Valdir Cechinel-Filho, PhD, is Professor and Researcher at the Chemical-Pharmaceutical Investigations Center, University of Vale do Itajaí in Brazil. The editor of five books, seventeen contributed chapters, and over 250 scientific papers and reviews, Dr. Filho is also Associate Editor of Pharmaceutical Biology, a member of the editorial boards of several journals, and a reviewer for many journals, including European Journal of Medicinal Chemistry, Journal of Pharmacy and Pharmacology, Natural Product Research, Planta Medica, and Journal of Agricultural and Food Chemistry.

Contributors xv
Preface xix
1 Natural Products in Drug Discovery: Recent Advances 1
Gordon M. Cragg, Paul G. Grothaus, and David J. Newman
1.1 Introduction 1
1.2 The Role of Traditional Medicine and Plants in Drug Discovery 2
1.3 The Role of Marine Organisms in Drug Discovery 4
1.4 The Role of Microorganisms in Drug Discovery: An Historical Perspective 6
1.5 Other Sources 8
1.6 The Importance of Natural Products in Drug Discovery and Development 8
1.7 Classical Natural Sources: Untapped Potential 10
1.8 The Unexplored Potential of Microbial Diversity 10 1.9 Development of Drugs From Natural Products: A Multidisciplinary Process 19
1.10 Conclusions 26
References 27
2 Modern Approaches in the Search for New Active Compounds from Crude Extracts of Natural Sources 43
Emerson F. Queiroz, Kurt Hostettmann, and Jean-Luc Wolfender
2.1 Introduction 43
2.2 Selection of the Natural Matrices 45
2.3 Rapid Online Identification and Dereplication 46
2.4 HPLC-Hyphenated Methods for Natural Product Identification 46 2.5 Studies on Natural Products Using LC-NMR, Microflow NMR, and SPE-NMR 57
2.6 Application of Direct NMR Methods for Chemical Profiling of Crude Extracts 67 2.7 Conclusions 69
References 71
3 Natural Products as Lead Compounds in Medicinal Chemistry 81
Eliezer J. Barreiro, Carlos A. M. Fraga, and Lidia M. Lima
3.1 Medicinal Chemistry Definition and the Importance of the Lead Compound in Drug Discovery 81
3.2 Natural Products as Drugs 84 3.4 Natural Products as Lead Compounds for New Drug Candidates 107
3.5 Conclusions 113
Acknowledgments 115
References 115
4 The Importance of Structural Manipulation of Natural Compounds in Drug Discovery and Development 127
Arturo San Feliciano, María Á . Castro, José L. López-Perez, and Esther del Olmo
4.1 Introduction 127
4.2 Chemomodulation of Podophyllotoxin Cyclolignans 132 4.3 Chemoinduction of Bioactivity on Dihydrostilbenoids 140
4.4 Chemoinduction and Chemomodulation of the Antiparasitic Activity of Stilbenoids 150
4.5 Conclusions 152
Acknowledgments 153
References 153
5 The Action of Plants and their Constituents on the Central Nervous System 161
Fúlvio R. Mendes, Giuseppina Negri, Joaquim M. Duarte-Almeida, Ricardo Tabach, and Elisaldo A. Carlini
5.1 Introduction 161
5.2 Plants with CNS Depressant Activity 162 5.3 Plants with the CNS Stimulant Activity 169
5.4 Plants Used as Antidepressants 174 5.5 Adaptogenic Plants 175
5.6 Plants Used to Treat Neurodegenerative Diseases 178 5.7 Plants with the Mind-Altering Activity 182
5.8 Plants Used Against Drug Dependence 188
5.9 Conclusions 188
Acknowledgments 191
References 191
6 The Role of Natural Products in Discovery of New Anti-Infective Agents with Emphasis on Antifungal Compounds 205
Maximiliano Sortino, Marcos Derita, Laura Svetaz, Marcela Raimondi, Melina Di Liberto, Elisa Petenatti, Mahabir Gupta, and Susana Zacchino
6.1 Infectious Diseases and Available Antimicrobial Agents 205
6.2 Fungal Infections and Available Antifungal Agents 206 6.3 The Need of New Antifungal Agents 208
6.4 From Antifungal Compounds to Antifungal Drugs: Some Considerations 223
6.5 Other Strategies Based on Non-targeted Assays 223
6.6 Strategies Based on Targeted Assays for the Discovery of Antifungal Compounds 226 6.7 Conclusion 229
References 229
7 Antiulcer Agents from Higher Plants 241
Luiz C. Klein-Júnior, José R. Santin, and Sérgio F. de Andrade
7.1 Introduction 241
7.2 Medicinal Plants with Antiulcer Activity 243 7.3 Secondary Metabolites as a Source of Anti-Ulcer Drug Leads 251
7.4 Conclusions 256
References 256
8 Recent Progress in the Chemistry and Biology of Paclitaxel (TaxolTM) and Related Taxanes 263
Jun Qi, Jielu Zhao, and David G. I. Kingston
8.1 Introduction 263
8.2 New Chemistry of Paclitaxel 265 8.3 Tubulin Binding 295
8.4 Pharmacology of Paclitaxel 306
8.5 Conclusions 318
References 319
9 Cancer Chemopreventive Activity of Higher Plants 337
A. Douglas Kinghorn, Yulin Ren, Jie Li, and Chung Ki Sung
9.1 Introduction 337
9.2 Potental Cancer Chemopreventive Agents from Selected Dietary Higher Plants 338
9.3 Conclusions 348
Acknowledgments 348
References 348
10 Medicinal Plants and Pharmaceutical Technology 359
Ruth M. Lucinda da Silva, Angélica G. Couto, and Tania M.B. Bresolin
10.1 Introduction 359
10.2 Supply of Herbal Materials 361
10.3 Harvest and Postharvest Processing 363 10.4 Extraction of Herbal Drugs 365
10.5 Dry Extracts 369
10.6 Phytopharmaceutical Dosage Forms 373 10.7 Quality Assurance and Quality Control of Herbal Drugs and Phytopharmaceuticals 377
References 387
11 Natural Products in Clinical Trials 395
Sigrun Chrubasik
11.1 The Quality of Clinical Trials 395
11.2 Examples of Clinical Studies with Natural Products 396
11.3 Evidence of Effectiveness 413
References 416
12 The Influence of Biotic and Abiotic Factors on the Production of Secondary Metabolites in Medicinal Plants 419
Dayana R. Gouvea, Leonardo Gobbo-Neto, and Norberto P. Lopes
12.1 Introduction 419
12.2 Biotic and Abiotic Factors that can Affect Biosynthesis and/or Metabolites Accumulation 422 12.3 Types of Observed Variations on Secondary Metabolites Content 431
12.4 Conclusions 439
References 440
13 Production of Bioactives Compounds: The Importance of Pictet-Spengler Reaction in the XXI Century 453
Pilar Menendez, Ilaria D'Acquarica, Giuliano Delle Monache, Francesca Ghirga, Andrea Calcaterra, Marco Barba, Alberto Macone, Alberto Boffi, Alessandra Bonamore, and Bruno Botta
13.1 Introduction 453
13.2 Variants and Applications 455
13.3 Asymmetric Synthesis 457
13.4 Chiral Auxiliary and Enantioselective Catalysis 459
13.5 Enzymatic Catalysis 465
13.6 The Pictet-Spengler Reaction at Present 468 13.7 Conclusions 478
Acknowledgment 480
References 480
14 Screening Methods for Drug Discovery from Plants 489
Alan L. Harvey
14.1 From Traditional to Phenotypic Screening 489
14.2 Molecular and Cellular Assays 490
14.3 Disease-Specific Assays 492 14.4 Conclusions 495
References 495
15 Phytotherapeutics - Intellectual Property Rights, Global Market, and Global Regulatory Guidelines 499
James D. McChesney, Raymond Cooper, and Kip Vought
15.1 Intellectual Property Rights 499
15.2 Biodiversity 501
15.3 Global Market Perspectives 502 15.4 Regulatory Perspectives 507
15.5 Conclusions 525
References 526
16 Cooperation Between the Pharmaceutical Industry and Academic Institutions in Drug Discovery 529
Valdir Cechinel-Filho, Rivaldo Niero, and Rosendo A. Yunes
16.1 Introduction 529
16.2 Interaction Between Academic Institutions and the Pharmaceutical Industry 530
16.3 Overview of the Global Pharmaceutical Market 534
16.4 Reorganization of the Pharmaceutical Industry 535 16.5 Conclusions 541
Acknowledgments 542
References 542
Index 545

An in-depth exploration of the applications of plant bioactive metabolites in drug research and development
Highlighting the complexity and applications of plant bioactive metabolites in organic and medicinal chemistry, Plant Bioactives and Drug Discovery: Principles, Practice, and Perspectives provides an in-depth overview of the ways in which plants can inform drug research and development. An edited volume featuring multidisciplinary international contributions from acclaimed scientists researching bioactive natural products, the book provides an incisive overview of one of the most important topics in pharmaceutical studies today.
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