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Min Lü 《Pesticide biochemistry and physiology》2008,90(2):114-118
Celangulin V (CA-V), a β-dihydroagrofuran sesquiterpene polyol ester, is extracted from the root bark of Chinese bittersweet, Celastrus augulatus Maxim. It exhibited selective toxicity against different insects. By CO-difference spectral and biochemical method, the effects of CA-V on two kinds of detoxification enzymes, cytochrome P450 (P450 and NADPH-cytochrome P450 reductase) and glutathione S-transferase, were investigated in oriental armyworm, Mythimna separata and black cutworm, Agrotis ypsilon. CA-V showed higher induction against P450 of M. separata than that of A. ypsilon. Treated by CA-V, the maximum absorption of M. separata increased 1.2 and 0.8 nm than the control, respectively. Meanwhile, compared with the control, the P450 content and NADPH-P450 reductase activity in treated M. separata larvae increased 1.46-, 2.26- and 1.26-, 2.56-fold, respectively. But in treated A. ypsilon larvae, they all increased a little more than those of control. So far as M. separata and A. ypsilon, whether there is exposure of CA-V or not, the P450 content and GST activity in A. ypsilon were obviously higher than those in M. separata. It suggested that the content or activity difference of these two kinds of detoxification enzymes may have important roles in the selective toxicity of CA-V in M. separata and A. ypsilon. 相似文献
3.
Bla Darvas Huw H. Rees Nigel Hoggard Mahmoud H. Tag El-Din Eiichi Kuwano Ivn Blai Tibor Timr 《Pest management science》1992,36(2):135-142
The cytochrome P-450-dependent microsomal and mitochondrial ecdysone 20-monooxygenase systems convert ecdysone into 20-hydroxyecdysone. The microsomal fraction of fat bodies of zero h wandering stage fleshfly larvae (Neobellieria bullata; Diptera: Sarcophagidae) has a high ecdysone 20- monooxygenase activity. The effects of cytochrome P-450 inhibitors were investigated in vitro on microsomal ecdysone 20-monooxygenase. Metyrapone, fenarimol and certain imidazole derivatives (KK-42, KK-110, KK-135 and PIM) are strong inhibitors. The IC50 value of KK-110, which is the strongest inhibitor, is 2 × 10?7 M. A triazolyl and two cyclopropylamine derivatives have low activity. The activities of different NADPH-cytochrome c (P-450) reductase inhibitors were also assessed; diquat dibromide is a moderate inhibitor of microsomal ecdysone 20-monooxygenase, while paraquat dichloride has no activity. In-vivo experiments with cytochrome P-450 inducers and inhibitors gave the following results: (a) fenarimol, FI-121, precocene-2 caused “permanent” first-instar larvae; (b) barbital, phenobarbital and their sodium salts caused significant delay in larval development; (c) PIM, PTM, metyrapone, KK-42, KK-135, J-2710, RH 5849 and colchicine caused moulting disturbances; (d) J-2710, PIM, PTM, KK-42, KK-135, RH 5849 and colchicine caused lethal spiracle and mandible malformation; (e) KK-110, fenarimol, barbital and phenobarbital caused precocious pupariation. 相似文献
4.
Genomic tools such as the availability of the Drosophila genome sequence, the relative ease of stable transformation, and DNA microarrays have made the fruit fly a powerful model in insecticide toxicology research. We have used transgenic promoter-GFP constructs to document the detailed pattern of induced Cyp6a2 gene expression in larval and adult Drosophila tissues. We also compared various insecticides and xenobiotics for their ability to induce this cytochrome P450 gene, and show that the pattern of Cyp6a2 inducibility is comparable to that of vertebrate CYP2B genes, and different from that of vertebrate CYP1A genes, suggesting a degree of evolutionary conservation for the “phenobarbital-type” induction mechanism. Our results are compared to the increasingly diverse reports on P450 induction that can be gleaned from whole genome or from “detox” microarray experiments in Drosophila. These suggest that only a third of the genomic repertoire of CYP genes is inducible by xenobiotics, and that there are distinct subsets of inducers/induced genes, suggesting multiple xenobiotic transduction mechanisms. A relationship between induction and resistance is not supported by expression data from the literature. The relative abundance of expression data now available is in contrast to the paucity of studies on functional expression of P450 enzymes, and this remains a challenge for our understanding of the toxicokinetic aspects of insecticide action. 相似文献
5.
Levels of microsomal epoxidation, N-demethylation, and cytochrome P-450 in the gut tissues of sixth instar southern armyworm larvae were considerably enhanced following oral in vivo treatment with a series of methylbenzenes. Induction increased with increasing methyl substitution and was maximal with pentamethylbenzene. The increase in microsomal activity occurred rapidly after initiation of treatment and the final levels of induction achieved were dependent on the concentration of the inducer in the diet and the time of exposure. Microsomal enzyme activity returned to control levels following termination of exposure and induction was blocked by puromycin and cycloheximide but not by actinomycin D. The in vivo tolerance of induced worms to orally administered carbaryl was increased in a manner reflecting the enhanced microsomal enzyme activity. 相似文献
6.
Katsuya Natsuhara Kei Shimada Toshiharu Tanaka Tadashi Miyata 《Pesticide biochemistry and physiology》2004,79(2):33-41
The permethrin resistant strain (TR-strain) of the beet armyworm, Spodoptera exigua (Hübner), has 92.5-fold resistance to permethrin (at LD50 level) compared to the permethrin susceptible strain (TS-strain). Bioassay involving permethrin mixed with piperonyl butoxide, an inhibitor of microsomal cytochrome P450s, significantly reduced the resistance ratio from 92.5- to 7.9-fold. However, S,S,S-tributylphosphorotrithioate and diethylmaleate which are inhibitors of esterases and glutathione S-transferase, respectively, did not affect the resistance level. These results indicate that the detoxification of permethrin in the TR-strain was primarily due to the cytochrome P450 monooxygenases. LD50 for permethrin was increased to 4.5-fold by the pre-treatment of phenobarbital in the TS-strain. The effect of induction by phenobarbital was almost completely overcome by the piperonyl butoxide treatment. However, it was observed that phenobarbital treatment did not cause any change in the toxicity of permethrin to TR strain. Since this result deviated from the expectation that the metabolism of phenobarbital in the TR-strain should be greater than that in the TS-strain, it was deemed necessary to compare the metabolism of phenobarbital between the TS- and TR-strains. Comparison was made based on the concentration of phenobarbital in the hemolymph and whole body. The results showed no significant difference in phenobarbital treatment between the two strains used in this study suggesting the possibility that the induction system in TS-strain is different from the TR-strain. 相似文献
7.
Diana K. Londoño Haichuan Wang Michael J. Lydy 《Pesticide biochemistry and physiology》2007,89(2):104-110
Previous studies performed in our laboratory have measured the effect of atrazine exposure on cytochrome P450-dependent monooxygenase activity and have found increased activity in midge larvae (Chironomus tentans) as a result of atrazine exposure (1-10 ppm). Here we report the cloning and expression of a specific C. tentans CYP4 gene that is responsive to atrazine induction with an open reading frame of 1678 bp which encodes a putative protein of 559 amino acid residues. Alignments of deduced amino acid sequences with other insect P450 genes and phylogenetic analysis indicated a high degree of similarity to other insect CYP4 genes. Northern blotting analysis employing a fragment of 1200 bp from the CYP4 gene as a probe indicated that the CYP4 gene was expressed in all developmental stages, but was expressed at highest levels in late instar larvae. Additionally, over-expression of CYP4 in C. tentans exposed to atrazine (10 mg/l) confirms the ability of atrazine to induce specific P450 genes and provides insight into potential consequences of atrazine exposure in aquatic organisms. 相似文献
8.
Houseflies, Musca domestica, L., were treated with the drugs phenobarbital and 3-methylcholanthrene to study the effects of these compounds as inducing agents of the microsomal oxidases, heptachlor epoxidase, and p-nitroanisole O-demethylase, and of DDT-dehydrochlorinase. Phenobarbital was active when applied by injection or as part of the diet but inactive when topically applied. The resulting increases in heptachlor epoxidase activity were as much as 25-fold that of the untreated controls. The net increase in enzyme activity after phenobarbital treatment was greater in an insecticide-susceptible strain, WHO-SRS strain, than in a carbamate-resistant strain. However, the phenobarbital induced increases in DDT-dehydrochlorinase were greater, about 2-fold, in the resistant strains than in the susceptible strain.The optimum dose for phenobarbital was 1% in the diet for a period of 3 days. None of the treatments with 3-MC, feeding, injection, exposure to residues, or topical, were effective in induction. 相似文献
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Stefanie Konanz 《Pesticide biochemistry and physiology》2004,79(2):49-57
Glutathione S-transferases (GSTs) are known to catalyze conjugations by facilitating the nucleophilic attack of the sulfhydryl group of endogenous reduced glutathione on electrophilic centers of a vast range of xenobiotic compounds, including insecticides and acaricides. Elevated levels of GSTs in the two-spotted spider mite, Tetranychus urticae Koch, have recently been associated with resistance to acaricides such as abamectin [Pestic. Biochem. Physiol. 72 (2002) 111]. GSTs from acaricide susceptible and resistant strains of T. urticae were purified by glutathione-agarose affinity chromatography and characterized by their Michaelis-Menten kinetics towards artificial substrates, i.e., 1-chloro-2,4-dinitrobenzene and monochlorobimane. The inhibitory potential of azocyclotin, dicumarol, and plumbagin was low (IC50 values > 100 μM), whereas ethacrynic acid was much more effective, exhibiting an IC50 value of 4.5 μM. GST activity is highest in 2-4-day-old female adults and dropped considerably with progressing age. Furthermore, molecular characteristics were determined for the first time of a GST from T. urticae, such as molecular weight (SDS-PAGE) and N-terminal amino acid sequencing (Edman degradation). Glutathione-agarose affinity purified GST from T. urticae strain WI has a molecular weight of 22.1 kDa. N-terminal amino acid sequencing revealed a homogeneity of ≈50% to insect GSTs closely related to insect class I GSTs (similar to mammalian Delta class GSTs). 相似文献
11.
Premysl Mikula Jana Blahova Marcela Havelkova Martin Hulak 《Pesticide biochemistry and physiology》2009,93(1):13-89
The aim of the study was to evaluate the effect of subchronic exposure to the herbicide LASSO MTX (alachlor 42% W/V) on biometric parameters and important liver biomarkers in the common carp (Cyprinus carpio). One year old fish were exposed for 28 days to LASSO MTX added to the tank water at concentrations of 240 and 2400 μg L−1. The exposure did not affect fish biometric parameters. Glutathione-S-tranferase (GST) activity in liver (hepatopancreas) remained unchanged in exposed fish when compared to controls. However, significant induction of total cytochrome P 450 (CYP 450), ethoxyresorufin-O-deethylase (EROD) activity and elevated glutathione (GSH) in liver of exposed fish were detected. 相似文献
12.
用 0 .2 mg/ g氰戊菊酯和 2 mg/ g苯巴比妥钠 (PB)拌饲料处理不同时间 ,对敏感种群 (HDS)和抗性种群 (KQR)棉铃虫不同组织的 P4 50诱导作用不同。两种诱导剂对 HDS种群棉铃虫的中肠、脂肪体和体壁的 P4 50都有明显的诱导作用 ,其中 PB诱导的最高倍数分别达 2 .2 4、2 .0 3和 1.6 0倍 ,氰戊菊酯诱导的最高倍数分别达 2 .14、2 .83和 1.2 8倍 ;两种诱导剂对 KQR种群棉铃虫的部分组织 P4 50也有一定的诱导作用 ,但不及对 HDS棉铃虫的显著 ,最高诱导倍数只有 :中肠 1.2 1倍 (PB)和 1.15倍 (氰戊菊酯 ) ,脂肪体 1.72倍 (PB) ;诱导作用除了表现出种群差异性 ,还表现出诱导剂差异、时间效应和组织特异性。尽管不同组织被诱导的程度不同 ,但两种群中中肠和脂肪体的 P4 50相对更容易被诱导 ,诱导倍数也较高 ;诱导达到最大值所需时间一般为 12～ 4 8h不等 ;两种诱导剂中 ,PB比氰戊菊酯对棉铃虫不同组织的P4 50具有更强的诱导作用。 相似文献
13.
The effect of phenobarbital and certain pesticides on glutathione S-transferase activity was investigated. The maximum amount of enzyme induction occurred 96 hr after phenobarbital treatment. Chlorinated hydrocarbons were more effective inducers than the other pesticides evaluated. Phenobarbital treatment did not alter the apparent Km value but altered the value of glutathione S-transferase to 3,4-dichloronitrobenzene. The amount of reduced glutathione was not increased by phenobarbital treatment. Pretreatment of house flies with phenobarbital provides some protection against methyl parathion, methyl paraoxon, azinphosmethyl, and methidathion toxicity. 相似文献
14.
S.J. Yu 《Pesticide biochemistry and physiology》1985,23(2):273-281
Microsomal sulfoxidation in fall armyworm (Spodoptera frugiperda) larvae was examined using phorate as substrate. The system required NADPH and was inhibited by CO and by piperonyl butoxide. Sulfoxidase activity was found in the alimentary canal, fat body, and Malpighian tubules, with the midgut being the most active. Microsomal substrates such as aldrin, heptachlor, biphenyl, and methyl parathion significantly inhibited the enzyme activity whereas p-nitroanisole and p-choloro-N-methylaniline had no effect. Enzyme activity increased during larval development, reaching a maximum shortly before pupation. Allelochemicals (monoterpenes, indoles, and flavones), drugs (phenobarbital and 3-methylcholanthrene), and host plants (corn cotton, parsnip, and parsley) significantly increased the enzyme activity. Increased phorate sulfoxidation through enzyme induction was found to decrease oral toxicity of phorate to the larvae. Analyses of internal insecticide revealed that, at various intervals, induced larvae retained less phorate and its oxidative metabolites than the controls. It was concluded that induction of phorate sulfoxidase activity results in an overall increase in the rate of phorate detoxication in this insect. 相似文献
15.
《Pesticide biochemistry and physiology》1986,25(3):346-357
Larvae of the southern armyworm, Spodoptera eridania (Cramer), grew well in the 15–30°C temperature range. Pupae survived poorly at 15°C but moths emerged from 85% of the pupae at 30°C. The time for development was prolonged at 15°C and larvae grew significantly bigger than at 30°C. Cytochrome P-450 content, cytochrome P-450 reductase, p-chloro N-methylaniline N-demethylation, methoxyresorufin 0-demethylation, and aldrin epoxidation activities were higher at 15°C than at 30°C. All cytochrome P-450 activities were more inducible by dietary pentamethylbenzene at 30°C than at 15°C. High cytochrome P-450-catalyzed activities were associated with increases in microsomal protein rather than with changes in membrane lipid or phospholipid content. Phosphatidylcholine was the major midgut membrane phospholipid. There was only a tendency towards increased unsaturation of the phospholipid fatty acyl moieties and lowered membrane phase transition temperature in cold-adapted larvae. Acute oral carbaryl toxicity was generally inversely correlated with cytochrome P-450 catalyzed activities. Carbaryl toxicity was decreased about 10-fold by pentamethylbenzene induction and about 3-fold by the lower acclimatization temperature. 相似文献
16.
Melissa C. Hardstone 《Pesticide biochemistry and physiology》2007,89(3):175-184
The cytochrome P450-dependent monooxygenases (P450s) are an important enzymatic system that metabolizes xenobiotics (e.g., pesticides), as well as endogenous compounds (e.g., hormones). P450-mediated metabolism can result in detoxification of insecticides such as pyrethroids, or can be involved in the bioactivation and detoxification of insecticides such as organophosphates. We isolated (from the JPAL strain) a permethrin resistant strain (ISOP450) of Culex pipiens quinquefasciatus, having 1300-fold permethrin resistance using standard backcrossing procedures. ISOP450 is highly related to the susceptible lab strain (SLAB) and the high resistance to permethrin is due solely to P450-mediated detoxification. This is the first time in mosquitoes that P450 monooxygenase involvement in pyrethroid resistance has been isolated and studied without the confounding effects of kdr. Resistance in ISOP450 is incompletely dominant (D = +0.3), autosomally linked, and monofactorally inherited. It is expressed in the larvae, but not in adults. Cross-resistance to pyrethroids lacking a 3-phenoxybenzyl moiety (tetramethrin, fenfluthrin, bioallethrin, and bifenthrin) ranged from 1.5- to 12-fold. ISOP450 had only limited (6.6- and 11-fold) cross-resistance to 3-phenoxybenzyl pyrethroids with an α-cyano group (cypermethrin and deltamethrin, respectively). Examination of cross-resistance patterns to organophosphate insecticides in ISOP450 showed an 8-fold resistance to fenitrothion, while low, but significant, levels of negative cross-resistance were found for malathion (RR = 0.84), temephos (RR = 0.73), and methyl-parathion (RR = 0.55). The importance and uniqueness of this P450 mechanism in insecticide resistance is discussed. 相似文献
17.
Deok Ho Kwon Jeong Joon Ahn J. Marshall Clark 《Pesticide biochemistry and physiology》2010,96(1):36-42
Molecular mechanisms of monocrotophos resistance in the two-spotted spider mite (TSSM), Tetranychus urticae Koch, were investigated. A monocrotophos-resistant strain (AD) showed ca. 3568- and 47.6-fold resistance compared to a susceptible strain (UD) and a moderately resistant strain (PyriF), respectively. No significant differences in detoxification enzyme activities, except for the cytochrome P450 monooxygenase activity, were found among the three strains. The sensitivity of acetylcholinesterase (AChE) to monocrotophos, however, was 90.6- and 41.9-fold less in AD strain compared to the UD and PyriF strains, respectively, indicating that AChE insensitivity mechanism plays a major role in monocrotophos resistance. When AChE gene (Tuace) sequences were compared, three point mutations (G228S, A391T and F439W) were identified in Tuace from the AD strain that likely contribute to the AChE insensitivity as predicted by structure analysis. Frequencies of the three mutations in field populations were predicted by quantitative sequencing (QS). Correlation analysis between the mutation frequency and actual resistance levels (LC50) of nine field populations suggested that the G228S mutation plays a more crucial role in resistance (r2 = 0.712) compared to the F439W mutation (r2 = 0.419). When correlated together, however, the correlation coefficient was substantially enhanced (r2 = 0.865), indicating that both the F439W and G228S mutations may work synergistically. The A391T mutation was homogeneously present in all field populations examined, suggesting that it may confer a basal level of resistance. 相似文献
18.
Daily 75 mg/kg phenobarbital ip injections for 3 days or 25 ppm dieldrin in the diet of mice for 14 days caused an increase in liver cytochrome P-450 and blood B-esterase. Liver A-esterase was not significantly increased. Under in vitro conditions, phenobarbital and dieldrin induced the oxidative as well as hydrolytic metabolism of dicrotophos, dimethoate, and phosphamidon by liver homogenates or combined microsomes plus 105,000g supernatant fractions. The concentration of dimethoxon was increased more than fourfold by the pretreatments after incubation for 4 hr at 37.5°C with NADPH added. The organophosphorus insecticides used in this study were not metabolized as well by the liver microsomes alone or 105,000g supernatant alone, as by the combination of microsomes and 105,000g supernatant. Under in vivo conditions in mice, phenobarbital and dieldrin treatments increased the urinary recovery of metabolites in the initial 6 hr after [14C]carbonyl-dimethoate or [14C]N-ethyl-phosphamidon administration. Analysis of urine showed that the inducers caused a more than sixfold increase in dimethoxon recovered and twofold increase in water-soluble nontoxic metabolites within 6 hr after dimethoate administration. With phosphamidon both inducers increased the rate of metabolism, and the total recovery in aqueous and chloroform fractions was decreased. These results suggest that increased dimethoate toxicity after phenobarbital and dieldrin treatments in whole animals results from stimulation of the activation of dimethoate to dimethoxon, while the increase in hydrolytic products after both pretreatments results in decreased toxicity of the direct acetylcholinesterase inhibitors, dicrotophos and phosphamidon. 相似文献
19.
Daniel R. Vincent Alison F. Moldenke Dan E. Farnsworth Leon C. Terriere 《Pesticide biochemistry and physiology》1985,23(2):171-181
Development and phenobarbital (PB) induction of microsomal cytochrome P-450, cytochrome P-450 reductase, two epoxidation, and two O-demethylation activities were examined in chronologically timed populations of insecticide-susceptible (NAIDM) and -resistant (Rutgers) house flies. Measurements of these enzymes started with the pharate adult stage and ended 5 days following eclosion. Untreated insects of both strains had comparable reductase levels, whereas cytochrome P-450 and associated monooxygenase activities were 1.5-fold or more higher in Rutgers. Maximum induction, as well as toxicity, occurred at a lower PB concentration in NAIDM than Rutgers. The drug caused consistently higher increases in enzymes and activities within 12 hr of starting treatment in both strains. When PB was withdrawn from treated flies (both strains) 48 hr after treatment began, specific activities (product min?1 mg protein?1) in all enzymes returned to control values in 24 hr while metabolic capacity (product min?1 insect?1) achieved control values within 48 hr. The changes in turnover numbers (pmol product min?1 pmol P-450?1), in conjunction with the differences in the monooxygenation of the four substrates, suggest that PB treatment induced both a quantitative and qualitative change in NAIDM monooxygenation but only a quantitative change in Rutgers monooxygenation. 相似文献