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1.
Knockdown and lethal activities of meta- and para-substituted benzyl (1R)-trans-chrysanthemates against the house fly were measured under synergistic conditions using piperonyl butoxide as an inhibitor of oxidative metabolism and NIA 16388 as an inhibitor of hydrolytic degradation. The variations in these activities were quantitatively analyzed in terms of physicochemical substituent effects using electronic, hydrophobic, and steric parameters of the aromatic substituents, and regression analysis. The most significant parameter in determining these activities is the steric bulkiness represented by the van der Waals voluem, the effect of which is highly specific to substituent positions. The substituent effects on knockdown and lethal activities against the house fly are shown to correspond well, respectively, with those on the convulsive and lethal activities against the American cockroach. The relationship between these symptomatic activities against the house fly and the neurophysiological activities determined by using excised nerve cords from American cockroaches were also quantitatively analyzed. Each house fly symptomatic activity was found to be analyzable by a linear combination of the neuroexcitatory and neuroblocking activity indices when the transport factor was separated by using the hydrophobicity parameter.  相似文献   

2.
The substituent effects on the symptomatic and neurophysiological activities of a number of substituted benzyl (1R)-trans-chrysanthemates against American cockroaches were quantitatively analyzed using electronic, hydrophobic, and steric parameters. The effects were shown to be highly specific to substituent positions except for those on the neuroblocking activity. Steric effect of substituents represented by van der Waals volume was found to play the most significant role in determining the variation in each activity. Peculiar substituent effects depending upon the bulkiness and position of substituents, which had been observed in the toxicity of this class of compounds, can be rationalized by the present analysis indicating that the optimum van der Waals volume of substituents is largest at the ortho and smallest at the para position.  相似文献   

3.
A procedure to evaluate the knockdown activity of pyrethroids against house flies in which metabolic factors could be eliminated as far as possible was established. With piperonyl butoxide and NIA 16388 as the inhibitors of oxidative and hydrolytic metabolism, respectively, the “intrinsic” knockdown potencies of 22 substituted benzyl (1R)-trans-chrysanthemates and related compounds were determined 2.5–3 hr after topical application to house flies. From the intrinsic knockdown potency and the rate of progress of the knockdown symptom from the earliest stage of intoxication, a “penetration” rate constant was estimated by first-order kinetics using a two-compartment model. The rate constant was correlated quantitatively with the hydrophobic parameter of the molecule. The lower the hydrophobicity, the higher the rate constant within the range of compounds used in this study.  相似文献   

4.
Lindane analogs, in which one or two chlorine atoms are replaced by various substituents, exhibit convulsive and lethal effects on Periplaneta americana (L.). Some analogs are as active as lindane. These effects are well related to the neuroexcitatory action which produces after-discharges in the central nervous system. Carbamate insecticides have potent convulsive and lethal effects on P. americana, which are also related to after-discharges produced in nerve cords. Convulsion caused by lindane analogs and carbamates is solely attributable to their neuroexcitatory effects on the nervous system, in spite of the difference in their ultimate modes of action.  相似文献   

5.
Quaternary organosilicon pyrethroid‐like ethers (five compounds) and alkanes (three compounds) were used for neurophysiological tests. Their activities in inducing repetitive firing in the central nervous cord of the American cockroach (Periplaneta americana) were evaluated by an extra‐cellular recording method. The ethers were more active than the corresponding alkanes. The ability of the compounds to cause conduction blockage was also measured using the same nerve preparations, but the effects were too weak to allow definitive activity values to be determined. The compounds prolonged the sodium tail‐current in the crayfish giant axon under voltage clamp conditions. The rate of decay of the tail‐current changed in parallel with the reported insecticidal activity against P americana. These findings indicated that tail‐current activity was the most useful nerve parameter in predicting insecticidal activity. Regression analysis of the numerical data together with those reported for other alkanes revealed that the higher the tail‐current activity, the higher the insecticidal activity when a structural feature and the hydrophobicity were considered separately. The insecticidal activity of the ethers was about seven‐fold higher than that of the alkanes with equivalent tail‐current activity and hydrophobicity. Variations in insecticidal activity were parabolically correlated with the hydrophobicity [(log P)opt = 9.1] when other factors were similar. © 2001 Society of Chemical Industry  相似文献   

6.
The neuroexciting activity of DDT and its analogs to produce repetitive responses on the nerve cord of Periplaneta americana was determined using the extracellular electrode method. The convulsive activity on P. americana and the insecticidal effect on Callosobruchus chinensis were also examined. It was found that the convulsive and insecticidal activities increase almost proportionally with increase in the neuroexciting activity within a set of p,p′-substituted DDT analogs. The intimate connections among these biological effects suggest that symptoms such as convulsion and death caused by DDT analogs are closely related with their neuroexcitory effect and there is a common mode of action in spite of differences in insect species.  相似文献   

7.
为了解亚致死剂量四聚乙醛对福寿螺的主要靶标酶和解毒酶活性的影响,研究了0.50mg/L的四聚乙醛处理不同时间后福寿螺不同组织中乙酰胆碱酯酶(AchE)、谷胱甘肽S-转移酶(GSTs)和多功能氧化酶(MFO)的活力变化。结果显示,四聚乙醛对福寿螺具有良好的杀灭效果,96hLC50为3.856mg/L,安全浓度为0.039mg/L;在用0.50mg/L的四聚乙醛处理的24h内,福寿螺鳃和腹足内AchE酶活力分别升高到未处理时的1.565和1.481倍而后下降,肝和肠组织内AchE酶活力分别下降为未处理时的0.132、0.282倍而后升高;不同组织中GSTs酶活力均呈现为"降低—升高—降低"的趋势;不同组织内MFO酶活力均为先下降后上升的趋势。研究表明0.50mg/L的四聚乙醛能诱导AchE、MFO和GST活性不同程度的增加,解毒酶MFO和GSTs可能在四聚乙醛的代谢中起着一定作用。  相似文献   

8.
Several glutathione S-transferases which catalyze the conjugation of reduced glutathione with organophosphorus triesters were separated from fat bodies of adult female American cockroaches, Periplaneta americana (L.). Two transferases (I, V) were active on diazinon and three transferases (II, III, IV) were active on methyl parathion. The transferase (I) active on the pyrimidinyl moiety of diazinon was distinguishable from the other transferases on the O-methyl portion of methyl parathion, as shown by chromatographic properties, and additionally it was almost inactive or less active on 3,4-dichloronitrobenzene, methyl iodide, p-nitrobenzyl chloride, trans-cinnamaldehyde, and 1,2-epoxy-3-(p-nitrophenoxy)propane. Transferase II had high activities with “aryl” and “aralkyl” compounds, transferase III with “epoxide” and “alkene,” and transferase IV with “alkyl,” “aryl,” and “aralkyl” compounds. This indicated that the transferases had overlapping substrate specificities. The molecular weight was 35,000–37,000 for both of the enzymes active on methyl parathion and diazinon. The pH optima with methyl parathion and diazinon were about 8.5 and 6.5, respectively. At a glutathione concentration of 5 mM, Michaelis constants were 0.28 and 0.13 mM for methyl parathion and diazinon, respectively.  相似文献   

9.
Female adult American cockroaches, Periplaneta americana L., showed definite age-dependent changes in levels of activity of the microsomal mixed-function oxidases. Cytochrome P-450 levels, EPN-detoxication, and p-nitroanisole O-demethylation activities were very low in young adult insects but increased steadily reaching a natural peak at about 100 days in fat body and at about 90 days in midgut and hindgut. The activities then declined rapidly reaching levels of young insects at about 130 to 140 days of age. NADPH-neotetrazolium-reductase activity was high in young insects, declined later in adult life, and returned to a peak at about 100 days.Injections of chlorcyclizine, a known microsomal enzyme inducer, significantly increased levels of cytochrome P-450, EPN-detoxication, p-nitroanisole O-demethylation, and NADPH-NT-reductase activities in young cockroaches. The drug injections were effective, however, only before the natural activity peak was reached. Beyond this point the injections had no inductive effect indicating that the microsomal oxidases in this insect are uninducible when normal enzyme levels are falling.NADPH-NT-reductase activity in male cockroaches, while being somewhat higher than in females, showed a similar age-dependent curve with the peak occurring at about 120 days.Age-dependent carbaryl resistance in male and female insects tended to follow levels of the microsomal oxidase activities. Fifty to 60-day-old insects, however, tended to be more resistant to the insecticide than microsomal enzyme levels would indicate.RNA levels of normal female insects showed age-dependent curves similar to those of the microsomal enzyme activities, being low in young adults and reaching a peak at about 100 days. Chlorcyclizine injections had little or no effect on total microsomal RNA levels.  相似文献   

10.
阿维菌素和氟虫腈对粘虫的毒杀作用比较   总被引：4，自引：0，他引：4  
测试比较了γ-氨基丁酸(GABA)受体毒剂阿维菌素、氟虫腈对粘虫的生物活性及体内GABA和谷氨酸(Glu)含量的影响。结果表明,阿维菌素对粘虫5龄幼虫的LD50为0.072 μg/头,而氟虫腈则为8.920 μg/头;阿维菌素的中毒症状分为麻痹期和死亡期,而氟虫腈的中毒症状可以明显地分为兴奋、痉挛、昏迷和死亡4个阶段。两种药剂均会造成试虫体内GABA和Glu代谢异常,其中阿维菌素可致Glu含量增加约1.8倍,使GABA的含量降低,在深度麻痹期仅为对照的71.3%;而氟虫腈可使Glu的含量先增加,在痉挛期达到对照的1.2倍,后降低至与对照同一水平,GABA则先保持不变,但粘虫昏迷后GABA含量降至对照的76.7%。  相似文献   

11.
A series of laboratory experiments were undertaken to compare the activities of four water-dilutable permethrin formulations against the cabbage looper Trichoplusia ni (Hubner). The formulations used were “Pounce 3.2 EC”, “Ambush 2.0 EC” and two novel formulations (containing evaporation retardants) supplied, for comparison, by Roussel Uclaf Environmental Health Ltd, Berkhamsted, UK (formerly Wellcome Environmental Health Ltd). Bioassays were developed to investigate the activity of the insecticides via topical, residual and residual/dietary routes of exposure. The test insects were exposed to insecticide droplets, of 200 μm diameter, either directly or indirectly (on cabbage leaves or parafilm) using an on-demand droplet generator. Following exposure to insecticide, the test species were confined in petri dishes and mortality assessments were made at 24 h after treatment. The results were analyzed using probits. The results indicated that up to 15-fold differences in activity between formulations may occur when exposure is via residual contact on an artificial waxy surface (parafilm). The novel formulations were found to be far more active than the standard EC formulations. These differences in activity were significantly correlated with the dynamic surface tension and droplet spread upon cabbage leaves of the formulations. The results are discussed in terms of the bioavailability of pyrethroids upon waxy surfaces and also in terms of the potential for manipulating the pick-up of pesticides from plant surfaces.  相似文献   

12.
The biochemical process by which various pyrethroid insecticides affect membrane-bound ATPase activities of the squid nervous system was examined. Of the five ATP-hydrolyzing systems tested, only Ca2+-stimulated ATPase activities are seen to be clearly affected by pyrethroids. It was found that the “natural type” pyrethroids (e.g., pyrethrin and allethrin) primarily inhibit Ca-ATPase activity whereas the “highly modified type” pyrethroids (e.g., cypermethrin and decamethrin) mainly inhibit Ca + Mg-ATPase. permethrin, which is considered to possess structural similarities to both the natural type and the highly modified type pyrethroids, was found to have an intermediate property in terms of its inhibitory potency to both Ca- and Ca + Mg-ATPase activities. The level of inhibition of Ca2+-stimulated ATPase activities was generally high in the retinal axons and optic lobe synaptosomes but lowest in the axoplasmic preparations.  相似文献   

13.
BACKGROUND: The development of resistance to imidacloprid in eastern US populations of the Colorado potato beetle (CPB), Leptinotarsa decemlineata (Say), threatens this critical use for neonicotinoid insecticides. Previous pharmacokinetic studies with resistant adult CPBs provided no explanation for the high resistance level (over 200-fold) to topically applied imidacloprid. The authors assessed the neural activity of imidacloprid by recording spontaneous activity from a motor nerve leaving the isolated central nervous system to compare the sensitivity of the latter to imidacloprid between susceptible and resistant CPBs. RESULTS: On the isolated central nervous system, imidacloprid was initially neuroexcitatory, and neuroinhibitory at higher concentrations. The neuroexcitatory action of imidacloprid was blocked by coapplication of a specific nAChR antagonist, methyllycaconitine, indicating that it is a result of action on nAChRs. The sensitivity to the neuroexcitatory and inhibitory activities of imidacloprid varied independently among individuals in each population. The sensitivity of the central nervous system of resistant CPBs to excitation by imidacloprid did not differ from that of susceptible insects, but the sensitivity to inhibition by imidacloprid was reduced 52- to 58-fold, indicating a possible change in the sensitivity of at least one subgroup of nAChRs. CONCLUSION: This study provides evidence that reduced nerve sensitivity to the blocking action of imidacloprid is associated with imidacloprid resistance in the CPB.  相似文献   

14.
增效剂NIA16388对溴氰菊酯增效机理的研究   总被引：1，自引：0，他引：1  
以抗溴氰菊酯品系家蝇(Del-R) 为试材,测定了NIA 对溴氰菊酯的增效作用,结果表明:NIA 对溴氰菊酯有极显著的增效作用。此后对NIA 的增效机理进行了研究,实验证明:NIA 可抑制家蝇体内羧酸酯酶的活性,I50值分别为2.14(±0.22)×10-7mo l·L-1(α-NA )和1.09(±0.39) ×10-9mol·L -1(β-NA ) ,N IA 为4.20×10- 4mol·L- 1时, 其对多功能氧化酶的抑制率达78.63(±0.13)%;此外,NIA 对神经靶标部位的AChE 也有抑制作用, I50值为2.37(±0169)×10- 5mo l·L - 1。几方面综合作用的结果, 使其表现出明显的增效效果。  相似文献   

15.
The variations in the light-dependent herbicidal activity against Echinochloa oryzicola of a number of 4-pyridone-3-carboxanilides with various substituents on the anilide and pyridone rings have been examined by use of physicochemical substituent parameters and regression analysis. The effects of substituents of the anilide ring were such that the activity was related parabolically not only with the substituent hydrophobicity (π) but also with the steric bulk parameter (Es) of the bulkier ortho substituent. The effect of substituents at the 1-position of the pyridone ring was analysed with steric(STERIMOL L and B5) and electronic(γ1) parameters. That of substituents at the 5-position of the pyridone ring was explained by a parabolic function of a steric (MR) parameter. Analyses of the activity of 105 analogs confirmed that our previous selection of a candidate compound in this series for field trials was indeed appropriate in terms of physicochemical substituent effects.  相似文献   

16.
Thirteen pyrethroid-type esters of substituted 1(or 3)-hydroxymethylimidazolidine-2, 4-dione were synthesised and their knockdown activities against houseflies, mosquitoes and cockroaches were examined. Knockdown activities of 2,4-dioxo-1-prop-2-ynylimidazolidin-3-ylmethyl esters in oil solutions were higher than those of known knockdown pyrethroids; three of the compounds also possessed strong knockdown and flushing-out activities against cockroaches.  相似文献   

17.
The racemic product of metolachlor contains two R-enantiomers and two S-enantiomers. S-Metolachlor is a more effective herbicidal agent than rac-metolachlor; currently, it is widely used instead of rac-metolachlor. The comparative toxicity of rac- and S-metolachlor was assessed on the basis of their effects on some enzyme activities of the fifth instar of the silkworm, Bombyx mori L. These results suggest that rac-metolachlor and S-metolachlor have different effects on enzyme activities of fifth-instar silkworm larvae. Hemolymph lactate dehydrogenase and catalase activity levels in silkworms treated with rac-metolachlor were much lower than those in silkworms treated with S-metolachlor. Control hemolymph ACP activity was 44-73% higher than that of rac-metolachlor-treated hemolymph, but the difference was not large between S-metolachlor treatment and the control. Midgut alkaline phosphatase activity of silkworms treated with rac-metolachlor was 46% lower than control activity, and the effect of S-metolachlor on midgut alkaline phosphatase activity was minor. The difference between the two herbicides was apparent mainly during the first 5 days of the fifth instar, and then gradually disappeared. It is shown that compared with S-metolachlor, rac-metolachlor is more toxic to economically important silkworms because of its effects on some enzymes and on metabolism.  相似文献   

18.
The insecticidal activity of lindane analogs, in which some chlorine atoms were replaced by other groups susceptible to microsomal oxidative metabolism, was determined against mosquitos, house flies, and German cockroaches. When tested with a synergist, piperonyl butoxide, one of the methylthio analogs was as active as lindane, whereas several others were also highly active. By examining the ratio of synergized and unsynergized LD50 values (synergistic ratio value), the highly insecticidal methylthio, methoxy, and methyl analogs appear to undergo metabolic detoxication effectively in house flies. By means of in vitro metabolism experiments using microsomal fraction from house fly abdomen, the methoxy, ethoxy, and methylthio analogs were shown to be metabolized rapidly at similar rates. The synergized insecticidal activities of these compounds against various insect species relate linearly with each other, suggesting that the oxidative degradation is inhibited by the synergist to a similar extent and that the transport process to the site of action is not a limiting factor in determining the relative insecticidal activity.  相似文献   

19.
American cockroaches injected with sublethal doses of DDT (0.75 μg/roach) at 5-day intervals showed a 40% reduction in oligomycin-sensitive Mg2+ATPase from muscle homogenates, and a 23% reduction of Na+-K+ATPase from nerve cords. Thus, the maximum effect measured occurred with the same enzyme and tissue as determined from in vitro studies. The metabolite, DDE, used at 15 μg per roach, gave no significant change in activity of the ATPase system following injection. In contrast, high single doses of DDT (7.5 μg/roach) and 100 μg DDE and dicofol per roach caused over 30% increase in oligomycin-sensitive Mg2+ATPase of muscle and a 10–15% increase in Na+-K+ATPase of nerve cords measured 24 and 48 hr later. While a similar response was observed for Mg2+ATPase activities in cockroaches that were immobilized, the increase in enzyme activities were much greater than that caused by the pesticides.  相似文献   

20.
Physicochemical properties of biological interest were measured for hexachlorocyclohexane (benzene hexachloride) isomers, including solubility in water and in aqueous protein solutions, partition coefficients between organic solvents and water, and some “adsorption equilibrium” constants between the macromolecules and water. Some of the properties show a correlation with the free energy-related hydrophobic parameter “π”.  相似文献   

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