Insecticides Design Using Advanced Technologies

By: Isaac Ishaaya (Editor), Ralf Nauen (Editor), A. Rami Horowitz (Editor)

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Hardcover | 4 January 2007

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332 Pages

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23.5 x 15.88 x 1.91

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Among the highlights of this book are the use of nanotechnology to increase potency of available insecticides, the use of genetic engineering techniques for controlling insect pests, the development of novel insecticides that bind to unique biochemical receptors, the exploration of natural products as a source for environmentally acceptable insecticides, and the use of insect genomics and cell lines for determining biological and biochemical modes of action of new insecticides.

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Nanosuspensions: Emerging Novel Agrochemical Formulations	p. 1
Introduction	p. 1
Solubility Enhancement Through Nanoization	p. 3
Stabilization of Nanosuspensions	p. 7
Preparation of Nanosuspensions	p. 14
Top-Down Methods	p. 14
Nanoparticles by Milling Technologies	p. 14
Nanoparticles via High-Pressure Homogenization	p. 16
Sonication	p. 17
Bottom-Up Methods	p. 17
Controlled Precipitation	p. 17
Reactive Precipitation	p. 17
Solvent Displacement Method	p. 18
Aerosol Procedures	p. 23
Microemulsion Template Methods	p. 23
Supercritical Fluid Methods	p. 23
Characterization of Nanoparticulate Systems	p. 24
Mean Particle Size and Particle-Size Distribution	p. 25
Surface Area	p. 25
Particle Charge (Zeta Potential)	p. 25
Contact Angle	p. 26
Morphology and Crystalline State	p. 26
Saturation Solubility and Dissolution Rate	p. 26
Nanoformulations of Crop-Protection Chemicals	p. 26
Nanoparticulate Formulations of Novaluron	p. 28
Novaluron: A Novel IGR	p. 28
Preparation of Nanosuspensions of Novaluron	p. 29
Comparative Efficacy of Nanosuspension Formulations of Novaluron	p. 29
Conclusions	p. 32
References	p. 32
Pharmacokinetics: Computational Versus Experimental Approaches to Optimize Insecticidal Chemistry	p. 41
Introduction	p. 41
Drug Design by the Pharmaceutical Industry	p. 42
Insecticide Design by the Crop-Protection Industry	p. 42
Aims and Scope of this Review	p. 43
Pharmacokinetic Modeling	p. 43
Mathematical and Conceptual Pharmacokinetic Models	p. 44
Simple Experimental Approaches	p. 44
Penetration Through Isolated Cuticles	p. 47
Rotating Diffusion Cell Studies	p. 47
Penetration of Imidacloprid (IMI) Across Isolated Gut and Cuticle	p. 49
Retention of Applied IMI in the Integument of S. littoralis	p. 50
Uptake by Isolated Target Tissue	p. 51
Compartmental Modeling	p. 52
Simple Models	p. 53
Two-Compartment PK Models	p. 53
Complex Models	p. 54
The Complexity of the Insect Body Plan	p. 55
A Three-Compartment Model and Oscillatory Movement of Material Between Tissue Compartments	p. 57
Physiological Models	p. 58
Movement Between Tissues, Tissue Equilibria and Routes of Loss	p. 59
Relative Tissue Affinities and Partitioning	p. 60
Potential Use of Pharmacokinetics in Insecticide Design—the Way Ahead	p. 62
Estimating Pharmacokinetic/Dynamic Parameters from Time/Dose/Response Data	p. 62
Conclusions	p. 64
References	p. 64
High-Throughput Screening and Insect Genomics for New Insecticide Leads	p. 67
Introduction	p. 67
Approaches for Insecticide Lead Identification	p. 68
HTS Using Established Agrochemical Targets	p. 70
Insecticides Based on New Insect Targets	p. 74
Knowledge-Based New Target Identification	p. 76
Genomic Studies and Model Organisms	p. 80
Identifying a New MOA from Active Chemistry	p. 81
Conclusions	p. 83
References	p. 83
Transgenic and Paratransgenic Insects in Crop Protection	p. 87
Introduction	p. 87
The Sterile Insect Technique	p. 87
Conditional Lethal Genes	p. 88
Regulatory Aspects	p. 89
Symbiosis and Microbiology	p. 90
Symbiotic Control of Disease Transmission	p. 90
Dental Caries	p. 92
Pierce's Disease	p. 92
The Vector Insect	p. 93
The Symbiont	p. 94
Genetic Engineering of GWSS/Grapevine Bacterial Symbionts	p. 95
Competitive Displacement	p. 95
Quorum Sensing	p. 97
Practical Consideration	p. 98
Conclusions	p. 99
References	p. 100
Future Insecticides Targeting Genes Involved in the Regulation of Molting and Metamorphosis	p. 105
Introduction	p. 105
Hormonal Regulation of Molting and Metamorphosis	p. 106
PTTH	p. 106
Introduction	p. 106
Biosynthesis	p. 106
Mode of Action	p. 106
Ecdysone	p. 107
Introduction	p. 107
Biosynthesis	p. 107
Mode of Action	p. 108
Juvenile Hormone	p. 109
Introduction	p. 109
Biosynthesis	p. 109
Mode of Action	p. 110
Ecdysis-Controlling Neuropeptides	p. 112
Introduction	p. 112
Biosynthesis	p. 112
Mode of Action	p. 113
Bursicon	p. 114
Introduction	p. 114
Biosynthesis	p. 114
Mode of Action	p. 115
Genes Involved in Molting and Metamorphosis as Target Sites for the Design of Biorational Insecticides	p. 115
Success Stories	p. 115
Ecdysone Analogs	p. 115
JH Analogs	p. 117
Hormones, Receptors and Transcription Factors as Target Sites	p. 119
Biosynthetic Enzymes as Target Sites	p. 119
Juvenile Hormone	p. 119
Ecdysone	p. 123
Utilization of Genes Involved in Molting and Metamorphosis for Development of Pest Management Tools	p. 124
Small Molecules	p. 124
Use of Genes Involved in Molting and Metamorphosis in Alternate Pest-Management Methods	p. 124
References	p. 126
Trypsin Modulating Oostatic Factor for Developing Resistant Crops	p. 135
Introduction	p. 135
Biochemical and Physiological Studies	p. 136
The Discovery of Mosquito TMOF	p. 136
Biological Activity and Mode of Action of TMOF	p. 137
Inhibition of Trypsin Biosynthesis by TMOF in Other Insects	p. 139
Genetic Characterization and Expression of TMOF	p. 141
The Effect of TMOF and Its Analogues on Insect Larvae	p. 141
Molecular Biology Studies	p. 142
Cloning and Expression of Aea-TMOF by TMV, Chlorella, Saccharomyces cerevisia, Tobacco and Alfalfa Plants	p. 142
Insect Resistance and Safety Issues	p. 144
Potential Resistance Development to TMOF	p. 144
Safety of TMOF	p. 145
References	p. 147
Nicotinic Acetylcholine Receptors as a Continuous Source for Rational Insecticides	p. 151
Introduction	p. 151
Structure of the Nicotinic Acetylcholine Receptors (nAChRs)	p. 153
Structure of the Insect nAChRs	p. 154
Agonists vs. Antagonists	p. 155
Neonicotinoid Insecticides	p. 156
Bioisosteric Segments of Neonicotinoids	p. 157
Natural Products Active on nAChR	p. 158
Ligand Binding	p. 163
Acetylcholine Binding Protein (AChBP)	p. 164
Comparison AChBP vs. nAChR -Subunit	p. 166
Nicotinic Pharmacophore Models	p. 168
Binding Models of Neonicotinoids by 3D Pharmacophore Mapping	p. 170
Ring Systems vs. Noncyclic Neonicotinoids	p. 172
Isosteric Alternatives to the Heterocyclic N-Substituents	p. 177
Bioisosteric Pharmacophors of Neonicotinoids	p. 178
Photoaffinity Probes for Insect nAChRs	p. 179
Selectivity for Insect vs. Mammalian nAChRs	p. 179
nAChR-Based Screening Assays	p. 181
Resistance	p. 181
Concluding Remarks and Prospects	p. 184
References	p. 184
Mitochondrial Electron Transport Complexes as Biochemical Target Sites for Insecticides and Acaricides	p. 197
The Mitochondrial Electron Transport Chain	p. 197
Overview of Respiratory Electron Transport and Chemiosmotic Coupling	p. 197
Respiratory Electron Transport Complexes	p. 198
Respiratory Electron Transport Complexes as Target Sites for Insecticides	p. 200
NADH: ubiquinone Oxidoreductase (Complex I)	p. 201
Structural Aspects Related to Mechanism	p. 201
Complex I Inhibitors as Insecticides and Acaricides	p. 203
ubihydroquinone: cytochrome c Oxidoreductase	p. 206
Structure and Enzymatic Mechanism	p. 206
Complex III Inhibitors with Insecticidal and Acaricidal Activity	p. 208
ß-Methoxyacrylates	p. 209
2-Hydroxynaphthoquinones	p. 210
The Respiratory Chain as Insecticide Target Site-Summary and Outlook	p. 211
References	p. 211
Inhibition of Programmed Cell Death by Baculoviruses: Potential in Pest-Management Strategies	p. 217
Introduction	p. 217
The Baculoviruses	p. 220
Molecular Basis of Apoptosis	p. 222
Caspases	p. 222
IAPs	p. 223
P35	p. 224
Conclusions	p. 228
References	p. 229
Plant Natural Products as a Source for Developing Environmentally Acceptable Insecticides	p. 235
Introduction	p. 235
From Pyrethrum to Synthetic Pyrethroids	p. 236
Azadirachtin and Related Limonoids from the Meliaceae	p. 236
Acetogenins from the Annonaceae	p. 239
Alkaloids from Stemonaceae	p. 240
Napthoquinones from the Scrophulariaceae	p. 241
Rocaglamides from Aglaia (Meliaceae)	p. 242
Monoterpenoids from Plant Essential oils	p. 243
Conclusions	p. 244
References	p. 245
Essential Oils as Biorational Insecticides-Potencyand Mode of Action	p. 249
Introduction	p. 249
Essential oils Activities on Insect Pests	p. 250
Plant Resistance	p. 250
Insecticidal Activity	p. 250
Repellency	p. 251
Anti-feedant	p. 251
Efficacy of Essential oils as Fumigants for the Control of Stored-Product Insects	p. 251
Insecticidal Mode of Action of Essential Oil-Toxicity	p. 253
Introduction	p. 253
Neurotransmitters in Insects	p. 255
Inhibitory Activity of Essential Oils on Acetylcholinesterase (AchE)	p. 256
Inhibitory Activity of Essential Oils on Octopaminergic Sites	p. 257
Concluding Remarks	p. 259
References	p. 260
Insect Cell Lines as Tools in Insecticide Mode of Action Research	p. 263
Introduction	p. 263
Insect Cell Cultures	p. 265
Endocrine Strategies	p. 267
Screening for Ecdysteroid and Juvenile Hormone Activities	p. 267
Ecdysteroid	p. 269
Juvenile Hormones	p. 279
Insect-Specific Metabolic Pathways with Chitin and Cuticle Synthesis	p. 280
Other Insect Targets Related to the Insect Neurological/Nerve, Energy Metabolism and Muscle System	p. 287
Insect Cell Lines as Proxies for Bacillus thuringiensis Insecticidal Proteins	p. 288
Suitability of Insect Cell Lines as Sentinels for Environmental Toxicity and Chemistry	p. 290
Elucidation of Insecticide Resistance Mechanisms Using Insect Cell Lines	p. 291
Conclusions	p. 293
References	p. 294
Index	p. 305
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Insecticides Design Using Advanced Technologies

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