Botanical Leads for Drug Discovery

Preface
Acknowledgements
Contents
Editor and Contributors
About the Editor
Contributors
List of Figures
List of Tables
1: Plant-Derived Drug Discovery: Introduction to Recent Approaches
1.1 Introduction
1.2 Plants as Potential Sources for Natural Products
1.3 Criteria for the Plant Selection
1.3.1 Ethnomedicinal Uses or Information from Traditional Medicine Systems
1.3.2 Chemosystematic Criteria
1.3.3 Ecological Approach
1.3.4 Random Collection
1.4 Authentication of Plant Material
1.5 Extraction Methods
1.6 Natural Product Library
1.7 Bioassay-Guided Isolation
1.8 Dereplication and Hyphenated Techniques
1.8.1 Liquid Chromatography-Mass Spectrometry
1.8.2 Capillary Electrophoresis-Mass Spectrometry (CE-MS)
1.8.3 Gas Chromatography-Mass Spectrometry (GC-MS)
1.8.4 Chemical Derivatization
1.8.5 Liquid Chromatography-Photo Diode Array Detector (LC-PDA)
1.8.6 Liquid Chromatography-Infrared Spectroscopy (LC-IR)
1.8.7 Liquid Chromatography-Nuclear Magnetic Resonance Spectroscopy (LC-NMR)
1.9 Multiple Hyphenated Techniques
1.10 Case Study
1.11 Impact on Synthetic Medicinal Chemistry
1.11.1 Semi-synthesis and Derivatization
1.11.2 Synthesis Inspired by Natural Products
1.11.3 Diverted Synthesis
1.12 Conclusion
References
2: Herbal Medicines as a Rational Alternative for Treatment of Human Diseases
2.1 Introduction
2.2 Traditional Knowledge of Herbal Medicines (HMs)
2.2.1 Ayurveda
2.2.2 Traditional Chinese Medicines (TCMs)
2.2.3 Kampo
2.2.4 Unani Medicines
2.2.5 Russian Herbal Medicines
2.2.6 Africa Traditional Herbal Medicines
2.2.7 Traditional Medicines of Korea: Sasang Constitutional Medicines (SCM)
2.3 Past, Present, and Future Scenario of Human Disease Prevention by Plant Products
2.4 Prevention of Important Diseases Using Herbal Medicines (HMs)
2.4.1 HMs Against Malaria
2.4.2 HMs Against Diabetes
2.4.3 HMs Against Cancer
2.4.4 HMs Against Alzheimer´s and Parkinson´s
2.4.5 HMs Against HIV
2.4.6 HMs Against Bacterial Food Poisoning and Fungal Mycotoxicosis
2.4.7 HMs Against Tuberculosis
2.4.8 HMs Against Epilepsy
2.4.9 HMs Against Hepatitis
2.4.10 HMs Against Multiple Sclerosis
2.5 Complementary and Alternative Medicine (CAM): Modern Technological Platform for Reverse Pharmacology
2.6 Safety Paradigm of Traditional Herbal Medicine
2.7 Conclusion and Future Prospective
References
3: Effect of Natural Products on Improvement of Blood Pathophysiology for Management of Sickle Cell Anemia
3.1 Introduction
3.2 Current Treatment Options of SCA
3.3 Prospects of Natural Products for the Treatment of SCA
3.4 Conclusion
References
4: Anti-inflammatory Activity of Medicinal Plants: Present Status and Future Perspectives
4.1 Introduction
4.2 Anti-inflammatory Effects of Plant Extracts
4.3 Anti-inflammatory Activity of Essential Oils
4.4 Anti-inflammatory Effects of Isoflavones
4.5 Anti-inflammatory Effects of Polyphenols
4.6 Role of Fermentation in Increasing Anti-inflammatory Properties of Herbs
4.7 Conclusion
References
5: Cannabinoids as Promising Anti-inflammatory Agent
5.1 Introduction
5.2 Pharmacokinetic-Pharmacodynamic Profile
5.3 Uses in Different Inflammatory Disease Condition
5.3.1 Rheumatoid Arthritis (RA)
5.3.2 Type 1 Diabetes Mellitus (DM1)
5.3.3 Multiple Sclerosis (MS)
5.3.4 Alzheimer´s Disease (AD)
5.3.5 Edema and Hyperalgesia
5.3.6 Inflammatory Lung Diseases (ILD)
5.3.7 Atherosclerosis
5.4 Conclusion
References
6: Plant Volatile Organic Compounds and Neuroregenerative Health
6.1 Introduction
6.2 Plant VOCs
6.2.1 Plant VOCs - Definition
6.2.2 Biosynthesis and Chemical Nature of Plant VOCs
6.2.3 Analysis of Plant VOCs
6.2.4 Functions of Plant VOCs Within Plant and Habitat
6.3 Effects of Plant VOCs on Human Health
6.3.1 Antimicrobial Effects
6.3.2 Respiratory Ailments
6.3.3 Skin Healing Properties
6.3.4 Antioxidant Properties
6.3.5 Quality of Life Improvement in Cancer Patients
6.3.6 Pain and Inflammation
6.3.7 Other Health Benefits
6.4 Neurological Health and Plants VOCs
6.4.1 Neurological Disorders
6.4.2 Essential Oils, and Their Volatiles - Role in Neurological Health
6.4.2.1 Acorus
6.4.2.2 Basil
6.4.2.3 Cedarwood
6.4.2.4 Gotukola
6.4.2.5 Jasmine
6.4.2.6 Lavender
6.4.2.7 Lemon Balm
6.4.2.8 Peppermint
6.4.2.9 Rose
6.4.2.10 Rosemary
6.4.2.11 Sage
6.4.2.12 Sandalwood
6.4.2.13 Su-He-Xiang-Wan
6.5 Conclusion
References
7: Medicinal Plants and Their Role in Inflammation: A Close Look on Future Drug Discovery
7.1 Introduction
7.2 Research Methodology
7.3 Results and Discussion
7.3.1 Plants Used as Anti-inflammation
7.3.1.1 Achillea millefolium
7.3.1.2 Aconitum heterophyllum
7.3.1.3 Azadirachta indica
7.3.1.4 Aegle marmelos
7.3.1.5 Annona squamosa
7.3.1.6 Bryophyllum pinnatum
7.3.1.7 Cassia fistula
7.3.1.8 Emblica officinalis
7.3.1.9 Hedera rhombea
7.3.1.10 Pluchea indica
7.3.1.11 Piper ovatum
7.3.1.12 Piper longum
7.3.1.13 Ricinus communis
7.3.1.14 Senna occidentalis
7.3.1.15 Sida cordifolia
7.3.1.16 Swertia chirata
7.3.1.17 Thespesia populnea
7.3.1.18 Zingiber officinale
7.3.2 Mechanism of Inflammation
7.3.3 Generic Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
7.3.4 Future Drug Perspectives
7.3.5 Patents (Table 7.2)
7.4 Conclusion
References
8: Phytochemistry and Pharmacological Activities of Rhodiola imbricata Edgew., a High Value Medicinal Herb of Cold Desert Hima...
8.1 Introduction
8.2 Morphology and Distribution of Golden Root
8.3 Traditional Uses
8.4 Phytochemistry
8.5 Phyto-chemotypes Identified through GC-MS
8.5.1 Phyto-chemotypes Identified from n-Hexane Root Extract
8.5.2 Phyto-chemotypes Identified from Chloroform and Dichloromethane Root Extract
8.5.3 Phyto-chemotypes Identified from Ethyl Acetate Root Extract
8.5.4 Phyto-chemotypes Identified from Ethanol Root Extract
8.6 Biological Aspects
8.6.1 Immunomodulatory Activity
8.6.1.1 IL-6, TNF-α, and NO Production
8.6.1.2 Phosphorylated IκB in PBMCs
8.6.1.3 Activation of Transcription Factor NF-κB in PBMCs
8.6.2 Radiomodulatory and Free-Radical Scavenging Activity
8.6.2.1 Electron Donation Ability of Hydro-alcoholic Fractionated Extract
8.6.2.2 O-2 Quenching Ability of Hydro-alcoholic Fractionated Extract
8.6.2.3 NO Scavenging Potential of Hydro-alcoholic Fractionated Extract
8.6.2.4 Erythrocyte Protection Potential of Hydro-Alcoholic Fractionated Extract
8.6.3 Anti-cellular and Immunomodulatory Activity
8.6.3.1 Hemolytic Activity
8.6.3.2 Effect on HL60 and EL-4 Cells Proliferation
8.6.3.3 ELISPOT Assay for TNF-α
8.6.4 Immunopotentiating Activity
8.6.5 Anticancer Activity
8.6.5.1 Effect on Cell Viability
8.6.5.2 Effect on Proliferation of K-562 Cells
8.6.5.3 Measurement of ROS in K-562 Cells
8.6.5.4 Effect on Apoptosis
8.6.5.5 Effect on Cell Cycle
8.6.5.6 Effect on NK Cell Cytotoxicity
8.6.6 Radioprotective Activity
8.6.6.1 Maximum Tolerated Dose (MTD)
8.6.6.2 Hemopoietic Stem Cells Protection
8.6.7 Dermal Wound Healing
8.6.8 Immunological Properties of R. imbricata Aqueous Extract
8.6.8.1 TLR4-MD2 Expression by Flow Cytometry
8.6.8.2 Enhanced Intracellular Granzyme-B Production
8.6.8.3 Increased Production of TH1 Cytokines
8.6.9 Antiproliferative Activity
8.6.10 Radioprotective Activity
8.6.11 Safety Study
8.6.12 Antioxidant Activity
8.6.12.1 Free Radical Scavenging Activity
8.6.12.2 Effect on Anti-Lipid Peroxidation Activity
8.6.12.3 Total Phenolic Content
8.6.12.4 Hydrogen Peroxide Radical Scavenging Activity
8.6.12.5 Total Flavonoid Content
8.6.13 Antioxidative Effect during Cold, Hypoxia, and Restraint Exposure
8.6.13.1 Adaptogenic Activity
8.6.13.2 Acute Toxicity
8.6.14 Cytoprotective Activity
8.6.15 Hepatoprotective Activity
8.6.15.1 Acute Toxicity
8.6.15.2 Effect on Hematological Parameters
8.6.15.3 Effect on Serum Biochemical Markers
8.6.15.4 Effect on In Vivo Antioxidant Activity
8.6.15.5 Histopathological Examination
8.7 Future Direction
References
9: Phyllanthus amarus Schum. and Thonn. as Herbal Medicine: Ethnobotany, Phytochemistry, and Pharmacology Aspects
9.1 Introduction
9.2 Ethnobotany
9.3 Phytochemistry
9.4 Pharmacological Activity
9.5 Phytochemical Analysis by Analytical Techniques
9.6 Patents
9.7 Conclusion
References
10: Medicinal Applications of Cannabidiol from the Genus Cannabis L.
10.1 Introduction
10.2 Morphology of the Genus Cannabis
10.2.1 Cannabis sativa
10.2.2 Cannabis indica
10.2.3 Cannabis ruderalis
10.2.4 Cannabis afghanica
10.3 Ethnobotanical Usages of Cannabis
10.4 Chemical Constituents of Cannabis
10.4.1 Tetrahydrocannabinol
10.4.2 Cannabinol
10.4.3 Cannabigerol
10.4.4 Cannabichromenes (CBC)
10.4.5 Cannabidiol
10.4.6 Cannabinodiol
10.4.7 Cannabielsoin
10.4.8 Cannabicyclol
10.4.9 Cannabitriol
10.5 Origin and Chemical Structure of Cannabidiol
10.5.1 Stereoisomers of Cannabidiol
10.5.2 Synthesis of Cannabidiol
10.5.3 Natural Homologues of Cannabidiol
10.5.4 Biosynthesis of THC and CBD (Fig. 10.15)
10.6 Pharmacological Applications of Cannabidiol (CBD)
10.6.1 Neurodegenerative Disorder
10.6.1.1 Parkinson Disease (PD)
10.6.1.2 Huntington Disease
10.6.1.3 Prion Diseases
10.6.1.4 Multiple Sclerosis (MS)
10.6.1.5 Epilepsy
10.6.1.6 Autism
10.6.1.7 Anxiolytic
10.6.1.8 Alzheimer´s Disease
10.6.1.9 Depression
10.6.1.10 Post-traumatic Stress Disorders (PTSD)
10.6.2 Diabetes Mellitus
10.6.3 Rheumatoid Arthritis and Ankylosing Spondylitis
10.6.4 Anticancer Activity
10.6.4.1 CBD and Leukaemia/Lymphoma
10.6.4.2 Angiogenesis
10.6.5 Cannabidiol in Pain Management
10.6.5.1 Neuropathic Pain
10.6.5.2 Cancer Pain
10.6.5.3 Additional Pain-Related Therapeutic Benefits of Cannabinoids
10.6.6 HIV/AIDS
10.6.7 Nausea and Vomiting
10.6.8 Antipsychotic Effect of CBD
10.6.9 CBD for Recreational Use
10.7 Pharmacology of Cannabidiol
10.7.1 Routes of Administration and Dosage
10.7.2 Pharmacokinetics
10.7.3 Pharmacodynamics
10.7.4 Toxicology
10.7.5 Adverse Effects
10.7.6 Mechanism of Action of Cannabidiol
10.8 Marketing Approvals of CBD as Medicinal Product
10.8.1 Sativex
10.8.2 Epidiolex
10.8.2.1 Arvisol
10.8.3 ZYN002
10.9 Legal Aspects of CBD and Cannabis
10.10 Conclusion and Future Direction
References
11: Genetic Variability in Ocimum L. Germplasm: Medicinal and Economic Potential for Value Addition and Product Development
11.1 Introduction
11.2 Methodology
11.3 Results and Discussion
11.4 Conclusion
References
12: Chemical Constituents and Pharmacological Activities of Marrubium vulgare L., an Important Medicinal Herb
12.1 Introduction
12.2 Methodology
12.3 Morphological Description
12.4 Traditional Uses of Marrubium vulgare
12.5 Phytochemistry
12.5.1 Diterpenoids
12.5.2 Flavonoids
12.5.3 Phenylpropanoid and Phenylethanoid Glycosides
12.5.4 Active Compounds in Essential Oil of Marrubium vulgare
12.5.5 Other Chemical Constituents
12.6 Pharmacological Activities
12.6.1 Anti-inflammatory Activity
12.6.2 Analgesic and Antinociceptive Activities
12.6.3 Antiodematogenic Activity
12.6.4 Antispasmodic Activity
12.6.5 Gastroprotective Activity
12.6.6 Antihypertensive Properties
12.6.7 Antidiabetic and Antihyperlipidemic Activities
12.6.8 Antihepatotoxic Activity
12.6.9 Antioxidant Activity
12.6.10 Antimicrobial Activity
12.6.11 Anticancer Activity
12.6.12 Antiprotozoal, Molluscicidal, and Mosquitocidal Activities
12.7 Conclusion and Future Perspectives
References
13: Ethnobotany as a Science of Preserving Traditional Knowledge: Traditional Uses of Wild Medicinal Plants from District Reas...
13.1 Introduction
13.2 Study Area: Geography and Climate
13.3 Methodology: Survey, Collection and Data Investigation
13.4 Results
13.4.1 Vegetation Composition and Distribution of Plant Species
13.4.2 Species-Family Relationship
13.4.3 Ethnobotanical Information
13.4.3.1 Double Usage
13.4.3.2 Multi-usage
13.4.3.3 Plant Usage Classification
13.5 Discussion and Compared Studies
13.6 Conclusion
References
14: Medicinal Value of High-Altitude Plants of Indian Himalaya
14.1 Introduction
14.2 Medicinal Plants from High-Altitude Himalayan Region
14.3 Plants Growing in High-Altitude Region
14.3.1 Aconitum heterophyllum
14.3.1.1 General Note on A. heterophyllum
14.3.1.2 Chemical Constituents of Aconitum heterophyllum
14.3.1.3 Molecular Structure of Aconitum heterophyllum
14.3.1.4 Medicinal Uses of A. heterophyllum
14.3.1.4.1 Digestive Disease
14.3.1.4.2 Respiratory Disease
14.3.1.4.3 Urinary System
14.3.1.4.4 Reproductive System
14.3.1.5 Pharmacological Uses
14.3.1.5.1 Hepatoprotective Activity
14.3.1.5.2 Miscellaneous Activities
14.3.1.6 Safety and Toxicity Studies
14.3.2 Hippophae rhamnoides
14.3.2.1 General Note on Hippophae rhamnoides
14.3.2.2 Chemical Constituents of Hippophae rhamnoides
14.3.2.3 Molecular Structures of H. rhamnoides
14.3.2.4 Medicinal Uses of Hippophae rhamnoides
14.3.2.5 Pharmacological Uses of Hippophae rhamnoides
14.3.2.5.1 Antimicrobial and Antitumoral Effects
14.3.2.5.2 Antibacterial and Antiviral Effects
14.3.2.5.3 Antiulcer Effects
14.3.2.5.4 Antiradiation Effects
14.3.2.5.5 Liver Diseases
14.3.2.5.6 Dermatological Effects
14.3.2.6 Safety and Toxicity Studies of Hippophae rhamnoides
14.3.3 Inula racemosa
14.3.3.1 General Note of Inula racemosa
14.3.3.2 Chemical Constituents of Inula racemosa
14.3.3.3 Molecular Structures of Inula racemosa
14.3.3.4 Medicinal Uses of Inula racemosa
14.3.3.5 Pharmacological Uses of Inula racemosa
14.3.3.5.1 Anti-inflammatory Activity
14.3.3.5.2 Analgesic Effect
14.3.3.5.3 Antibacterial Activity
14.3.3.5.4 Antioxidant Activity
14.3.3.5.5 Cardioprotective Activity
14.3.3.5.6 Adaptgenicity Potential
14.3.3.6 Toxicology and Dosage of I. racemosa
14.3.4 Rhodiola rosea
14.3.4.1 General Notes of Rhodiola rosea
14.3.4.2 Chemical Constituents of Rhodiola rosea
14.3.4.3 Molecular Structures of Rhodiola rosea Chemical Constituents
14.3.4.4 Medicinal Importance of Rhodiola rosea
14.3.4.5 Pharmacological and Clinical Studies of Rhodiola rosea
14.3.4.5.1 Effects on Central Nervous System of Rhodiola rosea
14.3.4.5.2 Antioxidant Properties of Rhodiola rosea
14.3.4.5.3 Against Neuro-Inflammation of Rhodiola rosea
14.3.4.5.4 Effects on Physical Work Capacity of Rhodiola rosea
14.3.4.5.5 Cardioprotective Effects of Rhodiola rosea
14.3.4.5.6 Effect on Endocrine and Reproductive Activity of Rhodiola rosea
14.3.4.5.7 Effect on Oncogenic Kinase PAK of Rhodiola rosea
14.3.4.5.8 Antiaddiction Effect of Rhodiola rosea
14.3.4.5.9 Antistroke Effect of Rhodiola rosea
14.3.4.6 Toxicity of Rhodiola rosea
14.3.5 Sinopodophyllum hexandrum
14.3.5.1 General Note of Sinopodophyllum hexandrum
14.3.5.2 Chemical Constituents of Sinopodophyllum hexandrum
14.3.5.3 Medicinal Uses of Sinopodophyllum hexandrum
14.3.5.4 Pharmacological Applications of Sinopodophyllum hexandrum
14.3.5.4.1 Radioprotection of Sinopodophyllum hexandrum
14.3.5.4.2 Anti-inflammatory Activity of Sinopodophyllum hexandrum
14.3.5.4.3 Insecticidal Activity of Sinopodophyllum hexandrum
14.3.5.4.4 Anticancer Activity of Sinopodophyllum hexandrum
14.3.5.4.5 Antifungal Activity of Sinopodophyllum hexandrum
14.3.5.5 Toxicological Data of Sinopodophyllum hexandrum
14.4 Why High-Altitude Plants Are Different from Low Elevation Plants?
14.5 Conclusion and Future Direction
References
15: Medicinal Plants of District Kupwara Used in the Treatment of Human Diseases and Their Associated Biological Functions
15.1 Introduction
15.2 Material and Methods
15.2.1 Study Area
15.2.2 Data Analysis
15.3 Results and Discussions
15.3.1 Plant Parts Used as Medicine and Mode of Utilization
15.3.2 Previous Research Studies and Comparison with Present Outcomes
15.4 Conclusion
References
16: Capsicum chinense Jacq.: Ethnobotany, Bioactivity and Future Prospects
16.1 Introduction
16.2 Taxonomic Position
16.3 Botanical Enumeration
16.4 History
16.5 Ethnobotanical Usages
16.6 Bioactivity of the Plant
16.6.1 Effect of Chilli on Weight Loss
16.6.2 In Antipain Therapy
16.6.3 Regulation of Body Temperature
16.6.4 Cancer Prevention
16.6.5 Source of Antioxidant and Anti-inflammatory
16.6.6 As Antimicrobial Agent
16.6.7 Remedy for Gastric Ulcer
16.6.8 Cardiovascular Activity
16.6.9 Other Non-pharmacological Applications
16.7 Business Potential and Future Prospects
16.8 Conclusion
References
17: Indigenous Plant Knowledge for Human Health Care from Jasrota Wildlife Sanctuary (Western Himalaya), India
17.1 Introduction
17.2 Materials and Methods
17.2.1 Study Area
17.2.2 Medicinal Plant Survey and Data Collection
17.2.3 Data Analysis
17.3 Results and Discussion
17.3.1 Demography of Informants
17.3.2 Floristic Description
17.3.3 Frequency Index (FI)
17.4 Conclusion
References
18: Ethanobotany and Phytochemistry of Lantana camara L. (Verbenaceae)
18.1 Introduction
18.2 Taxonomic Classification
18.3 Plant Morphology
18.4 Ecology and Habitat
18.5 Geographical Distribution
18.6 Ethnobotany
18.7 Phytochemistry
18.8 Conclusion
References
19: Cymbopogon winterianus Jowitt ex Bor, a Hub for Various Industrial and Pharmaceutical Applications
19.1 Introduction
19.2 Botanical Description
19.3 High-Yielding Varieties
19.4 Extraction of Essential Oil
19.5 Chemical Composition of Essential Oil
19.6 Biological Activities and Pharmaceutical Importance
19.6.1 Anticonvulsant Activity
19.6.2 Antimicrobial Activity
19.6.3 Antinociceptive and Anti-inflammatory Activity
19.6.4 Cardiovascular Effect
19.6.5 Weedicides
19.6.6 Molluscicidal Activity
19.6.7 Insecticidal Activity
19.6.8 Acaricidal Activity
19.6.9 Aromatherapy
19.6.10 Perfumery and Cosmetic Industry
19.6.11 Bioresource from Waste Biomass
19.6.12 Other Uses
19.7 Global Market and Demand
19.8 Conclusion
References
20: Botanical Sources, Chemistry Aspects and Biological Functions of Berberine: An Updated Critical Review
20.1 Introduction
20.2 Botanical Sources and Traditional Use
20.3 Methods of Extraction
20.4 Isolation and Quantification Methods
20.5 Chemistry Aspects
20.6 Biological Activities
20.6.1 Antimicrobial Properties
20.6.2 Antidiarrhoeal Activity
20.6.3 Immunomodulatory Activity
20.6.4 Antihyperglycaemic Effect
20.6.5 Antioxidant Properties
20.6.6 Hepatoprotective Properties
20.6.7 Cardiovascular Functions
20.6.8 Anticarcinogenic Properties: Antitumor and Apoptosis Functions
20.6.9 Miscellaneous Functions of Berberine
20.7 Clinical Trials and Recommendations
20.8 Patents
20.9 Conclusion
References
Glossary