麦田新型除草剂砜吡草唑的除草活性

杂草严重影响小麦的丰产丰收,而使用除草剂是麦田杂草防除中最经济有效的手段。砜吡草唑是新型广谱、高活性的苗前土壤处理除草剂。明确砜吡草唑对麦田杂草的除草活性是该药剂在麦田应用的重要内容。本文采用温室盆栽法研究了其对麦田常见杂草的杀草谱及除草活性。研究结果表明:砜吡草唑土壤处理对麦田禾本科杂草鹅观草Roegneria kamoji、多花黑麦草Lolium multiflorum、雀麦Bromus japonicus、棒头草Polypogon fugax、蜡烛草Phleum paniculatum,阔叶杂草大巢菜Vicia sativa、播娘蒿Descurainia sophia、麦家公Lithospermum arvense、泽漆Euphorbia helioscopia具有良好的防除效果,但对节节麦Aegilops tauschii和野燕麦Avena fatua的防除效果略差。在推荐剂量180 g/hm^2下,对鹅观草、多花黑麦草、雀麦、棒头草、蜡烛草、大巢菜、播娘蒿、麦家公、泽漆的株抑制率和鲜重抑制率均可达到90%以上。而对节节麦和野燕麦的ED 90分别为209.54和886.43 g/hm^2,高于砜吡草唑的田间推荐剂量。砜吡草唑具有广泛的杀草谱及较高的除草活性,可作为小麦田杂草化学防除的重要候选药剂。     

嘧啶胺类杀菌剂的作用机制

本文介绍了几种嘧啶类杀菌新品种（ｐｙｒｉｍｎｅｔｈａｎｉｌ，嘧菌胺ｍｅｐａｎｉｐｙｒｉｍ，ｃｙｐｒｏｄｉｎｅｌ）的作用机制，该类药剂在离体条件下对病菌的抗菌性很弱，但用于寄主植物上却表现很好的防治效果，该类药剂能抑制病菌甲硫氨酸的生物合成和细胞壁降解酶的分泌，从而影响病菌侵入寄主植物。     

新型除草剂丙酯草醚的作用机理

采用常规的室内生测和生化方法,开展新型除草剂丙酯草醚的作用机理研究.试验结果表明:同时添加5mg/L浓度的三种支链氨基酸即缬氨酸、亮氨酸和异亮氨酸能完全恢复丙酯草醚对高粱茎的生长抑制作用,而添加相同浓度的单一支链氨基酸只能部分消除其抑制作用.离体条件下,丙酯草醚IC50＞100mg/L,而双草醚IC50值为10-5～10-4mg/L,说明丙酯草醚对离体ALS没有抑制作用;活体条件下,丙酯草醚对ALS有一定的抑制作用,且随着处理时间的延长,酶活力降低,对ALS的抑制作用增加.因此,丙酯草醚使植物体内必需的支链氨基酸合成受阻,仍然属于ALS抑制剂,但其作用方式不同于磺酰脲类和嘧啶水杨酸类除草剂等典型的ALS抑制剂,它类似于前体农药,即在植物体内通过代谢活化来发挥作用.     

Mechanism of action and selectivity of a novel herbicide,fenquinotrione

Fenquinotrione is a novel herbicide that can control a wide range of broadleaf and sedge weeds with excellent rice selectivity. We revealed that fenquinotrione potently inhibited the 4-hydroxyphenylpyruvate dioxygenase (HPPD) activity in Arabidopsis thaliana with an IC₅₀ of 44.7 nM. The docking study suggested that the 1,3-diketone moiety of fenquinotrione formed a bidentate interaction with Fe(II) at the active site. Furthermore, π–π stacking interactions occurred between the oxoquinoxaline ring and the conserved Phe409 and Phe452 rings, indicating that fenquinotrione competes with the substrate, similar to existing HPPD inhibitors. A more than 16-fold difference in the herbicidal activity of fenquinotrione in rice and the sedge, Schoenoplectus juncoides, was observed. However, fenquinotrione showed high inhibitory activity against rice HPPD. Comparative metabolism study suggested that the potent demethylating metabolism followed by glucose conjugation in rice was responsible for the selectivity of fenquinotrione.     

Chlorophyll fluorescence as a marker for herbicide mechanisms of action

Photosynthesis is the single most important source of O₂ and organic chemical energy necessary to support all non-autotrophic life forms. Plants compartmentalize this elaborate biochemical process within chloroplasts in order to safely harness the power of solar energy and convert it into usable chemical units. Stresses (biotic or abiotic) that challenge the integrity of the plant cell are likely to affect photosynthesis and alter chlorophyll fluorescence. A simple three-step assay was developed to test selected herbicides representative of the known herbicide mechanisms of action and a number of natural phytotoxins to determine their effect on photosynthesis as measured by chlorophyll fluorescence. The most active compounds were those interacting directly with photosynthesis (inhibitors of photosystem I and II), those inhibiting carotenoid synthesis, and those with mechanisms of action generating reactive oxygen species and lipid peroxidation (uncouplers and inhibitors of protoporphyrinogen oxidase). Other active compounds targeted lipids (very-long-chain fatty acid synthase and removal of cuticular waxes). Therefore, induced chlorophyll fluorescence is a good biomarker to help identify certain herbicide modes of action and their dependence on light for bioactivity.     

A novel genomic approach to herbicide and herbicide mode of action discovery

A herbicide with a new mode of action has not been commercialized for more than 30 years. A recent paper describes a novel genomic approach to herbicide and herbicide mode of action discovery. Analysis of a microbial gene cluster revealed that it encodes genes for both the biosynthetic pathway for production of the sesquiterpene aspterric acid and an aspterric acid‐resistant form of dihydroxy acid dehydratase (DHAD), its target enzyme. Aspterric acid is weak compared with commercial synthetic herbicides, and whether DHAD is a good herbicide target is unclear from this study. Nevertheless, this genomic approach provides a novel strategy for the discovery of herbicides with new modes action. © 2018 Society of Chemical Industry     

Plant cell membrane as a marker for light-dependent and light-independent herbicide mechanisms of action

Plant cells possess a number of membrane bound organelles that play important roles in compartmentalizing a large number of biochemical pathways and physiological functions that have potentially harmful intermediates or by-products. The plasma membrane is particularly important as it holds the entire cellular structure whole and is at the interface between the cell and its environment. Consequently, breaches in the integrity of the lipid bilayer, often via reactive oxygen species (ROS)-induced stress membrane peroxidation, result in uncontrolled electrolyte leakage and in cell death. A simple 3-step bioassay was developed to identify compounds that cause electrolyte leakage and to differentiate light-dependent mechanisms of action from those that work in darkness. Herbicides representative of all known modes of action (as well as several natural phytotoxins) were selected to survey their effects on membrane integrity of cucumber cotyledon discs. The most active compounds were those that are known to generate ROS such as the electron diverters and uncouplers (paraquat and dinoterb) and those that either were photodynamic (cercosporin) or caused the accumulation of photodynamic products (acifluorfen-methyl and sulfentrazone). Other active compounds targeted lipids (diclofop-methyl, triclosan and pelargonic acid) or formed pores in the plasma membrane (syringomycin). Herbicides that inhibit amino acid, protein, nucleotide, cell wall or microtubule synthesis did not have any effect. Therefore, it was concluded that the plant plasma membrane is a good biomarker to help identify certain herbicide modes of action and their dependence on light for bioactivity.     

Flufenacet herbicide treatment phenocopies the fiddlehead mutant in Arabidopsis thaliana

In order to study the mode of action of herbicides we conducted a pilot study analysing phenotype and gene expression of flufenacet- and benfuresate-treated Arabidopsis thaliana (L) Heynhoe plants. Treatments with either herbicide caused phenocopies of the known Arabidopsis mutant fiddlehead, displaying fused organs and the typical fiddlehead-like inflorescence. Herbicide treatments of other plant species, including monocots, also gave rise to analogous organ fusions, indicating the presence of the target in a broad range of plants. Furthermore, many other herbicides with a proposed similar mode of action, eg chloroacetanilides, produced comparable fusion phenotypes in plants. The fiddlehead gene encodes a putative very-long-chain fatty acid elongase (VLCFAE), which corroborates earlier biochemical results pointing to the inhibition of VLCFA synthesis as mode of action of flufenacet. Gene expression profiles of herbicide-treated plants using the first 8247 gene Arabidopsis gene array of Affymetrix provided additional clues in support of inhibition of VLCFA synthesis. We discuss fiddlehead-like elongases as plant specific targets for flufenacet and many other herbicides.     

On the mechanism of selectivity of the corn herbicide BAS 662H: a combination of the novel auxin transport inhibitor diflufenzopyr and the auxin herbicide dicamba

BAS 662H, a 1:2.5 combination of the semicarbazone-type auxin transport inhibitor diflufenzopyr and the auxin herbicide dicamba, is used as a post-emergence herbicide in corn. The combination has been observed to provide more effective broadleaf weed control and improved tolerance in corn than typical rates of dicamba used alone. In order to analyze this phenomenon, the uptake, translocation, metabolism and action of both compounds, applied alone and in combination, were investigated in Amaranthus retroflexus L, Galium aparine L and corn (Zea mays L). When plants at the third-leaf stage were foliarly treated with diflufenzopyr and dicamba equivalent to field rates of 100 and 250 gha-1, respectively, diflufenzopyr synergistically increased dicamba-induced 1-aminocyclopropane-1-carboxylic acid (ACC) synthase activity and ethylene formation in G aparine and even more in A retroflexus, followed by accumulations of (+)-abscisic acid (ABA) in the shoot tissue within 20 h. This correlated with subsequent growth inhibition, hydrogen peroxide overproduction and progressive tissue damage. Diflufenzopyr also enhanced the activity of other auxin herbicides, such as quinclorac and picloram, and of the synthetic auxin, 1-naphthaleneacetic acid. After foliar and root application of [14C]diflufenzopyr, alone or as BAS 662H, considerably lower tissue concentrations and systemic translocation of radioactivity beyond treated plant parts were found in corn, compared to G aparine and particularly A retroflexus. Furthermore, diflufenzopyr decreased foliar uptake of [14C]dicamba by c 50% selectively in corn, compared to the treatment alone. Metabolism of [14C]diflufenzopyr was more rapid in corn than in the weed species. In combination, the two compounds had no mutual effect on their metabolic degradation. In BAS 662H, diflufenzopyr synergizes the herbicidal activity of dicamba in sensitive weed species. In corn this effect is prevented by a more rapid metabolism of diflufenzopyr, coupled with lower uptake and translocation. Selectivity of BAS 662H is additionally favoured by a higher crop tolerance to dicamba because of reduced foliar uptake of this herbicide in corn under the influence of diflufenzopyr.     

Susceptibility of a broad-leaved weed, Acanthospermum hispidum, to the grass herbicide fluazifop-butyl

Broad-leaved plants are generally resistant to aryloxyphenoxypropionate (AOPP) and cyclohexanedione (CHD) herbicides. In laboratory experiments, however, we confirmed that Acanthospermum hispidum , a Compositae weed, was susceptible to one of the AOPP herbicides, fluazifop-butyl, but tolerant to other AOPP herbicides (quizalofop-ethyl and fenoxaprop-ethyl) and a CHD herbicide (sethoxydim). The symptoms induced by fluazifop-butyl in A. hispidum (wilting and necrosis) were distinctly different from those induced in oat (chlorosis). The period required to cause seedling death of A. hispidum (48–72 h) was shorter than that of oat ( ca 15 days). The ( R )-enantiomer of fluazifop-butyl was more active on this weed. In oat, lipid biosynthesis and acetyl-CoA carboxylase (ACCase) activity were inhibited, and electrolyte leakage from the shoots was increased by fluazifop-butyl and sethoxydim. In the case of A. hispidum , the membrane permeability increased and the lipid biosynthesis was inhibited only by fluazifop-butyl. These results indicate that A. hispidum is particularly sensitive to fluazifop-butyl, and its mechanism of action in the plant may be different from its mechanism of action in oat.     

新型化合物唑嘧氯草胺的作用机制

采用培养皿法和常规生化方法,研究了新型除草剂唑嘧氯草胺(暂定名,代号:ZJ-2725)的作用机制。结果显示,同时添加20mg/L浓度的缬氨酸、亮氨酸和异亮氨酸能完全恢复唑嘧氯草胺对苘麻芽的生长抑制作用,而添加相同浓度的单一支链氨基酸只能部分消除其抑制作用。离体条件下,随着唑嘧氯草胺浓度的增大,对乙酰乳酸合成酶(ALS)活性的抑制率增加,ALS活性随反应时间的延长而增加,且两者之间符合Michaelis-Meten方程;活体条件下,唑嘧氯草胺对苘麻的ALS也表现出明显的抑制作用,ALS活性明显下降。表明唑嘧氯草胺在植物体内抑制了3种支链氨基酸的生物合成,进而导致植物蛋白质合成受阻而使植物生长受到抑制,ALS即为唑嘧氯草胺的作用靶标。     

Anthranilic diamides: A new class of insecticides with a novel mode of action, ryanodine receptor activation

Development of insecticides with unique modes of action is necessary to combat widespread insecticide resistance. A new class of insecticides has been discovered, the anthranilic diamides, that provides exceptional control through action on a novel target, the ryanodine receptor. Anthranilic diamides potently activate this receptor, releasing stored calcium from the sarcoendoplasmic reticulum causing impaired regulation of muscle contraction. Expression of a recombinant Drosophila ryanodine receptor in a lepidopteran cell line confers sensitivity to anthranilic diamides similar to that observed with native receptors. Ligand-binding studies with radiolabeled ryanodine and radiolabeled anthranilic diamide in Periplaneta americana reveal a single, saturable binding site for this chemistry distinct from that of ryanodine. Further, calcium mobilization studies using mammalian cell lines indicate anthranilic diamides exhibit >500-fold differential selectivity toward insect, over mammalian, receptors. Consequently, anthranilic diamides offer a novel pharmacological tool for calcium signaling research in addition to a unique alternative to existing pest-management strategies.     

Nematocidal quassinoids and bicyclophosphorothionates: a possible common mode of action on the GABA receptor

The present study was undertaken to identify noncompetitive γ-aminobutyric acid receptor (GABAR) antagonists that are effective in nematodes, as well as to examine the hypothesis that the noncompetitive antagonism of the GABAR underlies the nematocidal activity of quassinoids against free-living nematodes of the Diplogastridae family. First, 14 known GABAR antagonists were screened for the effectiveness of their nematocidal activity in Diplogastridae. As a result, 3-isopropyl-1-phospha-2,6,7-trioxabicyclo[2.2.2]octane 1-sulfides (3-isopropyl-BPTs) were found to have high nematocidal activities, and 4-cyclohexyl-3-isopropyl-BPT (23) and 3-isopropyl-4-(2-propenyl)-BPT (27) were the two most potent analogues; these compounds are equipotent to samaderine B and more potent than the anthelmintic abamectin. 23-resistant nematodes, selected by challenge with 23, showed cross-resistance to samaderine B. 23 (10 μM) reduced [³H]23 binding to nematode membranes by 30.4%. Samaderine B (10 μM) resulted in a similar level of the inhibition, but had neither additive nor synergistic effects on the 23 inhibition of [³H]23 binding. These findings suggest that samaderine B shares a common binding site with the GABAR antagonist 23 in Diplogastridae. The results of comparative molecular field analysis, a method of three-dimensional quantitative structure-activity relationship analysis, supported this conclusion.     

Changes in free amino acid pools can predict the mode of action of herbicides

Studies were conducted to determine the short-term changes in free amino acid levels in the meristematic zone of maize after treatment with various herbicides with different modes of action. These herbicides included inhibitors of various amino acid biosynthetic pathways, photosynthesis, and fatty acids biosynthesis. Inhibitors of various amino acid biosynthetic pathways caused specific reduction in the pools of amino acids being produced by the particular pathway. Inhibitors of other metabolic pathways also caused significant changes in pools of various amino acids. Very similar changes in the pools of amino acids were seen in plants treated with different chemical classes of inhibitors affecting a certain metabolic pathway. However, the changes were quite different between inhibitors of different metabolic processes. The data generated from these studies could be used as a diagnostic tool to determine the mode of action of novel herbicides.     

The carboxyterminal processing protease of D1 protein: Herbicidal activity of novel inhibitors of the recombinant and native spinach enzymes

The carboxyterminal processing protease of D1 protein (CtpA) is predicted to be an excellent target for the discovery of a general broad-spectrum herbicide. Directed and random screening of compounds against recombinant spinach CtpA (rCtpA) has led to the discovery of five different chemical classes of inhibitors. Lead compounds from each inhibitor class were investigated for their in vitro effects on the activities of both recombinant and native spinach CtpA. All of the lead compounds have K_i values of less than 50 μM when tested against rCtpA, and all except one showed competitive inhibition. Results from partially purified native CtpA from spinach were similar to those from the recombinant form of the enzyme, thus validating the use of rCtpA in the inhibitor screen. Compounds from three of the classes of CtpA inhibitors show in vivo herbicidal activity against Arabidopsis thaliana when applied either by addition to growth media or by spraying the leaves. Transgenic Arabidopsis plants which over-express CtpA showed greater resistance to the compounds than wild-type plants providing evidence that these inhibitors are directly acting against CtpA.