吩嗪-1-羧酸及其类似物的合成研究进展

天然产物吩嗪-1-羧酸（PCA）作为重要的微生物代谢产物,在假单胞菌属（Pseudomonads）和链霉菌属（Streptomycetes）等微生物分泌物中广泛存在,具有医用抗肺癌活性及抗水稻纹枯病、西瓜枯萎病、辣椒疫病、小麦全蚀病、西瓜炭疽病和油菜菌核病等病原菌的广谱性农用抗菌活性,对人畜和环境无害,并具有独特的化学结构,是研发绿色农药的理想化合物。文章综述了吩嗪-1-羧酸及其类似物在微生物发酵及化学合成方面的研究进展,分析了各合成路线中的关键反应,讨论了各合成方法的优缺点。     

番茄灰霉病菌高效杀菌剂筛选及新型混剂研究

为了筛选对番茄灰霉病菌(Botrytis cinerea)抑制活性较高的杀菌剂及新型混剂,采用菌丝生长速率法测定了8种化学杀菌剂、拮抗菌发酵上清液及其与化学杀菌剂的混配剂对番茄灰霉病菌的抑制活性。结果表明,咯菌腈、咪鲜胺、戊唑醇和腈菌唑对番茄灰霉病菌的抑制活性较高,EC₅₀值分别达0.031 92、0.057 18、0.185 60、0.805 30 μg·mL^-1;其次为异菌脲、嘧霉胺和百菌清,EC₅₀值分别为4.204 90、5.949 90和8.816 30 μg·mL^-1;代森锰锌的抑菌效果最差,EC₅₀值为103.519 40 μg·mL^-1。解淀粉芽孢杆菌(Bacillus amyloliquefaciens)gfj-4培养72 h所产发酵上清液对番茄灰霉病菌的EC₅₀为76.9 mL·L^-1。采用Horsfall的复配方法,设计发酵上清液与咪鲜胺、戊唑醇、代森锰锌、咯菌腈和异菌脲分别以体积比6:4、4:6、8:2、9:1和7:3的比例复配,毒性比分别为1.61、1.60、1.53、1.38和1.32,具有显著的增效作用。     

新疆红枣黑斑病防治药剂筛选

为了有效控制新疆红枣黑斑病的发生及危害,采用抑菌圈比较、毒力测定及田间药效试验相结合的方法对20种杀菌剂进行筛选。通过抑菌圈比较发现,80%乙蒜素、50%氯溴异氰尿酸、40%多·福、40%氟硅唑、50%乙嘧酚、72%霜脲锰锌、37%苯醚甲环唑和5%己唑醇8种杀菌剂抑菌力较强,抑菌半径在1.83~3.80 cm。对其毒力测定结果表明,40%氟硅唑对红枣黑斑病菌的毒力最大,EC50值(抑菌中质量浓度)为35.89 mg/L;其次为5%己唑醇,EC50值为58.24 mg/L;其余6种药剂EC50值为113.11~517.13 mg/L。选取抑菌效果好且稳定的4种药剂进行田间防治试验,结果表明,80%乙蒜素最终防效最高(65.3%),5%己唑醇次之(61.7%),其余2种药剂(50%氯溴异氰尿酸、40%氟硅唑)的防效为52.7%~56.3%。综上,80%乙蒜素和5%己唑醇防效最好,可作为当前防治新疆红枣黑斑病的主打药剂。     

2种杀菌剂对籼粳交水稻品种‘甬优12’稻曲病防治效果及机理研究

为探明高效杀菌剂用药量和防治时期对水稻稻曲病的防治效果及防治机理,研究了2种杀菌剂的3个用药量和8个用药时期对籼粳交水稻品种‘甬优12’稻曲病的防效。结果表明,在推荐用量范围内对稻曲病防治效果较好,随着用量上升防效有提高趋势,但除喜奥300 g/hm~2用药量防效显著低于其他处理外,用药量不是影响防效的关键因素;2种杀菌剂在破口前20天就开始具有一定防效,越接近开花期,防效越明显,破口后防效开始呈下降趋势,其中喜奥在齐穗期后防效下降较为迅速。因此认为,稻曲病在侵染‘甬优12’的关键时期是在开花期,可选用长效高效杀菌剂,于破口前进行防治。     

梨黑斑病菌抗药性检测及其对啶酰菌胺的敏感性基线

黑斑病是梨的主要病害之一,近年来不少地区反映多菌灵等传统常用杀菌剂对其防治效果已出现下降。作者从浙江、江苏和安徽3省分离了252株梨黑斑病菌Alternaria kikuchiana,采用菌丝生长速率法检测了其抗药性发生情况。结果发现:所检测的黑斑病菌群体(n=252)对苯并咪唑类杀菌剂多菌灵的抗性频率为57.1%,且全部为高水平抗性(HR);对二甲酰亚胺类杀菌剂异菌脲的抗性频率为46.8%,全部为低水平抗性(LR);对甾醇脱甲基抑制剂类杀菌剂苯醚甲环唑的抗性为低水平(LR)及中等水平(MR),抗性频率均为28.6%;表明梨黑斑病菌对常用杀菌剂已产生较为严重的抗性。供试252株梨黑斑病菌对琥珀酸脱氢酶抑制剂啶酰菌胺的EC50值分布在0.12~3.85μg/m L之间,平均EC50值为(1.21±0.12)μg/m L,且其分布呈近似正态的单峰曲线。研究表明,啶酰菌胺可作为潜在的梨黑斑病防治替代药剂,其平均EC50值(1.21±0.12)μg/m L可作为梨黑斑病菌对啶酰菌胺的敏感性基线。     

Do some IPM concepts contribute to the development of fungicide resistance? Lessons learned from the apple scab pathosystem in the United States

One goal of integrated pest management (IPM) as it is currently practiced is an overall reduction in fungicide use in the management of plant disease. Repeated and long‐term success of the early broad‐spectrum fungicides led to optimism about the capabilities of fungicides, but to an underestimation of the risk of fungicide resistance within agriculture. In 1913, Paul Ehrlich recognized that it was best to ‘hit hard and hit early’ to prevent microbes from evolving resistance to treatment. This tenet conflicts with the fungicide reduction strategies that have been widely promoted over the past 40 years as integral to IPM. The authors hypothesize that the approaches used to implement IPM have contributed to fungicide resistance problems and may still be driving that process in apple scab management and in IPM requests for proposals. This paper also proposes that IPM as it is currently practiced for plant diseases of perennial systems has been based on the wrong model, and that conceptual shifts in thinking are needed to address the problem of fungicide resistance. © 2013 Society of Chemical Industry     

北京地区草莓灰霉病菌对异菌脲的抗性及抗性分子机制

由灰葡萄孢(Botrytis cinerea Pers.)引起的草莓灰霉病是草莓上危害严重的病害之一。为了解北京地区草莓灰霉病菌对二甲酰亚胺类常用杀菌剂异菌脲的抗性,本研究采用最低抑制浓度法分别检测了2013年和2014年从北京地区15个草莓园采集的共计121株草莓灰霉病菌对异菌脲的抗性。结果表明,北京地区草莓灰霉病菌对异菌脲存在较高的抗性频率,2014年较2013年的抗性频率略有上升,由40.4%上升为45.3%。不同草莓园菌株的抗性频率差异很大,可能与用药水平有关。2014年的低抗、中抗和高抗菌株数分别占检测菌株总数的9.4%、28.1%和7.8%。利用PCR技术扩增编码组氨酸激酶基因BcOS1中与二甲酰亚胺抗性相关的区段,对抗性菌株的分子机制进行了初步研究,结果表明BcOS1基因第1 214位核苷酸发生了2类突变:以第Ⅰ类为主,菌株的抗性水平为中抗和高抗,由ATC突变为AGC,导致第365位氨基酸由异亮氨酸变为丝氨酸;第Ⅱ类菌株为低抗,由ATC突变AAC,导致第365位氨基酸由异亮氨酸变为天冬酰胺。     

Engineering for disease resistance: persistent obstacles clouding tangible opportunities

The accelerating pace of gene discovery, coupled with novel plant breeding technologies, provides tangible opportunities with which to engineer disease resistance into agricultural and horticultural crops. This is especially the case for potato, wheat, apple and banana, which are afflicted with fungal and bacterial diseases that impact significantly on each crop's economic viability. Yet public scepticism and burdensome regulatory systems remain the two primary obstacles preventing the translation of research discoveries into cultivars of agronomic value. In this perspective review, the potential to address these issues is explained, and specific opportunities arising from recent genomics‐based initiatives are highlighted as clear examples of what can be achieved in respect of developing disease resistance in crop species. There is an urgent need to tackle the challenge of agrichemical dependency in current crop production systems, and, while engineering for disease resistance is possible, it is not the sole solution and should not be proclaimed as so. Instead, all systems must be given due consideration, with none dismissed in the absence of science‐based support, thereby ensuring that future cropping systems have the necessary advantage over those pathogens that continue to inflict losses year after year. © 2014 Society of Chemical Industry