Pharmacokinetics of Intravenous Fenvalerate in Cattle Treated Topically with a Low Dose of Piperonyl Butoxide

Experiments were conducted to identify pharmacokinetic interactions between topically applied piperonyl butoxide and intravenous fenvalerate in cattle (Angus steers). Intact fenvalerate in plasma was derivatized by condensation with acetone and measured by negative chemical ionization gas chromatography/mass spectrometry. Noncompartmental pharmacokinetic analyses indicated that the elimination-phase rate constant (β, 0·00069 (±0·00006) min^-1), mean residence time (172 (±14) min), systemic clearance (10·4 (±0·7) ml min^-1 kg^-1) or volume at steady state (1800 (±230) ml kg^-1) were not changed (P>0·05) after topical application of a low dose of piperonyl butoxide. These data indicate that topical application of a low dose of the metabolic synergist piperonyl butoxide would not be expected to modify the in-vivo disposition of fenvalerate in cattle. © of SCI.     

Disposition kinetics of cypermethrin and fenvalerate in black bengal lactating goats

Disposition kinetics of cypermethrin and fenvalerate were investigated in lactating black Bengal goats following single dose intravenous administration at 57 and 45 mg kg^?1 respectively. The maximum and minimum blood concentrations of cypermethrin were 18.49 (±3.17) and 0.06 (±0.002) μg ml^?1, while the corresponding values for fenvalerate were 14.58 (±2.37) and 0.04 (±0.005) μg ml^?1 respectively. Both cypermethrin and fenvalerate remained present in blood for 36 h. The mean t1/2β) and Vd_area values were 5.56 (±0.28) h and 10.38 (±2.20) litre kg^?1 for cypermethrin and 5.66 (±0.35) h and 11.31 (±2.20) litre kg^?1 respectively for fenvalerate. Both cypermethrin and fenvalerate persisted in goat milk for 36 h. The t1/2β) and AUC values of fenvalerate were 7.37 (±1.84) h and 122.38 (±11.65) μg h ml^?1 whilst the corresponding values for cypermethrin were 6.66 (±1.54) h and 99.48 (±7.81) μg h ml^?1 in milk respectively.     

Disposition kinetics,cytotoxicity and residues of fenvalerate in tissues following oral administration to goats

Disposition kinetics in goats of fenvalerate [(RS)-α-cyano-3-phenoxybenzyl (RS)-2-(4-chlorophenyl)-3-methylbutyrate] were studied after oral administration at 5 mg kg^?1. The insecticide persisted in blood for up to 48 h. The V_d(area), t_1/2(β), and t_1/2(Ka), of fenvalerate were 12.14 (±0.39) litre kg^?1, 12.25 (±0.25) h and 0.63 (±0.11)h, while the AUC and Cl_B values were respectively 7.35 (±0.39) μg h ml^?1 and 0.68 (±0.04) litre kg^?1 h^?1. The residues in tissues reached a peak four days after insecticide administration and then started to decline. Maximum residue was found in the adrenal gland, followed by liver, kidney and intestine. Both GOT and GPT activities in kidney tissue, but only GPT activities in liver tissue had decreased significantly 4, 8 and 22 days post-administration. The fenvalerate did not produce any significant effects on serum acetylcholinesterase, cholesterol or protein levels in goats. Histopathological examination showed fatty changes in the periphery of lobule, congestion in sinusoid, haemolysis in central vein, necrosis and periportal fibrosis around the central vein of liver, and necrosis in kidney of fenvalerate-treated goats.     

Toxico‐kinetics,recovery efficiency and microsomal changes following administration of deltamethrin to black Bengal goats

A study of the toxico‐kinetics, recovery percentage from different substrates, cytotoxicity and role of cytochrome P₄₅₀ and b₅ of liver microsome in the metabolism of deltamethrin were carried out in female black Bengal goat. The ALD₅₀ value of deltamethrin in goat by intravenous route lies between 0.2 and 0.6 mg kg^?1. Intravenous disposition kinetics using a dose of 0.2 mg kg^?1 showed that the maximum blood concentration of deltamethrin was recorded at 0.5 min, followed by rapid decline, and a minimum concentration was detected at 6 min after administration. The following values were obtained : Vd_area 0.148 (± 0.02) litre kg^?1; t_1/2 (α) 0.22 (± 0.02) min; t_1/2 (β) 2.17 (± 0.37) min; K_el 1.05 (± 0.24) min^?1; AUC 4.30(± 0.45) µg min ml^?1; Cl_B 0.05 (± 0.006) litre kg^?1 min^?1; T～B 1.93 (± 0.58); fc 0.40(± 0.05). After 10 min, liver retained the maximum residue, and heart, adrenal gland, kidney, spleen, fat and brain also held the insecticide; liver, fat, heart and spleen retained residue after 30 min, and bone, liver and fat retained residue after 60 min of intravenous administration. Oral absorption of deltamethrin was poor and inconsistent, and approximately 65% of administered dose was recovered from faeces and gastrointestinal contents. The excretion of deltamethrin through urine was meagre, and only 0.01 and 0.013% of the administered dose was recovered after 3 and 5 days of oral administration respectively. All the tissues retained the residue after 3 days; while fat, rumen, reticulum, omasum, abomasum, large and small intestine and bone retained the residue after 5 days of oral administration; and the percentage recoveries were 1.73 and 0.027 respectively. Deltamethrin reduced the level of cytochrome P₄₅₀ content of liver microsomal pellet of goat after 5 days of oral administration. Histopathological examination of liver, kidney, heart, spleen brain and lung sections of treated goats did not reveal any pathological changes. © 2001 Society of Chemical Industry     

Some physicochemical and environmental factors affecting transformation rates and sorption of the herbicide metamitron in soil

In addition to the molecular structure of a pesticide, environmental conditions may influence its persistence through their effect on the growth and activity of pesticide-degrading micro-organisms. As a result, transformation rates may decrease rapidly when a compound is leached into subsoil. Metamitron sorption isotherms were determined and incubation series were set up for a sandy loam soil, simulating single and combination effects that occur during transport of metamitron into subsoils. K_OC values increased with increasing depth from 185 to 700 litre kg⁻¹. A combination of conditions that are unfavourable for microbial activity, such as low temperature (5°C), low concentrations (0·5 mg kg⁻¹) and a large sorbed fraction (K_OC = 700) resulted in half-lives of over one year. Oxygen inhibition decreased the transformation rate of metamitron from 0·058 to 0·019 day⁻¹. In order of significance, the transformation of metamitron appears to be a function of temperature, oxygen availability and sorption to organic carbon. Increasing doses did not change transformation rates significantly, although different transformation pathways were observed.     

Pharmacokinetics of sulfluramid and its metabolite desethylsulfluramid after intravenous and intraruminal administration of sulfluramid to sheep

Pharmacokinetic properties and tissue residues of the insecticide sulfluramid (I) and its major metabolite desethylsulfluramid (II) were determined in healthy sheep after bolus intravenous (IV) administration (5 and 15 mg kg⁻¹; n = 10) and bolus intraruminal (IR) administration (100 and 400 mg kg⁻¹; n = 12) of I . Depression, lethargy, and dyspnea were noted for 4 h after the higher IV dose, but not after the other IV or IR doses. The time courses of the mean blood concentrations of I and II were best described by a two-compartment open model with rapid distribution and slow elimination phases. The blood-to-plasma concentration ratios for I and II were 1.43 (± 0.50) and 26.7 (± 9.41), respectively, suggesting binding of II to red blood cells. The T_1/2β values for I and II for the higher IV dose of I were 15.3 (± 4.68) h and 63.4 (± 4.75) h and for the higher IR dose of I , 31.5 (± 5.41) h and 74.9 (± 7.49) h, respectively. Bioavailability was 28.6 (± 2.96)% for the lower IR dose and 19.5 (± 0.99)% for the higher IR dose. C_max values for II were higher in female than male sheep after IR administration of I . Only II was found in tissue samples, with the highest concentration being in liver (9.4 (± 5.2) µg g⁻¹). © 1999 Society of Chemical Industry     

Aerobic Metabolism of Flupropacil in Sandy Loam Soil

The aerobic soil metabolism of [¹⁴C]flupropacil (isopropyl 2-chloro-5-(1,2,3,6-tetrahydro-3-methyl-2,6-dioxo-4-trifluoromethylpyrimidin-1-yl)benzoate) was determined in microbially active, sieved (2-mm) sandy loam soil with a soil moisture content of 75% at 1/3 bar. The soil was treated with [¹⁴C]flupropacil at 0·5 mg kg⁻¹ (twice the field use rate) and placed in incubation flasks connected to a series of traps (50 g litre⁻¹ NaOH, 0·5M H₂SO₄, ethylene glycol) and incubated at 25(±1)°C. Soil was sampled at 0, 3, 9, 20, 30, 48, 76, 120, 181 and 238 days of aerobic incubation. Volatiles were collected once every two weeks and on the day of soil sampling. Flupropacil metabolized with a half-life of 79 days under aerobic conditions. The major metabolite was flupropacil acid which accounted for up to 69·1% of the initially applied radioactivity at Day 238. Each of the two minor metabolites detected at the end of the study accounted for less than 0·5%. One of the minor metabolites was identified as C4242 acid (2-chloro-5-(1,2,3,6-tetrahydro-2,6-dioxo-4-trifluoromethylpyrimidin-1-yl)benzoic acid). Only a negligible portion (less than 0·3%) of the applied flupropacil was mineralized to [¹⁴C]carbon dioxide. Extractable radioactivity ranged from 78·9% to 95·5%, with bound residues accounting for 3·2%–23·4%. The material balance ranged from 91·6% to 104·4%.     

Leaching of Methyl Isothiocyanate in Plainfield Sand Chemigated with Metam-Sodium

Soil column studies were undertaken to investigate the influence of soil water content and irrigation on leaching, distribution and persistence of methyl isothiocyanate (MITC) in a sandy soil chemigated with the soil fumigant metam-sodium. No leaching was obtained from columns at low water content (0·042 or 0·074 cm³ cm⁻³). However, 8·4 (±2·8), 34·2 (±7·4) and 119·4 (±8·3) μg of MITC leached from columns at 0·105, 0·137 and 0·168 cm³ cm⁻³ water content, respectively. Increased leaching resulted from sprinkler application of 25-mm of water to columns at 0·137 cm³ cm⁻³ water content. Leaching of MITC constituted only a small fraction of the amount applied even in the worst case. Methyl isothiocyanate persisted in soil for 15 days at 2°C in varying amounts under the different water regimes. Relatively high amounts of MITC residues (8–12 mg kg⁻¹ soil) were detected in the top 25-cm layer of all the soil columns. Degradation was the major pathway of dissipation for the chemical despite the soil water regime.     

Presence of Muscarinic Acetylcholine Receptors in the Cattle Tick Boophilus microplus and in Epithelial Tissue Culture Cells of Chironomus tentans

A muscarinic acetylcholine receptor (mAChR) has been demonstrated and partially characterized in larvae of the cattle tick Boophilus microplus. Its properties are compared with mAChR from an epithelial cell line from the dipteran insect Chironomus tentans. Competition studies with cholinergic ligands of different specificity revealed the muscarinic nature of the cholinergic receptors investigated in both species. In homogenates from tick larvae, specific binding sites for [³H]quinuclidinyl benzilate (QNB) with high affinity (1·2±(0·13) nM ; B_max 22·5 pmol mg protein⁻¹) were detected that do not bind nicotinic compounds specifically. The estimated IC₅₀ values for nicotine, imidacloprid and α-bungarotoxin were all in the mM range. Additionally, with tick larvae, high-affinity nicotinic binding sites were detected with [³H]nicotine which could be displaced by high concentrations of imidacloprid or QNB. The estimated IC₅₀ values for nicotine, α-bungarotoxin, imidacloprid and QNB were 43(±8) nM , 0·8(±0·2) μM , 2·8(±0·6) μM and 78(±1·9) μM , respectively. With homogenates of the non-neuronal insect cell line from C. tentans, only high-affinity binding sites for [³H]QNB were found. Muscarinic antagonists selectively displaced [³H]quinuclidinyl benzilate (QNB) binding to tick larvae homogenates. The mAChR of B. microplus preferred pirenzepine (IC₅₀ 2·13(±1·02) μM ) among different subtype-specific mAChR antagonists (4-DAMP had IC₅₀ 49·9(±9·13) μM and methoctramine had IC₅₀ 121(±14·2) μM ) indicating a type of binding site similar to the vertebrate M1 mAChR subtype. The tick muscarinic receptor seems to be a G-protein-coupled receptor, as concluded from the 4·8-fold reduction in receptor affinity for binding of the muscarinic agonist oxotremorine M upon treatment with the non-hydrolysable GTP-analogue γ-S-GTP. Binding data for the agonists oxotremorine M (IC₅₀ 71·3(±19·6) μM ) and carbachol (IC₅₀ 253(±87·1) μM ) parallel the biological efficacy of these compounds, in that, while oxotremorine M showed some activity against ticks, carbachol was ineffective.     

防治桃小食心虫越冬幼虫的有效药剂及其降解动态

研究树下土表施药防治桃小食心虫越冬幼虫的取代药剂。用毒土法测定了分属4类的13种药剂对桃小食心虫越冬幼虫的触杀毒力,其结果以毒死蜱、三唑磷、高效氯氟氰菊酯、甲基对硫磷和辛硫磷毒力较高,LC_(90)值依次为18．38、22．48、35．95、47．63及49．57 mg·kg~(-1),甲氰菊酯、丙溴磷、阿维菌素、甲胺基阿维菌素、氰戊菊酯、马拉硫磷、丙硫克百威和丁硫克百威LC_(90)值处于77．11～205．86mg·kg~(-1)之间。用高效液相色谱法测定了毒力较高的毒死蜱、三唑磷、高效氯氟氰菊酯以及阿维菌素在土壤中的降解动态,半衰期分别为8．28、11．37、10．17及19．70天。欲达30天的有效控制期,按LC_(90)值计算,这4种药剂在土壤中的初施浓度应分别为226．36、139．90、278．03及346．81mg·kg~(-1)。从药剂毒力、降解速率、相同控制期所需剂量及应用成本综合评价,毒死蜱、三唑磷具有较高的应用价值。     

Residues of Mecoprop in Post-emergence-Treated Wheat and Oat

The dissipation of mecoprop in wheat (Triticum aestivum L.) and oat (Avena sativa L.) was monitored over a growing season following post-emergence application of the dimethylamine salt of mecoprop to each crop at 1·1 kg ha^?1. Residues of mecoprop, as its methyl ester, were determined gas chromatographically using electrolytic conductivity detection. Initial residues in wheat (119 (±20) mg kg^?1) and oat (95·3 (± 10·0) mg kg^?1) on the day of application (four-leaf stage of wheat and four- to five-leaf stage of oat) decreased to 0·1 to 0·2 mg kg^?1, respectively, within six weeks. Residues were non-detectable in the mature seed of both crops. Recoveries of mecoprop were in the order of 90% from the green tissue and seed of both crops fortified at 0·05 mg kg^?1.     

Laboratory Evaluation of the Novel Naturally Derived Compound Spinosad against Ceratitiscapitata

Laboratory studies were conducted to determine the effect of the naturally derived compound spinosad on Ceratitis capitata Wied. (Diptera, Tephritidae). The organophosphate fenthion was used as a standard. Direct dose-dependent mortality and reduced fecundity were observed in oral treatment of adults with spinosad. The LC₉₀ values 14 h and seven days after treatment were 19·50 and 0·49 mg litre⁻¹ respectively. Fenthion was less active (the LC₅₀ eight days after treatment was 1·17 mg litre⁻¹) and did not affect the fecundity of the fly. Adults were also very susceptible to spinosad and fenthion via residual contact. For spinosad, 100% mortality was recorded 48 h after treatment for a dose of 10 mg litre⁻¹. Spinosad was more effective than fenthion in suppressing larval development when neonate larvae were reared on treated diet supplemented with a range of concentrations from 0·02 to 0·83 mg kg⁻¹ diet. Last-instar larvae were much less susceptible to spinosad or fenthion when exposed via dipping or when they pupated in treated medium and both products had similar performance. A lack of ovicidal activity was observed in direct egg-treatments with spinosad but significant reductions from 1 mg litre⁻¹ onwards were recorded for fenthion.     

Degradation of [14C]Terbuthylazine and [14C]Atrazine in Laboratory Soil Microcosms

The degradation and formation of major chlorinated metabolites of terbuthylazine and atrazine in three soils (loamy clay, calcareous clay and high clay) were studied in laboratory experiments using molecules labelled with ¹⁴C on the s-triazine ring. Soil microcosms were treated with the equivalent of 1 kg ha^-1 of herbicide and incubated in the dark for 45 days at 20(±1)°C. The quantity of [¹⁴C]carbon dioxide evolved in the soils treated with atrazine was negligible and could not be attributed to mineralization of the parent molecule. The mineralization of terbuthylazine accounted for 0·9–1·2% of the initial radioactivity. In the soils studied, the extrapolated half-lives varied from 88 to 116 days for terbuthylazine and 66 to 105 days for atrazine, with no significant differences for the three soils and the two molecules. The deethyl metabolites of the two s-triazines and the deisopropyl-atrazine metabolite appeared during the incubation in the three soils. The completely dealkylated metabolite was not detected in any of the soils. After 45 days of incubation, the non-extractable soil residues for the high clay, loamy clay and calcareous clay soils represented for terbuthylazine, 33·5, 38·3 and 43·1% and for atrazine, 19·8, 20·8 and 22·3% of the initial radioactivity. © 1997 SCI.     

Binding Sites for Ca2+-Channel Effectors and Ryanodine in Periplaneta americana—Possible Targets for New Insecticides

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. K_D values of 0·95 nM (B_max=550 fmol mg⁻¹ protein) and 0·75 nM (B_max=213 fmol mg⁻¹ protein) were determined respectively. A lower-affinity binding site was identified in binding studies with verapamil (K_D=7·4 nM and B_max=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.     

诊断施肥综合法（DRIS）在渭北旱塬红富士 苹果营养诊断中的应用

本研究通过提前叶片采样时期,运用诊断施肥综合法(DRIS)对不同产量水平红富士苹果进行了叶片矿质营养诊断,以期为早期红富士苹果营养诊断与科学施肥提供依据.测定诊断结果表明,渭北旱塬红富士苹果叶片N、P、K、Ca、Mg、Cu、Fe、Mn、Zn的适宜值分别为26.04±3.50 g·kg-1、2.84+0.74 g·kg-1、15.05±4.08 g·kg-1、14.25±3.04 g·kg-1、3.15±0.73 g·kg-1、12.69±3.14 mg· kg-1、262.87±82.05 mg·kg-1、96.33±33.35 mg·kg-1、23.57±10.13 mg·kg-1.选择的DRIS诊断参数中,除N/Zn、Cu/P、P/Zn、Ca/Zn、Mg/Zn和Cu/Zn外,30种表示形式的变异系数均表现出低产组(＜ 25 kg·tree-1)大于高产组(＜25 kg·tree-1);高产组和低产组的养分不平衡指数(NII)分别为73和88.相对于高产组,低产组元素间关系更不平衡.总体而言,渭北旱塬区红富士苹果园除产量高于41.3kg· tree-需肥顺序排在第一位的元素为Cu外,其它均为P;需肥顺序排在第二位的元素高产为K,低产果园仅当产量低于10.2 kg·tree-1时为K,其余为Zn;而排在第三位的,高产均为Ca,低产均为Mg.     

Fate of chlorsulfuron in the environment. 1. Laboratory evaluations

The behaviour and fate of chlorsulfuron in aqueous and soil systems were examined in laboratory studies. Aqueous hydrolysis was pH-dependent and followed pseudo-first-order degradation kinetics at 25°C, with faster hydrolysis occurring at pH 5 (half-life 24 days) than at either pH 7 or 9 (half-lives >365 days). Degradation occurred primarily by cleavage of the sulfonylurea bridge to form the major metabolites chlorobenzenesulfonamide (2-chlorobenzenesulfonamide) and triazine amine (4-methoxy-6-methyl-1,3,5-triazin-2-amine). This route is a major degradation pathway in water and soil systems. Aqueous photolysis (corrected for hydrolysis) proceeded much more slowly (half-life 198 days) than aqueous hydrolysis and is not expected to contribute significantly to overall degradation. Hydrolysis in soil thin-layer plates exposed to light (half-life 80 days), however, progressed at a much faster rate than in dark controls (half life 130 days), which suggests that a mechanism other than direct photolysis may have been operative. An aerobic soil metabolism study (25°C) in a Keyport silt loam soil (pH 6·4, 2·8% OM) showed that degradation was rapid (half-life 20 days). Dissipation in an anaerobic sediment/water system (initial pH of water phase 6·7, final pH 7·4) progressed much more slowly (half-life >365 days) than in aerobic soil systems. Major degradation products in aerobic soil included the chlorobenzenesulfonamide and triazine amine as in the aqueous hydrolysis study. Neither of these degradation products exhibited phytotoxicity to a variety of crop and weed species in a glasshouse experiment, and both exhibited an acute toxicological profile similar to that of chlorsulfuron in a battery of standard tests. Demethylation of the 4-methoxy group on the triazine moiety and subsequent cleavage of the triazine ring is another pathway found in both aqueous solution and soils, though different bonds on the triazine amine appear to be cleaved in the two systems. Hydroxylation of the benzenesulfonamide moiety is a minor degradation pathway found in soils. Two soils amended with 0·1 and 1·0 mg kg^-1 chlorsulfuron showed slight stimulation of nitrification. The 1·0 mg kg^-1 concentration of chlorsulfuron resulted in minor stimulation and inhibition of ¹⁴C-cellulose and ¹⁴C-protein degradation, respectively, in the same soils. Batch equilibrium adsorption studies conducted on four soils showed that adsorption was low in this system (K_oc 13–54). Soil thin-layer chromatography of chlorsulfuron (R_f=0·55–0·86) and its major degradation products demonstrated that the chlorobenzenesulfonamide (R_f=0·34–0·68) had slightly less mobility and that the triazine amine (R_f=0·035–0·40) was much less mobile than chlorsulfuron. In an aged column leaching study, subsamples of a Fallsington sandy loam (pH_water 5·6, OM 1·4%) or a Flanagan silt loam (pH_water 6·4, OM 4·0%) were treated with chlorsulfuron, aged moist for 30 days in a glasshouse and then placed upon a prewet column of the same soil type prior to initiation of leaching. This treatment resulted in the retention of much more total radioactivity (including degradation products) than by a prewet column, where initiation of leaching began immediately after chlorsulfuron application, without aging (primarily chlorsulfuron parent). © 1998 SCI     

Organophosphorus and synergised synthetic pyrethroid insecticides as grain protectants for stored sorghum

A field experiment was carried out on bulk sorghum stored for 26 weeks in concrete silos in South Queensland. No natural infestation occurred. Laboratory bioassays of treated grain, in which malathion-resistant strains of insects were added to grain samples, indicated that all the treatments were generally effective. Deltamethrin (2mg kg⁻¹)+piperonyl butoxide (8mg kg⁻¹), fenitrothion (12mg kg⁻¹)+fenvalerate (1 mg kg⁻¹)+piperonyl butoxide (8mg kg⁻¹), and fenitrothion (12mg kg⁻¹)+phenothrin (2mg kg⁻¹)+piperonyl butoxide (8mg kg⁻¹) controlled typical malathion-resistant strains of Sitophilus oryzae (L.), Rhyzopertha dominica (F.), Tribolium castaneum (Herbst) and Ephestia cautella (Walker). Pirimiphos-methyl (6mg kg⁻¹)+permethrin (1mg kg⁻¹)+piperonyl butoxide (8mg kg⁻¹) allowed some survival of adults and progeny production by S. oryzae after 12 weeks, and by one strain of R. dominica throughout. Chemical assays established that the residues and rates of breakdown of these grain protectants on sorghum conformed to the general pattern on other cereal grains. Residues at the conclusion of the experiment were below the individual Maximum Residue Limits recommended by the Codex Alimentarius Commission.     

猕猴桃园和小麦—玉米轮作田两种土地利用方式对土壤养分状况的影响

为深入了解不同土地利用方式下土壤养分水平的差异及施肥和管理中存在的问题,选取陕西省周至县农耕区为研究区域,采用地统计分析和GIS相结合的方法,研究了猕猴桃园和小麦—玉米轮作田两种不同土地利用类型下土壤养分含量、养分相关性、空间变异特征及其分布格局。结果表明:猕猴桃园有机质、碱解氮、有效磷和速效钾4种养分含量分别为:(19.55±3.13)g·kg~(~(-1)),(80.58±14.69)mg·kg~(~(-1)),(23.37±6.09)mg·kg~(~(-1)),(102.79±12.74)mg·kg~(~(-1)),pH值为7.32±0.49;小麦—玉米农田有机质、碱解氮、有效磷和速效钾4种养分含量分别为:(19.43±2.63)g·kg~(~(-1)),(78.80±11.39)mg·kg~(~(-1)),(24.83±6.06)mg·kg~(~(-1)),(95.03±11.75)mg·kg~(~(-1)),pH值为7.41±0.58。猕猴桃园土壤有机质、碱解氮和速效钾含量均高于小麦—玉米农田,仅有效磷含量比小麦—玉米农田偏低。研究区主要养分要素的变异系数都处于10%~100%,属于中等空间变异性。在猕猴桃园中,有机质、碱解氮、有效磷、速效钾两两之间均呈极显著或显著正相关;在小麦—玉米农田,pH值与有机质表现出显著负相关。研究区土壤有效磷含量较为丰富,碱解氮含量处于中等偏高水平,有机质含量处于中等偏低水平,而速效钾含量总体缺乏。整体上猕猴桃园比小麦—玉米农田养分水平高,这主要与不同的田间管理和施肥状况有关。因此,今后应采取维持氮肥、控制磷肥、增加钾肥的措施,并十分重视有机肥的使用。此外,针对不同土地利用类型和土壤肥力状况进行分区培肥管理,普及科学施肥,提高肥料利用效率也是提升土壤肥力水平的重要措施。     

Effect of the ecdysone agonists,RH-2485 and tebufenozide,on the southwestern corn borer,Diatraea grandiosella

The effect of the ecdysone agonists RH-2485 (proposed name methoxyfenozide) and tebufenozide (RH-5992), was examined on eggs and larvae of the southwestern corn borer, Diatraea grandiosella Dyar. Both compounds exhibited a concentration-dependent ovicidal activity. More than 95% of eggs died when egg masses were dipped in solutions of 100 or 200 mg liter^-1 of either compound in acetone+distilled water (1+1 by volume). Although some eggs treated with 1 or 10 mg liter^-1 of the compounds hatched, the survival rate was low. Newly hatched larvae were fed for seven days on an artificial diet containing RH-2485 or tebufenozide. The LC₅₀ values were 0·049 mg kg^-1 for RH-2485 and 0·185 mg kg^-1 for tebufenozide, showing that RH-2485 was about four times more active than was tebufenozide. Although increasing the time of exposure to either compound decreased the LC₅₀ value significantly, the relative potency of RH-2485 versus tebufenozide was not changed. Newly ecdysed 4th-instar larvae fed with diets containing 0·125, 0·25 or 0·5 mg kg^-1 RH-2485 or tebufenozide ceased feeding approximately 8 h after exposure, indicating that larvae had prematurely entered a molting cycle. Larvae treated with RH-2485 ecdysed earlier and died more quickly than those treated with tebufenozide. Ingestion of sublethal concentrations of RH-2485 (0·005 and 0·01 mg kg^-1) or tebufenozide (0·03 and 0·06 mg kg^-1) retarded larval growth, and decreased pupal weight and adult emergence. Increasing exposure time to tebufenozide tended to increase the larval mortality, significantly retarded larval growth, and decreased the mean weights of male and female pupae and adult emergence. RH-2485 (0·125 and 0·25 mg kg^-1) and tebufenozide (0·25 and 0·5 mg kg^-1) were lethal to newly hatched larvae, even after diets containing these compounds were held for 20 days at 30°C under long days (16 h light: 8 h dark). Our results suggest that field trials to assess the potential of RH-2485 and tebufenozide to control D. grandiosella are warranted. © 1998 SCI     

Cholinesterase inhibition by methamidophos and its subsequent reactivation

Methamidophos (O,S-dimethylphosphoramidothioate, Monitor) is an organophosphorus, cholinesterase-inhibiting insecticide. The rate constant (k_i) for inhibiting rat plasma cholinesterase (ChE) was 1.57 ± 0.03 × 10³M^?1 min^?1, for rat erythrocyte ChE was 8.86 ± 1.10 × 10³M^?1 min^?1, and for rat brain ChE was 6.58 ± 0.42 M^?1 min^?1. Brain and plasma cholinesterases spontaneously recovered from over 90% inhibition at 30 min to 50% inhibition in 4 and 14 hr, respectively. Pralidoxime increased the rate of reactivation in vitro. In vivo, rats poisoned with methamidophos exhibited signs of cholinergic stimulation. The LD₅₀ of ip methamidophos in male rats was 15 ± 0.7 mg/kg. Pralidoxime (60 mg/kg) and atropine (10 mg/kg) given with the methamidophos increased the LD₅₀ to 52 ± 4.9 mg/kg and 60 ± 0.4 mg/kg, respectively. In rats given 12.5 mg methamidophos (an LD₂₀), ChE activity was depressed 95 ± 12.5% in plasma, 92 ± 0.6% in stomach, and 88 ± 1% in brain at 1 hr after injection. At 48 hr after injection ChE activity had returned to 60% or more of control values in each of the tissues. Administration of a single dose of 60 mg/kg of pralidoxime along with methamidophos did not increase ChE activities at the times and places it was measured.