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At least 1,207 records · Page 67Linked to original sources
PubMed2003

Modulation of sodium channels by the oxadiazine insecticide indoxacarb and its N-decarbomethoxylated metabolite in rat dorsal root ganglion neurons.

The effects of the oxadiazine insecticide indoxacarb and its N-decarbomethoxylated metabolite (DCJW) on tetrodotoxin-resistant (TTX-R) voltage-gated sodium channels in rat dorsal ganglion neurons were studied using the whole-cell patch clamp technique. Indoxacarb and DCJW suppressed the peak amplitude of action potentials, and DCJW exhibited a faster time course and higher potency than indoxacarb in the blocking effects. In voltage-clamp experiments, indoxacarb and DCJW suppressed TTX-R sodium currents in a time-dependent manner without a steady-state level of suppression. IC50 values for indoxacarb and DCJW on TTX-R sodium currents were estimated to be 10.7 and 0.8 microM after 25 min of bath application, respectively. DCJW was about 10 times more potent than indoxacarb in blocking TTX-R sodium currents. Although the suppressive effects of indoxacarb were partially reversible after washout with drug-free external solution, no recovery of sodium current was observed in DCJW treated neurons after prolonged washout. In current-voltage relationships, both indoxacarb and DCJW blocked the sodium currents to the same degree in the entire range of membrane potentials. The sodium conductance-voltage curve was not shifted along the voltage axis by indoxacarb and DCJW at 10 microM. In contrast, the steady-state inactivation curves were shifted in the hyperpolarizing direction by indoxacarb as well as by DCJW. Based on these results, it was concluded that indoxacarb and DCJW potently blocked the TTX-R sodium channel in rat DRG neurons with hyperpolarizing shifts of the steady-state inactivation curves, suggesting preferential association of the insecticides to the inactivated state of sodium channels. The small structural variation between indoxacarb and DCJW resulted in clear differences in potency for blocking sodium channels and reversibility after washout.

Action Potentials↗
PubMed2026

Functional analysis of down-regulated CYP6AE gene clusters involved in the insecticidal mechanism of lycorine against Spodoptera litura.

BACKGROUND: Plants have evolved abundant defensive secondary metabolites to resist insect herbivores. Lycorine is an alkaloid with insecticidal activity from Amaryllidaceae plants, which the destructive pest Spodoptera litura naturally avoids. Cytochrome P450 enzymes are central to xenobiotic detoxification in insects, but the mechanism by which lycorine acts against S. litura remains unknown. This study aimed to reveal the toxic mechanism of lycorine focusing on P450-mediated detoxification. RESULTS: Lycorine exhibited substantial toxicity to first-instar S. litura larvae (LD50 = 0.55 μg larva-1). Subsequently, when fifth-instar larvae were exposed to a sublethal dose (LD30) of lycorine, Lyc disrupted metabolic pathways, damaged Malpighian tubules, and induced oxidative stress. Furthermore, lycorine strongly repressed a CYP6AE gene cluster (CYP6AE47, CYP6AE50, CYP6AE70, CYP6AE138 and CYP6AE139) and decreased total P450 activity to 45% in the Malpighian tubules. RNAi co-silencing of these cluster genes increased larval mortality (+30%) under lycorine treatment. Finally, molecular docking and microscale thermophoresis analyses further confirmed direct binding between Lyc and this CYP6AE gene cluster, with the strongest affinity observed for CYP6AE47 (Kd = 518.5 nM). A key residue, ARG170, may be vital for the interaction between Lyc and CYP6AE47. CONCLUSIONS: These results demonstrate that the insecticidal mechanism of Lyc involves suppressing the expression and function of a CYP6AE gene cluster, thereby impairing detoxification capacity, which leads to Lyc accumulation and larval mortality. Elucidation of the detoxification system-targeted mechanism for this plant-derived compound provides a foundation for developing novel, sustainable pest management strategies against S. litura and potentially other noctuid pests. © 2026 Society of Chemical Industry.

Animals↗
PubMed2003

Correlations of the electrophysiological activity of neonicotinoids with their binding and insecticidal activities.

The electrophysiological actions of various neonicotinoids, including substituted benzyl derivatives, against recombinant Drosophila SAD/chicken beta2 hybrid nicotinic acetylcholine receptor (nAChR) were measured to analyze the relationships between the in vivo (insecticidal) and in vitro (binding and agonist) activities. Most of the neonicotinoids tested were capable of inducing inward currents by activating the hybrid nAChRs expressed in Xenopus laevis oocytes, whereas some compounds had no agonist activity and only blocked the acetylcholine-induced currents. Variations in the agonist activity were well correlated with those in the binding potency evaluated using [3H]imidacloprid as well as insecticidal activities.

Algorithms↗
PubMed2004

Effectiveness of twelve insecticides applied topically to diapausing larvae of the codling moth, Cydia pomonella L.

Dose-mortality curves were established for 12 insecticides administered by topical application to diapausing larvae from a susceptible codling moth strain. Toxicity varied greatly among the insecticides tested. LC50 values ranged from 0.1 mg kg(-1) for fenoxycarb to over 2800 mg kg(-1) for diflubenzuron and indoxacarb. Discriminating dose levels were determined from dose-mortality reference curves for the detection of resistance in field-collected diapausing larvae.

Animals↗
PubMed2004

Insecticidal activity of chemical constituents from Aristolochia pubescens against Anticarsia gemmatalis larvae.

Acetone and ethanol extracts of the tubercula and several compounds isolated from Aristolochia pubescens (Willd) were bioassayed on velvetbean caterpillars, Anticarsia gemmatalis (Hübner), for evaluation of the insecticidal activities. Of the extracts subjected to bioassay, the acetone extract showed the highest activity. (-)-Cubebin did not show activity against soybean caterpillars, whereas aristolochic acid and ent-kaur-15-en-17-ol increased the larval period. These compounds, and (+)-eudesmin and (+)-sesamin, reduced the viability of this period, giving rise to malformed adults. These extracts and compounds are therefore potential botanical insecticide agents for the control of velvetbean caterpillars in soybean crops.

Animals↗
PubMed2004

Effects of insecticides and defoliants applied alone and in combination for control of overwintering boll weevil (Anthonomus grandis; Coleoptera: Curculionidae)--laboratory and field studies.

In laboratory, greenhouse and field tests, we determined the effects of combining full rates of the defoliants tribufos and thidiazuron and the herbicide thifensulfuron-methyl with half rates of the insecticides lambda-cyhalothrin or azinphos-methyl, and the combination of tribufos and thidiazuron, both in half rates, on mortality of the boll weevil, Anthonomus grandis grandis Boheman and on the quality of defoliation. Tribufos, 0.47 kg ha(-1) and tribufos, 0.235 kg ha(-1) + thidiazuron, 0.125 kg ha(-1) exhibited a slightly toxic effect to boll weevil, while tribufos, 0.47 kg ha(-1) + lambda-cyhalothrin, 0.019 kg ha(-1), tribufos, 0.47 kg ha(-1) + azinphos-methyl, 0.14 kg ha(-1), and tribufos, 0.235 kg ha(-1) + thidiazuron, 0.125 kg ha(-1) + azinphos-methyl, 0.14 kg ha(-l), provided control of boll weevil as good as or better than full-rate azinphos-methyl or lambda-cyhalothrin alone owing to synergistic effects. Thidiazuron or thifensulfuron-methyl alone or in combination with insecticides did not affect boll weevil mortality. Treatment with tribufos + thidiazuron, both at half rate, significantly increased defoliation compared to full rates of tribufos or thidiazuron alone, and provided adequate defoliation for approximately the same cost per hectare.

Age Factors↗
PubMed2005

Synthesis and insecticidal activities of novel oxime ether pyrethroids.

A series of novel 2-methylthio-3'/4'-substituted acetophenone oxime O-ethers were synthesized by the reaction of the corresponding acetophenone oximes with halides of pyrethroid alcohols in the presence of sodium hydroxide and phase-transfer catalysis or with triethyl quaternary ammonium salts of halides of pyrethroid alcohols in the presence of sodium hydroxide. These compounds showed notable insecticidal activity against Homopteran and Lepidopteran pests. 2-Methylthio-4'-fluoroacetophenone oxime O-[(2-methylbiphenyl-3-yl)methyl] ether was more effective than the commercial insecticides chlorfenapyr and fenvalerate.

Animals↗
PubMed2005

Use of the RFLP-PCR diagnostic test for characterizing MACE and kdr insecticide resistance in the peach potato aphid Myzus persicae.

The peach-potato aphid Myzus persicae (Sulzer) has developed a number of insecticide resistance mechanisms owing to the high selective pressure produced by world-wide insecticide treatments. Knowledge of the geographical distribution and the temporal evolution of these resistant phenotypes helps to develop suitable pest-management programs. Current understanding of the major mechanisms of resistance at the molecular level makes it possible to diagnose the presence of modified acetylcholinesterase (MACE) or knockdown resistance (kdr). This paper describes a rapid method for the identification of both resistance mechanisms in a single molecular assay by using restriction fragment length polymorphism of PCR products (RFLP-PCR) in individual as well as pooled aphids.

Acetylcholinesterase↗
PubMed2005

The influence of post-exposure temperature on the toxicity of insecticides to Ostrinia nubilalis (Lepidoptera: Crambidae).

The influence of post-treatment temperature on the toxicities of two pyrethroids (lambda-cyhalothrin and bifenthrin), a carbamate (methomyl) and a spinosyn (spinosad) to Ostrinia nubilalis (Hubner) larvae was evaluated in laboratory assays. From 24 to 35 degrees C, the toxicities of the pyrethroids decreased 9.5- and 13.6-fold while spinosad toxicity decreased 3.8-fold. The toxicity of methomyl did not change significantly. The results demonstrate that the most effective insecticide against a pest may vary with environmental conditions. In situations where comparable products from multiple insecticide classes are available, temperature should be included as a factor in the decision-making process.

Animals↗
PubMed2006

Characterization of an insecticidal coumarin from Boenninghausenia albiflora.

The leaves of Boenninghausenia albiflora afforded an insecticidal coumarin which was identified as murraxocin (7-methoxy-8-[1'-ethoxy-2'-hydroxy-3'-methyl-but-3'enyl]-coumarin) (1), on the basis of extensive 1- and 2-dimensional NMR experiments. This compound has previously been isolated from Murraya exotica but this is the first report of the full (1)H and (13)C data for this compound. This natural product was evaluated against important forest insect pests and was active against Plecoptera reflexa, Clostera cupreata and Crypsiptya coclesalis at different concentrations varying from 1.0% to 5% w/v. In the crude extract 70% mortality was observed, and for compound 1 80% mortality was observed at a concentration of 1.0% w/v. The percentage of insect mortality increased in a dose-dependent manner. Coumarins are poorly studied insecticides and there is potential to exploit this chemically simple group of natural products.

Animals↗
PubMed2005

Insecticidal compounds of the biofilm-forming cyanobacterium Fischerella sp. (ATCC 43239).

Cyanobacterial biofilms are grazed by many different benthic invertebrates. In particular, larvae of insects are often present in great numbers and exert strong grazing pressure on cyanobacteria. Along with morphological adaptations, allelochemicals may have been developed as defense mechanisms against insect larvae. To investigate the chemical defense of biofilm-forming cyanobacteria, larvae of Chironomus sp., a widely distributed genus in this habitat, were used. Ten artificial biofilms of axenic and nonaxenic cyanobacteria were screened for insecticidal activity against Chironomus sp. Fischerella 43239 was the cyanobacterium that exhibited the highest acute toxicity. A bioassay-guided isolation procedure was used to study the compounds responsible for toxicity in more detail. A toxic fraction was obtained when the 60% methanolic extract of Fischerella 43239 was separated on a C18 HPLC column. Electrospray mass spectrometry indicated the presence of several compounds in this fraction. The successful separation into individual compounds was achieved by HPLC on a cyanopropyl column. The heavily clustered quasimolecular ions observed on an electrospray mass spectrometer and the absorption spectra of the separated compounds were indicative of indole derivatives. The existence in the benthic cyanobacterium Fischerella 43239 of strong insecticidal metabolites that serve as chemical protection agents against insect larvae is supported by the data.

Adaptation, Physiological↗
PubMed1994

Toxicity of a new molt-inducing insecticide (RH-5992) to aquatic macroinvertebrates.

The molt-inducing insecticide RH-5992, a potent ecdysone agonist, is being evaluated for potential use in forestry to control defoliating lepidopterans. The possible adverse effects of RH-5992 on nontarget aquatic organisms were studied in two test systems. Acute lethal effects were determined for one aquatic amphipod and 11 species of aquatic insects in laboratory flowthrough toxicity tests. Lethal and behavioral effects (drift response) on the amphipod and 8 species of stream insects were also evaluated under natural environmental conditions and more realistic exposure regimens in outdoor stream channels. There were no significant effects on drift or survival of the test species exposed to RH-5992 at the maximum test concentration of 3.5 mg/liter (100x the worst-case expected environmental concentration) in laboratory toxicity tests and stream channel treatments. Mortality of the amphipod Gammarus sp. in one toxicity test was considered an artifact, because there was no significant mortality in subsequent tests at concentrations up to 7.0 mg/liter, or in stream channels treated at 3.5 mg/liter. Yellow birch leaves were sprayed with RH-5992 at a rate of 50 g/ha and tested for residual toxic effects on two species of shredding invertebrates in the outdoor stream channels. There was no feeding inhibition or lethal effect on either test species resulting from consumption of the contaminated foliage. The candidate insecticide RH-5992 does not appear to pose undue risk of direct adverse effects to aquatic macroinvertebrates, particularly in water bodies where residues are likely to be short lived following aerial applications (e.g., lotic systems).

Animals↗
PubMed1997

Nontarget effects of neem-based insecticides on aquatic invertebrates.

Neem-based insecticides are being investigated as alternatives to synthetic insecticides for the control of forest insect pests in Canada. Because the proposed use pattern against forest defoliators often necessitates spraying near shoreline areas, an assessment of adverse effects of neem on nontarget aquatic invertebrates was warranted. Acute lethal effects of two neem-based formulations on eight species of macroinvertebrates were determined in flow-through screening tests at 10 times the expected environmental concentration (0.35 mg/liter). Significant mortality occurred only in the mayfly Isonychia bicolor/rufa exposed to one formulation, and further tests were conducted to determine a concentration-dependent response. The LC50 for I. bicolor/rufa was estimated at 1.12 mg/liter; the LC10 was 0.63 mg/liter. Three detritivorous species were tested at expected environmental concentrations (0.035 mg/liter) at longer exposures in aquatic microcosms to determine effects of the two formulations on feeding rates and survival. Neither formulation caused significant mortality or antifeedant effects after a 28-day exposure. The implications of these results for forest pest management operations are discussed.

Animals↗
PubMed2002

Effects of Sevin (carbaryl insecticide) on early life stages of zebrafish (Danio rerio).

Sevin brand carbaryl insecticide is one of the most commonly used insecticides in the United States, with great potential for leaching into ground- and surface water reserves. Its possible teratogenic effects were tested on zebrafish eggs in four dilutions of decreasing concentration. The average mortality rate was low, indicating that Sevin does not directly kill embryos at these concentrations. Eggs and embryos were consistently smaller than the control starting at 24 h after spawning until hatching. Embryos in the highest concentration took up to twice as long to hatch as the control. This delayed hatching time increases vulnerability to predation. In addition, as minnows are lower on the food chain, bioaccumulation of Sevin in tissues may increase in larger predators, affecting their metabolism and reproduction.

Animals↗
PubMed2001

Metabolites of organophosphorous insecticides in urine specimens from inhabitants of a residential area.

The most frequently used pesticide in U.S. homes, as well as in schools and day care centers, is chlorpyrifos. In 1998, this insecticide was detected in household dust from the former U.S. Forces housing estates in Frankfurt am Main, Germany, resulting from its earlier use up to 1993, i.e., at least 4 years ago. This led to great concern in the new inhabitants. To investigate their internal exposure to the substance, they were offered the opportunity of taking part in biomonitoring examinations. Children playing on the floor were assumed to be especially at risk due to increased exposure to chlorpyrifos via oral or dermal intake. A total of 1146 inhabitants took part in this voluntary investigation. All of them stated that they had never used chlorpyrifos in their homes. Spot urine samples of the study participants were analyzed for six metabolites of organophosphorous insecticides [dimethylphosphate (DMP), diethylphosphate (DEP), dimethylthiophosphate (DMTP), diethylthiophosphate (DETP), dimethyldithiophosphate (DMDTP), and diethyldithiophosphate (DEDTP)] using a very sensitive gas chromatographic method with mass-selective detection and a limit of detection of 1 microg/L. No evidence was found of increased internal exposure due to former chlorpyrifos application in these homes (>4 years ago), either in children or in adults. The median values and 95th percentiles of the urinary metabolite concentrations in 484 adults were (microg/g creatinine): DMP, 15.5 and 102.5; DMTP, 13.5 and 125.8; DMDTP, <1 and 13.1; DEP, 2.1 and 11.6; DETP, <1 and 6.4; DEDTP, both <1. The urinary metabolite concentrations in children <6 years of age were higher; this was caused mainly by lower creatinine concentrations. To conclude, no increase in internal exposure due to former indoor application of chlorpyrifos could be found, and the reference values published for internal organophosphate exposure in adults in Germany were confirmed. However, as shown in other environmental studies, the urinary excretion of organophosphorous metabolites exceeds dietary intake several fold; this has been estimated from the data in various duplicate dietary studies. This observation calls for further investigation.

Adolescent↗
PubMed1993

Inhibition patterns of brain acetylcholinesterase and hepatic and plasma aliesterases following exposures to three phosphorothionate insecticides and their oxons in rats.

Rats were administered high sublethal intraperitoneal dosages of the phosphorothionate insecticides parathion, methyl parathion, and chlorpyrifos, and their oxons. Acetylcholinesterase activities in cerebral cortex and medulla oblongata and aliesterase activities in liver and plasma were monitored at 2 hr and 1, 2, and 4 days after exposure. The maximal inhibition of brain acetylcholinesterase activity was not immediate with parathion and chlorpyrifos, reflecting the time required for bioactivation of the phosphorothionates as well as the effectiveness of the aliesterases to inactivate much of the hepatically generated oxons. In contrast, brain acetylcholinesterase activities were more quickly inhibited following administration of paraoxon and chlorpyrifos-oxon, which do not require bioactivation. Brain acetylcholinesterase was also rapidly inhibited following administration of methyl parathion and methyl paraoxon, reflecting the low sensitivity of the aliesterases to methyl paraoxon. Aliesterases were inhibited to a greater extent than acetylcholinesterase at each sampling time with parathion and chlorpyrifos and their oxons, whereas the reverse was true with methyl parathion and methyl paraoxon. All of the above patterns correlate with the in vitro sensitivities of acetylcholinesterase and aliesterases to the oxons. The very prolonged inhibition of esterase activities following chlorpyrifos treatment probably results from its substantially greater lipophilicity compared to the other compounds, which would allow it to be stored and released for gradual bioactivation. The data reported indicate that the disposition and effects of different phosphorothionate insecticides will be influenced by the sensitivities of target and nontarget esterases for their oxons and by their lipophilicity, and that predictions of in vivo responses can be made from in vitro data.

Acetylcholinesterase↗
PubMed1997

The effects of the phosphorothioate insecticide fenitrothion on mammalian cytochrome P450-dependent metabolism of estradiol.

Phosphorothioate insecticides, such as fenitrothion, are suicide substrates of cytochromes P450 (P450). These compounds undergo oxidative desulfuration by P450 resulting in the release and subsequent binding of atomic sulfur to the enzyme. Consequently, the P450-dependent metabolism of certain endogenous substrates could be inhibited by exposure to these insecticides. Formation of 2-hydroxyestradiol (2-OHE2), 4-hydroxyestradiol (4-OHE2), 16 alpha-hydroxyestrone (16 alpha-OHE1), and estriol in mammals occurs by P450-dependent hydroxylation of estradiol at various positions on the steroid nucleus. In the present study, pretreatment of male Swiss Webster mice with increasing doses of fenitrothion resulted in dose-dependent biphasic decreases in 2-OHE2 and 4-OHE2 production in mouse hepatic microsomes compared to control, with substantial decreases even at a dosage as low as 7 mg/kg. Fenitrothion pretreatment also resulted in dose-dependent biphasic increases in 16 alpha-OHE1 and estriol production, along with substantial increases in estrone formation, probably as a result of shunting from the inhibition of 2- and 4-hydroxylation. These data suggest that exposure to fenitrothion might alter estradiol metabolism by inhibition of certain P450 isozymes.

Animals↗
PubMed1995

Characterization of baculovirus insecticides expressing tailored Bacillus thuringiensis CryIA(b) crystal proteins.

Full-length, truncated, and mature forms of the CryIA(b) insecticidal crystal protein gene of Bacillus thuringiensis were engineered into the p10 locus of Autographa californica nuclear polyhdrosis virus (AcNPV). A signal sequence of Heliothis virescens juvenile hormone esterase was introduced at the N-terminus of these constructs to induce secretion. All recombinants, except those containing the mature toxin, produced high levels of CryIA(b) ICPs in insect cells. Thirty percent of the intracellular protoxin was N-glycosylated, suggesting that the protoxin was translocated across the ER membrane. Secretion into the medium, however, was limited. The production of the mature toxin was poor as a result of its cytotoxicity to insect cells. In a bioassay against second instar Spodoptera exigua larvae, using a recombinant expressing the Androctonus australis scorpion toxin gene in the same p10 locus as a positive control, the median survival time of AcNPV recombinants expressing the various B. thuringiensis CryIA(b) ICP constructs was not significant different from that of wild-type AcNPV. This suggests that production and/or secretion of B. thuringiensis (pro)toxins by AcNPV p10 recombinant viruses does not increase insecticidal activity since (i) the protoxins produced are inactive and not likely to be activated in vivo; (ii) secretion of the B. thuringiensis protoxins is poor; and (iii) production of the mature toxins results in cytotoxicity.

Animals↗