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1.
The kinetics of accumulation and elimination of lethal doses of [14C]carbofuran in the hemolymph of the house fly suggest a one-compartment open model. Carbofuran in the hemolymph appeared to be in equilibrium with that in the tissues very soon after treatment.Following topical application of carbofuran, the rate of onset of symptoms of poisoning was correlated with the amount of carbofuran in the hemolymph, and the onset of convulsions only occurred after the concentration of carbofuran in the hemolymph reached μM levels. This value correlated well with neurobioassays of known concentrations of carbofuran perfused in saline onto the isolated thoracic ganglion.Following topical doses, carbofuran concentration in the hemolymph reached a peak within an hour and then gradually declined. At an LD60 dose, the initial decline in carbofuran concentration in the hemolymph over time was significantly slower than the decline after an LD10 dose, suggesting saturation kinetics.Hemolymph was collected from house flies for up to 3 hr following topical application of toxic amounts of carbofuran. Thereafter, hemolymph volume decreased and blood samples could not be collected. Curiously, hemolymph samples could be collected for 5 hr from house flies that were injected with toxic doses of carbofuran.  相似文献   

2.
Treatment of the metathoracic ganglion of the cockroach, Blaberus discoidalis, with dieldrin (HEOD) at a concentration of 10?5M produced changes in spontaneous efferent activity and afterdischarge in efferent pathways. Pretreatment with sesamex markedly reduced the spontaneous activity caused by dieldrin and also reduced the latency of appearance of symptoms from 60 min to nearly 30 min. However, pretreatment with sesamex did not alter the intensity and duration of the dieldrin-induced synaptic afterdischarge. Pretreatment of cockroaches with sesamex did not measurably change the toxicity of dieldrin in vivo.  相似文献   

3.
The potent pyrethroid insecticide NRDC 157 (I; 3-phenoxybenzyl (1R, cis)-3 - (2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate) and its insecticidally inactive 1S, cis enantiomer (II) have similar cuticular penetration rates and are detectable in the hemolymph, nerve cord, fat body, and midgut of the American cockroach, Periplaneta americana, within 2 hr of topical application at 0.17 μg/g, a just-lethal dose of I. At this dose, both enantiomers show similar distribution patterns in these tissues, but symptoms of intoxication are seen only with I. Steady state concentrations of both enantiomers in the hemolymph and nerve cord are between 1.2 × 10?7 and 1.7 × 10?7M. I and II are not detectably hydrolyzed by fat body, nerve cord, and hemolymph preparations and are not detectably oxidized by fat body preparations in vitro, but a very low oxidation rate is measured for II, but not I, in nerve cord preparations. These results do not demonstrate a pharmacokinetic basis for the difference in insecticidal activity between enantiomers and therefore it is likely that the site of pyrethroid action is stereospecific. The use of the inactive enantiomer II as a model to study the effects of dose on penetration and distribution in the absence of symptoms is explored.  相似文献   

4.
A rat hepatocyte suspension effectively epoxidized aldrin to dieldrin with a Vmax of 7.19 mol/mol P-450/min and a Km of 9.27 μM. Viability and metabolic activity were stable for 6 hr after isolation when cells were maintained at room temperature (20°C) with the gentle introduction of O2CO2 onto the surface of the suspension. The cytochrome P-450 content of the suspension was 303 pmol/106 cells. Primary maintenance culture of the cells also epoxidized aldrin. During culture for 3 days, metabolic activity decreased slowly day by day. Metabolic activity of microsomal fraction from rat liver was also examined. Microsomes epoxidized aldrin with a Vmax of 5.11 mol/mol P-450/min and a Km of 1.64 μM. Significant loss of some subspecies of cytochrome P-450 during fractionation of liver homogenate was indicated.  相似文献   

5.
Microorganisms which inhabit the surface of blowflies, Calliphora erythorcephala, were identified as Bacillus spp., Micrococcus spp., Proteus spp., Streptococcus spp., and yeasts. These microorganisms were able to metabolize [14C]dieldrin incorporated into their culture media. Micrococcus spp. converted up to 29% of the applied dose of dieldrin to its more polar metabolites while the lowest ability to breakdown dieldrin was associated with Streptococcus spp. which metabolized nearly 0.8% of the applied dose. The addition of sesamex into microbial cultures partly inhibited the breakdown of dieldrin. Cuticular microflora of blowflies were controlled by the topical application of a mixture of gentamicin and amphotericin B. Pretreatment of blowflies with these antibiotics blocked dieldrin metabolism, to a certain degree, in the epicuticular wax layer. The formation of some of the metabolites, which were uniquely confined to the external lipid layer of blowflies, was found to be due to the activity of certain microorganisms. Therefore, microorganisms living on the surface of blowflies were found to play a role in the metabolism of topically applied [14C]dieldrin. There was a loss in the recovery of the dose of dieldrin applied to blowflies with the lapse of time. This was principally due to its volatilization from treated insects. The volatilization of [14C]dieldrin from different surfaces was also studied. The loss of the applied dose of dieldrin from various surfaces was in the order of glass > aluminum > fiberglass > DEAE-cellulose paper > silica gel G.  相似文献   

6.
The effects of two pesticides, dieldrin and captan, upon the growth and macromolecular syntheses of the vegetative cells of Dictyostelium discoideum strain Ax-2 were investigated. Dieldrin at a concentration of 5 μg/ml inhibited growth as well as the synthesis of RNA, DNA, and protein, while as little as 1 μg/ml of captan produced the same effects. After a 1-hr exposure to either pesticide, all macromolecular syntheses ceased. Within a period of 5 to 10 hr the amoebae began to shrink, and eventually some lysis occurred. Lysis was most pronounced in cells incubated with captan. When the amoebae were grown in the presence of 5 μg/ml of either pesticide and then washed and resuspended in fresh medium, the effects on growth were annulled. No growth inhibition was observed when 0.05 M cysteine was added prior to the addition of 5 μg/ml of captan. Further experimentation to study possible degradation effects of these two synthetic pesticides upon RNA and protein molecules showed that breakdown of these macromolecules into TCA-soluble units did not occur. Preliminary studies have also shown that [2-14C]uracil and [14C]amino acids are taken up in their respective pools in the presence of captan or dieldrin.  相似文献   

7.
The direct effects of tepp, methyl paraoxon, DDT, dieldrin, aldicarb, dimetilan, rotenone, allethrin, and oxythioquinox were surveyed on cockroach brain adenyl cyclase and phosphodiesterase in vitro. The most striking result of this survey was the observation that oxythioquinox is a potent inhibitor of phosphodiesterase. The inhibitory activities of seven different quinoxalinedithiol derivatives were compared with those of methyl-xanthines and SQ 65,442 on phosphodiesterases from cockroach brain, rat brain, and beef heart. Although I50 values of the quinoxaline inhibitors were found to be in the μM range, solubility deficiencies apparently limit their effectiveness with inhibition reaching limiting values of about 70–90% as concentrations are increased. Evaluation of the quinoxaline inhibitors to enhance the accumulation of cyclic AMP in the assay of adenyl cyclase did not demonstrate any significant advantage over the use of aminophylline, a standard inhibitor for this purpose. A new assay for phosphodiesterase, involving separation of substrate from product on aluminum oxide columns, was developed by modification of similar techniques utilized in the assay of adenyl cyclase.  相似文献   

8.
Using radiotracer methodology and dissection techniques it was demonstrated that [14]chlorpyrifos and/or its 14C-labeled metabolite(s) concentrated mainly in the gut tissues and malpighian tubules of American cockroaches, Periplaneta americana (Linnaeus), following sorption from a treated surface. Significantly lower (P ≤ 0.10) amounts of 14C were present in testes samples and no radioactive material was detected in brain tissue. After 41.5–48 hr of exposure of adult male American cockroaches to sublethal concentrations of [14C]chlorpyrifos, radioactivity was detected in the hemolymph of all cockroaches tested. The hemolymph accounted for 30.83% of the total sorbed 14C. A parabiotic experiment confirmed translocation of chlorpyrifos and/or its 14C-labeled metabolite(s) in hemolymph.  相似文献   

9.
The binding in vitro of 14C-DDT to proteins from the hemolymph of the American cockroach was shown by means of electrophoresis and isoelectric focusing on polyacrylamide gels. The study of 14C-DDT penetration into the insect implies the hemolymph as one of the possible manners by which this insecticide could penetrate the central nervous system, and other target organs. The possibility of DDT being transported by the hemolymph bound to lipoproteins is discussed.  相似文献   

10.
The concentration of psoralens in celery (Apium graveolens L.), variety ‘Tender Crisp’, harvested 120 days after planting, was 12 μg g-1 f.wt, compared with 18 μg g-1 f.wt in celery harvested 150 days after planting. After 1 month of storage at 2°C, concentrations of psoralens in the 120- and 150-day-old celery were 82 and 118 μg g-1 f.wt, respectively. Concentrations of psoralens in the 120- and 150-day-old celery inoculated withBotrytis cinerea Pers., after 1 month of storage at 2°C, were 266 and 294 μg g-1 f.wt, respectively.  相似文献   

11.
The nature of the picrotoxinin receptor was studied using the central nervous system (CNS) of the American cockroach. It first was confirmed by using an electrophysiological technique that the abdominal nerve cord of the American cockroach was sensitive to picrotoxinin. By using a [3H]α-dihydropicrotoxinin binding test it was determined that the picrotoxinin receptor in CNS of this insect had a higher affinity toward picrotoxinin and heptachlor epoxide than the corresponding receptor in the rat brain. Also, the cockroach brain preparation had a higher percentage of specific binding in the total binding, making this material suitable for receptor studies. By using a sucrose density centrifugation technique, it was determined that the fraction sedimented at the interphase of 1.0 to 1.2 M sucrose at 100,000g contained the highest level of specific binding site. The receptor showed a sensitivity to all insecticidal cyclodienes tested, namely photodieldrin, oxychlordane, endrin, heptachlor epoxide, γ-chlordane, dieldrin, aldrin, heptachlor, and isodrin (expressed in the order of potency). Among four BHC isomers, the γ-isomer showed the highest potency to bind with this receptor.  相似文献   

12.
Sesquiterpene lactones, natural constitutents of the Asteraceae, are toxic to the grasshopper, Melanoplus sanguinipes, when injected into the hemocoel at doses greater than 0.25 μmol/300 mg insect. Dose-dependent sublethal symptoms range from a slight reduction in normal locomotory ability to severe locomotory impairment or paralysis, leading to death. The symptoms appear to be irreversible. Of the four compounds subjected to dose-response testing, parthenin was the most toxic with and LD50 in adult male grasshoppers of 0.55 μmol/insect. Structure-activity relationships for four of the six lactones tested indicate that compounds containing a cyclopentenone ring are equitoxic to males and females, whereas those lacking this functional group are approximately 4 × more toxic to males than females. In contrast to their sensitivity to injected lactones, adult male grasshoppers can tolerate ingestion or topical administration of up to 4 μmol of these compounds without any adverse effects. These results suggest that the integument and alimentary canal in this species provide effective barriers limiting the bioavailability of sesquiterpene lactones to the hemolymph in nature. Possible target sites and mechanisms-of-action for sesquiterpene lactones (once in the bloodstream) are discussed.  相似文献   

13.
Vernolate (0, 8, 16, 31, 62, 125.0, or 250.0 ppbw) incorporated into sand inhibited the growth of wheat (Triticum aestivum L. cv Holley) at 125.0 ppbw. These growth inhibition and morphological responses were virtually identical to wheat response to EPTC at 125 ppbw. 14C from vernolate (carbonyl labeled) (125.0 ppbw) was absorbed into wheat seedlings at approximately 1.8 μM on the presumption that the 14C present was [14C]vernolate. Since the response of wheat to the thiocarbamate herbicides resembles a gibberellic acid (GA) deficiency and cell enlargement requires the presence of functional plasmalemmas and tonoplasts, the question of membrane disruption by excessive concentrations of thiocarbamate herbicides and potential reversal thereof by GA3 was studied by measuring the efflux of K+, Na+, and Mg2+. GA3 (0.003 μM) stimulated lettuce leaf disc growth in diameter and fresh weight. This GA-stimulated increase in size and weight was reversed by 1 mM EPTC. Betacyanin efflux from beet leaf tonoplasts was increased by 1 mM EPTC and this efflux was not reversed by exogenous GA3 (0.3 μM). This influence by supraoptimal EPTC concentrations was shown to be via membrane disruption, which obviated any possible GA influence by eliminating the functionality of the membranes requisite to the development of a GA response. It is concluded that viable mode-of-action studies must measure physiological responses consistent with the symptomology of herbicide responses normally observed with each herbicide at field concentrations.  相似文献   

14.
l-[U-14C]sucrose accumulation by phloem sieve tube members (PSTM) of wheat (Triticum aestivum L. ‘Holley’) and sorghum (Sorghum bicolor L. ‘G522 DR’) was inhibited by the nonpermeant sulfhydryl inhibitor p-chloromercuribenzenesulfonic acid (PCMBS), and this inhibition was reversed by the permeant sulfhydryl protectants dithiothreitol (DTT) and dithioerythritol (DTE). S-Ethyl dipropylthiocarbamate (EPTC) (≤0.1 mM) did not inhibit [14C]sucrose accumulation by wheat or sorghum PSTM. N-N-Diallyl-2-chloroacetamide (CDAA) (1 mM) inhibited [14C]sucrose accumulation by sorghum but not by wheat PSTM. The inhibition of [14C]sucrose accumulation in sorghum PSTM by the membrane permeant CDAA was reversed by DTT. Sorghum growth was inhibited by <1 μM CDAA. Membrane permeant 2-chloroallyl diethyldithiocarbamate (CDEC) (0.1 mM) inhibited [14C]sucrose accumulation by PSTM of sorghum but not wheat. The inhibition of sucrose accumulation in sorghum PSTM by 0.1 mM CDEC was reversed by DDT.  相似文献   

15.
Enzymatically isolated leaf cells from navy beans (Phaseolus vulgaris L., cv. “Tuscola”) were used to study the effect of buthidazole (3-[5-(1,1-dimethylethyl)-1,3,4-thiadiazol-2-yl]-4-hydroxy-1-methyl-2-imidazolidinone) and tebuthiuron (N-[5-(1,1-dimethylethyl)-1,3,4-thiadiazol-2-yl]-N,N′-dimethylurea) on photosynthesis, protein, ribonucleic acid (RNA), and lipid synthesis. The incorporation of NaH14CO3, [14C]leucine, [14C]uracil, and [14C]acetic acid as substrates for the respective metabolic process was measured. Time-course and concentration studies included incubation periods of 30, 60, and 120 min and concentrations of 0.1, 1, 10, and 100 μM of both herbicides. Photosynthesis was very sensitive to both buthidazole and tebuthiuron and was inhibited in 30 min by 0.1 μM concentrations. RNA and lipid syntheses were inhibited 50 and 87%, respectively, by buthidazole and 42 and 64%, respectively, by tebuthiuron after 120 min at 100 μM concentration. Protein synthesis was not affected by any herbicide at any concentration or any exposure time period. The inhibitory effects of buthidazole and tebuthiuron on RNA and lipid syntheses may be involved in the ultimate herbicidal action of these herbicidal chemicals.  相似文献   

16.
Dieldrin and two of its metabolites, 6,7-trans-dihydroaldrindiol, and 6,7-cis-dihydroaldrindiol, were studied with regard to their toxicity to the American cockroach, effects on ganglia of the ventral nerve cord, and penetration into the ventral nerve cord of poisoned cockroaches. An approximate LD50 for injected doses of dieldrin was 0.45 mg/kg. After injection at 115 mg/kg, the trans isomer of aldrin diol caused about 70%, and the cis isomer about 50% mortality. Injected doses of 40 mg/kg of the three compounds appeared in the ventral nerve cord to the extent of 0.13–0.26% of the doses. Dieldrin was more potent, but slower acting than the diols in causing synaptic after-discharge and elevated spontaneous activity in isolated nerve cords. The results are discussed in relation to other studies on these compounds. It was concluded that, in the American cockroach, dieldrin, rather than either of the diols, is the insecticidal agent in dieldrin poisoning, and that metabolic conversion of dieldrin to the cis and/or trans aldrindiol constitutes a detoxification.  相似文献   

17.
Cytoplasmic uptake of carbendazim (methyl benzimidazol-2-yl carbamate; MBC) from an aqueous solution was demonstrated with isolated mesophyll cells. About 2.5% of the labelled MBC (ring-2-[14C]) in the treatment solution (1.85 μg/ml) was taken up in 44 h. When cotyledons of cucumber seedling were treated with either 347 or 36 μg [14C]-MBC/plant 1.11 and 0.13% were extracted, respectively, from the remainder of the plant, 5 days after treatment. Greatest amounts were detected in shoot apices. Likewise, when MBC and benomyl were applied at the dose of 2 μmol, 0.34 and 0.57% were detected in the untreated part of the plant with a bioassay procedure. Foliar application with 347 or 36 μg[14C]-MBC/leaf resulted in the translocation of 1.68 and 0.11% out of the treated area. By scalding the living cells of the petiole translocation was prevented suggesting that long distance movement occurred in the symplast. During a period of 14 days 1.56% of [14C]-MBC applied to cucumber leaves was metabolised and respired as CO2. This degradation was assumed to occur enzymically within the symplast.  相似文献   

18.
By employing intracellular electrodes on the 6th abdominal ganglion, Cartap hydrochloride 10?5M caused in all experiments a block of the provoked stimulus transmission and a decrease of the cell membrane resting potential; the giant fiber conduction was not affected. In the experiments with extracellular electrodes Cartap 10?5M provoked a marked increase of the spontaneous activity followed by block which partially disappeared after washing. The same effects were obtained on spontaneous activity when Cartap 10?5M was used on the denervated 6th abdominal ganglion and in experiments conducted at 0 Ca2+ or at 20 mM Mg2+. Cartap 10?5M did not affect the response to direct or indirect stimulation of cockroach neuromuscular preparation. These results tend to confirm that Cartap affects the postsynaptic region of the ganglionic nervous junction. The possible cause of the resting potential decrease is also discussed.  相似文献   

19.
N,N-Diallyl-2-chloroacetamide (CDAA) (0.25 ppmw; I μM) inhibited growth of 14-day-old sorghum (Sorghum bicolor (L) Moench. cv Funks G 522DR) when the herbicide was incorporated into sand. Kaurene oxidation was inhibited in a cell-free enzyme preparation from 4-day-old unruptured, etiolated coleoptiles. CDAA (1 μM) inhibited incorporation of [14C]mevalonic acid into kauren-19-oic acid (50%), with resultant increases in concentration of precursors. Thus, inhibition of gibberellin precursor biosynthesis was demonstrated, and this activity would explain many of the morphogenic and biochemical responses of grasses to CDAA.  相似文献   

20.
Two different methods were used to analyze the effects of topical and bath applications of low concentrations of deltamethrin. The first method enabled the analysis of the receptor potential as well as that of the spike activity generated by mechanical or electrical stimulation of the mechano-receptor. The second method enabled recording of the conducted spike activity originating from a mechanical stimulation of the receptor and propagated along the sensory nerve. Topical application of small amounts of deltamethrin (10−9 to 10−7 g) had little effect on the receptor potential induced by mechanical stimulation of the sensory hair but blocked the action potentials within a few minutes. Electrical stimulation of the receptor cell revealed that conduction in the dendrite was affected first by the insecticide. The effects of topical application on conducted activity were compared with those of bath applications (2 × 10−8 to 2 × 10−7 M) and no significant difference was found, suggesting a rapid penetration of the insecticide through the cuticle. These effects were not reversible and this absence of reversibility was not correlated with the integrity of the barrier which protects the receptor cell from rapid changes in the ionic composition of the hemolymph. Deltamethrin was never found to induce bursts of activity in the mechanoreceptor cell under investigation either at rest or following mechanical or electrical stimulation. There are, however, some indications that other receptor cells may respond differently to this insecticide.  相似文献   

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