Biochemical sites of insecticide action and resistance

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書誌事項

Biochemical sites of insecticide action and resistance

Isaac Ishaaya (ed.)

Springer, c2001

大学図書館所蔵 件 / 全4件

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注記

Includes bibliographical references and index

内容説明・目次

内容説明

In recent years many of the conventional methods of insect control by broad spectrum synthetic chemicals have come under scrutiny because of their unde sirable effects on human health and the environment. In addition, some classes of pesticide chemistry, which generated resistance problems and severely affected the environment, are no longer used. It is against this background that the authors of this book present up-to-date findings-relating to biochemical sites that can serve as targets for developing insecticides with selective prop erties, and as the basis for the elucidation of resistance mechanisms and countermeasures. The book consists of eight chapters relating to biochemical targets for insec ticide action and seven chapters relating to biochemical modes of resistance and countermeasures. The authors of the chapters are world leaders in pesti cide chemistry, biochemical modes of action and mechanisms of resistance. Biochemical sites such as chitin formation, juvenile hormone and ecdysone receptors, acetylcholine and GABA receptors, ion channels, and neuropeptides are potential targets for insecticide action. The progress made in recent years in molecular biology (presented in depth in this volume) has led to the iden tification of genes that confer mechanisms of resistance, such as increased detoxification, decreased penetration and insensitive target sites. A combina tion of factors can lead to potentiation of the resistance level. Classifications of these mechanisms are termed gene amplification, changes in structural genes, and modification of gene expression.

目次

Biochemical Processes Related to Insecticide Action: an Overview.- 1 Introduction.- 2 Chitin Synthesis Inhibition.- 3 Ecdysone and Juvenile Hormone Receptors.- 4 Acetylcholine Receptors.- 5 GABA and Glutamate Receptors and Ion Channels.- 6 Other Biochemical Sites.- 7 Conclusions.- References.- GABA and Glutamate Receptors as Biochemical Sites for Insecticide Action.- 1 Introduction.- 2 GABA Receptors in Mammals and Insects.- 2.1 Classification of GABA Receptors.- 2.2 Structure and Physiological Role of Insect GABA Receptors.- 2.3 Pharmacology of GABA Receptors.- 3 Summary of Effects of Convulsants and Avermectins on the GABA Receptor.- 3.1 Polychlorocycloalkanes and Related Norbornanes.- 3.2 Picrodendrin and Silphinene Natural Products.- 3.3 Fipronil and Fipronil Analogs.- 3.4 Trioxabicyclooctanes and Related Compounds.- 3.5 New Avermectins and the Mammalian GABA Receptor.- 3.6 Altered GABA Receptors in Resistance.- 3.7 Resistance to New and Experimental Insecticides.- 4 Glutamate-Gated Chloride Channels.- 4.1 Physiology, Pharmacology, and Molecular Structure.- 4.2 Effects of the Avermectins.- 4.3 New Avermectins and Their Uses.- 4.4 Target Site Resistance to the Avermectins.- 5 Conclusions.- References.- Insecticides Affecting Voltage-Gated Ion Channels.- 1 Insecticides and Ion Channels.- 1.1 Scope and Aim.- 1.2 Voltage-Gated Ion Channels.- 2 Industrial Insecticides Targeting Ion Channels.- 2.1 Insecticides of the Voltage-Gated Sodium Channels.- 2.2 Insecticides of the Potassium and Calcium Channels.- 3 The Functional Diversity of Insecticides.- 3.1 Multiplicity of Effects.- 3.2 Distinction Between Mammals and Insects.- 4 Neurotoxic Polypeptides.- 4.1 Animal Group Specificity.- 4.2 Insect-Selective Neurotoxins Affecting the Voltage-Gated Sodium Channels.- 4.2.1 Scorpion Venom Toxins.- 4.2.2 Spider Venom Toxins.- 4.3 Insect-Selective Neurotoxins Affecting the Voltage-Gated Calcium Channel.- 5 Recombinant Baculovirus Bioinsecticides.- 6 Allosteric Coupling and Allosteric Antagonism.- References.- Acetylcholine Receptors as Sites for Developing Neonicotinoid Insecticides.- 1 Introduction.- 2 Insect Nicotinic Acetylcholine Receptors.- 2.1 Structure.- 2.2 Diversity.- 3 Compounds Acting on the Nicotinic Acetylcholine Receptor.- 3.1 Radioligand Binding Studies.- 3.2 Neonicotinoids.- 3.2.1 Imidacloprid and Related Structures.- 3.2.2 Mannich Adducts as Experimental Pro-Neonicotinoids.- 4 Electrophysiological Considerations.- 4.1 Whole Cell Voltage Clamp of Native Neuron Preparations.- 4.1.1 Correlation Between Electrophysiology and Radioligand Binding Studies.- 4.2 Agonists vs. Antagonists.- 4.3 Receptor Subtypes in Locusta migratoria.- References.- Ecdysteroid and Juvenile Hormone Receptors: Properties and Importance in Developing Novel Insecticides.- 1 Introduction.- 2 Ecdysteroids.- 2.1 Biology, Endocrinology and Molecular Biology.- 2.2 Receptors and Other Target Sites.- 2.3 Non-Steroidal Ecdysone Analogs and Their Mode of Action.- 2.4 Receptor-Based Screening Assays.- 2.5 Future Directions.- 3 Juvenile Hormone.- 3.1 Biology, Endocrinology and Molecular Biology.- 3.2 Receptors and Other Target Sites.- 3.3 JH Analogs and Their Modes of Action.- 3.4 Receptor-Based Screening Assays.- 3.5 Future Directions.- References.- Imaginal Discs and Tissue Cultures as Targets for Insecticide Action.- 1 Introduction.- 2 Imaginal Discs as Targets of Insect Hormones in Vivo and in Vitro.- 3 Insecticide Action in Vitro: Juvenile Hormone Mimics.- 4 Insecticide Action in Vitro: Chitin Synthesis Inhibitors.- 4.1 Organ Cultures.- 4.2 Cell Lines.- 5 Insecticide Action in Vitro: Ecdysteroid Agonists.- 5.1 Organ Cultures.- 5.2 Cell Lines.- References.- Insect Neuropeptide Antagonists: a Novel Approach for Insect Control.- 1 Introduction.- 2 Backbone Cyclic Neuropeptide-Based Antagonist (BBC-NBA) Approach.- 2.1 Determination of the Active Sequence in the Neuropeptide.- 2.2 Development of a Competitive Lead Antagonist.- 2.3 Improvement of the Antagonistic Activity by Conformational Constraint.- 2.4 Backbone Cyclization: a Tool for Imposing Conformational Constraint on Peptides.- 2.5 Cycloscan: Conformationally Constrained BBC Peptide Libraries.- 3 Pheromone Biosynthesis Activating Neuropeptide.- 4 Implementation of the BBC-NBA Strategy to the Pyrokinin/PBAN Family.- 5 Conversion of Neuropeptide Antagonists into Insecticide Prototypes.- 6 Concluding Remarks.- References.- Ion Balance in the Lepidopteran Midgut and Insecticidal Action of Bacillus thuringiensis.- 1 Introduction.- 2 Pathogenesis.- 3 Dependence of Host and Pathogen on Midgut pH.- 4 Midgut K+ and H+ Regulation.- 4.1 The K+ Pump.- 4.2 The 2K+/1ATP Model for Midgut Alkalization.- 4.3 The 1K+/1ATP Model for Midgut Alkalization.- 4.4 Transmembrane and Transepithelial Ion Gradients.- 5 Disruption of Midgut Ion Homeostasis by Bacillus thuringiensis.- 5.1 In Vivo Changes.- 5.2 In Vitro Changes.- 5.3 What is the Source of the Elevated Hemolymph K+?.- 5.4 Larval Paralysis and Mortality Factors.- 5.5 ?-Endotoxin Effects on K+-Dependent Uptake of Amino Acids.- 5.6 Correlating ?-Endotoxin Effects on the Isolated Midgut with Insecticidal Activity.- 6 Receptor Binding and Ion-Channel Formation.- 6.1 Receptor Binding.- 6.2 Ion-Channel Formation in Artificial Membranes and BBMVs.- 6.3 Insect Cell Lines as Proxies for Midgut Cells In Vivo.- 7 Membrane Insertion and Pore Formation.- 8 Conclusions and Thoughts.- References.- Evolution of Amplified Esterase Genes as a Mode of Insecticide Resistance In Aphids.- 1 Introduction.- 2 Biochemistry of Esterase-Based Resistance in M. persicae.- 3 Molecular Genetics of Esterase Overproduction.- 3.1 Esterase Genes in Susceptible Aphids.- 3.Organization of Amplified Esterase Genes.- 3.3 Cytogenetic Studies of Amplified Esterases.- 4 Expression of Esterase Genes.- 5 Wider Implications.- References.- Insensitive Acetylcholinesterase as Sites for Resistance to Organophosphates and Carbamates in Insects: Insensitive Acetylcholinesterase Confers Resistance in Lepidoptera.- 1 Introduction.- 2 Acetylcholinesterase as a Resistance Mechanism.- 3 Insensitive AChE in Lepidopteran Species.- 4 Insensitive AChE in H. punctigera.- 5 Forms of AChE in Lepidoptera.- 6 Effects of Altered AChE on Acetylcholine Hydrolysis.- 7 Inhibition Ratios and Toxicity in Lepidoptera.- 8 Cross Resistance Between Organophosphates and Carbamates in Lepidoptera.- 9 Genetics of Resistance in Lepidoptera.- 10 Fitness of Resistance in Lepidoptera.- 11 Evolution.- 12 Control of Altered AChE in Lepidoptera.- 13 Population Genetics and Monitoring.- 14 Conclusions.- References.- Glutathione S-Transferases and Insect Resistance to Insecticides.- 1 Introduction.- 2 General Features of Glutathione S-Transferases (GSTs).- 2.1 Roles.- 2.2 Biochemical and Physiological Characteristics.- 2.3 Structure, Regulation, and Evolution of GST Genes.- 3 Insect GSTs.- 3.1 Roles.- 3.2 Biochemical and Physiological Characteristics.- 3.3 GSTs and Insecticide Resistance.- 3.4 Molecular Biology Studies.- 4 GST Studies of Several Insects.- 4.1 Drosophila melanogaster.- 4.2 Musca domestica.- 4.3 Anopheles gambiae.- 4.4 Plutella xylostella.- 5 Concluding Remarks.- References.- Cytochrome P450 Monooxygenases and Insecticide Resistance: Lessons from CYP6D.- 1 Cytochrome P450 Monooxygenases.- 2 Insecticide Resistance.- 3 Monooxygenase-Mediated Insecticide Resistance.- 4 CYP6D1 and Insecticide Resistance.- 5 Summary of the Lessons Learned from CYP6D1.- References.- Mechanisms of Organophosphate Resistance in Insects.- 1 Introduction.- 2 Physiological Mechanisms of Resistance.- 2.1 Resistance Mechanisms Involving Enhanced Biotransformation.- 2.1.1 Cytochrome-P450-Dependent Monooxygenases.- 2.1.2 Glutathione S-Transferases.- 2.1.3 Hydrolytic Enzymes.- 2.1.3.1 Quantitative Changes (Gene Amplification).- 2.1.3.2 Qualitative Changes.- 2.2 Target Site Insensitivity.- 2.3 Interactions Between Resistance Mechanisms.- 3 Summary.- References.- Insect Midgut as a Site for Insecticide Detoxification and Resistance.- 1 Introduction.- 2 The Insect Gut: a Natural Digestive-Absorption Architecture.- 3 Enzymatic Metabolism of Pesticide Involved in Resistance.- 4 Impact of Ingestion, and Penetration and Disposition in the Insect Body on Resistance to Pesticides.- 5 Attempts for Chemical Modeling of Digestion and Absorption in Insect Midgut.- 6 In Vitro Gut Cultures for Insecticidal Activity Studies.- References.- Impact of Insecticide Resistance Mechanisms on Management Strategies.- 1 Introduction.- 2 Overview of Resistance Mechanisms.- 3 Overview of Resistance Management Tactics.- 4 Diagnosing Resistance.- 4.1 In Vitro Assays for Diagnosing Resistance.- 5 Overpowering Resistance Mechanisms.- 6 Resolving and Exploiting Cross-Resistance.- 7 Conclusions.- References.

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