day-old eggs, produced levels of synergism nearly similar to those achieved on newly deposited eggs. On the other hand, the mixtures cypermethrin/methomyl, and fenvalerate with methoprene or triprene, showed comparatively lower levels of synergism. However, the synergistic action of the mixture cypermethrin/methoprene, previously detected on newly deposited eggs, became an additive effect on 1-2-day-old eggs. Only the mixtures fenvalerate/diflubenzuron, cypermethrin/triprene and fenvalerate/methoprene showed synergism on 2-3-day-old eggs. The mixtures which showed synergistic effects on 0-1-day-old eggs of the S strain were further tested on eggs of various ages of the diflubenzuron-resistant (Rd) strain. As regards 0-1-day-old eggs, only the combinations cypermethrin/triprene, methomyl/methoprene and fenvalerate/methoprene produced additive effects. The mixture cypermethrin/diflubenzuron was still synergistic against newly deposited eggs of the Rd strain, in a manner similar to that indicated with the S strain. Apparent levels of antagonism were shown to the other insecticide-juvenoid mixtures as well as to the diflubenzuron/methoprene combination. The combinations cypermethrin/methomyl and fenvalerate/diflubenzuron had some effect on the freshly deposited eggs of the Rd strain but produced lower levels of potentiation. With the increase in age of the eggs, the mixture cypermethrin/diflubenzuron showed a lower level of synergism on the 1-2 day-old eggs than was observed in younger eggs. The additive effects, previously detected with some of the mixtures on newly deposited eggs became an antagonistic effect for the 1-2-day-old eggs. The eggs at this stage were more able to resist thejoint action of the other mixtures tested. Moreover, with further increase in the age of the eggs, the combination cypermethrin/diflubenzuron produced a lower level of potentiation on 2-3 day-old eggs, followed by fenvalerate/diflubenzuron at an even lower level, while the other mixtures showed various levels of antagonism.  相似文献   

2.
Egg hatch of two nitidulids,Carpophilus hemipterus L. andUrophorus humeralis F., was affected by the chitin synthesis inhibitor triflumuron (Alsystin; BAY SIR 8514)via the adult stage of the beetle. This occurred by exposure to treated diets, by a brief dip of the adults in aqueous dilutions of the toxicant, or by contact with a treated plastic netting cage. Exposure of adults ofC. hemipterus for 24 h to 0.0125%, 0.00125%, 0.00025% or 0.000125% and ofU. humeralis to 0.0125% a.i.-treated diets completely prevented hatch of eggs laid during the subsequent 48 h on an untreated diet. Although at first sterile eggs were obtained with adults of either nitidulid species transferred to an untreated diet after 24 h exposure to the 0.0125%-treated diet, egg viability gradually recovered. The speed of recovery and the course of mortality of larvae that hatched from eggs laid by treated adults, indicated thatC. hemipterus was more susceptible thanU. humeralis to triflumuron. DippingC. hemipterus adults — males or females — in 0.0125% a.i. triflumuron also resulted in complete prevention of egg hatch. Similar results were obtained by a 1-h contact of adults with treated cages. Triflumuron had no direct ovicidal activity against the two species at the concentrations used but was very effective against larvae of both species. At 0.0125% a.i., 3-5-mm-long larvae ofU. humeralis were more tolerant than newly hatched larvae and than 3-5-mm-long larvae ofC. hemipterus. Application of 0.0125% a.i. triflumuron in a date palm grove did not prevent fruit infestation by nitidulid adults but, due to prevention of egg hatch, almost no larval development was observed.  相似文献   

3.
Phosphine (PH3) is a widely used and ideal fumigant employed to control insect pests in stored grains and other commodities. Chemically, PH3 is a strong reducing agent and mainly affects the mitochondrial transport system in insects. PH3 toxicity to insects is also associated with oxidative imbalances. Besides inducing mortality, PH3 is shown to delay hatching and adversely affect fecundity/fertility of several stored product insect pests. Recent studies have demonstrated the utility of Caenorhabditis elegans as a model organism to obtain basic insights on the toxic implications of PH3. In the present study, we have examined the impact of PH3 on the development of C. elegans and the involvement of glutathione (GSH) in its developmental toxicity. We exposed eggs of C. elegans to two concentrations of PH3 (0.04 and 0.06 mg/L) either in the presence or absence of a GSH depleting agent, diethyl maleate (DEM, 5 mM) for 72 h. PH3 exposure caused significant delay in the post embryonic development among worms as characterized by the inability of hatched worms to attain gravid adult stage by the end of 72 h. Interestingly, among worms co-exposed to DEM + PH3, the decrease in GSH levels was associated with more pronounced developmental delay compared to that of worms exposed to PH3per se. Concomitantly, PH3-induced depletion of glutathione was associated with significant alterations in activities of key antioxidant enzymes. Our data demonstrate the vital role of GSH and antioxidant defenses among worms developing under PH3 exposure. Interestingly, this finding also unfolds newer possibilities for developing strategies to disrupt antioxidant defenses in insect pests to enhance the efficacy of PH3 treatment for the control of stored product insects.  相似文献   

4.
Mitochondria were isolated from eggs of Spodoptera littoralis. With succinate (+pyruvate) as substrate, respiratory control ratios between 1.70 and 2.54 were obtained. Uncouplers and the energy transfer inhibitor oligomycin influenced these mitochondria in the well-known manner. The uncoupling activity of chlordimeform in vitro was very weak and decreased with increasing age of the eggs. Electron transport in mitochondria from chlordimeform-treated eggs was not uncoupled. Therefore, it is concluded that the ovicidal effect of this pesticide is not due to its uncoupling effect.  相似文献   

5.
Diflubenzuron, 1-(4-chlorophenyl)-3-(2,6-difluorobenzoyl)urea, possesses larvicidal and ovicidal activities. On larvae it acts mainly as a stomach poison, yet it sometimes exhibits important contact activity. Though all instars can be controlled, older instars are generally less susceptible than younger ones. Histological inspections of Leptinotarsa decemlineata larvae revealed that after ending exposure to the compound, distortions in newly deposited cuticular layers decreased gradually. Ovicidal effects resulted from direct contact of diflubenzuron with eggs or from contamination of females by contact or feeding. Electron microscopic observations of embryos of Leptinotarsa decemlineata, contaminated via the female, also showed disturbed cuticule formation, suggesting a similar activity of the compound in larvae and in eggs. Spraying the eggs of Leucoptera scitella shows the compound to be mainly ovidical at a rate of 100 mg litre?1, whilst with lower concentrations (10 and 1 mg litre?1) the young larval instar will be killed. The levels of cross-resistance to diflubenzuron as a larvicide are low and the compound can be used effectively in the field against populations that are highly resistant to conventional insecticides. Laboratory and field results, based on larvicidal and ovicidal activities of diflubenzuron, are discussed in respect of species belonging to the Diptera, Lepidoptera, Coleoptera, Acarina (Phyllocoptruta oleivora) and Hemiptera (Eurydema oleraceum and Psylla piri).  相似文献   

6.
N‐(4‐phenoxyphenyl)‐2‐pyridinecarboxamide (1) was synthesized from commercially available materials and its ovicidal and larvicidal activity against Cydia pomonella (L) was tested. The compound showed a LC50 of 0.98 mg ml−1 when eggs less than 24 h were sprayed using a Potter Tower, but it had no effect when eggs older than this were sprayed. The compound did not have larvicidal activity when larvae were treated with 1200 µg g−1. However, the larval head capsules were smaller than those in the controls when treated at this concentration. To assess its possible juvenile‐hormone‐like activity, the compound was topically applied to young pupae of Tribolium confusum duVal, where it produced clear juvenilization effects, which were dependent on the applied dose. © 2000 Society of Chemical Industry  相似文献   

7.
Pyriproxyfen, an analog of the juvenile hormone (JH) in insects, has been evaluated in vivo and in vitro on an important stored product pest, the mealworm Tenebrio molitor. On newly ecdysed pupae, this insect growth regulator (IGR) was applied topically (at 0.10 and 0.20 μg/insect). Enzyme immunoassay measurements showed a decrease of the ecdysteroid titer in the hemolymph of treated specimens. In addition, the treatment induced an increase of the protein concentration in the hemolymph, however, there was no significant effect on the protein band pattern. Using in vitro pupal integument explant cultures, pyriproxyfen (at 1 and 10 μM in the medium) caused a significant inhibition of ecdysteroid amounts and of the thickness of new cuticle secreted. These new results are discussed in relation to the physiology of this IGR with a JH action.  相似文献   

8.
The insecticidal activity of lauric, oleic and linoleic acids against Callosobruchus maculatus on cowpea was investigated in laboratory bioassays. In pre-oviposition grain treatments, it was found that, at dosages between 1.96 and 11.59 kg-lauric acid had no effect on progeny development, while the oily oleic and linoleic acids were active in reducing progeny development. The active fatty acids had no effect on oviposition (in no-choice experiments) or on mortality of adults or larvae that successfully penetrated treated cowpea seeds, and their insecticidal activity, like that of fixed vegetable oils, depended mainly on ovicidal action. When applied to cowpeas in a pure state, oleic acid had an LC50 value of 1.64mlkg?1, which made it approximately 3 and 8 times more toxic against eggs of C. maculatus than groundnut oil and linoleic acid respectively. When the ovicidal activities of the three fatty acids were tested by dipping egg-infested seeds in acetone- based solutions, they were all found to be similarly toxic, lauric, oleic and linoleic acids having LC50, values of 40, 38 and 26 ml litre?1 respectively (with overlapping 95% C.L.). These values made them 2-4 times more toxic than acetone-based solutions of groundnut and traditional coconut oils. The possibility of employing fatty acids in large-scale and traditional small-scale food storage systems is discussed.  相似文献   

9.
The results showed that survival rates of Biomphalaria alexandrina snails, reproductive potential and hatchability of eggs were evaluated post exposure to Basudin, Selecron and Colchicine. As well, DNA and RNA changes in the cells of ovotestis-digestive gland complex of treated snails were estimated. The current molluscicide Bayluscide was used as a reference compound.The pesticide Selecron proved to be more toxic to B. alexandrina snails than Basudin and Colchicine. Juvenile snails were dead post 3 weeks of exposure to the sublethal concentration LC0 of either Selecron or Basudin, while 26.75% of snails still alive at Bayluscide treatment. In addition, exposure of adult snails to LC0 of Selecron for 24 h/week for 4 weeks markedly reduced their reproductive rate (R0) by 89.9%. Moreover, snails’ eggs failed to hatch post 24 h of exposure to LC90 of either Selecron, Basudin or Bayluscide. Electrophoretic analysis indicated a decrease in the molecular weight of intact DNA in the ovotestis-digestive gland complex of snails treated with 250 ppm of Colchicine and LC25 of Selecron, as it scored 1.2 and 76 bp, respectively, compared to 166.46 bp for control group, while the vice versa was recorded for RNA intensity. It was concluded that the tested pesticides have deleterious effects on snails’ reproductive rate, their eggs and the intensities of DNA and RNA in their ovotestis-digestive gland complex. Therefore, it is expected that reaching of such pesticides to snails’ habitats in water courses during plant pests control could minimize the population density of the snails intermediate hosts of schistosomiasis, hence probably interrupt and reduce the transmission of this parasite.  相似文献   

10.
BACKGROUND: The Asian citrus psyllid (ACP), Diaphorina citri Kuwayama, is a vector of bacteria presumably responsible for huanglongbing (HLB) disease in citrus. In this laboratory study, an investigation was made of the activity of pyriproxyfen, a juvenile hormone mimic, on ACP eggs, nymphs and adults to evaluate its potential as a biorational insecticide for inclusion in an integrated pest management (IPM) program for ACP. RESULTS: Irrespective of egg age, timing or method of treatment, a significantly lower percentage of eggs (5–29%) hatched after exposure to 64 and 128 µg mL?1 of pyriproxyfen. Only 0–36% of early instars (first, second and third) and 25–74% of late instars (fourth and fifth) survived to adults following exposure to 16, 32 and 64 µg mL?1 of pyriproxyfen. However, 15–20% of adults that emerged following treatment as late instars exhibited morphological abnormalities. Furthermore, pyriproxyfen adversely affected reproduction (fecundity and fertility) of adults that emerged from treated fifth instars or that were treated topically with 0.04 µg as adults. CONCLUSIONS: Application of pyriproxyfen at 64 µg mL?1 resulted in greater inhibition of egg hatch and suppression of adult emergence compared with lower rates. Pyriproxyfen also markedly reduced female fecundity and egg viability for adults that were exposed either as fifth instars or as newly emerged adults. The ovicidal, larvicidal and reproductive effects against ACP suggest that pyriproxyfen is suitable for integration into an IPM program for ACP. Copyright © 2009 Society of Chemical Industry  相似文献   

11.
新化合物HNPC-A3066的杀螨活性及田间防治效果研究   总被引：1，自引：1，他引：0  
HNPC-A3066 {(E,Z) 2- 亚甲基]胺]氧]甲基]苯基]-3-甲氧基丙烯酸甲酯｝是由湖南化工研究院开发的甲氧丙烯酸酯类新型杀螨剂。采用农药生物技术测定了HNPC-A3066对棉红蜘蛛Tetranychus urticae的杀螨活性和作用方式。结果表明,HNPC-A3066对棉红蜘蛛具有良好的触杀、杀卵作用,但内吸活性很低。采用浸渍法和浸玻片法处理后48 h,对雌成螨的LC50值分别为3.33和 4.02 mg/L;浸玻片法处理后24 h,对若螨的LC50值为0.74 mg/L,浸渍法处理后7 d,对卵的LC50值为2.02 mg/L。田间药效试验结果表明,在有效成分浓度为80~160 mg/L时,施药后1、3、7和14 d,HNPC-A3066对棉红蜘蛛、柑桔红蜘蛛Panonychus citri和苹果红蜘蛛Panonychus ulmi的防效分别大于77.88％、75.33％和72.65％,且对作物和天敌安全。  相似文献   

12.
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13.
The effect of the ecdysone agonists RH-2485 (proposed name methoxyfenozide) and tebufenozide (RH-5992), was examined on eggs and larvae of the southwestern corn borer, Diatraea grandiosella Dyar. Both compounds exhibited a concentration-dependent ovicidal activity. More than 95% of eggs died when egg masses were dipped in solutions of 100 or 200 mg liter-1 of either compound in acetone+distilled water (1+1 by volume). Although some eggs treated with 1 or 10 mg liter-1 of the compounds hatched, the survival rate was low. Newly hatched larvae were fed for seven days on an artificial diet containing RH-2485 or tebufenozide. The LC50 values were 0·049 mg kg-1 for RH-2485 and 0·185 mg kg-1 for tebufenozide, showing that RH-2485 was about four times more active than was tebufenozide. Although increasing the time of exposure to either compound decreased the LC50 value significantly, the relative potency of RH-2485 versus tebufenozide was not changed. Newly ecdysed 4th-instar larvae fed with diets containing 0·125, 0·25 or 0·5 mg kg-1 RH-2485 or tebufenozide ceased feeding approximately 8 h after exposure, indicating that larvae had prematurely entered a molting cycle. Larvae treated with RH-2485 ecdysed earlier and died more quickly than those treated with tebufenozide. Ingestion of sublethal concentrations of RH-2485 (0·005 and 0·01 mg kg-1) or tebufenozide (0·03 and 0·06 mg kg-1) retarded larval growth, and decreased pupal weight and adult emergence. Increasing exposure time to tebufenozide tended to increase the larval mortality, significantly retarded larval growth, and decreased the mean weights of male and female pupae and adult emergence. RH-2485 (0·125 and 0·25 mg kg-1) and tebufenozide (0·25 and 0·5 mg kg-1) were lethal to newly hatched larvae, even after diets containing these compounds were held for 20 days at 30°C under long days (16 h light: 8 h dark). Our results suggest that field trials to assess the potential of RH-2485 and tebufenozide to control D. grandiosella are warranted. © 1998 SCI  相似文献   

14.
The fluorescent insect growth regulator 5[[[5-(dimethylamino)-1-naphthalenyl]amino]-1,3-benzodioxole (DNSAB) forms a metabolite complex with house-fly microsomal cytochrome P-450. Formation of the metabolite complex is dependent on the presence of NADPH and O2; NADH supports the reaction at a reduced rate. The presence of antibodies to house-fly cytochrome c (P-450) reductase in reaction mixtures inhibits the complex formation, indicating that the reductase is necessary for transfer of electrons from NADPH to cytochrome P-450 to complete the reaction. In the oxidized form, the metabolite complex has a single absorbance maximum at 431 nm, whereas the reduced form has two absorbance maxima at 426 (major) and 455 nm (minor). The pH of the media affects the extinction of the 426- and 455-nm Soret bands; increased pH decreases the extinction of the 426-nm band and increases the extinction of 455-nm band. Formation of the DNSAB metabolite-cytochrome P-450 complex decreases the amount of CO-reactive cytochrome P-450 by 24%. The metabolite complex is not dissociable by treatment with ferricyanide or by using centrifugation techniques. Dissociation is accomplished by addition of DNSAB to the oxidized metabolite complex. Kinetic analysis of the complex formation gives apparent Km and Vmax values at 2.55 ± 1.0 μM and 1.1 ± 0.4 × 10?2 ΔA min?1 nmol?1 cytochrome P-450, respectively. Addition of juvenile hormone [(E,E)-cis-methyl-10,11-epoxy-7-ethyl-3,11-dimethyl-2,6-tridecadienoate; JH] to the reaction medium competitively inhibits the formation of the metabolite complex giving an inhibition constant of 16 μM. DNSAB synergized the lethal effects of JH against Aedes aegypti larvae threefold; however, JH did not synergize DNSAB. These data suggest that DNSAB may acquire its hormonal qualities by complexing a species of cytochrome P-450 that metabolizes JH, thereby prolonging the in vivo lifetime of this hormone.  相似文献   

15.
A series of 27 substituted thio-1,1,1-trifluoropropanones was synthesized by reacting the corresponding thiol with 1,1,1-trifluoro-3-bromopropanone. The resulting sulfides were screened as inhibitors of hemolymph juvenile hormone esterase and α-naphthyl acetate esterase activity of the cabbage looper, Trichoplusia ni, electric eel acetylcholinesterase, bovine trypsin, and bovine α-chymotrypsin. The presence of the sulfide bond increased the inhibitory potency on all of the enzymes tested when compared with compounds lacking the sulfide. In general, the compounds proved to be poor inhibitors of chymotrypsin and moderate inhibitors of trypsin. By varying the substituent on the sulfide, good inhibitory activity was obtained on α-naphthyl acetate esterase, acetylcholinesterase, while some of the compounds proved to be extremely powerful inhibitors of juvenile hormone esterase. The most powerful inhibitor tested was 3-octylthio-1,1,1-trifluoro-2-propanone, with an I50 of 2.3 × 10?9M on JH esterase. This compound showed a molar refractivity similar to that of the JH II backbone, was not toxic to T. ni, and was moderately toxic to mice, with a 48-hr LD50 of >750 mg/kg. It effectively delayed pupation when applied to prewandering larvae of T. ni, as expected for a JH esterase inhibitor. Thus, some members of this series are promising for evaluating the role of JH esterase in insect development. The series also indicates that, by varying the substituent on the sulfide moiety, potent “transition-state” inhibitors can be developed for a wide variety of esterases and proteases.  相似文献   

16.
Biosynthesis of juvenile hormone in the tobacco hornworm, Manduca sexta, is inhibited by the bisthiolcarbamate juvenoid N-ethyl-1,2-bis(isobutylthiolcarbamoyl)ethane both in vitro and in vivo. In vitro an extremely steep dose-response curve was obtained with an ID50 value of 6 × 10?6M. However, in vivo topical treatment with the compound resulted in mild JH antagonistic symptoms, suggesting rapid metabolism of the compound. In agreement with results from metabolic studies performed on plants and in mammals, sulfoxidation of the thiocarbamate S-(4-chlorobenzyl)N,N-diethylthiocarbamate resulted in an enhanced inhibitory effect on JH biosynthesis in vitro. This suggests that the corresponding thiocarbamate sulfoxides may act as intermediates in carbomylating critical thiol sites important in the terpenoid biosynthesis pathway. Furthermore, this study shows that these prototype compounds are interesting tools for further investigation of chemical inhibition of JH biosynthesis in insects.  相似文献   

17.
Fractions derived from Clerodendrum phlomidis Linn. F. and isolated compounds from chloroform extract were evaluated against Earias vittella Fab. for their ovicidal and oviposition deterrent activities. There were 12 fractions obtained with silica gel column chromatographic techniques using different solvent systems. Among the fractions, fraction 5 recorded maximum ovicidal activity of 68.49% and oviposition deterrent activity of 100% at 1000 ppm concentration followed by 500 ppm concentration. The active fraction was further purified using HPLC. The purified fraction was subjected to UV, 1HNMR, 13CNMR, IR and EI-Mass spectroscopy and their spectral data confirmed the compound pectolinaringenin which belongs to the flavonoids. The compound pectolinaringenin was screened for its ovicidal and oviposition deterrent activities. It showed maximum ovicidal activity of 64.29% and oviposition deterrent activity of 100% at 100 ppm concentration against E. vittella. To the best of our knowledge, this is the first report of fractions and isolated compounds from C. phlomidis evaluated against E. vittella for their ovicidal and oviposition deterrent activities. The results from the present investigation clearly suggest that the active fraction or the isolated compound could be used to develop a novel pesticidal formulation to control economically important agricultural pests.  相似文献   

18.
20种杀虫剂对草地贪夜蛾的杀卵活性   总被引：2，自引：0，他引：2  
在前期测定14种杀虫剂对草地贪夜蛾杀卵活性的基础上,本文采用浸渍法又测定了20种不同类型杀虫剂的杀卵活性,以期为草地贪夜蛾卵期防治药剂的选择提供更全面的参考。结果表明,所测的20种杀虫剂均具有一定的杀卵活性。在100 mg/L浓度下,溴氰菊酯、高效氯氰菊酯和乙基多杀菌素表现出出色的杀卵活性,能够完全抑制卵的孵化,杀虫双的杀卵活性最差,低于10%。而噻虫胺、氯虫苯甲酰胺、高效氯氟氰菊酯、多杀霉素、联苯菊酯、噻虫啉、氧乐果、噻虫嗪、甲氰菊酯、烯啶虫胺和啶虫脒的杀卵活性相对较好,其校正死亡率在70.95%～98.52%之间,毒死蜱、吡虫啉、辛硫磷、虫螨腈和杀虫单的杀卵活性相对较差,在42.26%～61.51%之间。在10 mg/L浓度下,噻虫胺、乙基多杀菌素和噻虫啉的杀卵活性均在70%以上,而杀虫双、毒死蜱和烯啶虫胺的杀卵活性低于15%。特别是在100 mg/L和10 mg/L浓度下,新烟碱类杀虫剂噻虫胺和噻虫啉对草地贪夜蛾表现出较高的杀卵活性,分别为98.52%、76.91%和89.37%、72.44%。上述药剂在田间对草地贪夜蛾的杀卵效果还有待进一步验证。  相似文献   

19.
In the present study, we report on the changes observed in the kinetic properties of pyruvate kinase (PK) from whole body homogenate in the three developmental stages of the insect Tenebrio molitor after insecticide or acetone injection, and after injury and 24 h starvation. The apparent Km value of the enzyme towards phosphoenolpyruvate was higher in the pupae stage than in the rest developmental stages although the same enzyme type appears to be present throughout the life span of the insect as judged by its Vmax and sensitivity towards ATP and Alanine. The highest specific activity, twice as high as that of larvae and pupae, was observed in adults. Starvation resulted to activation of the enzyme by increasing the Km value in the two feeding stages, namely larvae and adult, while injury had the opposite effect. Acetone injection did not have any significant effect at any stage. Insecticide injection had varying effects, depending upon the developmental stage, the dose and the type of the insecticide. In larvae, low doses of methyl paraoxon and methyl parathion activated the enzyme but as the dose increased the Km value returned to normal levels. Low dose of decamethrin activated the enzyme also but at high dose it caused a severe inactivation as judged by a fivefold increase of the observed Km. In pupae, decamethrin had no effect, methyl parathion had similar effects to those observed in larvae, and methyl paraoxon caused activation of the enzyme at any dose given. In the adult stage none of the injected insecticides had any effect on the Km value although Vmax and specific activity were significantly altered.  相似文献   

20.
The inhibitory effects of a recently introduced series of the titled compounds on insect and mammalian acetylcholinesterase (AChE) activity were examined, where the median inhibition concentration (I50) and the inhibition kinetic parameters, bimolecular inhibition rate constant (ki), affinity constant (Ka), and phosphorylation rate constant (kp), were determined for each compound. Results indicated that all examined dioxaphospholenes had less inhibitory effects on mammalian AChE than fenitrothion, a commercial pesticide with moderate mammalian toxicity. The highest selectivity was obtained with compounds containing glutamic and leucine moieties (2.70 and 2.18, respectively) while selectivity of fenitrothion was 0.93. The low inhibitory effects of the examined dioxaphospholenes on mammalian AChE were attributed to their low phosphorylation rates (kp < 2.2 min−1) compared to that of fenitrothion (kp = 4.84 min−1). QSAR equations indicated that the inhibition process is controlled mainly by both the phosphorylation rate (direct effect) and the affinity of compounds toward the enzyme (inverse effect). Although the compounds’ hydrophobicity had no effects on the inhibition process, it affects the compounds’ toxicity since it affects the ability of compounds to penetrate insects to reach the enzyme active site.  相似文献   

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