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.     

不同类型和叶龄水稻对双草醚的敏感性差异

为了明确双草醚对不同类型和叶龄水稻的安全性,采用室内整株生测法测定了粳稻、籼稻和杂交稻代表品种不同叶龄(1~1.5叶期、2~3叶期、4~5叶期)对双草醚的敏感性。药后目测,低剂量双草醚处理对水稻株高略有抑制;双草醚高剂量处理水稻叶片黄化且株高明显受抑制,但是随着药后时间的推移,水稻叶色有所恢复。药后15d,相同叶龄下,粳稻对双草醚最敏感,籼稻次之,杂交稻耐药性最强;1~1.5叶期水稻对双草醚最敏感,随着叶龄的增长,水稻对双草醚的耐药性逐渐提高。     

耳叶水苋对乙酰乳酸合成酶抑制剂的抗性及其分子机制初探

近年来长江下游地区稻田耳叶水苋Ammannia arenaria H.B.K.危害十分严重。采用盆栽法首次测定了耳叶水苋对苄嘧磺隆等药剂的抗性水平,同时分析了其抗性和敏感种群间乙酰乳酸合成酶(ALS)基因的DNA序列及其RNA表达差异。结果表明:采自浙江嘉兴(JX110)、江苏苏州(JS039)、浙江宁波(NB0143-05)和安徽广德(AH014)的耳叶水苋生物型对苄嘧磺隆的抗性指数(RI)分别为67.90、17.59、44.63和8.37,对苄嘧磺隆表现出中高水平抗性的生物型对五氟磺草胺、双草醚及咪唑乙烟酸也产生了低水平的抗性。获得了耳叶水苋ALS基因全长核苷酸序列2235 bp,编码667个氨基酸,仅发现NB0143-05等3种抗性生物型ALS酶的氨基酸序列非保守区第93位的亮氨酸被脯氨酸取代。然而,NB0143-05的ALS酶对ALS抑制剂的敏感性大幅度降低(RI 37.04),且在苄嘧磺隆处理后4 d的ALS基因表达量是敏感生物型(HZ001)的1.86倍。这表明,ALS酶对药剂的敏感性降低以及被苄嘧磺隆诱导后ALS基因表达量显著增加,很可能是耳叶水苋生物型NB0143-05对ALS抑制剂产生抗性的原因。     

稻稗HJHL-715种群对五氟磺草胺的抗药性水平及抗性机理分析

为明确东北稻区稻稗Echinochloa oryzoides HJHL-715种群对五氟磺草胺的抗性水平及抗性机制,采用整株生物测定法测定稻稗种群对五氟磺草胺的敏感性,明确抗性种群的交互抗性和多抗性情况,研究3种细胞色素P450抑制剂对其敏感性的影响;并应用分子生物学方法进行稻稗的乙酰乳酸合酶(acetolactate synthase,ALS)离体活性测定、ALS基因序列分析及其表达量测定。结果表明:在东北稻区,五氟磺草胺对稻稗HJHL-715种群鲜重的抑制中剂量GR50为62.53 g/hm^2;稻稗HJHL-715的ALS基因序列中未发现氨基酸突变,其ALS离体活性与敏感种群的ALS离体活性无显著性差异,ALS基因表达量显著低于敏感种群。1-氨基苯并三唑(1-aminobenzotriazole,ABT)、胡椒基丁醚(piperomyl butoxide,PBO)、马拉硫磷3种P450抑制剂显著提高了稻稗HJHL-715种群对五氟磺草胺的敏感性,使其对五氟磺草胺的GR50由原来的62.53 g/hm^2分别下降到5.78、5.02、3.53 g/hm^2。表明东北稻区已经出现了对五氟磺草胺具有高水平抗性的稻稗种群,稻稗HJHL-715种群对五氟磺草胺的抗性很可能是由细胞色素P450介导的代谢增强所致。     

双草醚的科学正确使用

正双草醚属于嘧啶苯甲酸类除草剂,又名双嘧草醚,是高活性的乙酰乳酸合成酶(ALS)抑制剂,施药后能很快被杂草的茎叶吸收,并传导至整个植株,抑制植物分生组织生长,从而杀死杂草。双草醚高效、广谱、用量极低,可有效防除稻田稗草及其他禾本科杂草,兼治大多数阔叶杂草、一些莎草科杂草以及对其他除草剂产生抗性的稗草,如稗草、双穗雀稗、稻李氏禾、马唐、匍茎剪股颖、看麦娘、东北甜茅、狼巴草、异形莎草、日照瓢拂草、碎米莎草、萤     

双草醚的科学正确使用

双草醚属于嘧啶苯甲酸类除草剂,又名双嘧草醚。是活性高的乙酰乳酸合成酶（ALS）抑制剂,施药后能很快被杂草的茎叶吸收,并传导至整个植株,抑制植物分生组织生长,从而杀死杂草。该药剂高效、广谱、用量极低,可有效防除稻田稗草及其他禾本科杂草,兼治大多数阔叶杂草、一些莎草科杂草及对其他除草剂产生抗性的稗草,如稗草、双穗雀稗、稻李氏禾、马唐、匍茎剪股颖、看麦娘、东北甜茅、狼巴草、异形莎草、日照瓢拂草、碎米莎草、萤蔺、日本草、扁秆草、鸭舌草、雨久花、野慈菇、泽泻、眼子菜、谷精草、牛毛毡、节节菜、陌上菜、水竹叶、空心莲子草、花蔺等水稻田常见的绝大部分杂草。对大龄稗草和双穗雀稗有特效,可杀死一至七叶期的稗草。在农田生态系统中,除水稻、部分莎草以外的其他植物,对其均表现一定程度的敏感。     

新型乙酰乳酸合成酶（ALS）抑制剂作用机理的研究进展

ALS抑制剂类除草剂具有活性高、选择性强、对哺乳动物安全等优异特点,因而倍受各国政府、工农业界、学术界以及公众的关注。本文通过对ALS抑制剂及其致毒机制的理论研究,对ALS抑制剂的作用机理做了详细的阐述,力求反映ALS抑制剂的最新研究进展和发展动态,为进一步推动ALS抑制剂的发展及ALS相关基因功能的研究提供理论支持。     

转基因抗草铵膦水稻99-1和普通粳稻越富与稗草竞争性的比较

2001～2003年分别按照替换试验设计的模型盆栽抗草铵膦转基因水稻991与稗草、普通粳稻越富与稗草,比较这两个水稻品种与稗草的竞争力。水稻和稗草按照4:0、3:1、2∶2、1∶3和0∶4的比例混种。统计分析结果表明,普通粳稻越富和转基因水稻991对稗草的敏感性存在显著差异。在稗草存在下,转基因抗草铵膦水稻991的干重和根长受稗草抑制程度大于普通粳稻越富;而叶面积指数的趋势相反,991的入侵能力明显低于越富。综合评价为在与稗草的竞争性方面,普通粳稻越富优于转基因抗草铵膦水稻991。     

新型安全剂解决双草醚安全性问题

双草醚是组合化学公司开发的嘧啶水杨酸类除草剂,是高活性的乙酰乳酸合成酶（ALS）抑制剂,通过抑制植株所必需的支链氨基酸的生物合成来阻止细胞分裂,从而使植株停止生长,最终死亡。双草醚可有效防除稻田中的稗草及其他禾本科杂草,兼治大多数阔叶杂草、一些莎草科杂草,对二氯喹啉酸产生抗性的稗草亦有较好的防效。     

几种植物提取物光活化他感生长抑制作用研究

用1％浓度的黄皮种子、万寿菊根甲醇提取物和猪毛蒿精油处理稗草、含羞草、小麦、油菜和水稻催芽露白的种子，经光照与非光照处理，测定对5种受试植物的生长抑制活性。结果表明，黄皮、万寿菊和猪毛蒿的提取物对受试的5种植物表现出一定的光活化抑制生长活性。黄皮提取物对5种受试植物的根长抑制率均在50％左右，对小麦和油菜茎长抑制率达50％以上，对稗草、水稻、含羞草茎长抑制率较低，均在30％以下。万寿菊提取物对稗草和含羞草具有显著的光活化抑制生长活性。光照处理后的根、茎伸长抑制活性比非光照处理高出6倍。1％浓度的猪毛蒿精油无论是光照处理或非光照处理，对5种受试植物根、茎的伸长抑制率均在90％以上，显示出强烈的异株克生现象。     

Studies of the New Herbicide KIH-6127. Part III. Synthesis and Structure–Activity Studies of Analogues of KIH-6127 against Barnyard Grass (Echinochloa oryzicola)*

The previously evaluated prototype, methyl 6-acetyl-2-[(4,6-dimethoxypyrimidin-2-yl)oxy]benzoate, was modified by the introduction of an oximino group. Further extensive synthetic modifications were then made to the 6-alkyl moiety (R¹), the ester moiety (R²), the alkoxyimino moiety (R³), the bridge-atom (X) and the 4,6-disubstituted-pyrimidine moiety (A, B, Z). Structure–activity relationships of the synthesized compounds were studied by examining their herbicidal activity against Barnyard grass (Echinochloa oryzicola) in paddy rice at various growth stages, including pre-emergence. The novel herbicide methyl 2-[(4,6-dimethoxypyrimidin-2-yl)oxy]-6-[1-(methoxyimino)ethyl]benzoate, (KIH-6127) was found to be the most effective compound. The commercial development of this compound is currently in progress. © 1997 SCI.     

Herbicide-resistant barnyardgrass (Echinochloa crus-galli) in global rice production

Barnyardgrass (Echinochloa crus-galli (L.) Beauv.), an annual species of the family Poaceae, is a major weed problem in rice-producing countries throughout the globe. Synthetic herbicides can effectively control this grass in rice paddies, but the development of resistant biotypes after the continuous use of the same active ingredients has led to low herbicide efficacy and yield losses. In this review, a summary of resistant-barnyardgrass cases in global rice production is reported based on data from the International Herbicide-Resistant Weed Database. The first case of resistant barnyardgrass in rice paddies was to the photosystem-II inhibitor propanil in the late 1980s. Eighty-five (85) out of 116 cases in the period from 1986 to 2022 refer to resistant barnyardgrass (E. crus-galli var. crus-galli, E. crus-galli var. formosensis and E. crus-galli var. zelayensis) in 16 countries. Barnyardgrass has been found resistant to acetolactate synthase (ALS) inhibitors (34 cases), acetyl-CoA carboxylase (ACCase) inhibitors (23 cases), photosystem-II inhibitors (11 cases), auxin mimics/cellulose biosynthesis inhibitors (9 cases), very long chain fatty acid inhibitors (6 cases), and microtubule assembly inhibitors (1 case). The majority of all resistance cases reported to the active ingredients penoxsulam, bispyribac-sodium, and imazamox (ALS inhibitors), cyhalofop-butyl and fenoxaprop-ethyl (ACCase inhibitors), propanil (photosystem-II inhibitors), and quinclorac (auxin mimics/cellulose biosynthesis inhibitors). Although target-site resistance with specific mutations has been identified, non-target site resistance mainly through herbicide detoxification is also of great concern increasing the chance of multiple herbicide resistance evolution. Rotation of herbicides should be adopted concerning the modes of action used as well as the application methods to mitigate resistance evolution of this weed in rice paddies.     

广东省水稻田稗对五氟磺草胺的抗性分析

为明确广东省水稻田杂草稗Echinochloa crus-galli对五氟磺草胺的抗性现状及其可能的抗性机理,采用整株剂量反应法测定不同地区稗种群对五氟磺草胺的抗性水平,对不同稗种群的乙酰乳酸合成酶（acetolactate synthase,ALS）基因片段进行扩增测序,分析细胞色素P450酶（cytochrome P450 monooxygenase,P450）和谷胱甘肽-S-转移酶（glutathione-S-transferase,GST）抑制剂胡椒基丁醚（piperonylbutoxide,PBO）和4-氯-7-硝基-2,1,3-苯并氧杂噁二唑（4-chloro-7-nitro-1,2,3-benzoxadiazole,NBD-Cl）对不同稗种群抗性水平的影响,并对替代药剂进行筛选。结果显示,广东省水稻田多数稗种群对五氟磺草胺仍表现敏感,但采自湛江市的1个种群BC-7对五氟磺草胺产生了抗性,抗性倍数达6.5倍。与敏感种群BC-2相比,BC-7种群并未发生已报道的ALS靶标抗性相关突变。PBO和NBD-Cl均可显著提高BC-7种群对五氟磺草胺的敏感性,其干重抑制中量GR₅₀由31.1 g/hm²分别降为11.0 g/hm²和24.7 g/hm²。BC-7种群对氰氟草酯和噁唑酰草胺仍较敏感,但对二氯喹啉酸和双草醚产生了抗性。表明P450和GST介导的代谢抗性是稗BC-7种群产生抗性的重要原因,氰氟草酯和噁唑酰草胺适用于治理该抗性种群。     

萘二甲酸酐减轻胺苯磺隆对水稻药害的作用机制

通过在离体和活体条件下萘二甲酸酐（NA）对水稻乙酰乳酸合成酶（ALS）活力的影响,进行NA减轻胺苯磺隆对水稻药害作用机制研究。离体条件下,NA对水稻幼苗ALS的活力影响很小,且未能产奋勇安苯磺隆对ALS活性的抑制作用。活体条件下,NA提高幼苗ALS活力达40％,且抵消胺苯磺隆对ALS活力的抑制作用,说明NA减轻胺苯磺隆对水稻药害的作用机制是NA间接激活靶标酶ALS。     

小麦田看麦娘对甲基二磺隆的抗性水平及分子机制初探

看麦娘是中国长江中下游地区稻茬麦田的主要恶性杂草之一,甲基二磺隆是防治小麦田看麦娘等禾本科杂草的重要除草剂.该研究团队前期在安徽省凤台县小麦田采集到疑似抗性种群看麦娘(AHFT-01),为明确其对甲基二磺隆的抗性发生情况及潜在的抗性机制,采用温室盆栽法在整株水平上测定了该种群对甲基二磺隆及其他乙酰乳酸合成酶(ALS)抑...     

除草剂农美利的稻田除草效果及生理作用

以 Facet(活性成份 quinclorac)为对照 ,测试了农美利的稻田除草效果。试验结果表明 :农美利是一个较优秀的直播稻田苗后除草剂 ,除草率可达 10 0 % ,适宜用量 2 mg/ m2 ,适宜使用时期为水稻一叶一心期～五叶一心期。对水稻的营养生长有一定的抑制作用 ,但其抑制效应是可逆的。农美利对水稻和稗草的生理影响研究结果表明 ,农美利的除草作用在于对光合速率、呼吸强度、叶绿素含量的影响 ,其强度在杂草与水稻之间有显著差异     

寄主植物上喷药对大螟产卵选择性的影响

为明确稻田适量喷施保护性农药是否影响周边香根草对水稻螟虫的诱集效果,通过室内盆栽试验测定了在水稻和香根草上分别喷施氯虫苯甲酰胺对大螟成虫趋性及产卵选择性的影响。结果表明:在水稻上喷药后第1天,栖息在香根草上的大螟雌、雄成虫总量分别为4.2头和3.8头,显著高于水稻上雌、雄成虫的总量1.00头和0.60头;在水稻上喷药后1~3 d接入大螟,在水稻上不产卵,直到第6天才出现卵块;喷药后6 d和12 d接入大螟,在香根草上的卵粒数分别为287.2粒和309.2粒,显著高于其在水稻上的57.2粒和81.4粒,约为水稻上的5.0倍和3.8倍。在香根草上喷药后1~3 d接入大螟,成虫选择水稻居多,在香根草上的产卵量为0;喷药后6 d接入大螟,成虫对2种寄主植物的选择性无显著差异;喷药后12 d接入大螟,在香根草上的成虫数量为9.8头,约为水稻上的2.5倍,产卵量也约为水稻上的1.9倍,二者均差异显著。表明香根草喷施氯虫苯甲酰胺后其对大螟的诱集作用有一定影响,但这种影响会随着施药时间的延长而逐渐减弱。     

EK-2612, a new cyclohexane-1,3-dione possessing selectivity between rice (Oryza sativa) and barnyardgrass (Echinochloa crus-galli)

A newly synthesized experimental compound, EK-2612 is one of the class of cyclohexane-1,3-diones which are commonly known to be grasskillers. A greenhouse study was conducted to evaluate the herbicidal performances of EK-2612 on several grass species in comparison with tralkoxydim, a commercialized cyclohexanedione derivative. Like tralkoxydim, the compound EK-2612 showed excellent control efficacy on most grass weeds tested through foliar application rates between 250 and 63 g AI ha(-1). Unlike tralkoxydim, however, EK-2612 showed a good rice safety, and there was no rice damage observed at the level below 125 g AI ha(-1), while rice injury developed at the same application rates of tralkoxydim. With this rice safety, EK-2612 controlled barnyardgrass effectively up to the two-leaf stage under both submerged and dried paddy conditions. An in vitro ACCase assay indicated that EK-2612 is a strong ACCase inhibitor; however, the dose-response was not substantially different in rice and barnryardgrass, showing I50 values of 0.1 and 0.12 microM, respectively. These results suggest that the compound EK-2612 is targeting plant ACCase, but the whole-plant rice safety is not attributable to a different inhibition of the target site in rice from that in barnyardgrass.     

Cross-resistance pattern and alternative herbicides for Cyperus difformis resistant to sulfonylurea herbicides in Korea

A Cyperus difformis L accession from Chonnam province, Korea was tested for resistance to the sulfonylurea herbicide, imazosulfuron. The accession was confirmed to be resistant (R) and was cross-resistant to other sulfonylurea herbicides, bensulfuron-methyl, cyclosulfamuron and pyrazosulfuron-ethyl, the pyrimidinyl thiobenzoate herbicide, bispyribac-sodium, and the imidazolinone herbicide imazapyr, but not to imazaquin. Multiple resistance was tested using twelve herbicides with target sites other than acetolactate synthase (ALS). The R biotype could be controlled by other herbicides with different modes of action such as butachlor, carfentrazone-ethyl, clomeprop, dithiopyr, esprocarb, mefenacet, oxadiazon, pretilachlor, pyrazolate and thiobencarb, applied to soil at recommended rates. Several sulfonylurea herbicide-based mixtures can control both the R and S biotypes of C difformis, except sulfonylurea plus dimepiperate, molinate or pyriftalid, and pyrazolate plus butachlor. Although mixtures of sulfonylurea herbicides might be more effective, they should be avoided and used only in special cases. In terms of in vitro ALS activity, the R biotype was 1139-, 3583-, 1482-, 416-, 5- and 9-fold more resistant to bensulfuron-methyl, cyclosulfamuron, imazosulfuron, pyrazosulfuron-ethyl, bispyribac-sodium and imazapyr, respectively, than the S biotype. The in vivo ALS activity of the R biotype was also less affected by the sulfonylurea herbicides, imazosulfuron and pyrazosulfuron-ethyl, than the S biotype. Results of in vitro and in vivo ALS assays indicated that the resistance mechanism of C difformis to ALS inhibitor herbicides was primarily due to an alteration in the target enzyme, ALS. Greenhouse experiments showed delayed flowering and reduced seed production of the R biotype, which could possibly result in reduced fitness. This unusual observation needs to be confirmed in field situations.