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1.
The reactions of chlorothalonil with calf thymus histones, DNA, and isolated rat liver nuclei were studied utilizing labeled fungicide, polyacrylamide gel electrophoresis, and nucleohistone thermal denaturation. The reaction was dependent on pH, type of histones, and the histone and fungicide concentrations. In addition, two types of fungicide-histone binding patterns were observed. These patterns were characterized by the amount of label bound to protein after dialysis or after dialysis and acid precipitation. There was little binding of chlorothalonil to DNA. Polyacrylamide gel patterns of treated lysine-rich calf thymus histones were characterized by a loss of up to 80% of the stained protein without a change in the migration of the bands. Gel patterns of treated calf thymus whole histones were characterized by small variations in band density and minor loss of stained protein. The results of thermal denaturation experiments using chlorothalonil-treated lysine-rich histones and nontreated calf thymus DNA were not different from those using nontreated histones. Almost all of the radioactivity from [14C]chlorothalonil was bound by isolated rat liver nuclei. The binding patterns observed with rat liver nuclei were very similar to those using purified histones. Fractionation of proteins from treated nuclei revealed that the label was unequally distributed between the nuclear sap protein, ribonucleoprotein, and deoxyribonucleoprotein.  相似文献   

2.
Excretion and distribution of single and multiple intraperitoneal doses of [35S]captan and [14C]folpet were similar in normal and 70% hepatectomized male rats. After receiving the single dose of captan, the rats eliminate approximately 76% of the radioactivity in the urine after 72 hr. The elimination in the feces for the same time period was 13%. Normal rats administered single or multiple doses of [14C]folpet excreted nearly 100% of the total dose in the urine within the first 24 hr. Nuclei isolated from the liver of normal and 70% hepatectomized rats receiving multiple doses of [35S]captan contained 0.008–0.009 μg 35S/g of tissue. Appreciable amounts of the radioactivity from [35S]captan were bound by isolated nuclei from the livers of normal and partially hepatectomized rats. After a 1-hr treatment with [36S]captan, the nuclei were fractionated into nuclear sap protein, deoxyribonucleoprotein (including histones), acidic ribonucleoprotein, and “residual” protein fractions. These proteins in normal nuclei bound 10, 14, 39, and 16% of the total label, respectively, with essentially the same results obtained with nuclei from regenerating rat liver. When compared by polyacrylamide gel electrophoresis, acidic nuclear proteins from treated and nontreated normal nuclei were characterized by band diffusion and the presence or absence of Amido Schwartz-staining bands. None of the abovementioned effects on histones from treated nuclei were observed. Captan treatment of isolated nuclei also altered the extraction characteristics of the nuclear protein fractions, presumably because of extensive aggregation of thiol-containing nuclear proteins.  相似文献   

3.
A study was conducted concerning the inhibition of calf thymus nuclear DNA synthesis by captan. Captan was shown to be toxic to the in vitro incorporation of [3H]dTTP into calf thymus DNA, with an ID50 value of 0.16 mM being measured. This inhibition was determined to be independent of Mg2+ concentration. Although intact nuclear activities were affected, the soluble DNA polymerizing activity isolated from calf thymus nuclei exhibited no inhibition when exposed to captan. Treatment of purified calf thymus DNA with 10?5 and 10?4M captan caused an elevation of the Tm by 2 and 6°C, respectively. The inhibitory characteristic of captan on DNA polymerizing activities and the influence of this compound on the thermostability of DNA indicate a mechanism of inhibition which is located in the nucleus and is possibly related to the template function of DNA and/or with the nuclear DNA polymerizing enzymes.  相似文献   

4.
Captan, folpet, and perchloromethylmercaptan were effective inhibitors of Penicillium duponti p-nitrophenylpropionate esterase activity (I50 = 0.5 – 2 μM) whereas α-naphthyl acetate esterase activity was not affected by the presence of these compounds. Captan and folpet are both equally effective at pH 7.3 and 8.3. The ionic composition of the medium had strong effects on the degree of inhibition produced by all inhibitors but did not alter esterase activity. Neither succinamide nor phthalimide caused inhibition of the p-nitrophenylpropionate esterase activity: The trichloromethylmercaptan portion of these fungicides appears to be responsible for the observed inhibition. The rapidity of captan and folpet inhibition of esterase activity (complete in < 1 min) compared to the rates of spontaneous decomposition (t12 > 1 min) and the insensitivity of captan and folpet inhibition to hydrogen ion concentration suggest that generation of spontaneous decomposition products is not required for inhibition. The results are consistent with a mechanism in which the entire fungicide molecule binds to the protein followed by enzyme-promoted reactions of captan and folpet which result in loss of esterase activity.  相似文献   

5.
A method is described for the simultaneous determination of residues of five fungicides used for foliar treatment of apple and pear trees, and for postharvest application. After extraction, the mixture of these fungicides is cleaned-up on a ‘SEP PAK C18’ cartridge and the components determined by gas-liquid chromatography with electron-capture detection. The minimum detectable amounts in apples and pears, on a fresh weight basis, were 0.005mg kg−1 for vinclozolin, 0.010mg kg−1 for captan, folpet and iprodione, and 0.020 mg kg−1 for captafol. The percentage recovery for each fungicide (calculated by analysing four samples of untreated apples and pears, to which varying concentrations of each active ingredient had been added) varied for vinclozolin between 70.0 and 89.2, for captan between 72.0 and 83.8, for folpet between 73.0 and 93.0, for captafol between 70.8 and 91.8, and for iprodione between 75.1 and 97.1.  相似文献   

6.
The tissue distribution and excretion of 14C-labeled propham and chlorpropham were investigated in the adult female rat after a single oral dosage. The average 3-day urinary excretions of radioactivity were 55.9%, 82.6%, 79.5%, and 85.4% of an oral dose of chain [14C] chlorpropham, ring [14C] chlorpropham, chain [14C] propham, and ring [14C] propham, respectively. With chain [14C] chlorpropham 35.4 ± 7.5% of the administered radioactivity appeared in the respired air, whereas only 5.0 ± 0.8% was found in CO2 from chain [14C] propham. There was no significant difference in the rate of excretion or the route of elimination among rats receiving different oral dosages, ranging from less than 4 mg/kg to 200 mg/kg. The radioactivity was distributed in all tissues with highest concentration found in the kidney. The average biological half-life of 14C from chlorpropham and propham in most organs was short, ranging between 3 and 8 hr; however, in brain, fat, and muscle, the half-life was about twice the value for other organs.Both compounds were metabolized by hydrolytic and oxidative mechanisms and the resulting metabolites were excreted either as free forms or as conjugates.Subcellular distribution of 14C in the rat liver and kidney after an oral administration of chlorpropham and propham was investigated. The percentage distribution of 14C in the particulate and soluble fractions was dependent on the elapsed time after dosing.  相似文献   

7.
Addition of cysteine to the fungicides captan, folpet, dichlofluanid and captafol antagonizes the activity of these fungicides and results in the formation of volatile fungitoxicants. There is no relationship, however, between the vapour action upon reaction with cysteine and the fungitoxicity of these compounds.Samenvatting Cysteine heeft een antagonerend effect op de werking van captan, folpet, dichlofluanid en captafol (Tabel 1). Bij proeven in afgesloten ruimtes (twee petri schaaltjes, waarvan de één ongekeerd op de ander, Fig. 1) bleek vooral captan als gevolg van een reactie met cysteine een voorFusarium culmorum toxische damp af te geven, folpet deed dit daarentegen niet, en de twee andere fungiciden alleen in de hoogste concentratie (Tabel 1, Fig. 1). Er is dus weinig verband tussen de fungicide werking en de productie van fungicide dampen als gevolg van de reactie met thiolen.  相似文献   

8.
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   

9.
Ring- and carboxyl-labelled [14C]2,4-D were incubated under laboratory conditions, at the 2 g/g level, in a heavy clay, sandy loam, and clay loam at 85% of field capacity and 20 1C. The soils were extracted at regular intervals for 35 days with aqaeous acidic acetonitrile, and analysed for [14C]2,4-D and possible radioactive degradation products. Following solvent extraction, a portion of the soil residues were combusted in oxygen to determine unextracted radioactivity as [14C]carbon dioxide. The remaining soil residues were then treated with aqueous sodium hydroxide, and the radioactivity associated with the fulvic and humic soil components determined. In all soils there was a rapid decrease in the amounts of extractable radioacitivity, with only 5% of that applied being recoverable after 35 days. All recoverable radioactivity was attributable to [14C]2,4-D, and no [14C]-containing degradation products were observed. This loss of extractable radioactivity was accompanied by an increase in non-extractable radioactivity. Approximately 15% of the applied radioactivity, derived from carboxyl-labelled [14C]2,4-D, and 30% from the ring-labelled [14C]2,4-D was associated with the soil in a non-extractable form, after 35 days of incubation. After 35 days, less than 5% of the radioactivity from the carboxyl-labelled herbicide, and less than 10% of the ringlabelled material, was associated with the fulvic components derived from the three soils. Less than 5% of the applied radioactivities were identifiable with any of the humic acid components. It was considered that during the incubation [14C]2,4-D did not become bound or conjugated to soil components, and that non-extractable radioactivity associated with the three soil types resulted from incorporation of radioactive degradation products, such as [14C]carbon dioxide, into soil organic matter.  相似文献   

10.
Bromoxynil octanoate labelled with 14C in the ring or in the cyano-group was applied to wheat seedlings at the two-leaf or fully-tillered stage and at rates equivalent to up to 16 oz a.i./acre. The plants were grown either in environmental chambers under controlled conditions for up to 28 days, or outdoors under field conditions for various periods up to harvest. Initially, elimination of radioactivity occurred more rapidly with bromoxynil-cyano-[14C]-octanoate than with bromoxynil-ring-[14C]-octanoate, indicating metabolic attack on the cyano group. Under outdoor conditions with ring-[14C]-herbicide applied at the two-leaf stage, only 12% of the radioactivity was retained after 28 days, principally in the treated leaves. When application was made at fully-tillered stage, about 33% of the 14C was retained after 56 days, almost entirely in the treated senescent leaves at the base of the plant. There was very little translocation of the herbicide or of any major metabolite. The level of radioactivity in harvested grain and in straw more than 7.5 cm above the ground was very low, even after very late application of ring-[14C]-labelled herbicide. The amount of bromoxynil octanoate, together with any metabolite retaining part of the aromatic ring, did not collectively exceed the equivalent of approx. 0.01 parts/million bromoxynil octanoate.  相似文献   

11.
The influence of 1 and 50 mg active ingredient (AI) kg-1 soil of 17 fungicides on transformations of urea nitrogen in soil was studied by determining the amounts of urea hydrolysed and the amounts of nitrate and nitrite produced when samples of two coarse-textured and two fine-textured soils were incubated aerobically for various times after treatment with urea. When applied at the rate of 1 mg AI kg-1 soil, anilazine, benomyl, captan, chloranil, mancozeb and thiram retarded urea hydrolysis in the two coarse-textured soils and maneb retarded urea hydrolysis in all four of the soils used. Most of the fungicides tested retarded nitrification of urea nitrogen in the two coarse-textured soils when applied at the rate of 1 mg AI kg-1 soil, but only etridiazole markedly retarded nitrification of urea nitrogen in all of the soils used when applied at this rate. When the fungicides were applied at the rate of 50 mg AI kg-1 soil, anilazine, captan, chloranil, fenaminosulf, folpet, maneb, mancozeb and thiram retarded urea hydrolysis in the four soils studied, and all fungicides tested except chloroneb, fenarimol and iprodione retarded nitrification of urea nitrogen in these soils. One-way analysis of variance and correlation analyses indicated that the inhibitory effects of the 17 fungicides tested on nitrification of urea nitrogen in soil increased with decrease in the organic-matter content and increase in the sand content of the soil. © of SCI.  相似文献   

12.
The effects on DNA synthesis of the fungicide captan and several structurally related compounds were investigated in isolated bovine liver nuclei. Captan, folpet, captafol, and trichloromethanesulfenyl chloride inhibited DNA synthesis to the same degree with ID50 values of approximately 50 μM in a 40-min assay. The inhibition is concentration dependent and the degree of inhibition increases with time. Studies with structural analogs of captan indicated that inhibition of DNA synthesis by captan is mediated through the trichloromethylthio moiety of the captan molecule. In addition, the data indicate thiophosgene is probably not the toxic species involved in the inhibition of DNA synthesis. The isolated nuclei used in this study were shown to exhibit only a single DNA polymerase activity which was determined to be of the β or low-molecular-weight type. In addition to its inhibition in intact nuclei, captan inhibited the activity of the β polymerase in nuclear extracts as well as in partially purified enzyme preparations. These results indicate that captan inhibits DNA synthesis in our preparation of isolated nuclei by acting directly on the DNA polymerase-catalyzed reaction rather than by causing a nonspecific or indirect effect in the nuclear system such as alterations in the nuclear membrane or aggregation of the nuclei. The site of captan's inhibitory action is the DNA polymerase molecule. The interaction of captan with the polymerase results in irreversible inhibition of the enzyme. Interaction of captan with the template, if it occurs, does not appear to be involved in mediating the inhibition.  相似文献   

13.
The long term metabolism of [14C]MCPA and [14C]flamprop in wheat (Triticum aestivum) straw was found to involve incorporation of radioactivity as residues that were insoluble in acetone+water (1+1 by volume). A chemical and an enzymic solubilisation procedure were critically evaluated in attempts to release these residues for further examination. The chemical procedure resulted in complete solubilisation of all the radioactivity of both compounds in association with more than one cell wall fraction. However, routine quantitative analysis was found to be difficult for some fractions. Furthermore, the extracts did not appear to be suitable for investigation of the nature of the binding with the plant constituents. None of the enzymes employed in the enzymic procedures released significant amounts of the residues insoluble in the aqueous acetone. Despite these problems, the residues of MCPA that were insoluble in aqueous acetone were found to contain both the parent MCPA and its major metabolite 4-chloro-α-hydroxy-o-tolyloxyacetic acid.  相似文献   

14.
Phthalimide fungicides (captafol, captan and folpet) enhanced the accumulation of fenarimol by the mycelium of a wild-type strain and a fenarimol-resistant strain of Aspergillus nidulans. The accumulation is ascribed to inhibition of active efflux of fenarimol from the mycelium. It is assumed that the synergistic action observed between the phthalimide fungicides and fenarimol with respect to fungitoxicity, was caused by the increased accumulation of fenarimol.  相似文献   

15.
The behaviour of the morpholine fungicide fenpropimorph applied to soil was investigated in a laboratory chamber. The volatility and metabolism of a 14C-labelled fenpropimorph formulation (Corbel®) was studied after application to three soils (sandy loam, loamy clay and loamy sand), simulating a four-day weather scenario in the volatilization chamber. Additional experiments were conducted under standard climatic conditions over a period of 24 h using sandy soils with different pH values. The results of the first experiments showed that most of the radioactivity applied remained in the soils as unchanged fenpropimorph four days after application. In the experiments with the sandy loam and loamy clay, less than 5% of the applied radioactivity was removed by volatilization whereas 11·4% volatilized from the surface of the loamy sand. The comparatively higher volatilization of the fungicide from the loamy sand was confirmed by the later experiments indicating that higher soil pH favoured volatilization of [14C]fenpropimorph from sandy soils. Thus 5·6% (pH 5·0), 18·9% (pH 5·8) and 28·3% (pH 6·6) of the radioactivity applied volatilized within one day after application. The overall recoveries were between 93·8% and 111·3% in these experiments. © 1998 SCI  相似文献   

16.
The calcium channel and the ‘calcium release channel’ of muscle membrane of the cockroach Periplaneta americana have been characterized. Biological assays with calcium channel blockers and ryanodine on different insects and acari revealed pronounced insecticidal effects with ryanodine, but not with calcium channel blockers, at concentrations between 0·1 and 300 μg ml−1. Skeletal muscle membranes derived either from the tubular network or from the sarcoplasmatic reticulum of P. americana were characterized with respect to the binding of the dihydropyridine (DHP) [3H]isradipine (PN 200-110), the phenyl-alkylamine [3H]verapamil and the alkaloid [3H]ryanodine. Preliminary binding studies with the benzothiazepine [3H]diltiazem suggest a low-affinity binding site with a IC50 value of 3·3 μM . All binding sites tested were sensitive to treatment with proteinase K. Optimal conditions for binding of the radioligand ryanodine revealed the highest specific binding at pH 8 and at calcium chloride concentrations between 100 and 500 μM . EGTA at 10 μM abolished 95% of the ryanodine binding. Binding studies with calcium channel binding sites revealed a pronounced effect of low Ca2+ concentrations on specific isradipine binding, whereas verapamil and diltiazem binding were only reduced by the presence of 200 μM EGTA. With respect to high Ca2+ concentrations, specific binding of diltiazem, isradipine and verapamil was reduced by 73, 40 and 20%, respectively, at 5 mM Ca2+. Radioligand binding experiments showed high-affinity binding sites for ryanodine and isradipine. KD values of 0·95 nM (Bmax=550 fmol mg−1 protein) and 0·75 nM (Bmax=213 fmol mg−1 protein) were determined respectively. A lower-affinity binding site was identified in binding studies with verapamil (KD=7·4 nM and Bmax=27 fmol mg−1 protein). [3H]isradipine displacement studies with several dihydropyridines revealed the following ranking of affinity: nitrendipine>isradipine>Bay K8664≪nicardipine. Displacement of [3H]verapamil binding by effectors of the phenylalkylamine binding site showed that bepridil and S(-)verapamil had the highest affinities of the compounds tested followed by (±)verapamil, nor-methylverapamil and R(+)verapamil.  相似文献   

17.
A simple and rapid method for extracting benomyl residues from soils was compared with previous methods. Soil was extracted by shaking for 2 h at room temperature with (1:1) acetone/M aqueous ammonium chloride followed by clean-up by solvent partition and ultraviolet absorption estimation of carbendazim. Recoveries were comparable to those obtained by refluxing with methanolic hydrochloric acid for 4 h, hitherto the most efficient method reported, and were much greater than those obtained by extraction with ethyl acetate or chloroform. The new method gave more tractable extracts than those obtained by refluxing with methanolic hydrochloric acid, which form troublesome metal hydroxide precipitates during clean-up. In field experiments with 2-[14C]-benomyl and 2-[14C]-carbendazim, no radioactivity was found more than 25 mm from the soil surface during 10 months after surface application of 1 kg/ha. Carbendazim residues in soils from three field experiments indicated that its persistence is very sensitive to soil pH. The time for 50% loss of initial dose ranged from 26 months at pH 5.5 to less than 3 months at pH 7.2. Biological effectiveness in a crop may therefore depend markedly on differences in soil pH.  相似文献   

18.
The uptake and translocation of [14C]asulam (methyl 4-aminophenyl-sulphonylcarbamate), [14C]aminotriazole (1-H-1,2,4-triazol-3-ylamine) and [14C]glyphosate (N-(phosphonomethyl)glycine) were assessed in Equisetum arvense L. (field horsetail), a weed of mainly horticultural situations. Under controlled-environment conditions, 21°C day/18°C night and 70% r. h., the test herbicides were applied to 2-month-old and 2-year-old plants. Seven days following the application of 0.07-0.09 °Ci (1.14mg) of the test herbicides to young E. arvense, the accumulation of 14C-label (as percentage of applied radioactivity) in the treated shoots, untreated apical and basal shoots was as follows: [14C]asulam, 13.2, 0.18 and 1.02%; [14C] aminotriazole, 67.2, 3.65 and 1-91%; [14C]glyphosate, 35.9, 0.06 and 0.11%. The equivalent mean values for the accumulation of 14C-label in 2-year-old E. arvense were [14C]asulam, 12.0, 1-15 and 1.74%; [14C]aminotriazole, 58.6, 9.44 and 4.12%; [14C]glyphosate, 33.1, 0.79 and 2.32%. In the latter experiment, test plants received 0.25-0.30 °Ci (4mg) of herbicide, they were assessed after a 14-day period and the experiment was carried out at 3-week intervals between 2 June and 25 August on outdoor-grown plants. Irrespective of test herbicide or time of application, very low levels of 14C-label accumulated in the rhizome system. Only 0.2% of the applied radioactivity was recovered in 2-year-old plants and 0.4% in 2-month-old plants. In the young plants [14C]asulam accumulated greater amounts and concentrations of 14C-label in the rhizome apices and nodes than [14C]aminotriazole or [14C]glyphosate treatments. Inadequate control of E. arvense under field conditions may be due to limited basipetal translocation and accumulation of the test herbicides in the rhizome apices and nodes.  相似文献   

19.
In unwounded soybean hypocotyls, pulse labelled with [14C]phenylalanine and inoculated with Phytophthora megasperma f.sp. glycinea, rates of [14C]-incorporation and glyceollin I accumulation were higher in resistant than in susceptible responses throughout the time-course of the experiment. This distinction was masked in hypocotyls that were wounded and inoculated. In such hypocotyls, high rates of [14C]-incorporation developed that were similar for the first 11 h in resistant and susceptible responses, although much more glyceollin I accumulated in the former. High rates of [14C]-incorporation also developed in uninoculated wounded hypocotyls but only small amounts of glyceollin I of high specific radioactivity were detected. Estimates of phenylalanine ammonia-lyase activity indicated that the metabolic flux through phenylalanine was limited in wounded controls but potentially very high in resistant responses. Differences in rates of [14C]-incorporation and in specific radioactivity of accumulated glyceollin I presumably indicate differences in the relative contributions of mobile internal pools and externally applied phenylalanine, in addition to rates of biosynthesis. Rapid decline in [14C]-glyceollin I was demonstrated in wounded controls in pulse-ch0ase experiments with phenylalanine as chase, but not in inoculated hypocotyls, due to continued [14C]-incorporation during the chase period. Rapid metabolism was demonstrated in all interactions and in wounds when cinnamic acid was used as the chase, but there was no evidence that differences in glyceollin I accumulation were due to differential rates of metabolism. Additional evidence for metabolic activity was provided by pulse feeding with [14C]glyceollin I. It is concluded that the stimulus of wounding or infection induces a metabolic pathway in which glyceollin I is not an end product. The accumulation of higher levels of glyceollin I in resistant than in susceptible responses appears to be due to earlier initiation and subsequently higher rates of biosynthesis in the former.  相似文献   

20.
Intact mitochondria, isolated from red coxal muscle of the American cockroach (Periplaneta americana L.), were incubated in the presence of 1,1,1-trichloro-2,2-bis(4-chloro[14C]phenyl)ethane ([14C]DDT) to isolate a suspected binding site for DDT in the membrane sector of the mitochondrial ATPase. The requirements for the binding of DDT were compared with those for the binding of dicyclohexyl[14C]carbodi-imide([14C]DCCD), a potent inhibitory probe of mitochondrial ATPase activity. [14C]DDT appeared to bind to a proteolipid of the membrane sector, which also binds [14C]DCCD. Exchange experiments, with [14C]DCCD, [14C]DDT and unlabelled DDT at different concentrations, indicated that DDT and DCCD may be acting on a similar protein. This protein may act as the energy transducing protonophore required for the synthesis and hydrolysis of ATP in coupled mitochondria. Inhibition of mitochondrial ATPase activity may be a consequence of DDT and DCCD binding to this proteolipid protonophore, resulting in the disruption of energy transduction in muscle and nerve.  相似文献   

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