Evaluation of phenylaminopyrimidines as antifungal protein kinase inhibitors

The effects of diverse phenylaminopyrimidines (PAP), namely PAP-pyridines (type A), PAP-pyrazoles (type B) and PAP-thiazoles (type C), on Neurospora crassa Shear & Dodge has been investigated. The results revealed that type A strongly inhibit the in vitro growth of N crassa, whereas types B and C are much less active. A significant correlation was observed between the Neurospora growth inhibition and the intrinsic activity of type A compounds on the cyclin-dependent protein kinase p34(CDC2) of starfish, suggesting that the target of phenylaminopyrimidines in fungi is a cyclin-dependent protein kinase (CDK). The phenylaminopyrimidine-binding CDKs Phoss (major band) and CDC2 (minor band) involved in phosphorus uptake, glycogen synthesis and the cell cycle were identified from N crassa by affinity chromatography on phenylaminopyrimidine-sepharose. Comparative experiments with different protein kinases revealed the importance of the side chain of phenylaminopyrimidines for their target selectivity. A type B compound was found to selectively inhibit the MAP-kinase OS-2 involved in the osmoregulatory pathway of Neurospora.     

Characterization of the bound residues of the fungicide cyprodinil formed in plant cell suspension cultures of wheat

The non-extractable residues of the fungicide cyprodinil formed in heterotrophic cell suspension cultures of wheat were studied by application of [2-pyrimidyl-14C] or [2-pyrimidyl-13C]cyprodinil. The main objective was to examine whether solid-state and liquid 13C NMR spectroscopy can be used to examine plant bound residues of pesticides. For 14C experiments, wheat suspensions grown on glucose as carbon source were treated with 10 mg litre(-1) of 14C-cyprodinil. After incubation for 12 days, 20% of applied 14C was detected as non-extractable residues. The cell debris were treated with 0.1 M HCl (reflux), 1.0 M HCl (reflux), buffer, or 2 M NaOH (50 degrees C); Bj?rkman lignin and acidolysis lignin fractions were also prepared from the debris. Radioactivity liberated and solubilized by these procedures was examined by thin-layer chromatography and high-performance liquid chromatography. The results showed that cyprodinil and primary metabolites contributed to the fungicide's bound residues. Most of the residues (12% of applied 14C) remained associated with polar or polymeric/oligomeric endogenous cell materials in a stable manner. For the study with 13C-cyprodinil, wheat suspensions were cultivated on 13C-depleted glucose for four growth cycles, resulting in maximum 13C depletion of the natural cell components to about 0.10%. During the fourth cycle, 13C-labelled cyprodinil was applied, and cells were incubated (12 days). Cell debris was prepared and examined by solid-state 13C NMR spectroscopy. Debris was then treated as described above in the 14C experiment. Solubilized fractions were analyzed by liquid 13C NMR spectroscopy. However, none of the 13C NMR spectra recorded gave utilizable or unambiguous results, and all exhibited large inconsistencies, especially concerning the data from the conventional 14C experiment.     

Laboratory evaluation of a botanical natural product (<Emphasis Type="Italic">AkseBio2</Emphasis>) against the pear psylla<Emphasis Type="Italic">Cacopsylla pyri</Emphasis>

A botanical natural product,AkseBio2, was evaluated under laboratory conditions for its oviposition deterrent, ovicidal and larvicidal (nymphicidal) effects against the pear psyllaCacopsylla pyri (L.) (Hemiptera: Psyllidae). The product exhibited a strong oviposition deterrent effect for winterform and summerform females and caused a reduction in the total number of eggs laid in both choice and no-choice assays. Significant mortalities in freshly laid eggs (0–48 h) and various nymphal stages of the pest were recorded in toxicity assays. At a concentration of 0.1% (formulation), the highest biological activity of the product was recorded against the young (1st and 2nd) nymphal stages (up to 87.4% mortality) in comparison with the other biological stages of the pest. It was less active against the older (3rd-5th) nymphs, causing 62.1% mortality at the same concentration. In assays with non-target organisms, a significant negative effect was not observed. There were no significant changes on treated plants up to 7 days after treatment in any trial, nor was there any phytotoxicity on plant tissue as a result ofAkseBio2 treatments. The results suggest that the product can be used in psylla control instead of synthetic insecticides and may serve as an integrated pest management (IPM) component in pear orchards. http://www.phytoparasitica.org posting July 14, 2004.     

10种化学杀菌剂对苹果树腐烂病的防效评价

本试验通过采用抑制菌丝生长、促进伤口愈合以及在离体枝条上的保护和治疗试验,对市售的10种化学药剂进行了防治苹果树腐烂病效果的评价.这些药剂分别为甲硫·萘乙酸、腐植酸·铜、菌毒清、丙环唑、代森铵、丁香菌酯、噻霉酮、辛菌胺·醋酸盐、甲基硫菌灵(山西北方种业)和甲基硫菌灵(日本曹达).试验结果表明,不同的测试方法得到不同的排序.在抑菌试验中,抑菌作用最强的药剂是甲基硫菌灵(山西北方种业)和腐植酸·铜,抑菌带均为5.00 cm,其次为菌毒清、丙环唑和甲硫·萘乙酸.在伤口愈合试验中,甲基硫菌灵(日本曹达)和甲硫·萘乙酸对伤口的愈合作用最好,其愈伤组织宽度分别比对照宽2.00 mm和0.92 mm.在离体枝条保护作用试验中,甲硫·蕃乙酸、腐植酸·铜、甲基硫菌灵(日本曹达)处理均未发病.在离体枝条治疗作用试验中,甲硫·萘乙酸、菌毒清、代森铵、甲基硫菌灵(山西北方种业)、腐植酸·铜的病斑平均扩展面积均小于50 mm2,其中甲硫·萘乙酸和菌毒清的防效均为87.5％,病斑面积仅为对照的1.6％和2.2％.综合排序和分析认为,甲硫·萘乙酸是治疗腐烂病效果最好的药剂.     

生姜茎腐病防治药剂筛选研究

为筛选出对生姜茎腐病具有较明显防治效果的药剂,在离体条件下,测定了17种杀菌剂对生姜茎腐病菌菌丝体的抑制作用,并筛选抑菌效果明显的药剂进行田间试验.在室内筛选出了抑制效果较好的药剂8种.毒力测定表明,代森锰锌·精甲霜灵、代森锰锌·霜脲氰和烯酰吗啉对病菌抑制作用较强,其EC50分别为9.77、14.95、38.61 μg/mL.田间药效测定表明,代森锰锌·精甲霜灵对生姜茎腐病的防效高达81.45％,代森锰锌·霜脲氰的防效为47.09％.68％代森锰锌·精甲霜灵对生姜茎腐病的防治效果较好,可以在生产中推广应用.     

新疆有毒植物资源及其植物源杀虫剂开发应用前景

植物源杀虫剂(botanical insecticides)就是利用植物的某些部位或提取成分,加工成有杀虫作用的杀虫剂。在新疆,有毒植物资源种类繁多。通过介绍新疆有毒植物的资源概况,讨论有毒植物作为农业杀虫剂的应用现状和存在问题,提出其种质资源作为植物源杀虫剂的开发利用前景。     

N-(3,5-二甲氧基-4-烷氧基苯乙基)扁桃酰胺类杀菌剂的设计合成及杀菌活性

以第一个扁桃酰胺类杀菌剂双炔酰菌胺为模板,在炔丙氧基的邻位引入第二个甲氧基,设计合成了15个未见文献报道的 N-(3,5-二甲氧基-4-烷氧基苯乙基)扁桃酰胺类化合物(8a～8o),其结构通过核磁共振氢谱和高分辨质谱确认。初步的离体和活体杀菌试验结果表明,化合物 8e、8h和8o 对辣椒疫霉 Phytophthora capsici 具有较好的杀菌活性,其中 8h和8o 在62.5 mg/L下对辣椒疫霉活体抑制率达100%。     

Genetic analysis and molecular characterisation of laboratory and field mutants of Botryotinia fuckeliana (Botrytis cinerea) resistant to QoI fungicides

BACKGROUND: QoI fungicides, inhibitors of mitochondrial respiration, are considered to be at high risk of resistance development. In several phytopathogenic fungi, resistance is caused by mutations (most frequently G143A) in the mitochondrial cytochrome b (cytb) gene. The genetic and molecular basis of QoI resistance were investigated in laboratory and field mutants of Botryotinia fuckeliana (de Bary) Whetz. exhibiting in vitro reduced sensitivity to trifloxystrobin. RESULTS: B. fuckeliana mutants highly resistant to trifloxystrobin were obtained in the laboratory by spontaneous mutations in wild‐type strains, or from naturally infected plants on a medium amended with 1–3 mg L^?1 trifloxystrobin and 2 mM salicylhydroxamic acid, an inhibitor of alternative oxidase. No point mutations were detected, either in the complete nucleotide sequences of the cytb gene or in those of the aox and Rieske protein genes of laboratory mutants, whereas all field mutants carried the G143A mutation in the mitochondrial cytb gene. QoI resistance was always maternally inherited in ascospore progeny of sexual crosses of field mutants with sensitive reference strains. CONCLUSIONS: The G143A mutation in cytb gene is confirmed to be responsible for field resistance to QoIs in B. fuckeliana. Maternal inheritance of resistance to QoIs in progeny of sexual crosses confirmed that it is caused by extranuclear genetic determinants. In laboratory mutants the heteroplasmic state of mutated mitochondria could likely hamper the G143A detection, otherwise other gene(s) underlying different mechanisms of resistance could be involved. Copyright © 2012 Society of Chemical Industry     

“适地栽种”在园林绿化中的运用

园林绿化要达到良好的绿化和景观效果,在园林绿化设计和种植时就必须遵从"适地栽种"的原则,要做到这一点应从选树适地、改地适树、改地改树入手。     

不同土壤消毒剂和杀菌剂防治草莓土传病害的研究

利用3种土壤消毒剂和6种杀菌剂处理草莓育苗地和种植地,研究其对草莓土传性病害的防治效果及其对草莓育苗和产量的影响.结果表明,3种土壤消毒剂处理都明显降低育苗地和种植地中草莓苗炭疽病和枯萎病的发病率,防治效果较好的是三氯硝基甲烷和四氢-3,5-二甲基-1,3,5-噻二唑-2-硫酮.其中三氯硝基甲烷降低了土传病害的发病率,草莓苗发苗数量明显提高11.23％,产量也明显增加14.78％.使用6种杀菌剂后,炭疽病发病率显著降低,在第4次用药后15d,对照发病率高达89.3％,而75％戊唑醇·肟菌酯WG3000倍液和43％戊唑醇SC5000倍液处理的防治效果较好,炭疽病发病率仅为4.0％,防效分别高达98.41％和98.54％.