杀菌剂SPRI-90827分析方法的研究

采用高效液相色谱法,使用C18色谱柱,用紫外检测器对SPRI–90827进行了定量分析。该方法简单、快速、准确,标准偏差为0.85,变异系数为0.48%,平均回收率为99.7%。     

新型杀菌剂HNPC-A073的生物活性

通过室内、温室及田间试验,评价了新型杀菌剂HNPC-A073的生物活性。室内杀菌活性试验结果表明HNPC-A073在10～25μg·mL-1浓度下对供试的29种靶标病害中90%以上靶标均有抑制作用;温室及田间试验表明HNPC-A073对灰霉、菌核等多种病害具有良好防治效果。     

几种杀菌剂及混剂对葡萄褐斑病的生物活性测定

葡萄褐斑病是葡萄生产中的重要病害,其化学防治具有一定难度。测定了市场上用于防治该病害的10种主要杀菌剂的室内杀菌活性,活性较好的杀菌剂有40%氟硅唑EC、50%咪鲜胺WP、10%苯醚甲环唑WG。通过混剂筛选试验,10%苯醚甲环唑WG∶50%多菌灵WP(质量比4∶1、2∶1、1∶1)、40%氟硅唑EC∶70%代森锰锌WP(质量比4∶1、2∶1)、50%咪鲜胺WP∶70%甲基硫菌灵WP(质量比4∶1、2∶1、1∶1)是较好的杀菌剂组合,对葡萄褐斑病防效较好。     

农用杀菌剂腈菌唑光学对映体的生物活性

[目的]采用高效液相色谱法拆分制备了腈菌唑光学对映体.采用菌丝生长速率法测定了腈菌唑外消旋体及其对映体对苹果轮纹病菌、小麦赤霉病菌、梨黑斑病菌和番茄早疫病菌的生物活性,比较了对映体间杀菌活性的差异.[结果]对苹果轮纹病菌,(+)-腈菌唑和(-)-腈菌唑的EC50值分别为2.6441、8.6927 mg/L;对小麦赤霉病菌,二者的EC50值分别为0.7381、4.4157 mg/L;对于梨黑斑病菌,二者的EC50值分别为8.7899、20.7744 mg/L;对番茄早疫病菌,二者的EC50值分别为5.3120、12.8365 mg/L.[结论]对于供试菌种而言,[+)-腈菌唑杀菌活性显著优于(-)-腈菌唑.     

农用杀菌剂发展现状及展望

农业是杀菌剂使用量最大,所用品种最多,使用范围最广的一个领域。农用杀菌剂是指用于防治由各种病原微生物引起的植物病害的一类农药,一般指杀真菌剂,具有杀死病菌孢子、菌丝体或者抑制其发育、生长的作用。文章综述了三唑类、吡啶类、噁(咪)唑类等农用杀菌剂的结构及其生物活性,并展望了今后杀菌剂开发的研究方向。     

农用杀菌剂发展现状及展望

农业是杀菌剂使用量最大,所用品种最多,使用范围最广的一个领域。农用杀菌剂是指用于防治由各种病原微生物引起的植物病害的一类农药,一般指杀真菌剂,具有杀死病菌孢子、菌丝体或者抑制其发育、生长的作用。文章综述了三唑类、吡啶类、噁（咪）唑类等农用杀菌剂的结构及其生物活性,并展望了今后杀菌剂开发的研究方向。     

噻吩类杀菌剂的研究进展

概述了近年来文献报道的具有杀菌活性的噻吩类化合物的研究现状.按照化学结构的不同分别介绍了噻吩酰胺类、Stroburins类、联芳香环类、磺酰胺类、噻吩脲类、噻吩腙类及其他类共7类化合物的化学结构及生物活性.     

硫脲类化合物杀菌剂的合成

硫脲类化合物是一类具有广谱、高效的杀菌剂。为寻找更为优秀的杀菌剂新品种 ,选用了氨基嘧啶、氨基三唑酮、氨基三唑硫酮等含氮杂环化合物与烷氧羰基异硫氰酸酯反应 ,合成了 12个硫脲类衍生物 4 芳基 3 硫代脲酸酯类化合物 ,其中 10个化合物未见文献报道。通过氢谱 ( 1HNMR)、红外光谱 (IR) ,元素分析和熔点测定 ,确定了这 12个化合物的结构并对它们的杀菌毒力活性也进行了测定。这些参数将对筛选合成新的化合物提供科学依据     

具有农药生物活性的丙二腈类化合物的研究进展

简要介绍了具有农药生物活性的丙二腈类化合物的发展情况.文中主要涉及具有杀菌、除草活性的芳基亚甲基丙二腈、氨基亚甲基丙二腈及肼基亚甲基丙二腈具有杀虫活性的饱和直链丙二腈类化合物的化学结构和研究开发情况.     

Pyribencarb的合成与生物活性

[目的]Pyribencarb是由日本组合化学公司开发的一类具有新颖化学结构的QoI(quinone outside inhibitor)杀菌剂。为研究该类杀菌化合物,探索了其合成方法并进行了生物活性测定。[方法]以邻氯苄胺和6-甲基-2-吡啶甲醇为起始原料,共经过7步反应合成目标化合物pyribencarb,经核磁验证其结构。[结果]生物活性测定结果表明该化合物具有广谱的杀菌活性,对灰霉病、稻瘟病具有较好的防治效果,尤其对灰霉病有特效。[结论]Pyribencarb具有优异的杀菌活性,作为一类具有新颖化学结构的杀菌剂,值得进一步研究。     

根围细菌次生代谢物的生物活性筛选

从全国7个地区采集的植物根围土壤样品中分离得到1700余株植物根嗣细菌.采用室内离体筛选的试验方法,以5种植物病原细菌作为靶标,筛选研究得到有生物活性的菌株840株.其中10%的菌株对5种植物病原细菌都具有拮抗活性,其余菌株则仅对1种或几种病原细菌具有拈抗活性.从中进一步筛选得到对小麦白粉病也具有防治效果的菌株,其防治效果最高可达60%.将最终获得的同时对病原细菌有拮抗效果和真菌病害有防治效果的根围细菌作为以后深入研究的对象.     

放线菌SPRI-709084次级代谢产物的提取分离及结构鉴定

从青海省高原地区的土壤里筛选出一株能够产生除草活性物质的放线菌SPRI-709084,发酵液经过溶剂萃取、柱层析、薄层层析、高效液相色谱等过程分离纯化得到一种具有除草活性的化合物,命名为SPRI-709084A,该化合物在低浓度下可使杂草黄化,高浓度时可抑制种子发芽。经过质谱及核磁共振等分析确定：分子量为257、分子式为C14H15N3O2、结构与已知化合物吲哚霉素相同。     

放线菌SPRI-511356产除草活性物质的研究

从放线菌SPRI-511356次级代谢产物中分离得到具有生物活性的化合物,经过HPLC、LC/MS、核磁共振等分析,确定了其结构为β-1,4-二环己烯基-α-丙氨酸.该化合物具有除草活性.     

Examination of Secondary Metabolite Biosynthesis in Apicomplexa

Natural product discovery has traditionally relied on the isolation of small molecules from producing species, but genome-sequencing technology and advances in molecular biology techniques have expanded efforts to a wider array of organisms. Protists represent an underexplored kingdom for specialized metabolite searches despite bioinformatic analysis that suggests they harbor distinct biologically active small molecules. Specifically, pathogenic apicomplexan parasites, responsible for billions of global infections, have been found to possess multiple biosynthetic gene clusters, which hints at their capacity to produce polyketide metabolites. Biochemical studies have revealed unique features of apicomplexan polyketide synthases, but to date, the identity and function of the polyketides synthesized by these megaenzymes remains unknown. Herein, we discuss the potential for specialized metabolite production in protists and the possible evolution of polyketide biosynthetic gene clusters in apicomplexan parasites. We then focus on a polyketide synthase from the apicomplexan Toxoplasma gondii to discuss the unique domain architecture and properties of these proteins when compared to previously characterized systems, and further speculate on the possible functions for polyketides in these pathogenic parasites.     

植物次级代谢产物研究

近年来，人们对植物的次级代谢过程以及代谢产物进行了研究，并取得了较大的进展，研究表明，可以用基因编码的生物合成酶和基因编码的诱变蛋白来改变不同的合成路径，而且还使用抗敏抑制竞争性路径，依此来提高目标次级代谢产物的产率^[1]。     

Effects of Bleaching on Secondary Metabolite Chemistry of Alcyonacean Soft Corals

The loss of zooxanthellae during a short-term, experimentally simulated bleaching event resulted in significant changes to the secondary metabolite chemistry of the alcyonacean soft corals Sinularia flexibilis and Lobophytum compactum. The concentration of flexibilide, the most active cytotoxic secondary metabolite (with antimicrobial properties) in the tissues of Sinularia flexibilis increased by 126%, while that of its principal terpenoid algaecide, sinulariolide, simultaneously decreased to just 8% of that found in the controls. The changes were short lived, however, with concentrations of both compounds returning to control levels one month after bleaching; at the same time zooxanthellae levels were still only approximately 20% of the controls. Similarly, concentrations of isolobophytolide, the principal terpenoid secondary metabolite of Lobophytum compactum underwent a significant reduction for one month following bleaching. Like their nonbleached counterparts, both bleached individuals of Sinularia flexibilis and Lobophytum compactum experienced neither significant algal overgrowth nor predation following bleaching. Full recovery of zooxanthellae to baseline levels in all bleached corals occurred within four months. These results suggest that some soft corals are capable of surviving short-term bleaching events and the detrimental algal overgrowth that is often associated with bleaching, possibly by adjusting their secondary metabolite concentrations to suit specific needs. Support for the notion that resource allocation towards production of specific algaecides in bleached specimens translates also into higher protection was gained through analysis of naturally bleached soft corals. Bleached and overgrown individuals had significantly lower concentrations of species-specific algaecides than their bleached and unfouled and their unbleached counterparts.     

Antiproliferative,Antibacterial and Antifungal Activity of the Lichen Xanthoria parietina and Its Secondary Metabolite Parietin

Lichens are valuable natural resources used for centuries throughout the world as medicine, food, fodder, perfume, spices and dyes, as well as for other miscellaneous purposes. This study investigates the antiproliferative, antibacterial and antifungal activity of the acetone extract of the lichen Xanthoria parietina (Linnaeus) Theodor Fries and its major secondary metabolite, parietin. The extract and parietin were tested for antimicrobial activity against nine American Type Culture Collection standard and clinically isolated bacterial strains, and three fungal strains. Both showed strong antibacterial activity against all bacterial strains and matched clinical isolates, particularly against Staphylococcus aureus from standard and clinical sources. Among the fungi tested, Rhizoctonia solani was the most sensitive. The antiproliferative effects of the extract and parietin were also investigated in human breast cancer cells. The extract inhibited proliferation and induced apoptosis, both effects being accompanied by modulation of expression of cell cycle regulating genes such as p16, p27, cyclin D1 and cyclin A. It also mediated apoptosis by activating extrinsic and intrinsic cell death pathways, modulating Tumor Necrosis Factor-related apoptosis-inducing ligand (TRAIL) and B-cell lymphoma 2 (Bcl-2), and inducing Bcl-2-associated agonist of cell death (BAD) phosphorylation. Our results indicate that Xanthoria parietina is a major potential source of antimicrobial and anticancer substances.