Plant Bioactives and Drug Discovery: Principles, Practice, and Perspectives
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More About This Title Plant Bioactives and Drug Discovery: Principles, Practice, and Perspectives


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.

With coverage of strategic methods of natural compound isolation, structural manipulation, natural products in clinical trials, quality control, and more, and featuring case studies on medicinal plants, the book serves as a definitive guide to the field of plant biodiversity as it relates to medicine. In addition, chapters on using natural products as drugs that target specific disease areas, including neurological disorders, inflammation, infectious diseases, and cancer, illustrate the myriad possibilities for therapeutic applications.

Wide ranging and comprehensive, Plant Bioactives and Drug Discovery also includes important information on marketing, regulations, intellectual property rights, and academic-industry collaboration as they relate to plant-based drug research, making it an essential resource for advanced students and academic and industry professionals working in biochemical, pharmaceutical, and related fields.


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


“In conclusion, this book could be a useful guide not only for PhD students starting their activity in the field of plant metabolites, but also for more advanced researchers looking for a state-of-the-art overview of modern research in this fascinating field.”  (ChemMedChem, 1 March 2013)