Rat liver paraoxonase (paraoxon arylesterase)     

Jane E. McIlvain  Julita Timoszyk  Tsutomu Nakatsugawa 《Pesticide biochemistry and physiology》1984,21(2):162-169

Paraoxonase in the liver of male Sprague-Dawley rats was studied by using [phenyl-1-¹⁴C]paraoxon. Examination of the enzyme activity in subcellular fractions of liver homogenates indicated that hepatic paraoxonase is essentially a microsomal enzyme with a pH optimum of 7.5 to 7.8. Effects of calcium ions and EDTA on the enzyme suggested that active paraoxonase is a protein-calcium complex possibly with a range of affinity to calcium ion. Activity in homogenates declined with a half-life of 6 to 9 hr when stored at 0°C, apparently reflecting dissociation of calcium ions. Experiments with homogenates of perfused liver provided evidence that even without the contribution of calcium from blood, paraoxonase is almost fully active at the moment of homogenization. Possible reasons for the much reduced activity of paraoxonase in in vivo metabolism are discussed.  相似文献   

In vitro metabolism and interaction of profenofos by human, mouse and rat liver preparations     

Khaled Abass  Petri Reponen  Jorma Jalonen 《Pesticide biochemistry and physiology》2007,87(3):238-247

Biotransformations of profenofos were studied in vitro. Two metabolites, desthiopropylprofenofos and hydroxyprofenofos, were detected by LC-MS after incubation of profenofos with human liver homogenates and different mammalian liver microsomes. The rank order of desthiopropylprofenofos formation in liver microsomes based on intrinsic clearance (V_max/K_m) was mouse > human > rat, while for profenofos hydroxylation it was mouse > rat > human. In view of the ratio between desthiopropylation and hydroxylation intrinsic clearance rates, human liver microsomes were most active in profenofos bioactivation. The interspecies differences and interindividual variation were within range of the default uncertainty/safety factors for chemical risk assessment. CYP3A4, CYP2B6 and CYP2C19 were identified as profenofos-oxidizing enzymes in human liver on the basis of recombinant expressed enzymes and correlation with CYP model activities. The rank order of CYPs in profenofos activation was CYP3A4 > CYP2B6 > CYP2C19, whereas it was the contrary for profenofos hydroxylation. Profenofos inhibited relatively potently several human liver microsomal activities: the lowest IC₅₀ values were about 3 μM for CYP1A1/2 and CYP2B-associated activities. Profenofos is extensively metabolized by liver microsomal CYP enzymes and its interaction potential with several CYP activities is considerable.  相似文献   

Interaction of insecticides with the Ca²⁺-pump activity of sarcoplasmic reticulum     

M.C. Antunes-Madeira  Vitor M.C. Madeira 《Pesticide biochemistry and physiology》1982,17(2):185-190

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 $\text{Ca}{}^{\mathrm{2+}}\text{ATP}$ 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   

Inhibition of calmodulin-dependent enzymes in rat brain by hexachlorocyclohexane     

B. S. Basavarajappa  Bharathi P. Salimath 《Pest management science》1990,29(4):397-404

Ca²⁺ homeostasis is one of the major regulatory mechanisms operating in the nervous system, with calmodulin translating the Ca²⁺ message into cellular response. To check if hexachlorocyclohexane (HCH) acts as a calmodulin antagonist in the nervous system of rats, the in-vitro effect of HCH on calmodulin-dependent Ca²⁺-ATPase and cAMP-phosphodiesterase (PDE) in rat brain has been studied. In the membrane fraction from rat brain, a basal activity of Ca²⁺-ATPase was obtained in the absence of Ca²⁺. Inclusion of Ca²⁺ (1 mM) increased the enzyme activity by 70%. Further, addition of fluphenazine, a potent calmodulin antagonist, inhibited the Ca²⁺-dependent enzyme activity (IC₅₀ = 85 μM), demonstrating the calmodulin dependence of the enzyme activity. The Ca²⁺- and calmodulin-dependent Ca²⁺-ATPase was inhibited by HCH in a dose-dependent manner (IC₅₀ = 80–90 μM). Ca²⁺- and calmodulin-dependent cAMP-PDE from the cytosolic fraction of rat brain was inhibited by HCH (340 μM) by 79%. Addition of excess calmodulin reversed the inhibitory effects of HCH or fluphenazine on Ca²⁺-ATPase and cAMP-PDE, suggesting their direct interaction with calmodulin. By fluorescence interaction studies it has been shown that HCH interacts directly with calmodulin. These studies show that HCH may modulate the intracellular concentration of Ca²⁺ and cAMP, by decreasing the effectiveness of calmodulin towards its effector enzymes, resulting in an altered signal transduction in the nervous system.  相似文献   

Effects of glyphosate on uptake,translocation, and intracellular localization of metal cations in soybean (Glycine max) seedlings     

Stephen O. Duke  Kevin C. Vaughn  R.Don Wauchope 《Pesticide biochemistry and physiology》1985,24(3):384-394

Root-fed or foliar-applied glyphosate [N-(phosphonomethyl) glycine] reduced uptake and translocation of Ca²⁺ and Mg²⁺, but not K⁺, by soybean [Glycine max (L.) Merr. “Hill”] seedlings as measured by atomic absorption spectrometry. Histochemical techniques revealed that cells of secondary roots that were formed after glyphosate treatment were deficient in Ca²⁺. The relative distribution of Ca²⁺ in control root and leaf cells was mitochondria > plastids > cytoplasm. Glyphosate severely reduced Ca²⁺ content and eliminated intracellular concentration of Ca²⁺ in the mitochondria of both root and leaf cells. Glyphosate had no effects on K⁺ distribution at the ultrastructural level. These results support the view that glyphosate effects on distribution of divalent metal cations may be related directly or indirectly to the phytotoxicity of the herbicide.  相似文献   

The sensitivity of mitochondrial Mg2+ ATPase to DDT and analogs at different temperatures     

E.Y. Cheng  L.K. Cutkomp 《Pesticide biochemistry and physiology》1977,7(4):360-366

Oligomycin-sensitive (O-S) Mg²⁺ ATPase from American cockroach muscle was more sensitive to DDT, TDE, methoxychlor, and DDE at cool temperatures than at warm temperature, thus showing a negative temperature effect. In contrast, inhibition by acaricides dicofol, chlorfenethol, and Plictran shows a positive temperature effect. Oxidative phosphorylation in a mitochondrial preparation from cockroach coxal muscle was reduced by DDT, but the reduction was greater at a higher temperature (32°C) than at a cooler temperature (22°C). In addition, Na⁺K⁺ ATPase from cockroach nerve cord showed a positive temperature effect with DDT. The inhibition by DDT was much less on Na⁺K⁺ ATPase than on O-S Mg²⁺ ATPase. The negative temperature effect by DDT and analogs on O-S Mg²⁺ ATPase parallels toxicity effects on insects and fish as reported by numerous researchers. The results provide further evidence for this energy-regulating enzyme being a critical component in the biological action of DDT.  相似文献   

Single and simultaneous exposure of acetylcholinesterase to diazinon, chlorpyrifos and their photodegradation products     

Mirjana B. ?olovi?Danijela Z. Krsti?  Gordana S. Uš?umli?Vesna M. Vasi? 《Pesticide biochemistry and physiology》2011,100(1):16-22

In vitro inhibition of electric eel acetylcholinesterase (AChE) by single and simultaneous exposure to organophosphorus insecticides diazinon and chlorpyrifos, and their transformation products, formed due to photoinduced degradation, was investigated. Increasing concentrations of diazinon, chlorpyrifos and their oxidation products, diazoxon and chlorpyrifos-oxon, inhibited AChE in a concentration-dependent manner. IC₅₀ (20 min) values, obtained from the inhibition curves, were (in mol/l): (5.1 ± 0.3) × 10⁻⁸, (4.3 ± 0.2) × 10⁻⁶ and (3.0 ± 0.1) × 10⁻⁸ for diazoxon, chlorpyrifos and chlorpyrifos-oxon, respectively, while maximal diazinon concentration was lower than its IC₅₀ (20 min). Calculated K_I values, in mol/l, of 7.9 × 10⁻⁷, 9.6 × 10⁻⁶ and 4.3 × 10⁻⁷ were obtained for diazoxon, chlorpyrifos and chlorpyrifos-oxon, respectively. However, 2-isopropyl-4-methyl-6-pyrimidinol (IMP) and 3,5,6-trichloro-2-pyridinol, diazinon and chlorpyrifos hydrolysis products, did not noticeably affect the enzyme activity at all investigated concentrations. Additive inhibition effect was achieved for lower concentrations of the inhibitors (diazinon/diazoxon ?1 × 10⁻⁴/1 × 10⁻⁸ mol/l i.e., chlorpyrifos/chlorpyrifos-oxon ?2 × 10⁻⁶/3 × 10⁻⁸ mol/l), while an antagonistic effect was obtained for all higher concentrations of the organophosphates. Inhibitory power of 1 × 10⁻⁴ mol/l diazinon irradiated samples can be attributed mostly to the formation of diazoxon, while the presence of non-inhibiting photodegradation product IMP did not affect diazinon and diazoxon inhibitory efficiencies.  相似文献   

Nitroreductases in the Madagascar cockroach,Gromphadorhina portentosa     

H.A. Rose  R.G. Young 《Pesticide biochemistry and physiology》1973,3(3):243-252

Nitrobenzene reduction by tissue preparations of the Madagascar cockroach, Grompphadorhina portentosa, was studied in vitro. Active enzyme preparations were obtained from midgut, hindgut, fat body, and Malpighian tubules. Anaerobic conditions were essential for activity which was found in all subcellular fractions tested. The microsomal enzymes were strongly NADPH-dependent whereas the soluble enzymes were strongly NADH-dependent. Flavin addition stimulated activity greatly and it appeared that the true substrate for the nitroreductases was FMN and that nitrobenzene was nonenzymatically reduced by FMH₂.  相似文献   

Effects of dp-B on ATPase activity of insect plasma membrane     

Gao Ping  Liu Yanping  Liu Shigui 《Pesticide biochemistry and physiology》2004,80(3):133-162

Inhibition of ATPase from aphid plasma membrane, sarcoplasmic reticulum (SR), and brain synaptosomal plasma membrane of locust, by 1,5-diphenyl-2-penten-1-one (dp-B), was studied. Results demonstrated that dp-B exhibited the similar effects on ATPase found in the three membranes amongst which the plasma membrane Ca²⁺–Mg²⁺-ATPase is the primary target. The effects of dp-B on Ca²⁺–Mg²⁺-ATPase activity were bi-directional: the enzyme enhanced hydrolyzation when dp-B or Ca²⁺ concentrations were low but inhibited significantly when at high concentrations. The inhibition of Ca²⁺–Mg²⁺-ATPase by dp-B from brain synaptosomal plasma membrane of insect is higher than that from other organizational plasma membranes of the insect. Dp-B inhibiting Ca²⁺- and CaM-requiring ATPase activity may be an important mechanism by which the insect gets poisoned (for example aphid).  相似文献   

Metabolism of cisanilide (Cis-2,5-dimethyl-1-pyrrolidinecarboxanilide) by rat liver microsomes     

D.Stuart Frear  Harley R. Swanson 《Pesticide biochemistry and physiology》1976,6(1):52-57

Metabolism of [phenyl-¹⁴C] and [(2,5) pyrrolidine-¹⁴C] cisanilide was investigated in vitro with microsomal preparations from rat liver. Microsomal activity was associated with a mixed-function oxidase system that required O₂ and NADPH and was inhibited by CO. Two major ether-soluble metabolites were isolated. They were identified as primary oxidation products: 2-hydroxy-2,5-dimethyl-1-pyrrolidinecarboxanilide (A) and 4′-hydroxy-2,5-dimethyl-1-pyrrolidinecarboxanilide (B). Minor ether-soluble metabolites were also isolated. Precursor product studies and qualitative thin layer chromatography analysis of [pyrrolidine-¹⁴C] and methylated [phenyl-¹⁴C] hydrolysis products suggested that these metabolites were secondary oxidation products formed from metabolites A or B. One of these metabolites appeared to be the dihydroxy product 2,4′-dihydroxy-2,5-dimethyl-1-pyrrolidinecarboxanilide. Crude microsomal preparations (postmitochondrial supernatant fractions) also formed small quantities (<10%) of polar metabolites. Enzyme hydrolysis with β-glucuronidase (Escherichia coli) indicated that approximately 50% of these metabolites were glucuronides. Similarities and differences in cisanilide oxidation in vivo in plants and in vitro with rat liver microsomal preparations were discussed.  相似文献   

The role of tyrosinase in the inactivation of house fly microsomal mixed-function oxidases     

Daune L. Crankshaw  Matthew Zabik  Steven D. Aust 《Pesticide biochemistry and physiology》1977,7(6):564-572

The low mixed-function oxidase activity of house fly microsomes has been associated with low cytochrome P-450 content and NADPH-cytochrome c reductase activity. The microsomal cytochrome P-450 content and NADPH-cytochrome c reductase activity could be decreased by the addition of catechol and increased by the addition of cyanide to the homogenates. Similar results were obtained with rat liver microsomes treated with tyrosinase and catechol. During the inactivation of rat liver microsomal enzymes by tyrosinase and catechol, crosslinking of microsomal proteins occurred. These results suggest that the instability of house fly microsomal mixed-function oxidase may be due in part to the action of contaminating tyrosinase on endogenous substrates.  相似文献   

A comparison of DDT and its biodegradable analogues tested on ATPase enzymes in cockroach     

D. Desaiah  L.K. Cutkomp  R.B. Koch 《Pesticide biochemistry and physiology》1974,4(2):232-238

Analogues of DDT (ethoxymethyl and methoxymethio derivatives) compared with DDT for their inhibitory action on the ATPase system from tissues of the cockroach, Periplaneta americana show similar, but less inhibitory effects. The mitochondrial (oligomycin-sensitive) Mg²⁺ ATPase activity from coxal muscle preparations was more sensitive to DDT than the two analogues; whereas, the muscle and nerve cord homogenates showed about equal sensitivity to the biodegradable analogues. The mitochondrial Mg²⁺ ATPase from nerve cord preparation was more sensitive to the three compounds than the Na⁺K⁺ ATPase activity. The significance of these results in relation to recent reports on the effect of DDT on Na⁺K⁺ ATPase is discussed.  相似文献   

The in vivo sensitivity of ATPases to DDT,DDE, and physical immobilization in American cockroaches     

L.K. Cutkomp  D. Desaiah  E.Y. Cheng  E.V. Vea  R.B. Koch 《Pesticide biochemistry and physiology》1976,6(3):203-208

American cockroaches injected with sublethal doses of DDT (0.75 μg/roach) at 5-day intervals showed a 40% reduction in oligomycin-sensitive Mg²⁺ATPase from muscle homogenates, and a 23% reduction of Na⁺-K⁺ATPase from nerve cords. Thus, the maximum effect measured occurred with the same enzyme and tissue as determined from in vitro studies. The metabolite, DDE, used at 15 μg per roach, gave no significant change in activity of the ATPase system following injection. In contrast, high single doses of DDT (7.5 μg/roach) and 100 μg DDE and dicofol per roach caused over 30% increase in oligomycin-sensitive Mg²⁺ATPase of muscle and a 10–15% increase in Na⁺-K⁺ATPase of nerve cords measured 24 and 48 hr later. While a similar response was observed for Mg²⁺ATPase activities in cockroaches that were immobilized, the increase in enzyme activities were much greater than that caused by the pesticides.  相似文献   

Structural Effects of N-Arylcarbamoylpyrazolines on Calcium Uptake in Rat Brain Synaptosomes     

Riaz Hasan  Keiichiro Nishimura  Yoshiaki Nakagawa  Norio Kurihara  Tamio Ueno 《Pest management science》1996,46(3):221-225

N-Arylcarbamoylpyrazolines with various substituents at the para position of the carbamoyl benzene ring inhibited ATP-dependent Ca²⁺-uptake in synaptosomes prepared from the rat brain. The activity of these compounds was evaluated as log(1/I₅₀), the reciprocal logarithm of half inhibitory concentration, I₅₀ (m ), from the concentration–response curve for the inhibition of Ca²⁺-uptake. Among the compounds tested, methyl 3-(4-chlorophenyl)-4-methyl-1-[N-(4-trifluoromethylphenyl)carbamoyl]-2-pyrazoline-4-carboxylate was the most potent, the I₅₀ value of which as 9·12×10⁻⁷ m . Variations in the activity in terms of log(1/I₅₀) were quantitatively analysed using a substituent parameter, showing that the higher the electron-withdrawing effect of the substituent, the higher was the activity. The substituent effects were similar to those on insecticidal activity against the Americal cockroach. The higher the inhibitory activity against Ca²⁺ uptake, the higher seemed to be the insecticidal activity. Methyl(4S) - 3 - (4 - chlorophenyl) - 4 - methyl - 1 - [N - (4 - chlorophenyl)carbamoyl] - 2 - pyrazoline -4-carboxylate had higher inhibitory activity against Ca²⁺-uptake and higher in-secticidal activity than the R-isomer, but the difference was greater in theCa²⁺-uptake system.  相似文献   

Phenyltin compounds inhibit digestive enzymes of Tribolium confusum larvae     

Isaac Ishaaya  John E. Casida 《Pesticide biochemistry and physiology》1975,5(4):350-358

The potency of dietary phenyltin compounds in inhibiting the growth of first and fourth instar Tribolium confusum L. larvae and the gut proteolytic activity of fourth instar larvae decreases in the order of triphenyltin chloride (Ph₃SnCl) ? diphenyltin dichloride (Ph₂SnCl₂) ? phenyltin trichloride or tetraphenyltin. The growth retardation, which prolongs the larval stage without affecting pupation or emergence, may result from an antifeeding effect involving gut protease inhibition by Ph₃Sn⁺ and Ph₂Sn²⁺. Gut amylase and invertase activities are less sensitive than the protease activity to in vivo inhibition. Under in vitro conditions, relatively high concentrations of Ph₃SnCl and Ph₂SnCl₂ are required for inhibition, the order of enzyme sensitivity is protease > amylase > invertase, and Ph₂SnCl₂ is more potent than Ph₃SnCl. Proteins such as casein, albumin and hemoglobin, but not carbohydrates such as starch and sucrose bind Ph₃Sn⁺ so it is inaccessible for inhibition of digestive enzymes. The level of Ph₃Sn⁺ inhibiting gut protease in vivo is far below that necessary for in vitro inhibition of this enzyme activity. It is speculated that the in vivo inhibitory effects of Ph₃Sn⁺ and Ph₂Sn²⁺ on digestive enzymes may result from binding to the enzyme protein, its zymogen or to other proteins involved in production of the digestive enzymes.  相似文献   

Oxidation of pesticides by purified microsomal FAD-containing monooxygenase from mouse and pig liver     

Barbara P. Smyser  Patrick J. Sabourin  Ernest Hodgson 《Pesticide biochemistry and physiology》1985,24(3):368-374

The ability of purified microsomal FAD-containing monooxygenase from mouse and pig liver to oxidize pesticides has been investigated. The kinetic constants, K_m and V_max, were determined for a number of pesticide substrates including thioether-containing organophosphorus compounds and carbamates as well as (di)alkyldithiocarbamates. In general, the mouse liver enzyme had K_m values higher than those of the pig liver enzyme. Values for V_max were similar regardless of substrate, although the V_max typical of the mouse liver enzyme was approximately twice that of the pig liver enzyme. The thioether-containing organophosphorus compounds were the best substrates for both enzymes followed by the thioether-containing carbamates. The (di)alkyldithiocarbamates were relatively poor substrates for both pig and mouse liver microsomal FAD-containing monooxygenases.  相似文献   

Alterations of offspring heart muscle electrical activity transferred by rat male genitors chronically treated with lindane (γ-hexachlorocyclohexane) trace concentrations     

Martin-Pierre Sauviat  Gaston Godeau 《Pesticide biochemistry and physiology》2007,87(2):131-137

Using intracellular microelectrodes, we studied transmembrane resting and action potentials (AP) of left ventricle papillary muscles isolated from the heart of adult lindane-treated (TMG) and untreated (UMG) male genitor rat offspring, obtained by mating untreated female with males chronically treated and untreated with lindane (2 ppb) trace concentrations through beverage. The AP magnitude and duration (APD) were similar in both groups and their response to low temperature (22 °C) unchanged. Lowering the external Ca²⁺ concentration from 2.5 to 0.625 mM prolonged APD in the TMG group but not in the UMG group. In the TMG group, (i) cumulative addition of Sr²⁺ (1 mM) to the physiological solution prolonged APD; (ii) apamin (4 μM) and charybdotoxin (4 μM) prolonged the APD. In conclusion, our data revealed that an altered sensitivity of the Ca²⁺-induced Ca²⁺ inactivation of L-type Ca²⁺ channels and of Ca²⁺-activated K⁺ channels to Ca²⁺ has been transferred to TMG offspring.  相似文献   

Effect of liver enzyme induction on paraoxon metabolism in the rat     

Te-Yeh Ku  Paul A. Dahm 《Pesticide biochemistry and physiology》1973,3(2):175-188

Orally administered [1-¹⁴C]ethyl paraoxon, O,O-diethyl-O-p-nitrophenyl phosphate, is readily absorbed from the gastrointestinal tract of male albino rats. Radioactivity is essentially eliminated in 72 hr by excretion into urine and feces and by expiration as ¹⁴CO₂. Compounds with radioactivity in the urine are tentatively identified as diethyl phosphoric acid, desethyl paraoxon, ethanol, metabolites conjugated with amino acids, and paraoxon; the first compound is the predominant radioactive metabolite. Intraperitoneally injected phenobarbital, DDT, dieldrin, and endrin are inducers of microsomal enzymes that degrade paraoxon. The aryl phosphate-cleaving activity in vitro is not dependent on the addition of NADPH. O-Dealkylation of paraoxon is catalyzed by microsomal enzymes that require NADPH and oxygen and are inhibited by carbon monoxide. Microsomal enzymes from rats pretreated with enzyme inducers give an increased rate of O-dealkylation of paraoxon. Reduced glutathione has little or no effect on paraoxon degradation by either microsomal or soluble enzymes. Actinomycin D inhibits O-dealkylation of paraoxon in vivo, as indicated by reduction of ¹⁴CO₂ formation, and in vitro, as indicated by decreased activity of microsomal O-dealkylase. The role of microsomal mixed-function oxidases and NADPH-dependent O-dealkylase in the metabolism of organophosphorus insecticides is discussed.  相似文献   

Sulfur oxyacid production as a consequence of parathion desulfuration     

M. A. Morelli  T. Nakatsugawa 《Pesticide biochemistry and physiology》1979,10(3):243-250

Parathion desulfuration in vitro by the rat liver microsomal oxidase system gives rise to reactive sulfur atoms which either covalently bind to microsomal macromolecules, most likely as hydrodisulfides (-SSH) or appear as water-soluble metabolites. The latter were tentatively identified as sulfate, thiosulfate, and a minor amount of sulfite. Production of sulfate was enhanced by glutathione. Moreover, glutathione and other thiols removed covalently bound sulfur from the microsomal membranes and partially restored activity to enzymes known to be inactivated during parathion metabolism. A semilogarithmic plot of sulfur removal with time indicated at least two populations of covalently bound sulfur differing in the stability of the hydrodisulfide bond or accessibility to thiol compounds. The significance of transient hydrodisulfide formation with regard to the production of sulfur oxyacids is discussed. Both macromolecular and low molecular weight endogenous sulfhy dryl-containing biochemicals may play a role in preventing sulfur binding in vivo since only low level sulfur binding in liver homogenates was observed after the in vivo administration of parathion.  相似文献   

农药混剂的选择毒性研究   总被引：1，自引：0，他引：1  

林浩  邹柏祥  姜家良  陈巧云 《植物保护学报》1980,7(2):123-132

稻瘟净或异稻瘟净与乐果或马拉松混用,对抗性黑尾叶蝉有明显的增效作用,对小白鼠急性口服毒性也有所增加。小白鼠口服稻瘟净或异稻瘟净后,鼠肝中水解乐果和N—甲基正己酰胺的羧酰胺酶活力明显下降;水解醋酸α-萘酯的羧酸酯酶活力也被抑制。羊肝微粒体的羧酰胺酶在体外分别被稻瘟净、异稻瘟净、磷酸三苯酯、磷酸三甲苯酯、苯硫磷、氧乐果和西维因强烈抑制,它们的I_(50)值为1.3×10~(-8)—4.0×10~(-5)克分子浓度。稻瘟净、异稻瘟净、磷酸三苯酯和西维因分别是羊肝羧酰胺酶和羧酸酯酶的竞争性抑制剂,它们的K_i值在4.8×10~(-8)—1.0×10~(-7)克分子浓度之间。这些结果表明稻瘟净、异稻瘟净等增加乐果和马拉松对哺乳动物的毒性的机制,可能主要是由于它们抑制了哺乳动物体内正常解毒乐果和马拉松的水解酶。文中讨论了这些农药混剂的选择毒性问题。  相似文献