Preface ................................................... XV
List of Contributors .................................... XVII
1 Bioactive Phytocompounds: New Approaches in the
Phytosciences .............................................. 1
Ricardo Ramos Mendonga-Filho
1.1 Introduction ............................................... 2
1.2 Development of Fast Reliable Methods of Extraction
and High-Throughoutput Screening (HTS) of Crude Plant
Extracts: New Challenges ................................... 3
1.3 Antimicrobial Bioactive Phytocompounds from Extraction to
Identification: Process Standardization .................... 6
1.4 Problems Associated with the Efficacy, Stability and
Quality Control of Herbal Drags Preparations .............. 13
1.5 Novel Bioactive Phytocompounds Against Multidrug-
Resistant Bacteria/Fungi: The Management of Infectious
and Chronic Diseases ...................................... 17
1.6 Mode of Action of Bioactive Phytocompounds and their
Interactions with Macromolecules and Toxicity ............. 18
1.7 Bioactive Phytocompounds and Future Perspectives .......... 21
References ................................................ 23
2 Quality Control, Screening, Toxicity, and Regulation of
Herbal Drugs .............................................. 25
Wickramasinghe M. Bandaranayake
2.1 Introduction .............................................. 26
2.2 Preparation of Herbal Drugs ............................... 29
2.3 Quality Control of Herbal Drugs ........................... 30
2.3.1 Parameters for Quality Control of Herbal Drugs ..... 34
2.3.1.1 Microscopic Evaluation .................... 34
2.3.1.2 Determination of Foreign Matter ........... 34
2.3.1.3 Determination of Ash ...................... 35
2.3.1.4 Determination of Heavy Metals ............. 35
2.3.1.5 Determination of Microbial Contaminants
and Aflatoxins ............................ 35
2.3.1.6 Determination of Pesticide Residues ....... 36
2.3.1.7 Determination of Radioactive
Contamination ............................. 37
2.3.1.8 Analytical Methods ........................ 37
2.3.1.9 Validation ................................ 38
2.4 Herbal Supplements ........................................ 39
2.5 Adulteration of Herbal Drugs .............................. 40
2.6 Contamination of Herbal Drags and Herb-Drug Interactions .. 41
2.7 Toxicity of Herbal Drugs .................................. 43
2.8 Screening of Herbal Drugs ................................. 45
2.9 Labeling of Herbal Products ............................... 46
2.10 Policies and Regulations .................................. 47
2.11 Trends and Developments ................................... 49
2.12 Conclusions ............................................... 50
References ................................................ 53
3 Herbal Medicines: Prospects and Constraints ............... 59
Iqbal Ahmad, Farrukh Aqil, Farah Ahmad, and Mohammad
Owais
3.1 Introduction .............................................. 59
3.1.1 Traditional Systems of Medicine .................... 61
3.1.1.1 Asian Medicinal System .................... 61
3.1.1.2 European Herbalism ........................ 61
3.1.1.3 Neo-Western Herbalism ..................... 61
3.1.2 Modern Phytomedicine ............................... 61
3.2 Prospects for Herbal Medicine ............................. 62
3.2.1 Indian System-Based Herbal Medicine ................ 64
3.2.2 Progress in the Pharmacokinetics and
Bioavailability of Herbal Medicine ................. 67
3.3 Constraints in Herbal Medicine ............................ 68
3.3.1 Reproducibility of Biological Activity of Herbal
Extracts ........................................... 68
3.3.2 Toxicity and Adverse Effects ....................... 68
3.3.3 Adulteration and Contamination ..................... 69
3.3.4 Herb-Drag Interactions ............................. 69
3.3.5 Standardization .................................... 71
3.3.6 Regulatory Challenges of Asian Herbal Medicine ..... 71
3.4 Good Manufacturing Practice (GMP) for Herbal Medicine ..... 72
3.5 Improving the Quality, Safety and Efficacy of Herbal
Medicine .................................................. 72
3.5.1 Quality Management ................................. 73
3.5.2 Encouraging Mediculture ............................ 73
3.5.3 Correct Identification of Plant Material ........... 74
3.5.4 Minimizing Contamination in Herbal Medicine ........ 74
3.6 Conclusions .......................................... 74
Acknowledgments ........................................... 75
References ................................................ 76
4 Bioactive Phytocompounds and Products Traditionally Used
in Japan .................................................. 79
Jin-ichi Sasaki
4.1 Introduction .............................................. 80
4.2 Garlic .................................................... 80
4.2.1 Introduction ....................................... 80
4.2.2 Biological Effect of Garlic ........................ 81
4.2.2.1 Antibacterial Effects ..................... 81
4.2.2.2 Anticoagulation Effects ................... 84
4.2.2.3 Antioxidant Activity ...................... 86
4.2.2.4 Therapeutic Effects of Garlic Powder in
the Organophosphate Compound Poisoning
Mouse as a Model of SARS .................. 87
4.3 Mushroom .................................................. 87
4.3.1 Introduction ....................................... 87
4.3.2 Biological Effects ................................. 88
4.3.2.1 Antitumor Activity ........................ 88
4.4 Sweetcorn ................................................. 92
4.4.1 Introduction ....................................... 92
4.4.2 Biological Effects ................................. 92
4.4.2.1 Antitumor Activity of Sweetcorn ........... 92
4.5 Oil and Flavor of Tree Hiba (Japanese Cypress)
(Hinokitiol) .............................................. 94
4.5.1 Introduction ....................................... 94
4.5.2 Biological Effects ................................. 94
4.6 Conclusions ............................................... 95
Acknowledgments ........................................... 96
References ................................................ 96
5 Plant Extracts Used to Manage Bacterial, Fungal, and
Parasitic Infections in Southern Africa ................... 97
J.N. Boffand L.J. McGaw
5.1 Introduction .............................................. 98
5.2 Biodiversity in Southern Africa ........................... 99
5.3 Use of Plants in Southern African Traditional Medicine .... 99
5.4 The Need for Anti-Infective Agents ....................... 100
5.5 Selection of Plant Species to Investigate ................ 100
5.5.1 Ethnobotanical Approach ........................... 101
5.5.2 Chemotaxonomy ..................................... 101
5.5.3 Random Selection .................................. 101
5.6 Collecting, Drying, and Storage of Plant Material ........ 102
5.7 Extraction of Plant Material ............................. 103
5.7.1 Which is the Best Extractant? ..................... 103
5.7.2 Extraction Period and Efficiency .................. 104
5.7.3 Selective Extraction .............................. 104
5.7.4 Redissolving Extracts for Quantitative Data ....... 105
5.7.5 Storage of Extracts ............................... 105
5.8 Evaluating Quantitative Antimicrobial Activity ........... 105
5.9 Qualitative Biological Activity .......................... 106
5.10 Seipression of Results ................................... 107
5.11 Antibacterial Activity ................................... 108
5.12 Results on Antibacterial Activity Obtained with Members
of the Combretaceae ...................................... 109
5.12.1 Introduction ..................................... 109
5.12.2 Combretum erythrophyllum ......................... 109
5.12.3 Antibacterial Activity of Southern African
Members of the Combretaceae ...................... 209
5.12.4 Stability of Extracts ............................ 110
5.12.5 Anti-Inflammatory Activity ....................... 110
5.12.6 Other Activities of Extracts of Combretum
Species .......................................... 111
5.12.7 Isolation and Biological Activity of
Antibacterial Compounds from C. erythrophyllum ... 111
5.12.8 Combretum woodii ................................. 111
5.12.9 Unpublished Work on Other Members of the
Combretaceae ..................................... 112
5.13 Antifungal Activity ...................................... 112
5.14 Antiparasitic Activity ................................... 213
5.15 Other Anti-Infective Research in South Africa ............ 115
5.16 Cytotoxicity ............................................. 115
5.17 Ethnoveterinary Research ................................. 116
5.18 Determining the in vivo Efficacy of Extracts and
Isolated Compounds ....................................... 117
5.19 Conclusion ............................................... 118
References ............................................... 119
6 Biological and Toxicological Properties of Moroccan
Plant Extracts: Advances in Research ..................... 123
M. Larhsini
6.1 Introduction ............................................. 123
6.2 Ethnobotanic and Ethnopharmacology of Traditional
Moroccan Plants .......................................... 125
6.2.1 Ethnobotanic Surveys .............................. 125
6.2.2 Biological Activities ............................. 126
6.2.2.1 Antimicrobial Properties ................. 126
6.2.2.2 Antidiabetic Activity .................... 128
6.2.2.3 Other Biological Activities .............. 131
6.3 Toxicological Assays ..................................... 131
6.4 Conclusions .............................................. 132
References ............................................... 133
7 Anti-MRSA and Anti-VRE Activities of Phytoalexins and
Phytoncides Isolated from Tropical Plants ................ 137
Yoshikazu Sakagami
7.1 Introduction ............................................. 138
7.2 Phytoalexins and Phytoncides ............................. 139
7.3 Antibiotics .............................................. 140
7.4 Bacteria and Broth ....................................... 140
7.4.1 VRE ............................................... 140
7.4.2 VSE ............................................... 141
7.4.3 MRSA .............................................. 141
7.4.4 MSSA .............................................. 141
7.4.5 Broth ............................................. 141
7.5 Isolation of Phytoalexins and Phytoncides ................ 141
7.6 Minimum Inhibitory Concentration ......................... 142
7.7 Synergism of Antibacterial Compounds with Commercially
Available Antibiotics .................................... 142
7.8 Antibacterial Activities ................................. 143
7.8.1 Sophoraflavanone G ................................ 143
7.8.2 Calozeyloxanthone ................................. 144
7.8.3 α-Mangostin ....................................... 144
7.8.4 Gnemonol В and Gnetin E ........................... 145
7.8.5 Summary of MIC Values of Phytoalexin and
Phytoncide Against MRSA and VRE ................... 146
7.9 Synergism Between the Test Compounds and Commercial
Antibiotics Against VRE, MRSA, VSE, and MSSA ............. 147
7.9.1 Sophoraflavanone G ................................ 147
7.9.2 Calozeyloxanthone ................................. 148
7.9.3 α-Mangostin ....................................... 148
7.9.4 Stilbene Oligomer ................................. 151
7.9.5 Summary of Synergistic Effects Between the Test
Compounds and the Commercial Antibiotics Against
VRE and MRSA ...................................... 153
References ............................................... 154
8 Methods for Testing the Antimicrobial Activity of
Extracts ................................................. 157
Jenny M. Wilkinson
8.1 Introduction ............................................. 157
8.2 Antibacterial Assays ..................................... 158
8.2.1 Semi-Solid Substrate Methods ...................... 161
8.2.1.1 Disk Diffusion Method .................... 161
8.2.1.2 Agar Dilution Method ..................... 162
8.2.1.3 Broth Dilution Methods ................... 163
8.2.1.4 Thin-Layer Chromatography-Bioautography .. 164
8.3 Antifungal Assays ........................................ 165
8.4 In vivo Assessment of Antibacterial and Antifungal
Activity ................................................. 166
8.5 Methods for Assessing Antiviral Activity ................. 167
8.6 Screening of Plant Extracts for Antiparasitic Activity ... 167
8.7 Conclusions .............................................. 168
References ............................................... 169
9 Targeted Screening of Bioactive Plant Extracts and
Phytocompounds Against Problematic Croups of Multidrug-
Resistant Bacteria ....................................... 173
Farrukh Aqil, Iqbal Ahmad, and Mohammad Owais
9.1 Introduction ............................................. 174
9.1.1 Multiple Antibiotic Resistance in Bacteria ........ 174
9.1.2 Plants as a Source of Novel Bioactive Compounds ... 177
9.2 Approaches to Targeted Screening Against MDR Bacteria .... 179
9.2.1 MDR Efflux Pump Inhibitors from Plants ............ 180
9.2.2 ß-Lactamase Inhibitors ............................ 181
9.2.3 Synergy Between Phytocompounds and Antibiotics .... 182
9.2.4 Targeting Virulence and Pathogenicity ............. 185
9.2.5 Quorum Sensing Inhibitors ......................... 286
9.3 Other Potential Approaches ............................... 289
9.3.1 Targeting Gene Transfer Mechanisms ................ 289
9.3.2 Targeting R-Plasmid Elimination ................... 290
9.4 Conclusions and Future Directions ........................ 292
Acknowledgments .......................................... 292
References ............................................... 293
10 Activity of Plant Extracts and Plant-Derived Compounds
against Drug-Resistant Microorganisms .................... 199
Antonia Nostro
10.1 Introduction ............................................. 199
10.2 Plant Materials with General Antimicrobial Activity
Including some Drug-Resistant Strains .................... 200
10.3 Plant Materials with Specific Antimicrobial Activity
Against Drug-Resistant Strains ........................... 201
10.3.1 Drug-Resistant Gram-Positive Bacteria ............. 201
10.3.2 Drug-Resistant Gram-Negative Bacteria ............. 211
10.3.3 ' Other Drug-Resistant Microorganisms ............ 212
10.4 Plant Materials that Restore the Effectiveness of
Antimicrobial Agents and/or Inhibit Drug Resistance
Mechanisms ............................................... 223
10.4.1 Other Mechanisms .................................. 225
10.5 Conclusions .............................................. 226
References ............................................... 226
11 An Alternative Holistic Medicinal Approach to the Total
Management of Hepatic Disorders: A Novel Polyherbal
Formulation .............................................. 233
Mohammad Owais, Iqbal Ahmad, Shazia Khan, Umber Khan,
and Nadeem Ahmad
11.1 Introduction ............................................. 233
11.2 Conventional Medicines for Liver Disorders ............... 236
11.3 Herbal Medicines - Potential Therapeutic Agents with
Minimal Side-Effects ..................................... 237
11.4 Contributions of Elementology to Potential Treatments
for Hepatic Disorders .................................... 240
11.5 Other Alternatives in Liver Therapy ...................... 242
11.6 Conclusions .............................................. 242
References ............................................... 243
12 Traditional Plants and Herbal Remedies Used in the
Treatment of Diarrheal Disease: Mode of Action,
Quality, Efficacy, and Safety Considerations ............. 247
Enzo A. Palombo
12.1 Introduction ............................................. 248
12.2 Methods Used in the Evaluation of Bioactivity of
Medicinal Plants ......................................... 249
12.2.1 Antibacterial Activity ............................ 249
12.2.2 Antiprotozoal Activity ............................ 250
12.2.3 Antihelminthic Activity ........................... 250
12.2.4 Antiviral Activity ................................ 250
12.2.5 Antidiarrheal Activity ............................ 251
12.3 Traditional Medicinal Plants Used in the Treatment of
Diarrhea that Display Antimicrobial Activity ............. 252
12.4 Traditional Medicinal Plants Used in the Treatment of
Diarrhea that Display Antidiarrheal Activity ............. 255
12.5 Phytochemical Analysis, Identification of Active Plant
Components, and Mechanism of Action of Medicinal Plants
Used in the Treatment of Diarrhea ........................ 260
12.6 Quality, Efficacy, and Safety Considerations ............. 263
12.7 Conclusions .............................................. 266
Acknowledgments .......................................... 267
References ............................................... 267
13 Mutagenicity and Antimutagenicity of Medicinal Plants .... 271
Javed Musarrat, Farrukh Aqil, and Iqbal Ahmad
13.1 Introduction ............................................. 271
13.2 Plants as Protective Agents Against DNA Damage ........... 272
13.3 Antimutagenic Properties of Edible and Medicinal Plants .. 274
13.4 Mutagenicity of Plant Extracts and Phytocompounds ........ 279
13.5 "Janus Carcinogens and Mutagens" ......................... 280
13.6 Chemical Nature of Phytoantimutagenic Compounds .......... 281
13.6.1 Flavonoids ........................................ 282
13.6.2 Phenolic Compounds ................................ 282
13.6.3 Coumarins ......................................... 282
13.6.4 Diterpenoids ...................................... 282
13.6.5 Organosulfur Compounds ............................ 283
13.7 Assays for Mutagenicity and Antimutagenicity ............. 283
13.8 Paradigms in Antimutagenicity Research ................... 285
13.9 Conclusions .............................................. 285
References ............................................... 286
14 Potential of Plant-Derived Products in the Treatment
of Mycobacterial Infections .............................. 293
Deepa Bisht, Mohammad Owais, and K. Venkatesan
14.1 Introduction ............................................. 293
14.2 Current Therapy of Tuberculosis and Leprosy .............. 294
14.3 Need for Newer Antimycobacterial Drugs ................... 295
14.4 Plant Extracts ........................................... 295
14.5 Well-Characterized Plant-Derived Compounds ............... 297
14.5.1 Alkanes, Alkenes, Alkynes, Fatty Acids and their
Esters and Simple Aroma tics ...................... 297
14.5.2 Alkaloids ......................................... 299
14.5.3 Phenolics and Acetogenic Quinones ................. 302
14.5.4 Terpenes .......................................... 304
14.5.5 Steroids .......................................... 308
14.6 Conclusion ............................................... 308
Acknowledgements ......................................... 309
References ............................................... 309
15 Ethnomedicinal Antivirals: Scope and Opportunity ......... 313
Debprasad Chattopadhyay
15.1 Introduction ............................................. 313
15.1.1 Ethnomedicines and Drug Discovery ................. 314
15.1.2 Viruses: The Acellular Parasite of Cellular
Hosts ............................................. 315
15.1.2.1 Viral Infection Control .................. 316
15.2 Antiviral Ethnomedicines Against Common Virus Families ... 316
15.3 Major Groups of Antivirals from Plants ................... 321
15.3.1 Phenolics and Polyphenols ......................... 322
15.3.2 Coumarins ......................................... 323
15.3.3 Quinones .......................................... 324
15.3.4 Flavones, Flavonoids, and Flavonols ............... 324
15.3.5 Tannins ........................................... 327
15.3.6 Lignans ........................................... 327
15.3.7 Terpenoids and Essential Oils ..................... 328
15.3.8 Alkaloids ......................................... 329
15.3.9 Lectins, Polypeptides and Sugar-Containing
Compounds ......................................... 330
15.4 Mixtures and Other Compounds ............................. 330
15.5 Experimental Approaches .................................. 331
15.5.1 In Vitro Efficacy ................................. 332
15.5.2 Clinical Trials in Humans ......................... 332
15.6 Future Prospects ......................................... 334
15.7 Conclusions .............................................. 334
Acknowledgments .......................................... 335
References ............................................... 335
16 Immunomodulatory Effects of Phytocompounds ............... 341
Buket Cicioğlu Andoğan
16.1 Introduction ............................................. 342
16.1.1 General Properties and Classification of
Phytocompounds .................................... 342
16.2 Effect of Specific Medicinal Herbs on Immune System and
Immune Cells ............................................. 343
16.3 General Properties of Echinacea Species .................. 344
16.4 Effects of Echinacea Species on the Immune System and
Various Immune Cells ..................................... 345
16.5 Asteraceae ............................................... 349
16.6 Lithospermum erythrorhizon ............................... 351
16.7 Guarana .................................................. 352
16.8 Side and Adverse Effects of Some Phytocompounds .......... 352
16.9 Conclusion ............................................... 353
References ............................................... 354
17 Use of a Liposomal Delivery System for Herbal-Based
Therapeutics (with a Focus on Clove Oil) ................. 357
Nadeem Ahmad, Maroof Alam, Iqbal Ahmad, and Mohammad
Owais
17.1 Introduction ............................................. 357
17.1.1 Cinnamon Oil ...................................... 359
17.1.2 Oregano Oil ....................................... 359
17.1.3 Clove Oil ......................................... 359
17.1.3.1 Composition of the Clove Oil Used ........ 360
17.2 Rationale for Using Liposomized Formulation of Clove
Oil ...................................................... 361
17.2.1 Advantageous Properties of Liposomes .............. 362
17.3 Experiments Conducted to Develop Liposomal Clove Oil
Formulation .............................................. 362
17.3.1 Determination of MIC of Clove Oil against
Candida albicans .................................. 363
17.3.2 Determination of MIC of Clove Oil against
Escherichia coli .................................. 363
17.3.3 In Vitro Antibacterial Activity Test Results ...... 363
17.3.4 In Vitro Antifungal Activity Tests Results
(Table 17.4) ...................................... 364
17.3.5 In Vivo Antifungal Activity Test Results against
Experimental Vaginal Candidiasis .................. 364
17.3.5.1 Evaluation of Efficacy of Liposomized
Clove Oil ................................ 364
17.3.5.2 Evaluation of Route of Administration .... 365
17.4 Conclusions ......................................... 366
References ............................................... 366
Subject Index ................................................. 369
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