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.     

生物防治——害虫综合防治的重要内容

本文阐述了生物防治在综合防治中的重要性和如何全面正确认识生物防治技术。指出生物防治技术在生产上的成功应用,必须要注意与其他植保技术协调。文章还介绍了国内外成功的生防实例和生防必须遵循的基本原则。     

Natural products as pesticides: Two examples of stereoselective synthesis

The strategy and synthetic efforts leading to efficient stereoselective syntheses of thiangazole, a tris-thiazolinyl-oxazole metabolite isolated from Polyangium spp., and of hydantocidin, a spironucleoside metabolite isolated from Streptomyces hygroscopicus, are discussed.     

Perspective: present pesticide discovery paradigms promote the evolution of resistance – learn from nature and prioritize multi‐target site inhibitor design

For many years, the emphasis of industry discovery programs has been on finding new target sites of pesticides and finding pesticides that inhibit single targets. There had been an emphasis on genomics in finding single targets for potential pesticides. There is also the claim that registration of single target inhibiting pesticides is simpler if the mode of action is known. Conversely, if one looks at the evolution of resistance from an epidemiological perspective to ascertain which pesticides have been the most recalcitrant to evolutionary forces, it is those that have multiple target sites of action. Non‐target‐site resistances can evolve to multi‐target‐site inhibitors, but these resistances can often be overcome by structural modification of the pesticide. Industry has looked at pest‐toxic natural products as pesticide leads, but seems to have abandoned those where they can find no single target of action. Perhaps nature has been intelligent and evolved many natural products that are synergistic multi‐target‐site inhibitors, and that is why natural compounds have been active for millennia? We should be learning from nature while combining new chemistry technologies with vast accrued databases and computer aided design allowing fragment‐based discovery and scaffold hopping to produce multi‐target site inhibitors instead of single target pesticides. © 2019 Society of Chemical Industry     

Direct and indirect impacts of integrated pest management on pesticide use: a case of rice agriculture in Java, Indonesia

BACKGROUND: Integrated pest management (IPM) technology has been disseminated since 1989 in Indonesia to cut down pesticide use, but the adoption and diffusion of the technology are still debated. This study aims to estimate the models of demand for pesticides and to analyse the impact of IPM technology on pesticide use. Aggregate cross-section time series data from 1990-1998 are used.RESULTS: The results show that IPM technology reduces the use of pesticides by improving the process of rice production, such that pesticides are more efficiently used. In this case, the IPM technology is not a pest control technique.CONCLUSION There is an indication that IPM technology has been adopted by farmers. This is evidence that the IPM programme in Indonesia was successful in this area. Copyright (c) 2008 Society of Chemical Industry.     

微生物及其天然产物防治杂草的发展及展望

概述了利用微生物及其天然产物防治杂草的潜在优势和研究进展，介绍已商品化和具有开发潜力的微生物除草剂及具有除草活性的微生物天然植物毒素。     

Natural heritage values and comparative analyses of Kanas, China

Kanas is a National Nature Reserve and National 5A Scenic Area,and it is also high on China’s National Natural Heritage List. In this paper,with an integrated analysis and comparative geo-graphical approach,the genesis and current features of the Kanas landscape are analyzed systematically according to the criteria for outstanding universal values that must be met for designation by the United Nations as World Natural Heritage. It is concluded that Kanas has outstanding universal values in geosciences,biology and aesthetics. Through comparison with other World Natural Heritage sites of the same geological types,in the same biogeographic zone and in the same latitude,it is concluded that Kanas meets criteria vii,viii,ix and x for designation as World Natural Heritage. Thus,this work establishes a scientific foundation for nomination of Kanas for such a status.     

Insect peptide hormones: a selective review of their physiology and potential application for pest control

Our knowledge on primary structure, synthesis, release, receptor binding, structure-activity relationships, mode of action and degradation of, mainly, neuropeptides from insects has increased dramatically during the last 10 years or so. Here, five case studies are presented, which deal selectively with effects on: reproduction (trypsin modulating oostatic factor in mosquito); energy metabolism, locomotion and the immune system (adipokinetic hormones); water and ion balance, and feeding behaviour (diuretic hormones, kinins, sulfakinins); sex attraction (pheromone biosynthesis activating neuropeptide); and growth and development, and muscle activity (allatostatins). The literature is reviewed in the context of how the knowledge on neuropeptides has been and can be used for the design of novel, safe and selective compounds to control pest insects in the foreseeable future.     

Single and simultaneous exposure of acetylcholinesterase to diazinon, chlorpyrifos and their photodegradation products

In vitro inhibition of electric eel acetylcholinesterase (AChE) by single and simultaneous exposure to organophosphorus insecticides diazinon and chlorpyrifos, and their transformation products, formed due to photoinduced degradation, was investigated. Increasing concentrations of diazinon, chlorpyrifos and their oxidation products, diazoxon and chlorpyrifos-oxon, inhibited AChE in a concentration-dependent manner. IC₅₀ (20 min) values, obtained from the inhibition curves, were (in mol/l): (5.1 ± 0.3) × 10⁻⁸, (4.3 ± 0.2) × 10⁻⁶ and (3.0 ± 0.1) × 10⁻⁸ for diazoxon, chlorpyrifos and chlorpyrifos-oxon, respectively, while maximal diazinon concentration was lower than its IC₅₀ (20 min). Calculated K_I values, in mol/l, of 7.9 × 10⁻⁷, 9.6 × 10⁻⁶ and 4.3 × 10⁻⁷ were obtained for diazoxon, chlorpyrifos and chlorpyrifos-oxon, respectively. However, 2-isopropyl-4-methyl-6-pyrimidinol (IMP) and 3,5,6-trichloro-2-pyridinol, diazinon and chlorpyrifos hydrolysis products, did not noticeably affect the enzyme activity at all investigated concentrations. Additive inhibition effect was achieved for lower concentrations of the inhibitors (diazinon/diazoxon ?1 × 10⁻⁴/1 × 10⁻⁸ mol/l i.e., chlorpyrifos/chlorpyrifos-oxon ?2 × 10⁻⁶/3 × 10⁻⁸ mol/l), while an antagonistic effect was obtained for all higher concentrations of the organophosphates. Inhibitory power of 1 × 10⁻⁴ mol/l diazinon irradiated samples can be attributed mostly to the formation of diazoxon, while the presence of non-inhibiting photodegradation product IMP did not affect diazinon and diazoxon inhibitory efficiencies.     

Challenges and opportunities of unmanned aerial vehicles as a new tool for crop pest control

The application of pesticides is not simply delivering chemicals to the target area. It also involves considering the negative aspects and developing strategies to deal with them during the application process, to ensure the maximization of pesticides use efficiency and the maintenance of the ecosystem. Unmanned aerial vehicle (UAV) sprayers demonstrate unique advantages compared to traditional ground sprayers, particularly in terms of maneuverability and labor intensity reduction, showed great potential for chemical application in pest control. It is undeniable that there exist challenges in the practice of UAV spraying, such as higher potential risks of pesticide drift or pathogen transmission, uncertainty canopy deposition for different crops, and unexpected leaf breakage induced by downwash flow. Maximizing the utilization of downwash flow while avoiding lateral air movement outside the intended target crop area is a major issue for chemical application with UAV sprayers, particularly in light of the increasingly apparent consensus on the need for enhanced environmental protection during the chemical application process. It must be considered that the operation strategy in different scenarios and for different crop targets is not the same, unique requirements should be given on nozzle atomization, flight parameters, adjuvants and aircraft types in specific working situations. In future, the implementation of spray drift prediction, technical procedures development, and other solutions aimed at reducing pesticide drift and improving deposition quality, is expected to promote the adoption of UAV sprayers by more farmers. © 2023 Society of Chemical Industry.     

特用玉米及其病虫害发生与防治对策

我国玉米种植结构处于调整阶段 ,随着包括高油玉米、优质蛋白玉米、甜玉米和糯玉米等一系列特用玉米的发展 ,玉米病虫害发生危害规律也将随之发生变化。本文就我国玉米生产的现状、特用玉米发展与病虫害发生趋势进行了分析 ,并提出了防治对策。     

超级杂交中稻主要病虫药剂防治新技术

2006—2007年,在桃江县稻瘟病重发区应用超级杂交中稻主要病虫药剂防治新技术防治两优0293大田生育期主要病虫试验,结果表明：该技术可有效防控超级杂交中稻主要病虫危害,对大部分病虫防效好于常规施药技术,且比常规施药技术减少农药用量42.38%～68.59%、增产2.46%～118.00%;其中施用52.5%丙环唑•三环唑悬乳剂处理对稻瘟病的防效高、增产增效明显。     

IPM program development for an invasive pest: coordination, outreach and evaluation

BACKGROUND: Spotted wing drosophila (SWD), Drosophila suzukii Matsumura, was found along the west coast of the United States, beginning in 2008 and 2009, infesting a wide variety of small and stone fruit crops. This pest is a serious economic threat, as noted in its native range (Asia), because it lays eggs within ripening fruit before harvest, leading to crop loss. The aim of this paper is to describe the process in order to create collaboration, communication routes and evaluation methods in response to a new invasive pest. RESULTS: Funding was secured and a program (SWD*IPM) was quickly developed to address social, economic and biological components. Communication routes were outlined, and a stakeholder advisory panel was established to guide program objectives. A central website was created to host up‐to‐date information. An online monitoring and mapping program for D. suzukii in Oregon fruit‐growing regions illustrated the range, distribution and seasonal abundance of the pest. In addition, a program for backyard fruit growers was initiated to examine citizen scientists' roles in managing D. suzukii infestations in the urban setting. A monitoring kit, laminated educational cards, dry fly mounts and quick‐time videos were some of the tools used to educate growers. First‐year challenges for dealing with a new pest are discussed. CONCLUSION: The discovery and subsequent response to an exotic pest is information intensive and requires a well‐planned, coordinated Extension and evaluation effort. Copyright © 2011 Society of Chemical Industry     

Insecticidal activity of 23 essential oils and their major compounds against adult Lipaphis pseudobrassicae (Davis) (Aphididae: Homoptera)

Essential oils from 23 species of plants comprising 14 genera and 4 plant families were obtained by Clevenger-type water distillation. The major compounds in these essential oils were identified with GC-MS and their insecticidal activity against adult turnip aphids, Lipaphis pseudobrassicae (Davis), tested with dosage-mortality bioassays. We examined mortality only for viviparous adults because sizeable aphid populations on crucifer (Brassicaceae) hosts are largely produced by these wingless, parthenogenic females. Twenty-two of the oils were directly applied to aphid females in randomized blocks at concentrations of 0.0, 1.0, 2.5, 5.0 and 10.0 mg ml(-1). Essential oils mixed with a non-toxic emulsifying agent, dimethyl sulfoxide (DMSO), more easily penetrated the waxy insect cuticle. Probit analysis and LC(50) at three different exposures showed aphids were quickly incapacitated and killed by aliphatic aldehydes, phenols and monocyclic terpenes contained in Bifora and Satureja oils and at applied concentrations as low as 0.3 to 1.0 mg ml(-1). Only enough Pimpinella isaurica oil and its three phenylpropanoid fractions were available for testing at a single concentration of 10 mg ml(-1). We could not spare any additional P. isaurica oil for testing at other concentrations. Phenylpropanoids isolated from P. isaurica oil when recombined or left naturally blended in the oil were highly bioactive against L. pseudobrassicae at 10 mg ml(-1).     

Avermectins,a novel class of compounds: implications for use in arthropod pest control

对阿维菌素B_2a进行结构优化,在阿维菌素B_2a的C4\     

天然产物对红火蚁的生物活性研究进展

红火蚁是一种极具危险性的入侵物种,在入侵区给人民群众的身体健康带来严重威胁。目前主要利用人工合成的化学药剂防治红火蚁。然而,长期大量使用化学药剂会导致红火蚁产生耐药性和破坏生态环境等不良影响。近年来,越来越多的研究发现天然产物对红火蚁具有良好的触杀、驱避和熏蒸作用。本文就天然产物对红火蚁的生物活性及其开发为饵剂、触杀型药剂和驱避剂等的潜力以及应用效果进行简要总结与讨论,以期为红火蚁的绿色防控提供参考。     

Integrated pest management of coffee for small-scale farmers in East Africa: needs and limitations

Coffee in East Africa (Kenya, Tanzania and Uganda) is an important cash and export crop for small-scale farmers. The crop suffers heavy yield losses due to damage caused by a wide range of indigenous pests (insects, diseases, nematodes and weeds). Current recommended pest control measures include a combination of cultural, resistant/tolerant cultivars and the use of broad spectrum chemical pesticides. Chemical pesticides are far more popular at the farm level than any of the other recommended pest control measures. Coffee pest control strategies are often aimed at individual pests with little consideration of the implications for the total coffee pest complex and its agro-ecosystem. This unilateral approach has resulted in increased pest pressure on coffee and some of its companion crops, outbreak of new pests of coffee, development of pest strains resistant to the cheap and commonly available chemical pesticides, increased environmental problems, increased health risks to man and livestock and an overall increase in the costs of coffee production, thus forcing many farmers to neglect their coffee plantations. Measures to alleviate the above problems, particularly the high production costs, are needed to improve coffee production and increase the cash return to the small-scale farmer. Integrated pest management (IPM) offers the best prospects for solving the above problems. However, lack of national IPM policies, poor extension systems, inefficient research-extension-farmer linkage and the lack of a holistic approach will delay the development and implementation of appropriate, acceptable and sustainable IPM practices.     

Fungicidal potential of methoxylated flavones from citrus for in vitro control of Colletotrichum gloeosporioides, causal agent of anthracnose disease in tropical fruits

Four polymethoxylated flavones (3,5,6,7,3',4'-hexamethoxyflavone, 3,5,6,7,8,3',4'-heptamethoxyflavone, 5,6,7,8,4'-pentamethoxyflavone and 5,6,7,8,3',4'-hexamethoxyflavone) were isolated and characterized from cold-pressed orange oil. Their antifungal activities were evaluated against Colletotrichum gloeosporioides (Penz) Penz & Sacc, a major plant pathogen of fruits that causes significant damage to crops in tropical, sub-tropical and temperate regions. Methoxylated flavones were effective in inhibiting mycelial growth of the fungus. As flavone concentration increased, mycelial growth decreased. 5,6,7,8,3',4'-Hexamethoxyflavone completely inhibited the growth of Cgloeosporioides at a concentration of 100 microg ml(-1).     

Effect of the combined treatment of insecticides and an attractant for the control of Phloeotribus scarabaeoides,a pest of Olea europea

Different insecticides have been tested for the control of the olive bark beetle, Phloeotribus scarabaeoides Bern. This scolytid can be managed at two points in its biological cycle: in pruned logs, where it excavates reproduction galleries, or in living trees, after emergence from the logs, where it digs feeding galleries. In mortality laboratory bioassays, the efficiency of organophosphorus insecticides has been ranked as follows: chlorpyrifos + dimethoate < formothion < methidathion. Formothion and methidathion, the two most efficient, were sprayed on olive logs together with a pyrethroid insecticide, deltamethrin, and a formulation which combined an organophosphorus (fenitrothion) and a pyrethroid (cypermethrin) insecticide. Deltamethrin inhibited the excavation of new reproduction galleries and induced a repellent effect on the olive pest. In contrast, none of the organophosphorus insecticides or the combination, fenitrothion + cypermethrin, were able to control the olive bark beetle. In olive trees, deltamethrin controlled this olive pest without showing the repellent effect observed for logs. Ethylene, a plant hormone, has been reported as an attractant for the olive bark beetle. The use of dispensers which released ethylene increased the number of P. scarabaeoides approaching the treated olive trees, thus favouring its use in a lure-and-trap control system.