植物内生菌抗菌活性物质及其在果蔬采后保鲜中的应用进展

植物内生菌是寄生在植物组织中的一大类群特殊微生物,过去长期被忽略。然而越来越多的研究表明,植物内生菌是新型抗菌药物的宝贵资源,其代谢产物中存在一系列具有多样性结构的抗菌活性化合物。本文对近年来植物内生菌产生的抗菌活性物质及其抗菌效果进行了综述,简要介绍了植物内生菌在果蔬采后保鲜中的应用,同时总结了植物内生菌抗菌活性物质在当前实际研究中所遇到的问题。     

Natural products as a source of agrochemicals and leads for chemical synthesis

The use of natural products as a source of new agrochemicals and the procedures that can be undertaken to discover such compounds are reviewed using examples from both the literature and our own experiences. The commercial successes obtained to date show that natural products are a powerful source of new agrochemicals. The results from a survey of the views of the agrochemical industry of natural product work indicated a high level of interest, with 16 of the 19 companies that replied being involved in natural product work either through in-house or external programmes of work. Possible approaches to the key challenges of atural product work, for example choice of sources and screens, avoiding known metabolites and obtaining sufficient compound for biological evaluation, are discussed.     

From synthetic control to natural products: a focus on N‐heterocycles

Natural products containing a N‐heterocycle motif are widespread in nature and medicinal plants, in particular, have proved to be a source of almost unlimited N‐derived structures with high molecular diversity. Because of their intrinsic potential for use in both biomedical and agricultural applications, there is a general need for new compounds and for the synthesis of ‘natural‐inspired’ analogues. Importantly, transition of a natural product from discovery to a ‘market lead’ is associated with an increasingly challenging demand for more of the compound, which cannot be met by isolation from natural plant sources, often due to low extraction yields and uneven availability of the plant source itself. Synthesis remains the most reliable approach to provide valuable products for the market. In this review, a comprehensive overview of our contribution to synthetic access to N‐derived natural products is given. Major strengths of the proposed methodologies are discussed critically. © 2019 Society of Chemical Industry     

Discovery of highly insecticidal synthetic spinosyn mimics – CAMD enabled de novo design simplifying a complex natural product

Simplifying complex natural products: Computer modeling‐based design leads to highly insecticidal, chemically simpler synthetic mimics of the spinosyn natural products that are active in the field. © 2018 Society of Chemical Industry     

Insecticidal natural products: new rocaglamide derivatives from Aglaia roxburghiana

An Erratum for this article has been published in Pest Management Science 56(5) 493 (2000). In the course of the screening for novel, naturally occurring pesticides from the plant family Meliaceae, an extract of the stem bark of Aglaia roxburghiana was found to exhibit significant insecticidal activity. In addition to rocaglamide, a known insecticide isolated from several species of the genus Aglaia, 15 new natural products were isolated from this plant. Isolation and structure elucidation of the natural products is described. The outstanding insecticidal activities of some of the compounds as well as a structure–activity relationship study are presented. © 1999 Society of Chemical Industry     

Natural products as sources of herbicides: current status and future trends

Although natural product-based discovery strategies have not been as successful for herbicides as for other pesticides or pharmaceuticals, there have been some notable successes. Phosphinothricin, the biosynthetic version of glufosinate, and bialaphos are phytotoxic microbial products that have yielded commercial herbicides. Cinmethylin, a herbicidal analogue of cineole, has been sold in Europe and Asia. The triketone herbicides are derivatives of the plant-produced phytotoxin leptospermone. These products represent only a small fraction of commercialized herbicides, but they have each introduced a novel molecular target site for herbicides. Analysis of the literature reveals that phytotoxic natural products act on a large number of unexploited herbicide target sites. The pesticide industry's natural product discovery efforts have so far concentrated on microbially derived phytotoxins, primarily from non-pathogenic soil microbes, involving the screening of large numbers of exotic isolates. Plant pathogens usually produce potent phytotoxins, yet they have received relatively little attention. Even less effort has been made to discover plant-derived phytotoxins. Bioassay-directed isolation has been the preferred method of discovery after a producing organism is selected. This laborious approach often leads to rediscovery of known compounds. Modern tandem separation/chemical characterization instrumentation can eliminate much of this problem by identification of compounds before they are bioassayed.     

Natural products in plant protection

Natural products can be used to control pests and diseases in crops. These products include anorganic compounds, but also a variety of plant extracts. In the beginning of this century active microbial extracts were discovered as well. Synthetic crop protection chemicals were developed from about 1940 onwards and sustained progress in modern agriculture. The first generation chemicals have aspecific modes of toxic action and are in many instances deleterious to the environment. The second generation chemicals have specific modes of action and meet modern environmental requirements. A disadvantage of these chemicals is the potency of target organisms to acquire resistance. This condition urged agrochemical industry to develop chemicals with new modes of action. Such chemicals can be developed by using natural bioactive products as leads in synthesis programmes. This paper decribes the progress that was made in the development of natural bioactive compounds in pest and disease control.     

Natural products in plant protection

Natural products can be used to control pests and diseases in crops. These products include anorganic compounds, but also a variety of plant extracts. In the beginning of this century active microbial extracts were discovered as well. Synthetic crop protection chemicals were developed from about 1940 onwards and sustained progress in modern agriculture. The first generation chemicals have aspecific modes of toxic action and are in many instances deleterious to the environment. The second generation chemicals have specific modes of action and meet modern environmental requirements. A disadvantage of these chemicals is the potency of target organisms to acquire resistance. This condition urged agrochemical industry to develop chemicals with new modes of action. Such chemicals can be developed by using natural bioactive products as leads in synthesis programmes.This paper decribes the progress that was made in the development of natural bioactive compounds in pest and disease control.     

几种野生植物提取物对烟草花叶病毒病生物活性初报

利用天然物进行病虫害防治自古有之。天然活性物质的研究是农药研究的一个重要组成部分[1～3]。中国野生植物资源非常丰富,给从事此项工作的科研人员提供了得天独厚的条件。我们在北京郊区采集野生植物并经鉴定,在试验中作者发现:紫菀、茜草、风毛菊、盘果菊、瓦松、苦参、香薷的提取物在不同程度上表现出抗病毒、抑菌及植物生长调节活性。目前植物抗病毒剂难以满足生产需要,开发高效抗病毒剂势在必行。本文报道部分研究结果。1　材料与方法1.1　试验材料供试植物　采于北京郊区,经本校植物教研室鉴定为下列植物:苦参(SophoraflavesenceAit…     

Manufacture of optically active materials: An agrochemicals perspective

Against a background of the growing importance of single enantiomer agrochemicals, practical technologies for their production are reviewed. Methods range from extraction of natural products through to asymmetric synthesis and encompass physical, chemical and biological techniques.     

Plant-derived natural products exhibiting activity against formosan subterranean termites (Coptotermes formosanus)

The Formosan subterranean termite, Coptotermes formosanus Shiraki, is among the most devastating termite pests. Natural products derived from plant extracts were tested in a discovery programme for effective, environmentally friendly termite control agents. Among the natural products tested, vulgarone B (isolated from Artemisia douglasiana Besser), apiol (isolated from Ligusticum hultenii (Fern.) Calder & Taylor) and cnicin (isolated from Centaurea maculosa Lam.) exhibited significantly higher mortalities than in untreated controls in laboratory bioassay. These compounds are present at high levels in their respective plant sources and also possess other biological activities such as phytotoxic and antifungal properties.     

天然产物防治果蔬采后病害研究进展

果蔬采后病害的防治正朝着安全、环保的方向发展,各种生物防治方法成为研究的热点,天然产物用于控制果蔬采后病害的研究也受到了越来越多的关注。本文综述了风味化合物、精油、乙酸、茉莉酸类化合物、芥子油甙、蜂胶、植物提取物、壳聚糖、醋酸瓜类萎蔫醇等天然产物在果蔬采后病害防治中的研究、开发与应用,为未来的商业化开发提供新的思路。     

新疆的旅游资源及其开发利用

本文从自然风光、名胜古迹及灿烂文化与风俗民情和土特产品等方面来介绍新疆的主要旅游资源;并根据地域特点,提出了区域开发利用规划建议。     

The use of entomopathogenic fungi for the control of stored-grain insects

The present contribution discusses the recent advances in the biological control of stored-grain insects with entomopathogenic fungi (EF). Thus, the effect of formulated vs. unformulated strains of EF and the effect of combinations of EF with other components, i.e. diatomaceous earths (DEs), chemical insecticides, natural products and natural enemies against stored-product insects are reviewed. Very few formulations of EF strains have been developed and used, of which invert emulsion formulation (water-in-oil type) is considered the most important. A synergistic effect of EF is produced by combining them with DEs, chemical insecticides and natural products but not with natural enemies belonging to arthropods. Moreover, since the action of EF against insect pests in general, and stored-grain insects in particular, is compatible with the food safety and environmental regulations, a good perspective for these biocontrol agents is expected as alternatives to synthetic insecticides. The potential areas of future research on the effective use of EF as biocontrol agents of stored-grain insects and the constraints that are associated with the registration and commercialization of EF as biopesticides under storage conditions are also discussed. Suggestions for the possible ways for implementation of this technology in storage systems are also provided in the present study.     

Pesticidal compounds from higher plants

Higher plants offer an excellent source of biologically active natural products. Over the centuries numerous plants have been exploited as sources of insecticides, but nowadays traditional botanical insecticides play only a minor role in world agriculture. Nevertheless, plant natural products still have enormous potential to inspire and influence modern agrochemical research. Few plant natural products will ever reach the market as products per se, but others will provide lead structures for programmes of synthetic chemistry and hopefully follow the success story of the synthetic pyrethroids. Structurally complex compounds, which are not amenable to synthetic chemistry programmes, may also have a role to play by validating new modes of action for pesticides. Examples are presented of compounds exhibiting insecticidal, fungicidal and herbicidal effects. Consideration is also given to the development of screening programmes to detect new compounds with interesting biological properties. Careful experimental design and thorough recording of procedures and data are crucial to success. Badly designed programmes afford only weakly active compounds or show effects which cannot be reproduced at a later date. Natural product chemistry, whether based on higher plants, micro-organisms or other sources, is a very difficult science, but there is little doubt that dedicated research will eventually be rewarded with exciting new lead structures for industrial application.     

Natural product chemistry and its part in the defence against insects and fungi in agriculture†

This paper surveys our work on natural products as potential models for defensive substances against insect and fungal predators. Insecticides and repellents included are pyrethrins, rotenoids, lipid amides, phorbol esters, cordifolia germacranolides, nicandrenoids, mammeins, dihydroagarofuran esters, and cembrene diols. The fungal H-S toxins from Alternaria, and avenacins from oat roots are briefly considered. The avenacins provide an in-situ defence of oat roots against the destructive ‘Take-all’ fungus disease. © 1999 Society of Chemical Industry     

United States Department of Agriculture-Agricultural Research Service research on natural products for pest management

Recent research of the Agricultural Research Service of USDA on the use of natural products to manage pests is summarized. Studies of the use of both phytochemicals and diatomaceous earth to manage insect pests are discussed. Chemically characterized compounds, such as a saponin from pepper (Capsicum frutescens L), benzaldehyde, chitosan and 2-deoxy-D-glucose are being studied as natural fungicides. Resin glycosides for pathogen resistance in sweet potato and residues of semi-tropical leguminous plants for nematode control are also under investigation. Bioassay-guided isolation of compounds with potential use as herbicides or herbicide leads is underway at several locations. New natural phytotoxin molecular target sites (asparagine synthetase and fructose-1,6-bisphosphate aldolase) have been discovered. Weed control in sweet potato and rice by allelopathy is under investigation. Molecular approaches to enhance allelopathy in sorghum are also being undertaken. The genes for polyketide synthases involved in production of pesticidal polyketide compounds in fungi are found to provide clues for pesticide discovery. Gene expression profiles in response to fungicides and herbicides are being generated as tools to understand more fully the mode of action and to rapidly determine the molecular target site of new, natural fungicides and herbicides.     

Natural products: a strategic lead generation approach in crop protection discovery

With the anticipated population growth in the coming decades, the changing regulatory environment, and the continued emergence of resistance to commercial pesticides, there is a constant need to discover new lead chemistries with novel modes of action. We have established a portfolio of approaches to accelerate lead generation. One of these approaches capitalizes on the rich bioactivity of natural products (NPs), highlighted by the numerous examples of NP‐based crop protection compounds. Within Corteva Agriscience and the affiliated preceding companies, NPs have been a fruitful approach, for nearly three decades, to identifying and bringing to the market crop protection products inspired by or originating from NPs, . Included in these NP‐based crop protection products are the spinosyns family of insecticides, and those from more recent areas of NP‐based fungicidal chemistry, as highlighted in this perspective. © 2019 Society of Chemical Industry     

Activity of the botanical aphicides 1,5‐diphenyl‐1‐pentanone and 1,5‐diphenyl‐2‐penten‐1‐one on two species of Aphididnae

1,5‐Diphenyl‐1‐pentanone (A) and 1,5‐diphenyl‐2‐penten‐1‐one (B) are natural products extracted for the first time from Stellera chamaejasme. Laboratory bioassay showed that the two products have strong contact activity and very good anti‐feedant activity against Aphis gossypii and Schizaphis graminum. Both products showed dose‐dependent relationships for both forms of activity against the two aphids, the contact activity of B being about twice that of A. Both products were inferior to methomyl in contact activity but superior in anti‐feedant activity against the two aphids. This is the first report of aphicidal activity in these two compounds, which may represent a new class of aphicide. © 2001 Society of Chemical Industry     

天然除草活性化合物研究进展

综述了近年来国内外从天然产物中开发具有除草活性化合物的研究概况,着重介绍一些可能具有除草剂开发潜力的植物和微生物源化合物,并对生物除草剂的发展前景进行了展望.