Pesticidal natural products – status and future potential

There is a long history of using natural products as the basis for creating new pesticides but there is still a relatively low percentage of naturally derived pesticides relative to the number of pharmaceuticals derived from natural sources. Biopesticides as defined and regulated by the US Environmental Protection Agency (EPA) have been around for 70 years, starting with Bacillus thuringiensis, but they are experiencing rapid growth as the products have got better and more science‐based, and there are more restrictions on synthetic chemical pesticides. As such, biopesticides are still a small percentage (approximately US$3–4 billion) of the US$61.3 billion pesticide market. The growth of biopesticides is projected to outpace that of chemical pesticides, with compounded annual growth rates of between 10% and 20%. When integrated into crop production and pest management programs, biopesticides offer the potential for higher crop yields and quality than chemical‐only programs. Added benefits include reduction or elimination of chemical residues, therefore easing export, enabling delay in the development of resistance by pests and pathogens to chemicals and shorter field re‐entry, biodegradability and production using agricultural raw materials versus fossil fuels, and low risk to non‐target organisms, including pollinators. Challenges to the adoption of biopesticides include lack of awareness and education in how to deploy their unique modes of action in integrated programs, testing products alone versus in integrated programs, and lingering perceptions of cost and efficacy. © 2019 Society of Chemical Industry     

Biopesticides – towards increased consumer safety in the European Union

The introduction of new food safety regulations in the European Union has resulted in the withdrawal of many synthetic active substances used in plant protection products, in light of their potential or actual harmful effect on human and animal health, as well as on the environment. Alternatives to these compounds are being developed – naturally occurring pesticides, also referred to as biopesticides. The use of biopesticides in crop protection leads to decreased levels of pesticide residues in foods, and as a result to lower risk levels for the consumer. Biologically active agents defined as biopesticides are varied, and therefore application of the same environmental and consumer safety criteria to all of them is impossible. This presents serious complications in the approval of these pesticides as active plant protection products and in their registration. It needs to be stressed that, in the registration procedure of the European Union, biopesticides are subject to the same regulations as synthetic active substances. This situation has resulted in the need to introduce numerous new provisions in the legislation, as well as the preparation of new guidelines facilitating the registration of biopesticides. These activities aim to promote naturally originating pesticides. © 2014 Society of Chemical Industry     

Biopesticide based sustainable pest management for safer production of vegetable legumes and brassicas in Asia and Africa

Vegetables are one of the important crops which could alleviate poverty and malnutrition among the smallholder farmers in tropical Asia and Africa. However, a plethora of pests limit the productivity of these crops, leading to economic losses. Vegetable producers overwhelmingly rely on chemical pesticides in order to reduce pest‐caused economic losses. However, over‐reliance on chemical pesticides poses serious threats to human and environmental health. Hence, biopesticides offer a viable alternative to chemical pesticides in sustainable pest management programs. Baculoviruses such as nucleopolyhedrovirus (NPV) and granulovirus (GV) have been exploited as successful biological pesticides in agriculture, horticulture and forestry. Maruca vitrata multiple nucleocapsid NPV (MaviMNPV) was found to be a unique baculovirus specifically infecting pod borer on food legumes, and it has been successfully developed as a biopesticide in Asia and Africa. Entomopathogenic fungi also offer sustainable pest management options. Several strains of Metarhizium anisopliae and Beauveria bassiana have been tested and developed as biopesticides in Asia and Africa. This review specifically focuses on the discovery and development of entomopathogenic virus and fungi‐based biopesticides against major pests of vegetable legumes and brassicas in Asia and Africa. © 2019 Society of Chemical Industry     

Botanical Pesticides and Their Mode of Action

Pest management is facing economic and ecological challenge worldwide due to human and environmental hazards caused by majority of the synthetic pesticide chemicals. Identification of novel effective insecticidal compounds is essential to combat increasing resistance rates. Botanical pesticides have long been touted as attractive alternatives to synthetic chemical pesticides for pest management because botanicals reputedly pose little threat to the environment or to human health. The body of scientific literature documenting bioactivity of plant derivatives to arthropod pests continues to expand, yet only a handful of botanicals are currently used in agriculture in the industrialized world, and there are few prospects for commercial development of new botanical products. Pyrethrum and neem are well established commercially, pesticides based on plant essential oils have entered the marketplace, and the use of rotenone appears to be waning. A number of plant substances have been considered for use as pest antifeedants, repellents and toxicants, but apart from some natural mosquito repellents, a little commercial success has ensued for plant substances that modify arthropod behavior. Several factors appear to limit the success of botanicals, most notably regulatory barriers and the availability of competing products (newer synthetics and fermentation products) that are cost-effective and relatively safe compared with their predecessors. In the context of agricultural pest management, botanical pesticides are best suited for use in organic food production in industrialized countries but can play a much greater role in the production and postharvest protection of food in developing countries. Botanicals have been in use for a long time for pest control. The compounds offer many environmental advantages. However, their uses during the 20th century have been rather marginal compared with other bio-control methods of pests and pathogens. Improvement in the understanding of plant allelochemical mechanisms of activity offer new prospects for using these substances in crop protection. I’m trying in this article to present different kinds of botanical pesticides came from different recourses and their mode of actions as well as I will try to examine the reasons behind their limited use (disadvantages) and the actual crop protection developments involving biopesticides of plant origin for organic or traditional agricultures to keep our environment clean and safer for humankind and animals.     

Regulatory problems associated with natural products and biopesticides

For registration, the United States Environmental Protection Agency (USEPA) separates pesticides into conventional chemical pesticides and biochemical and microbial pesticides. Natural products generally fall into the latter category. The USEPA has specified the test requirements for registration in the United States in the guidelines for registration of biorational pesticides (Subdivision M of 40 CFR Part 158). A discussion of the regulatory issues requires some reference to the accompanying scientific developments. The potential application of chemicals that affect insect behavior and development appeared an extremely promising approach to the reduction of adverse environmental and health impacts associated with many conventional pesticides. In addition to these benefits, the new biopesticides generally affected a very specific range of target species. However, although juvenile hormones and semiochemicals offer exciting new approaches to pest control, and are potentially valuable components of pest management strategies, acceptance of these techniques has been slow. Commercial development has been difficult for several reasons. Regulatory requirements may appear burdensome. Unconventional pest-control technologies may call for special formulations or application equipment. It may not be easy to establish the efficacy of non-lethal potential techniques. Investigators who derive funds from the public sector may have neither responsibility nor resources to carry the technology beyond the experimental stage. Because most activities in this field have been heavily research-oriented, few workers have possessed the additional resources to obtain safety data or data to satisfy regulatory requirements. Difficulties in preparing and administering guidelines for registration of biopesticides lie in the novelty of the pest control agents and the diversity of the techniques involved in their effective use. Rapid advances in molecular biology and other disciplines continually strain the capabilities of regulators who are responsible for making safety assessments regarding pest-control agents. Although regulatory authorities are familiar with conventional pesticides, safety assessment of biopesticides calls for totally different approaches.     

Potential of biopesticides in agriculture

All living organisms are subject to predation, parasitism or competition from other organisms. The study of these interactions has led to the identification of many potential opportunities for the use of living organisms as biopesticides to protect agricultural crops against insect pests, fungal, bacterial and viral diseases, weeds, nematodes and mollusc pests. A range of biopesticide products (including as active agents bacteria, fungi, nematodes, protozoa, viruses and beneficial insects) are now available commercially for control of insect pests, fungal and bacterial diseases and weeds. However, world biopesticide sales in 1990 were estimated to be $120 million, representing less than 0–5% of the world agrochemical market. Over 90% of biopesticide sales are represented by a single product type, containing Bacillus thuringiensis Berl., for control of insect pests. Nevertheless, biopesticide sales are estimated to be increasing at 10–25% per annum whilst the world agrochemical market is static or even shrinking. There has been a significant renewal of commercial interest in biopesticides as evidenced by the substantial number of alliances forged between major agrochemical companies and biotechnology companies which allow these major companies access to marketing rights to novel biopesticides. This paper reviews the current commercial status of biopesticides and discusses the technical and commercial constraints which have impeded development of biopesticides in the past. Novel developments in R&D, which may enable some of these constraints to be overcome, are examined by reference to a number of specific examples (some of which arise from the author's own experience in a biotechnology company). The future prospects for biopesticides are discussed in the light of technical advances and commercial and regulatory requirements.     

Development of an integrated pest management programme for cotton. Part 2: Integration of a lucerne/cotton interplant system,food supplement sprays with biological and synthetic insecticides

Part 1 of the paper showed that the integration of a lucerne/ cotton interplant system with supplementary food sprays retained and increased populations of predatory insects in the cotton crop. The strategic use of biopesticides (Bacillus thuringiensis (Bt), nuclear polyhedrosis virus (NPV)) reduced the use of synthetic insecticides by 50% without sacrificing cotton yield and profitability. In economic terms, the average gross margin for the IPM plot was A$3255 compared with A$3020 and A$3218 for the plots treated with (1) conventional insecticides on transgenic (Ingard®) cotton and (2) conventional insecticides on non-transgenic cotton. The use of transgenic cotton affected a 25% saving on synthetic insecticide usage. The results clearly indicate that a refined IPM approach could have a distinctive advantages in terms of economic and environmental impacts on cotton production. The success of such an approach lies in a strict adherence to its methodology.     

Improving the efficacy of nuclear polyhedrosis virus and Bacillus thuringiensis against Helicoverpa spp. with ultra-violet light protected petroleum spray oils on cotton crops in Australia

Nuclear polyhedrosis virus (NPV) and Bacillus thuringiensis (Bt) are the most commonly used biopesticides for the control of Helicoverpa spp. larvae on cotton crops in Australia. The performance of NPV and Bt against Helicoverpa spp. larvae on cotton crops, is inconsistent and at times totally unsatisfactory against high densities of Helicoverpa spp. larvae. We determined the effect of mixing petroleum spray oils, containing ultra-violet light absorbing compounds, with NPV and Bt for efficacy against Helicoverpa spp. larvae, levels of cotton plant damage, and persistence of efficacy. The study showed that the efficacy and persistence of NPV and Bt were increased when mixed with petroleum spray oil (PSO?–?Canopy®) at the rate of 2% (v/v). In the field experiments, mixing NPV with 1 and 2% (v/v) PSO, increased Helicoverpa spp. mortality from 25.9 to 31.5 and 44.8%, respectively. Similarly, the mortality caused by Bt, when mixed with 1 and 2% (v/v) PSO, was increased from 31.5 to 36.0 and 48.2%, respectively. In addition, 1 and 2% PSO mixtures with NPV increased persistence of efficacy from 1.1 to 1.6 and 2.5 days, respectively, whilst persistence of Bt was increased from 1.5 to 1.8 and 2.6 days, respectively. In another study using potted cotton plants, in which the plants were left outdoors throughout the study, the average NPV induced mortality of first instar Helicoverpa larvae was increased from 20.9% to 35.9 and 43.4% by 1 and 2% (v/v) PSO, respectively. Persistence of NPV efficacy was enhanced by 2 and 3.1 times by 1 and 2% (v/v) PSO, respectively. Similarly, Bt induced mortality of Helicoverpa larvae was increased by 1 and 2% PSO from 68.1 to 78.8 and 83.2%, respectively, and the persistence of Bt efficacy was enhanced 1.3?–?2.0 times, respectively. In a mesh house study, young cotton plants, treated with a PSO/biopesticide mixture, suffered less leaf damage than cotton plants treated with the biopesticides alone. In conclusion, the results of this study showed synergies from the combined use of UV protected PSO and NPV or Bt, against Helicoverpa spp. larvae on cotton. Such a biopesticide-PSO combinations could be a useful tool for IPM program in cotton.     

Residue behaviour of fenvalerate,tau-fluvalinate,lambda-cyhalothrin and monocrotophos in eggplant (Solanum melongena L.) fruits

The persistence patterns of three synthetic pyrethroids—fenvalerate, tau-fluvalinate, lambda-cyhalothrin—and an organophosphorus insecticide, monocrotophos, on eggplant (Solanum melongena L.) have been evaluated. The extractable residues ranged from 0.05 to 0.45, 0.01 to 0.40, 0.003 to 0.09 and 0.09 to 0.32 μg g^?1 for fenvalerate, tau-fluvalinate, lambda-cyhalothrin and monocrotophos, respectively. Fenvalerate was the most persistent among the four, followed by monocrotophos, lambda-cyhalothrin and tau-fluvalinate. The Maximum Residue Limit (MRL) of these pesticides on S. melongena has not yet been documented. The present data may be useful for establishing MRL and assessing the amount of pesticide residues in this vegetable.     

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.     

浅议生物农药取代化学农药

近年来，“生物农药”已经有了发展，但也存在一些问题，把活性成分为化学物质的植物农药，抗生素农药等视为“生物农药”，从实用角度看，似为不妥；泛透“生物农药”安全，无公害的，科学依据不足；世界环发大会（1992）提出，到2000年，“生物农药”用量要占农药60%的口号已化为泡影，因为它的依据不足，仅为一个政治号召。     

Trichoderma as a biostimulator and biocontrol agent against Fusarium in the production of cereal crops: Opportunities and possibilities

Despite technological advances in global agriculture in recent years, the problem of pathogenic fungi in the production of cereal crops continues to be an issue. Currently, the high variability of weather factors that are considered unusual for specific locations affect the growth and physiology of pathogens attacking cereal crops. One of the most common plant protection methods is the use of synthetic pesticides; however, there is growing controversy over this approach due to the build-up of pesticides in the environment and the presence of their residues in food. The purpose of this literature review is to explore the current state of knowledge regarding the potential of using Trichoderma species as a biostimulator and for the biological protection of cereal crops against pathogenic fungi. Trichoderma fungi—through mycoparasitism, antibiosis and competition for space and nutrients—help to inhibit the growth of pathogens and have a positive impact on the growth of plants, including their root system, which is considered a desirable effect during drought episodes. It has also been demonstrated that Trichoderma fungi can convert Fusarium toxins into new metabolites that can be of lower toxicity. However, the highly limited number of in vivo studies investigating the use of these fungi for biocontrol in cereal crops remains an obstacle to the commercialization of Trichoderma fungi. It appears that the determination of their effectiveness in the biocontrol of cereal crops under variable weather and climate conditions presents a considerable challenge.     

小菜蛾对苏云金杆菌制剂的抗药性及其对策

作者首次报道了我国部分地区小菜蛾对Ｂｔ制剂的抗药性问题，华南、广州、深圳一带小菜蛾对Ｂｔ制剂的抗性比扬州小菜蛾强１０～２５倍，平均１７倍，而泰国曼谷小菜蛾的抗性又比华南的抗性小菜蛾增强４０％左右。抗性小菜蛾对Ｈ１、Ｈ３、Ｈ５、Ｈ７４个常用血清型的参试菌株均较敏感；试验结果还表明，小菜蛾在Ｂｔ与化学农药之间无交互抗性。Ｂｔ与化学农药复方制剂对小菜蛾有较好的防效，已在深圳、广州等地示范推广死亡率达８１．５～９０．９％。对防治抗Ｂｔ害虫的对策本文作了讨论     

Sensitivity analyses for four pesticide leaching models

Sensitivity analyses using a one-at-a-time approach were carried out for leaching models which have been widely used for pesticide registration in Europe (PELMO, PRZM, PESTLA and MACRO). Four scenarios were considered for simulation of the leaching of two theoretical pesticides in a sandy loam and a clay loam soil, each with a broad distribution across Europe. Input parameters were varied within bounds reflecting their uncertainty and the influence of these variations on model predictions was investigated for accumulated percolation at 1-m depth and pesticide loading in leachate. Predictions for the base-case scenarios differed between chromatographic models and the preferential flow model MACRO for which large but transient pesticide losses were predicted in the clay loam. Volumes of percolated water predicted by the four models were affected by a small number of input parameters and to a small extent only, suggesting that meteorological variables will be the main drivers of water balance predictions. In contrast to percolation, predictions for pesticide loss were found to be sensitive to a large number of input parameters and to a much greater extent. Parameters which had the largest influence on the prediction of pesticide loss were generally those related to chemical sorption (Freundlich exponent nf and distribution coefficient Kf) and degradation (either degradation rates or DT50, QTEN value). Nevertheless, a significant influence of soil properties (field capacity, bulk density or parameters defining the boundary between flow domains in MACRO) was also noted in at least one scenario for all models. Large sensitivities were reported for all models, especially PELMO and PRZM, and sensitivity was greater where only limited leaching was simulated. Uncertainty should be addressed in risk assessment procedures for crop-protection products.     

两种生物农药防治菜心黄曲条跳甲的研究

黄曲条跳甲 Phyllotreta striolata 是为害十字花科蔬菜的重大害虫?本文研究了种子丸粒化包衣?拌土撒施和叶面喷雾3种施药方式下苏云金杆菌 Bacillus thuringiensis G033A和金龟子绿僵菌 Metarhizium anisopliae CQMa421对为害菜心 Brassica campestris L. ssp. chinensis var. utilis 的黄曲条跳甲的防治效果?结果表明, 采用苏云金杆菌G033A和金龟子绿僵菌CQMa421进行种子丸粒化包衣处理的菜心, 叶片受害指数分别为6.71和9.93, 显著低于对照(31.79); 拌土撒施处理的菜心, 叶片受害指数分别为19.34和24.17, 显著低于对照(65.53); 〖JP+1〗叶面喷雾处理后第3?5?7天的校正防治效果分别为58.95%/52.37%?69.56%/64.04%和81.12%/70.09%?本研究探索了菜心生产中主要害虫的生物防治技术, 研究结果将为菜心生产过程黄曲条跳甲的有效防治提供技术支撑?     

Use of neem products/pesticides in cotton pest management

Products derived from leaves and kernels of neem (Azadirachta indica A. Jussieu) are becoming popular in plant protection programmes for cotton, mainly because synthetic pesticides have several undesirable effects. Neem derived pesticides have been found to be effective and economic in controlling major cotton pests. Neem products act both as systemic and as contact poisons and their effects are antifeedant, toxicological, repellent, sterility inducing or insect growth inhibiting. Furthermore, neem products appear to be environmentally safe and IPM compatible and have the potential to be adopted on a broad scale, together with other measures, to provide a low cost management strategy.     

Review: Resistance as a concomitant of modern crop protection

This paper reviews the impact of resistance to fungicides and insecticides/acaricides on the way crop protection is practised. It is now clear that resistance can develop to virtually any crop-protection product, in any pest, fungal pathogen or even weed. As a limiting factor in crop protection, it is a fact of life. A positive side-effect is the precision with which products are used today, with increasing implementation of Integrated Pest Management (IPM) programmes. This is a vital step towards sustainability. This paper describes: past experiences; current status of resistance; how resistance management influences current crop protection practices; regulatory aspects; and the outlook for the future. It concludes that EU regulations on resistance management must be simple and workable. Chemicals will continue to have a central role in optimising yields from the world's crops, as new tools, including biotechnology, become available for crop protection and resistance management. The crop-protection industry's innovations and product stewardship programmes will contribute to sustainable agriculture. This will provide continued benefits to users, the environment and society. ©1997 SCI     

Genetically engineering better fungal biopesticides

Microbial insect pathogens offer an alternative means of pest control with the potential to wean us off our heavy reliance on chemical pesticides. Insect pathogenic fungi play an important natural role in controlling disease vectors and agricultural pests. Most commercial products employ Ascomycetes in the genera Metarhizium and Beauveria. However, their utilization has been limited by inconsistent field results as a consequence of sensitivity to abiotic stresses and naturally low virulence. Other naturally occurring biocontrol agents also face these hurdles to successful application, but the availability of complete genomes and recombinant DNA technologies have facilitated design of multiple fungal pathogens with enhanced virulence and stress resistance. Many natural and synthetic genes have been inserted into entomopathogen genomes. Some of the biggest gains in virulence have been obtained using genes encoding neurotoxic peptides, peptides that manipulate host physiology and proteases and chitinases that degrade the insect cuticle. Prokaryotes, particularly extremophiles, are useful sources of genes for improving entomopathogen resistance to ultraviolet (UV) radiation. These biological insecticides are environmentally friendly and cost‐effective insect pest control options. © 2017 Society of Chemical Industry     

2019年及近年我国农药登记情况和特点分析

总结、分析了2019年及近年我国农药登记的基本情况和特点。最近7年来,每年微毒/低毒农药登记数量与当年农药登记总量的比值,及与本年度新增登记数量的比值均持续上升,其比值的年均值分别为82.0%和93.4%;环境友好的剂型在迅速增加,悬浮剂与本年度新增产品登记数量的比值一直处于领先位置,可分散油悬浮剂的比值增长突显,乳油比值在逐年递减;杀虫剂、杀菌剂和除草剂3大类农药登记数量与本年度新增登记数量的比值趋向显著平均;低风险的新农药登记数量在不断增加,生物源农药登记数量增长稳定,5年来其有效成分和产品的年均增长率分别为9.88%和9.46%。从政策和技术上促进特色小宗作物用药登记产品数量快速增加。上述特点表明,我国农药正朝着有利于人畜健康和生态环境安全的方向发展。