Fate of prothiofos (O-2,4-dichlorophenyl O-ethyl S-propyl phosphorodithioate) in rats

The fate of prothiofos (O-2,4-dichlorophenyl O-ethyl S-propyl phosphorodithioate) were studied in male rats 1, 3, 8, 24, 48, and 120 hr after oral administration. In the determination of prothiofos by gas chromatography-mass spectrometry, pentadeuteroethoxy-labeled prothiofos was used as the internal standard and the carrier of residual prothiofos. Prothiofos was rapidly absorbed from the small intestine and had substantially disappeared from the gastrointestinal tract within 24 hr after dosing. The residual concentrations of prothiofos in all organs analyzed, reached a maximum at 3 hr after dosing, and then diminished exponentially. The major urinary metabolites were 2,4-dichlorophenol (21% of administered prothiofos), its conjugated substances (26%), O-2,4-dichlorophenyl O-ethyl hydrogen phosphorothioate (14%), and O-2,4-dichlorophenyl O-ethyl hydrogen phosphate (25%). While prothiofos was found in the feces (3.8%), prothiofos oxygen analog (prothiofos-oxon) was scarcely detected in any excreta. Results obtained with a single dosing of prothiofos-oxon indicated that the oxygen analog formed from prothiofos in vivo was rapidly degraded through cleavage of the PS bond and the liberation of 2,4-dichlorophenol. The low mammalian toxicity of prothiofos is probably due to depropylthiolation in the molecule.     

Inhibition of conversion of geranylgeranyl-chlorophyll to phytol-chlorophyll by S-ethyl dipropylthiocarbamate (EPTC)

The influence of EPTC (S-ethyl dipropylthiocarbamate) on the hydrogenation of geranylgeranylchlorophyll (GG-Chl) to phytol-Chl was studied during the greening (6-, 12-, 18-, 24-, and 48-hr incandescent light exposure) of etiolated wheat [Triticum aestivum (L.) cv “Stacy”] and sorghum [Sorghum bicolor (L.) Moench cv “G 522DR”] seedlings grown in nutrient solution containing ¹⁴C-labeled sodium acetate. Chloroplast pigment synthesis occurred and small quantities of GG-Chl were found in both Chl^?a and Chl^?b. When wheat seedlings were greened for 48 hr in an EPTC concentration series (1 nM to 100 μM), geranylgeraniol (GG) content increased from 11% (control) to 60% (100 μM EPTC) of the isoprenoid alcohol esterified to chlorophyllide a, but Chl-b contained ≤1% GG-Chl at all concentrations of EPTC. Sorghum seedlings greened for 48 hr in the same EPTC concentration series contained about 3% GG (control) while 100 and 40% GG esterified to chlorophyllide a and chlorophyllide b, respectively, after 48 hr exposure to 100 μM EPTC. Thus, EPTC prevented hydrogenation of GG-Chl to phytol-Chl on the Chl molecule more in sorghum than in wheat.     

Kinetic properties of the inhibition of juvenile hormone esterase by two trifluoromethylketones and O-ethyl,S-phenyl phosphoramidothioate

Some inhibition kinetic properties and in vivo inhibition of the plasma juvenile hormone esterase from the cabbage looper (Trichoplusia ni Hübner) by one phosphoramidothioate and two trifluoromethylketones were examined. O-ethyl,S-phenyl phosphoramidothioate was shown to react irreversibly with the enzyme in a time-dependent manner, and the inhibition reaction can be factored into a reversible step with a dissociation constant, K_d, of 4.55 × 10^?5M followed by a phosphorylation step with a rate constant, k₂, of 1.98 min^?1. The phosphorylated enzyme did not show spontaneous recovery after 48 hr of dialysis. On the other hand, the two trifluoromethylketones were shown to act as reversible inhibitors, as their inhibited enzyme was regenerated completely after dialysis. However, 1,1,1,-trifluoro-3-thiooctylpropan-2-one, in contrast to 1,1,1-trifluorotetradecan-2-one, showed progressive time-dependent inhibition, and its reaction with the enzyme followed characteristic bimolecular second-order kinetics with a rate constant, k_i, of 3.37 × 10⁷M^?1 min^?1. The in vivo inhibition data of topically treated larvae at equimolar amounts of the tested compounds indicated rapid penetration, and the stability of the inhibition was higher for the phosphoramidothioate than for the trifluoromethylketones. The relationship of the mechanism of inhibition and the in vivo inhibition of these compounds to the understanding of the interactions between juvenile hormone and juvenile hormone esterase is discussed.     

S-Ethyl dipropylthiocarbamate, N,N-Diallyl-2-chloroacetamide,and 2-chloroallyl diethyldithiocarbamate influence on sulfhydryl-dependent sucrose accumulation

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

Stereodependent bioactivation of R(+)-ethyl S-propyl methylphosphonothioate: Is the S-oxide the active metabolite?

R(+)-Ethyl S-propyl methylphosphonothioate is bioactivated both in vivo and when perfused through isolated liver to give a product which is much more active as an inhibitor of acetylcholinesterase than the parent compound. The bioactivation does not occur in hepatectomised animals. Acetylcholinesterase inhibited by the active metabolite is not reactivated by pyridine-2-aldoxime methanesulphonate (P2S), whereas enzyme inhibited by the parent compound and its S(?) enantiomer is reactivatable. Attempts to identify the active metabolite were unsuccessful and experiments to explore its stability were inconclusive. Extensive in vitro studies of the inhibition of acetylcholinesterase by the enantiomers of ethyl S-propyl methylphosphonothioate and ethyl S-diisopropylaminoethyl methylphosphonothioates and subsequent reactivation of the enzyme by P2S showed that (a) there are large differences between the rates of inhibition of the R and S enantiomers of both compounds, (b) reactivation profiles are critically dependent on reaction conditions, and (c) the reactivation profiles of the R and S enantiomers of the former compound are indistinguishable under all conditions whereas differences are observed under some conditions for the latter pair of enantiomers. The results are discussed in terms of the possibility that the S-oxide of R(+)-ethyl S-propyl methylphosphonothioate is the active metabolite and it is concluded that this is unlikely.     

生物柴油作为精喹禾灵乳油中二甲苯替代溶剂的应用初探

为评价不同来源生物柴油作为溶剂配制精喹禾灵乳油的效果,采用气相色谱法测定了几种生物柴油中脂肪酸甲酯的种类及含量,利用相应制备的5%精喹禾灵乳油进行了防治禾本科杂草的盆栽试验,同时比较了不同生物柴油对药剂稀释液表面张力、干燥时间和在叶片表面沉积量等药液物理性状的影响。结果表明,用不同脂肪酸甲酯含量的生物柴油均能够制备出合格的5%精喹禾灵乳油,并且利用生物柴油制备的乳油在使用剂量为有效成分2 g/hm2时防效略高于常规以二甲苯为溶剂配制的乳油, 5 g/hm2和20 g/hm2剂量下无显著差异;生物柴油配制乳油稀释液与二甲苯配制乳油稀释液的表面张力差异不显著,但前者的沉积量则明显提高50%左右,能提高稀释液在小麦叶片的渗透速率。上述结果初步表明,生物柴油作为精喹禾灵乳油的替代溶剂具有一定的可行性。     

不同小麦品种(系)对赤霉病的抗性和麦穗组织中DON毒素积累分析

 为明确不同小麦品种(系)对赤霉病的抗性和麦穗组织中DON毒素积累水平,培育和利用抗赤霉病和DON毒素积累的品种提供资源和依据,本研究采用单小花滴注接种法对河南省的106个小麦品种(系)抗赤霉病性进行鉴定分析,并用ELISA测定了病穗组织中DON毒素水平。结果表明不同小麦品种(系)对赤霉病的抗性有显著差异,106个小麦品种(系)中未发现抗病和中抗材料,中感品种(系)有华育198、郑麦103和春丰0021等14个,占13.2%;感病的有曌式2010-06、百农898和中麦63等92个,占86.8%。不同小麦品种(系)籽粒、颖壳和穗轴中DON毒素积累水平有显著差异,籽粒中DON毒素水平在(0.70~287.63)mg/kg之间,其中郑03876、豫保1号和中麦63 的DON毒素水平在2 mg/kg 以下,为抗毒素材料;其他的103个品种DON毒素水平大于2 mg/kg;颖壳和穗轴中的DON毒素水平在(51.03~392.87)mg/kg之间,普遍比籽粒中DON毒素含量高。籽粒中DON毒素水平与小麦品种(系)的平均病害严重度间呈极显著正相关。     

脱氧雪腐镰刀菌烯醇( DON) 在小麦籽粒中的积累分析

 镰刀菌产生的脱氧雪腐镰刀菌烯醇(deoxynivalenol,DON)污染小麦后对人畜具有较大的毒害作用。为明确DON毒素在小麦籽粒中的积累数量及其与镰刀菌菌株、接菌数量、小麦品种和病害严重度的关系,试验采用单花滴注方法在5个抗病性不同的小麦品种上分别接种9 个禾谷镰刀菌菌株,每个菌株接种1 × 106 、1 × 105 和1 × 104 个/ mL 3 个分生孢子浓度,并利用ELISA 法测定收获麦粒中DON 毒素含量。结果表明,麦粒中DON 毒素含量差异主要是由于不同禾谷镰刀菌菌株产生毒素能力不同所致。接种菌株8003、4020 的所有麦粒中DON 毒素含量均显著高于相同条件下接种其他7 个菌株的小麦。当接种产毒素能力强的菌株时,小麦抗病品种表现出在一定程度上降低DON 毒素积累的能力。不同接菌浓度对小麦赤霉病的发病程度和麦粒中DON 毒素含量有显著影响,在相同条件下,接菌浓度越高,病害严重度越高,DON 毒素含量也越高;反之,接菌浓度越低,病害严重度越低,DON 毒素含量也越低。     

Photometric determination of methyl parathion GSH S-methyl transferase

Two methods are described for the assay of the enzyme that transfers a methyl group from methyl parathion (O,O-dimethyl-O, p-nitrophenyl phosphorothionate) to glutathione. A colorimetric assay depends on the measurement of alkali-soluble, chloroform-insoluble aromatic nitro compounds in the reaction mixture and a more rapid and sensitive direct spectrophotometric assay is described that uses the double wavelength Perkin-Elmer 356 Spectrophotometer. The utility of both methods has been demonstrated by the measurement of some kinetic constants and the distribution of the enzyme among some insects and vertebrates.     

Contribution to the toxic action of S-methyl fenitrothion

The toxicity of the S-methyl isomer of fenitrothion was found to be higher than that of both fenitrothion and technical fenitrothion. Repeated administration of the compound showed a rapid decrease in toxicity with decreasing doses.Excretion of p-nitro-m-cresol into the urine of rats was more rapid and the excreted amounts were larger from a single dose of the isomer than from fenitrothion.Single doses of the isomer increased the pentobarbitone sleeping time in mice at both 24 and 48 hr, but showed no change after 4 days. Administration of the isomer and purified fenitrothion to mice for 1 week had no effect on the pentobarbitone sleeping time, nor did a single dose of fenitrothion change the effectiveness of pentobarbitone.Dominant lethal tests in rats revealed a possible mutagenic effect from this compound.The anticholinesterase activity of the fenitrothion S-methyl isomer in vitro was found to be two to three times higher than that of fenitrothion.     

单轴等效线法评价精喹禾灵与灭草松相互作用的研究

为正确评价单子叶杂草防除剂与双子叶杂草防除剂的相互作用,以精喹禾灵与灭草松混用为实例对等效线法进行了改进,提出单轴等效线法及其增效倍数的计算方法。该研究结果表明,两种药剂混用对马唐Digitaria sanguinalis和反枝苋Amaranthus retroflexs均有增效作用,其平均增效倍数分别为0.42和0.34。采用单轴等效线法可以正确评价单子叶杂草防除剂与双子叶杂草防除剂的相互作用。     

施肥对旱地农田生态系统冬小麦干物质积累的影响

研究了施肥对时地冬小麦总茎数、顺面积系数及干物质积累和经济产量的影响,并探讨了这些生长因素与经济产量之间的关系。结果表明,施肥使冬小麦分蘖增多,总茎数和每公顷成穗数增加;使各生育期叶面积系数及干物质积累量增大,特别使灌浆期保持较高数值。不同施肥水平下的物质积累过程均可用指数方程ｙ＝ａｅ＾ｂ／ｘ很好拟合,而且方程中的ａ值随施肥水平提高而增大,ｂ值基本。相关分析表明,冬前、灌浆阶段冬小麦生长状况对经济     

Induction of glutathione S-aryl transferase by phenobarbital in the house fly

Induction of glutathione S-aryl transferase by phenobarbital was studied with three stains of house flies which differed in basal levels of the enzyme. The enzyme was shown to be inducible in two of the three strains tested and the amount of induction was inversely proportional to the basal level of enzyme activity. In dose-dependency tests, a high dose of phenobarbital, 10,000 ppm, was needed to cause significant levels of induction. In a time study, 48 hr was found to be the time at which the highest levels of induction occur. Similarities of this system to house fly microsomal oxidases are discussed.     

Influence of wheat streak mosaic virus infection on phenylpropanoid metabolism and the accumulation of phenolics and lignin in wheat

Wheat plants infected with wheat streak mosaic virus were studied for their physiological response to infection. Previous histological data suggest that wheat streak mosaic virus-induced deposits of phenolic nature are present along the bundle sheath and mesophyll cell walls. In this study, we examined this phenomenon further by analysis of phenolic compounds and enzymes involved in their synthesis. In infected plants, the amounts of free and wall-bound phenolic compounds increased slightly, and chromatography showed that the type of free phenolic compounds present had changed. The amount of lignin did not change due to infection. Enzyme assays showed that while phenylalanine ammonia lyase and tyrosine ammonia lyase activities decreased as they do in healthy plants, cinnamyl alcohol dehydrogenase activity stayed high throughout infection. In addition, peroxidase activities in infected plants decreased around the time that the leaves ceased to expand. These results suggest that the general phenylpropanoid pathway is stimulated upon infection, but that lignification is not.     

黄淮麦区主栽小麦品种抗茎基腐病评价及茎秆和籽粒中毒素积累分析

为明确黄淮麦区主栽小麦品种对茎基腐病的抗性水平、不同抗性指标的相关性,以及茎杆和籽粒中镰刀菌毒素积累情况,在采用苗期茎基部滴注法和成株期混合播种法进行抗性鉴定的基础上,本研究还利用超高效液相色谱高分辨质谱联用技术,测定了小麦茎杆和籽粒中6种常见镰刀菌毒素的含量.结果表明,供试的20个小麦品种中,苗期抗病、中抗、感病和高...     

不同时期灌溉对冬小麦物质积累与分配的影响

从物质积累和分配的角度研究了灌溉高产的原因。结果表明：在底墒水充足时,雌雄蕊分化前期灌水,有利于开花前的物质积累;在籽粒形成期,随干旱程度的加剧,籽粒形成对花前贮存物质的调运量增加,开花前植株越繁茂并且花后水分亏缺越严重,物质的转运量越高。     

盐胁迫下己唑醇铜配合物对小麦幼苗脯氨酸合成的影响

以己唑醇为配体与醋酸铜配合获得元素组成异化的己唑醇铜配合物。配合物对小麦种子浸种处理,待萌发生长至幼苗阶段将其进行NaCl胁迫处理,通过对幼苗脯氨酸含量以及脯氨酸合成酶基因P5CS、P5CR表达变化的测定,评价己唑醇铜配合物对植物抗盐能力的影响。结果表明：小麦幼苗脯氨酸含量随着盐浓度的增大及胁迫时间的延长而增加,200 mmol·L^-1 NaCl胁迫下,配合物处理后脯氨酸含量最高,达55.44 μg·g^-1,相比己唑醇和醋酸铜处理分别增加13.68%和58.45%;而100 mmol·L^-1 NaCl处理6 h,己唑醇铜配合物处理小麦幼苗的脯氨酸合成增幅最大,P5CS、P5CR表达量明显增加,在一定程度上缓解了小麦幼苗的渗透胁迫伤害。     

三种微生物肥料对春小麦产量及养分累积量的影响

为了验证甘肃省农科院土壤肥料与节水农业研究所微生物研究室研制的三种微生物肥料(生物氮肥、生物磷肥、复合菌肥)的肥效,通过大田试验,对它们在春小麦上的应用效果进行研究,结果表明,生物氮肥在替代一半化学氮肥时,春小麦籽粒和生物产量高于同量化肥和载体配施处理11.77%和12.42%,同时穗粒数增加13.80%,穗长增加6.20%,养分累积量提高17.38%~25.37%,与全量化肥配施时对春小麦产量无明显影响,但是可以提高养分累积量4.78%~14.30%。生物磷肥和复合菌肥与半量和全量化肥配施时,对春小麦增产效果不明显,但是生物磷肥与半量化学磷肥配施时,可以提高春小麦养分累积量4.03%~6.04%,与全量化肥配施时只对全磷的累积具有促进作用,而复合菌肥对春小麦的养分累积无明显影响。说明在供试的三种微生物肥料中,生物氮肥对春小麦产量和养分累积具有较强的促进作用,而且与半量化肥配施要优于与全量化肥配施,而生物磷肥和复合菌肥在春小麦上的应用效果不佳。     

Evidence that DDT-dehydrochlorinase from the house fly is a glutathione S-transferase

DDT-dehydrochlorinase has been isolated in a highly purified form by a procedure involving affinity chromatography, gel-permeation chromatography, and preparative isoelectrofocusing. At least two protein species appeared to possess DDT-dehydrochlorinase activity; the principal one of these was purified by a factor of 660-fold. This appeared to be dimeric with subunits of molecular weight of 23,000 and 25,000. Another protein with this activity appeared to consist of two identical subunits of M_r 25,000. The protein with greatest activity was isoelectric at pH 7.1. It was found to be homogeneous on analytical gel electrophoresis in both the presence and absence of SDS. The same protein generated a number of minor protein bands on analytical electrofocusing in polyacrylamide gels, but there is evidence that these bands may be artifactual. Both purified forms of the enzyme possessed substantial glutathione S-transferase activity with both CDNB and DCNB. An acidic protein, a dimer of subunits of M_r 23,000 had substantial GSH transferase activity with CDNB as substrate, but had no DDT-dehydrochlorinase activity.     

施用磷肥对春小麦产量与吸氮特性及土体中硝态氮累积的影响

通过宁夏引黄灌区田间小区试验,研究施磷量分别为0、60、120、180 kg/hm2对春小麦产量、磷肥利用率、吸氮特性和土壤中硝态氮累积的不同影响,旨在明确该区合理施磷量.结果表明:合理施用磷肥(60～120 kg/hm2)能提高春小麦籽粒产量和生物量.当施磷量为120 kg/hm2,小麦籽粒产量最高,为6 215 kg/hm2.春小麦氮素累积动态呈先增加后降低的趋势,增施磷肥能增加小麦吸氮量,但到成熟期春小麦地上部氮素累积出现损失,损失量达7.7%～13.4%.当施磷量分别为60、120、180 kg/hm2时,0～150 cm土层中的NO3--N累积量分别比对照减少了50.6、58.5、62.9 kg/hm2.综合考虑磷肥利用率、小麦产量和降低土体中NO3--N残留等方面的因素,磷肥当季施用量应该控制在60～120 kg/hm2.