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1.
A suspension culture of isolated rat hepatocytes was used to reproduce in vitro the paraoxon-induced release of hepatic β-glucuronidase observed in vivo. After a short latent period, exposure of hepatocytes to paraoxon at 10?7 to 10?4M resulted in a typical dose-dependent response, with highest release occurring at 10?4M paraoxon. With 10?3M paraoxon, however, response was anomalous with a much-decreased enzyme release. As expected from earlier results in vivo, SV1-oxon exhibited less effect than paraoxon.  相似文献   

2.
Isolated rat hepatocytes suspended in Waymouth's medium absorbed parathion rapidly and reversibly until the intracellular parathion concentration reached more than 300 times the ambient concentration. The distribution quotient q, defined as the ratio of intra- and extracellular concentrations at equilibrium, decreased when horse serum was added to the medium. The high hepatocyte affinity and rapid uptake of parathion suggested that this compound might be almost completely absorbed by periportal hepatocytes in the perfused liver and migrate downstream chromatographically through the lobule. Parathion infusion experiments verified this prediction and showed that the migration rate is dependent on the q value. The chromatographic feature may be useful as a basis for nonhistological investigation of intralobular hepatocyte heterogeneity. The lobule may function as a reverse-phase chromatograph also for many other unionized xenobiotics. Implications of the findings in the hepatic disposition of xenobiotics in vivo are discussed.  相似文献   

3.
The initial steps of the uptake of lindane by the liver were studied by using isolated rat hepatocytes. [U-14C]Lindane served as labeled indicator during the metabolite production. Results indicated a very fast uptake of the pesticide by the cells. During the first minute there were rapid exchanges between cells and medium; the rate of the uptake did not follow linear evolution. The metabolite production by the cells was time dependent. Up to eight metabolites were visualized during the first minute after the lindane addition. The time course of the uptake was concentration dependent. Profile evolution suggested that the cell metabolism was overloaded over 150 μM lindane. The depletion of hepatocytes in glutathion changed the partition of the radioactivity among the produced metabolites. At 37°C, the N2 gassing decreased the quantities of cyclohexane rings in the cells. This effect was reversed by preliminary addition of SKF 525A to the incubation medium; SKF 525A had no effect under O2 aeration. Isomers α and β of HCH, bromsulfophtalein interfered with the lindane transformation by the cells. Thus, isolated hepatocytes represented a sensitive intermediate preparation between perfused liver and homogenate experiments. They will be used for further comparison of the in vivo and in vitro metabolite formation corresponding to the elimination of lindane by the biliary pathway.  相似文献   

4.
Composition-concentration relationships between a series of C13/C14 polyoxyethylene primary alcohol (AE) surfactants and the foliar uptake enhancement of five model neutral organic compounds were examined in factorially designed experiments on wheat (Triticum aestivum L.) and field bean (Vicia faba L.) plants grown under controlled environment conditions. Model compounds were applied to leaves as c.0.2-μl droplets of 0.5 g litre?1 solutions in aqueous acetone in the absence or presence of surfactants at 0.2, 1 and 5g litre?1. Uptake of the highly water-soluble compound, methylglucose (log octanol-water partition coefficient (P) = - 3.0) was best enhanced by surfactants with high E (ethylene oxide) contents (AE15, AE20), whereas those of the lipophilic compounds, WL110547 (log P = 3.5) and permethrin (log P = 6.5), were increased more by surfactants of lower E contents, especially AE6. However, there was little difference between AE6, AE11, AE15 and AE20 in their ability to promote uptake of the two model compounds of intermediate polarity, phenylurea (log P = 0.8) and cyanazine (log P = 2.1). Absolute amounts of compound uptake were also influenced strongly by both surfactant concentration and plant species. Greatest amounts of uptake enhancement were often observed at high surfactant concentration (5 g litre?1) and on the waxy wheat leaves compared with the less waxy field bean leaves. The latter needed higher surfactant thresholds to produce significant improvements in uptake. Data from our experiments were used to construct a simple response surface model relating uptake enhancement to the E content of the surfactant added and to the physicochemical properties of the compound to be taken up. Qualitative predictions from this model might be useful in rationalising the design of agrochemical formulations.  相似文献   

5.
The uptake from foliar deposits of 10 14C-labelled compounds into each of 10 species of field-grown plants was measured 26 h after deposition by combustion of leaf tissue after removal of surface deposits. The compounds, which included eight pesticides, covered a wide range of lipophilicity and each was formulated in the same way; they were applied as droplets with a microsyringe. Uptake varied greatly between the species. All compounds were taken up well into maize and Xanthium pennsylvanicum, whereas relatively little entered the leaves of apple or orange. Uptake into the six other species varied according to the compound. Amongst the eight non-polar compounds, no relationship between the rate of uptake and molecular size was discerned, and only in X. pennsylvanicum was uptake related to the partition coefficient and water solubility. Considering all the compounds, weak relationships were observed between molecular cross-sectional area and uptake into four species. The range of the uptake rates (×130) was small compared with those of octan-1-ol-water partition coefficients (×1010) and water solublities (×107) shown by the 10 compounds. Possible reasons for the absence of correlations between the uptake and the molecular properties considered are discussed. The results are consistent with either separate routes of cuticular entry for non-polar and polar compounds, or a common route for both types of compound. The generally poor uptake by apple and orange leaves, which may be related to their thick cuticles, highlights the need to develop special formulations to optimise uptake into these species.  相似文献   

6.
Vetiver (Vetiveria zizanioides Nash) cells derived from an inflorescence were cultured in a modified N6 liquid medium supplemented with 10 µm 2,4‐D and 10 mm proline. Exponentially growing cell suspensions were subcultured with a selection medium containing glufosinate (ammonium dl ‐homoalanin‐4‐yl(methyl)phosphinate). The glufosinate‐resistant cells which can grow in a medium containing 5 × 10?5 M glufosinate was selected by a stepwise selection, and its I50 value was determined to be 4.2 × 10?5 M. The growth of susceptible cells was inhibited by lower concentrations of glufosinate and its I50 value was 2.5 × 10?7 M. This indicated that the selected cells were 170‐fold resistant compared with the susceptible cells. Glutamine synthetase (GS) activity of the resistant cells was twice as high as that of the susceptible cells. The I50 values of glufosinate were 3.2 × 10?5 M and 9.0 × 10?7 M for GS from the resistant and susceptible cells, respectively. The accumulation of ammonia caused by GS inhibition was higher in the susceptible cells. Absorption of [3,4–14C]glufosinate was not significantly different between the resistant and susceptible cells. Both cell types did not metabolize glufosinate. These results suggest that the resistance of the selected vetiver cell suspension to glufosinate is mainly due to increased GS activity and its decreased sensitivity to the herbicide.  相似文献   

7.
The binding of bis(p-chlorophenyl) acetic acid with bovine serum albumin has been monitored by observing the changes in the relaxation times of bis(p-chlorophenyl) acetic acid proton magnetic resonance peaks. The addition of bovine serum albumin to an aqueous solution of bis(p-chlorophenyl) acetic acid increased linewidths in a manner suggesting rapid, reversible binding. Line broadening was found to be greater for the ring protons than for the benzylic proton, indicating that the ring presents the stronger binding site. The equilibrium constant has been approximated. The binding results are discussed in terms of environmental and toxicological considerations.  相似文献   

8.
Lignin, an important component of plant tissues, adsorbed five systemic fungicides and one herbicide (carbendazim, triadimefon, nuarimol, triarimol, fenarimol and fluometuron) more strongly than bovine serum albumin, cellulose, ethylcellulose or sodium polygalacturonate. Significant correlations were found between the extent of the adsorption of the pesticides on the lignins extracted from three different plant species, and the log Poet (Poet is the octan-1-ol/water partition coefficient) of the compounds. The more lipophilic fungicides triarimol and fenarimol (log Poet about 2.6) were adsorbed to the greatest extent. Fluometuron, triadimefon and nuarimol (log Poet about 2.0) were moderately adsorbed, whereas carbendazim with the lowest log Poet (1.34 at pH 5.0), was adsorbed more than expected from its Poet value. The anomaly of carbendazim is discussed; it is ascribed to it's partial protonation at pH 5.0, whereas the other pesticides were non-ionised.  相似文献   

9.
The antifungal activity of 61 N-phenylsuccinimides and 16 N-phenyl-1,2-dimethylcyclopropanedicarboximides having various benzene ring substituents was determined against Botrytis cinerea by the agar medium dilution method. The structure-activity relationships were analyzed using such physicochemical substituent parameters as hydrophobic π, electronic σ0, steric E8, and HB (hydrogen bonding) values with the multiple regression technique. The π values were derived from log P (octanol-water partition coefficient) values for the N-monosubstituted-phenylsuccinimide system. The hydrophobic effect is significant only for m-substitutents. The stronger the electron withdrawal and the smaller the steric dimensions of the ring substituents, the greater is the activity. When substituents are hydrogen bond acceptors, the effect is to lower the activity. These features are almost identical between two series of compounds.  相似文献   

10.
The bioconcentration factors (BCF) for 15 pesticides by a freshwater fish (topmouth gudgeon) were measured under continuous flow conditions in water containing 5 to 20 μg litre?1 of each pesticide at the equilibrium condition. A significant correlation was found between the BCF by the fish and the water solubility of the pesticide or its partition coefficient (PC) between octan-1-01 and water. Moreover, a significant correlation was also found between the BCF by topmouth gudgeon and the acute toxicities to carp, rainbow trout and water flea. It would therefore appear that the bioconcentration potential of a pesticide by a fish may be predicted from knowledge of its solubility or PC, and that the acute toxicity of a pesticide to a fish may be predicted from knowledge of the BCF.  相似文献   

11.
The effects of nine phenoxy-phenoxypropionic acid derivatives and structurally related compounds on the incorporation of [14C]-acetate into free fatty acids in isolated bean and maize chloroplasts were studied. The compounds tested were esters and the corresponding free acids, OH-diclofop, a nonherbicidal metabolite of diclofop in plants, and d and l enantiomers of diclofop. Fatty acid biosynthesis in bean chloroplasts was not affected by all compounds. OH-Diclofop had a weak inhibitory effect on fatty acid synthesis in maize chloroplasts, while free acids were stronger inhibitors than the corresponding esters in the same system. Uptake studies with diclofop-methyl and diclofop indicated that the esters showed higher uptake rates in chloroplasts suspension. d-Diclofop (I50, 9 × 10?8M) was a more potent inhibitor than l-diclofop (I50, 4 × 10?6M). This agrees with the low herbicidal activity of the l enantiomer in vivo. The results suggest that the mode of action in this type of herbicide may be closely linked with the inhibition of fatty acid biosynthesis. The tolerance of beans could be based on an insensitivity of the target site.  相似文献   

12.
以番茄品种鑫语为试验材料,在开花盛果期喷施含Ca(NO_3)_2、Ca(H_2PO_4)_2、KSiO_4、Ca(NO_3)_2+KSiO_4及Ca(H_2PO_4)_2+KSiO_4的悬液,探讨钙硅单一及配合施用对设施春茬番茄根系生长、NPK吸收、产量及水分利用率的影响。结果表明:喷施钙硅悬液显著促进番茄根系生长及发育,显著促进根系和果实磷钾吸收;含钙悬液单独喷施处理的根系和果实氮吸收显著高于硅悬液及钙硅复配悬液;两种含钙悬液Ca(NO_3)_2和Ca(H_2PO_4)_2喷施处理取得最佳调控效果,与对照相比,分别使番茄增产9%和7%,水分利用率提升7、5.5 kg·m~(-3),喷施Ca(NO_3)_2+KSiO_4使番茄增产4.7%,水分利用率提升3.8 kg·m~(-3),喷施Ca(H_2PO_4)_2+KSiO_4和KSiO_4未取得显著的调控效果;含钙悬液单独喷施处理增加番茄产量与其促进根系发育及增加植株N吸收密切相关;两种含钙物质与KSiO_4对番茄产量的影响存在显著的交互效应,对产量的贡献呈:含钙物质含钙物质×KSiO_4KSiO_4。含钙悬液喷施技术简单高效,能实现番茄增产及生物节水能力提升。  相似文献   

13.
A series of 27 substituted aryl N-methoxy-N-methylcarbamates were synthesized and their ability to reversibly inhibit house fly-head and bovine-erythrocyte acetylcholinesterase and horse-serum cholinesterase was determined. These compounds were all competitive, reversible inhibitors of bovine erythrocyte acetylcholinesterase but some of them showed mixed competitive inhibition against the house fly-head and horse-serum enzymes. Dissociation constants (Ki) as small as 9.9 × 10?9M and as large as 1.4 × 10?4M were observed. A highly satisfactory correlation between log Ki for the inhibition of fly-head acetylcholinesterase by the N-methoxy-N-methylcarbamates and ?log I50 for the inhibition of the same enzyme by the corresponding methylcarbamates was noted. Analysis of the anticholinesterase data by multiple regression showed -log Ki to be related to Hansch's π constant and ring position terms. The results indicate that reversible binding of these compounds to acetylcholinesterase occurs by hydrophobic bonding.  相似文献   

14.
Effects of selected herbicides and respiratory inhibitors on leakage from tobacco (Nicotiana tabacum) cell suspension cultures were studied. Leakage was monitored by quantitation of fluorescein dye released from preloaded cells and by measuring conductivity changes in the suspension medium. The herbicides ioxynil, Barban, 2,4,5-T, MCPB, and PCP (10?6 to 10?4M) caused leakage of fluorescein dye and electrolytes within 2 hr of exposure to the herbicides. Potassium cyanide and 2,4-DNP caused appreciable leakage at the same concentrations. Similar responses were induced by anaerobiosis. Atrazine, metolachlor, paraquat, and nitrofen did not induce leakage when tested at concentrations of 10?6 to 10?4M.  相似文献   

15.
The influence of a number of commercial nonionic polyoxyethylene surfactants on the foliar penetration and movement of two systemic fungicides, ethirimol and diclobutrazol, was studied in outdoor-grown wheat plants at different growth stages and post-treatment temperatures in two consecutive growing seasons. Both fungicides were applied as ca 0·2 μl droplets of aqueous suspension formulations containing 0·5 g litre?1 of 14C-labelled active ingredient; surfactants were added to these suspensions at concentrations ranging from 0·2-10 g litre?1. To achieve optimum uptake of each fungicide the use of surfactants with different physicochemical properties was required. For diclobutrazol, a lipophilic compound, uptake of radiolabel was best with surfactants of low mean molar ethylene oxide (E) content (5-6) but it was necessary to use concentrations of ca 5 g litre?1 to attain this. The surfactant threshold concentration for uptake enhancement of radiolabel from ethirimol formulations (< 2 g litre?1) was much lower than that for diclobutrazol but surfactants with E contents > 10 induced the greatest amount of uptake. For both fungicides, surfactants with an aliphatic alcohol hydrophobe were generally more efficient in promoting their uptake than those with a nonylphenol moiety. The sorbitan-based surfactant ‘Tween 20’ proved to be an effective adjuvant only for the ethirimol formulation; the uptake enhancing properties of the block copolymer ‘Synperonic PE/F68’ were weak. Uptake performance could not be related to the spreading properties of the respective formulations on the wheat leaf surface or to differences in solubilisation of the two fungicides by the surfactants. Although surfactants could substantially increase the amount of acropetal transport of radiolabel from both fungicides, none of those tested specifically promoted it; a constant proportion of the radioactive dose absorbed by a treated leaf was usually exported away from the site of application. The results are discussed in the light of current theories about the mode of action of surfactants as spray adjuvants.  相似文献   

16.
Binding data were gathered for the cecropia juvenile hormone (methyl(E, E cis)-10,11-epoxy-7-ethyl-3,11-dimethyl-2,6-tridecadienoate) and two of its analogs {isopropyl(2E, 4E)-11-methoxy-3,7,11-trimethyl-2,4-dodecadienoate; (E)-4-[(6,7-epoxy-3,7-dimethyl-2-nonenyl)-oxyl]-1,2-(methylenedioxy)benzene} with bovine serum albumin and rat hepatic microsomal cytochrome P450. The proteins were found to bind the juvenile hormone and juvenile hormone analogs with affinity constants ranging from 105 to 106M?1. Thermodynamic calculations suggest that the binding of all three compounds is electrostatic in nature and that the size of the ether and ester substituents can greatly influence the binding to proteins. The juvenile hormone and its analogs all formed spectrally apparent Type I complexes with oxidized cytochrome P450; one of the juvenile hormone analogs formed a spectrally observable product adduct with reduced cytochrome P450. The product complex may contribute many of the hormonal effects observed for this compound.  相似文献   

17.
The organophosphorus insecticides, parathion and azinphos (10?5-10?4M), significantly stimulate the Ca2+-pump activity of sarcoplasmic reticulum, while malathion has a limited effect. The rates of Ca2+ translocation and ATP hydrolysis are both stimulated and, apparently, the Ca2+ATP ratio is improved. Parathion and azinphos maximally increase this ratio by 26 and 14%, respectively. The organochlorine compounds, DDT and aldrin, also stimulate the Ca2+ pump, and lindane has a reduced effect. These effects are smaller than those observed for parathion and azinphos. The order of effectiveness is similar to the toxicity of the compounds to mammals and can be described as follows: parathion > azinphos > DDT ≈ aldrin > malathion ≈ lindane.  相似文献   

18.
The inhibition of eel acetylcholinesterase and bovine erythrocyte acetylcholinesterase by the 4-nitrophenyl esters of methyl-, ethyl-, and isopropyl(phenyl)phosphinic acid (MPP, EPP, and IPP, respectively) was investigated at pH 6.90 in 0.067 M phosphate buffer (25.0°C) using stopped-flow instrumentation and automated data processing. Our evaluation of the dissociation constant, Kd, the unimolecular bonding rate constant, k2, and the bimolecular reaction constant, ki, are the first reported values for these constants for a homologous series of this class of organophosphorus compounds. The largest k1 value (29,428 M?1 sec?1) was observed for the reaction of eel acetylcholinesterase with 4-nitrophenyl methyl(phenyl)phosphinate. The smallest ki value (9.6 M?1 sec?1) was observed for the reaction of bovine erythrocyte acetylcholinesterase with 4-nitrophenyl isopropyl(phenyl)phosphinate.  相似文献   

19.
The interaction of a novel pesticide, NMD (spiro[(2R,3R,4S)-4-benzyloxy-2,3-iso-propylidenedioxy-1-oxacyclopentane-5,5′-(2-nitromethylene-1,3-diazacyclohexane)]), with bovine serum albumin (BSA) has been investigated by using absorption, fluorescence, and circular dichroism (CD) spectroscopy methods. Quenching of the fluorescence of BSA has been observed in the presence of NMD. The binding parameters were determined using Stern–Volmer equation. From the thermodynamic parameters calculated according to the van’t Hoff equation, the enthalpy change ΔH, and entropy change ΔS were found to be −2.71 kJ mol−1 and 82.56 J mol−1 K−1, respectively. These values suggested that, apart from an initial hydrophobic association, the complex is held together by van der Waals interactions and hydrogen bonding. These results provided a quantitative understanding of the binding of NMD to BSA, which is important in understanding its toxicity in vertebrates.  相似文献   

20.
BACKGROUND: The intermediate derivatisation method based on bioisosteric replacement led to the discovery of the lead strobilurin compound 5a. To produce new strobilurin analogues with improved activity, a series of substituted pyrimidines were synthesised and bioassayed. RESULTS: The compounds were identified by 1H NMR, IR, MS and elemental analysis. The highly active compound 5g was studied by X‐ray diffraction. Preliminary bioassays demonstrated that some of the title compounds exhibited excellent acaricidal activity against Tetranychus cinnabarinus (Boisd.) at 10 mg L?1. The relationship between structure and acaricidal activity is reported. CONCLUSION: The present work demonstrates that strobilurin derivatives containing pyrimidine moieties can be used as possible lead compounds for developing novel acaricides. Copyright © 2010 Society of Chemical Industry  相似文献   

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