Cannabis and Khat in Drug Discovery

The Discovery Pipeline and the Endocannabinoid System

1st Edition - August 9, 2024
Imprint: Elsevier Science
Editors: Andrew G. Mtewa, Tadele Mekuriya, Paul E. Alele, John O. Igoli, Fanuel Lampiao
Language: English
Paperback ISBN:
9 7 8 - 0 - 3 2 3 - 9 5 9 2 7 - 8
eBook ISBN:
9 7 8 - 0 - 3 2 3 - 9 5 9 2 8 - 5

Cannabis and Khat in Drug Discovery: The Discovery Pipeline and the Endocannabinoid System provides comprehensive coverage of two important psychoactive plants: Khat and Cannabis.… Read more

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Cannabis and Khat in Drug Discovery: The Discovery Pipeline and the Endocannabinoid System provides comprehensive coverage of two important psychoactive plants: Khat and Cannabis. Initial research has found that compounds and derivatives from Cannabis and Khat are found to have promising properties that can be used for the discovery, design and development of potential drug leads against various diseases. This book extensively discusses the drug discovery and allied sciences of these compounds in the drug discovery pipeline, including basic research and computer aided modeling in ligand-drug interactions and their interactions with the endocannabinoid system. Categorized into sections including, chemical analyses and bioassays, medicinal chemistry, chemical biology and pharmacology, clinical applications, and policy and regulations, this book covers the methods and protocols involved and will be of interest to students, researchers, policymakers and all those involved in drug discovery research.

Cover image
Title page
Table of Contents
Copyright
Dedication
List of contributors
Preface
Section 1: Background to cannabis and khat in the growing industrialization
Chapter 1. Introduction to cannabis and Catha edulis
Abstract
1.1 Introduction
1.2 Cannabis and khat in perspective
1.3 Conclusion
References
Chapter 2. Ethnobotanical utilisation and status of Cannabis sativa L.
Abstract
2.1 Introduction
2.2 Historical use of Cannabis sativa L.
2.3 Recent use of Cannabis sativa L.
2.4 Geographic distribution of traditional use of Cannabis Sativa L.
2.5 Significance of Cannabis sativa L.
2.6 Preparations of Cannabis sativa L.
2.7 Pharmacological studies related to Cannabis sativa L. use
2.8 Conclusion
References
Chapter 3. Cannabis chemotypes and chemovars
Abstract
3.1 Introduction
3.2 Classification of cannabis plants
3.3 Chemotypes and chemovars
3.4 Current work in cannabis research
3.5 The future of cannabis research
3.6 Conclusion
References
Chapter 4. Cannabinoids infused foods
Abstract
4.1 Introduction to cannabis-infused foods
4.2 Brief overview of the historical and cultural context of infusion
4.3 Infusing techniques
4.4 Dosage considerations, general stability testing and potency calculations
4.5 Health and wellness edibles
4.6 Legal and safety considerations
4.7 Future perspectives in cannabis-infused foods
References
Chapter 5. Water demand and management in the growth of cannabis industrialization
Abstract
5.1 Global water demand and water demand in farming
5.2 A general perspective of water demand in crop production
5.3 Water demand in cannabis Industry
5.4 Cannabis industry and water resources contamination
5.5 Water policy on hemp farming anywhere in the world
5.6 Conclusion and recommendations
References
Section 2: Chemical analyses
Chapter 6. Extraction and isolation of cannabinoids
Abstract
6.1 Introduction
6.2 Extraction of cannabinoids (conventional and nonconventional methods)
6.3 Extraction of cannabinoids from biological and forensic samples
6.4 Preparative isolation of cannabinoids
6.5 Transformation of cannabinoids (during plant processing as drying, extraction, external factors as light)
6.6 Metabolomics and chemometric tools for analysis of cannabinoids
6.7 Conclusion
References
Chapter 7. Chromatographic fingerprinting and spectroscopic profiling of cannabinoids
Abstract
7.1 Introduction
7.2 Separation, identification, and characterization methods used on C. sativa L
7.3 Conclusions
References
Chapter 8. Antiviral properties of cannabidiol for the management of COVID-19
Abstract
8.1 Introduction
8.2 Cannabidiol viral immune responses
8.3 Cannabinoid receptors
8.4 Important methods and clinical applications of cannabinoids
8.5 Current applications
8.6 Future projections
8.7 Conclusions
References
Chapter 9. In vivo and in vitro assays, and safety profiles of cannabinoids
Abstract
9.1 Introduction
9.2 Biomedical research on cannabinoids
9.3 Safety profile of cannabinoids
9.4 Perspectives
9.5 Conclusions
References
Chapter 10. Immunomodulatory properties of cannabinoids; a molecular insight
Abstract
10.1 Introduction
10.2 Immunomodulatory activities of endocannabinoids
10.3 Immunomodulatory properties of phytocannabinoids
10.4 Conclusion and prospects
References
Chapter 11. Phytochemistry of Catha edulis
Abstract
11.1 Introduction
11.2 Phytochemistry of Catha edulis
11.3 Future prospects of Khat
11.4 Conclusions
References
Section 3: Medicinal chemistry, chemical biology, and pharmacology in cannabis and khat
Chapter 12. Molecular mechanisms of cannabinergics
Abstract
12.1 Introduction
12.2 Cannabinoid receptors: molecular mechanisms of signal transduction and their biochemical effects
12.3 Endocannabinergics: a counterbalance of signals mediated by anandamide and 2-arachidonoylglycerol
12.4 Molecular mechanisms of phytocannabinoid-mediated addiction
12.5 Conclusion and future prospects
References
Chapter 13. Biosynthesis of endocannabinoids and phytocannabinoids
Abstract
13.1 Introduction
13.2 Biosynthesis of endocannabinoids
13.3 The biosynthesis of phytocannabinoids
13.4 Conclusion and prospects
References
Chapter 14. Cannabinoid ligands and receptors
Abstract
14.1 Endocannabinoid system
14.2 Cannabinoid legends
14.3 Cannabinoid receptors distribution
14.4 Cannabinoid receptors and cannabinoid receptors signaling
14.5 Clinical use of the compounds that target the endocannabinoid system
References
Chapter 15. Pharmacologically active ingredients from Catha edulis
Abstract
15.1 Introduction
15.2 Active ingredients from Catha edulis
15.3 Techniques for determination of the active ingredients
15.4 Summary
References
Chapter 16. Interactions of Catha edulis Forsk with CB2 receptors
Abstract
16.1 Introduction
16.2 The endocannabinoid system
16.3 Catha edulis Forsk
16.4 Conclusion and recommendations
References
Chapter 17. Modeling cannabis and Catha edulis bioactives and derivatives: insights from computational and theoretical predictions
Abstract
17.1 Introduction
17.2 Computer-aided drug discovery approaches for cannabis and Khat drug discovery
17.3 Structure-based drug designing (SBDD) in cannabis and Khat drug
17.4 Ligand-based drug designing (LBDD) in Khat and cannabis drug discovery
17.5 Application of chemoinformatics to cannabis and Khat phytochemicals
17.6 Physicochemical property profiling studies
17.7 Chemical space visualization
17.8 Scaffold analysis
17.9 Pharmacokinetic and toxicity prediction
17.10 Conclusion and future prospects
References
Chapter 18. Endophyte-aided drug discovery: design, and development from psychotic plants
Abstract
18.1 Introduction
18.2 Natural products as sources of drugs
18.3 Bioactive compounds derived from endophytes
18.4 Drug discovery and design from endophyte-derived compounds
18.5 Computational approaches
18.6 Drug development of endophytes-derived compounds
18.7 Challenges associated with endophyte derivation of medicines and potential solutions
18.8 Lessons and future perspectives
18.9 Conclusion
References
Chapter 19. The chemistry and pharmacology of tetrahydrocannabinol and cannabidiol
Abstract
19.1 Introduction
19.2 Chemistry of cannabidiol
19.3 Acid cyclizations of cannabidiol
19.4 Reactions of cannabidiol under basic conditions
19.5 Oxidation of cannabidiol and cannabidiol acid
19.6 Photochemical reactions of cannabidiol
19.7 Pharmacology of cannabidiol
19.8 Anticonvulsive effects of cannabidiol
19.9 Sedative and anxiolytic effects of cannabidiol
19.10 Hypnotic effects of cannabidiol
19.11 Antipsychotic effects of cannabidiol
19.12 Antiinflammatory effects of cannabidiol
19.13 Anticancer effects of cannabidiol
19.14 Bone formation and structure healing
19.15 Antiischemic effects of cannabidiol
19.16 Antivomiting effects of cannabidiol
19.17 Neuroprotective and neurodegenerative effects of cannabidiol
19.18 Gastrointestinal effects of cannabidiol
19.19 Chemistry of tetrahydrocannabinol (THC)
19.20 Pharmacology of tetrahydrocannabinol
19.21 Antinausea effects of tetrahydrocannabinol
19.22 Antiinflammatory effect of tetrahydrocannabinol
19.23 Neurodegenerative diseases and neuroprotection
19.24 Multiple sclerosis
19.25 Parkinson’s disease
19.26 Anxiety and fear
19.27 Epilepsy
19.28 Sleep
19.29 Huntington’s disease
19.30 Schizophrenia
19.31 Gilles De La Tourette’s syndrome
19.32 Alzheimers disease (AD)
19.33 Antitumor effect of tetrahydrocannabinol
19.34 Effects of tetrahydrocannabinol on cancer
19.35 Analgesic effects of tetrahydrocannabinol
19.36 Gastrointestinal disorders
19.37 Diseases of energy metabolism
19.38 Cardiovascular disorders
19.39 Asthma
19.40 Glaucoma
19.41 Cachexia and anorexia
19.42 Conclusion
References
Chapter 20. Medicinal chemistry of cannabinoids
Abstract
20.1 Introduction
20.2 Cannabinoids
20.3 Endocannabinoids
20.4 Potential therapeutic applications: cannabinoid-based therapeutics
20.5 Conclusions
References
Section 4: Catha edulis and cannabinoids in disease management; clinical aspects
Chapter 21. Cannabis in pain management
Abstract
21.1 Introduction
21.2 Historical significance of cannabis
21.3 Cannabis phytochemistry
21.4 Male vs. female cannabis
21.5 Chemical composition of cannabis
21.6 A brief history of cannabis and pain
21.7 Cannabinoids for pain management
21.8 Current evidence relating to the use of cannabis for chronic pain
21.9 Conclusion
References
Chapter 22. Cannabis in anticancer drug development
Abstract
22.1 Introduction
22.2 Cancer therapy approaches in conventional practice
22.3 Marketed anticancer drugs from plants
22.4 Drug likeness of anticancer compound from cannabis
22.5 The endocannabinoid system
22.6 Anticancer activity of phytocannabinoids and synthetic cannabinoids
22.7 Conclusion
References
Chapter 23. Catha edulis in cancer management
Abstract
23.1 Introduction
23.2 Habitat of Catha edulis
23.3 Chemical composition of Catha edulis
23.4 Medicinal properties of Catha edulis
23.5 Antiinflammatory properties
23.6 Antibacterial properties
23.7 Antifungal properties
23.8 Analgesic properties
23.9 Appetite suppression
23.10 Cardiovascular effects
23.11 Cytotoxic influence of Catha edulis on carcinoma
23.12 Anticancer potential of Catha edulis
23.13 Inhibition of cancer cell proliferation
23.14 Antioxidant activity
23.15 Immune system modulation
23.16 Conclusion
References
Chapter 24. Cannabis in antimicrobial drug development
Abstract
24.1 Introduction
24.2 Conclusion
References
Chapter 25. Cannabis in posttraumatic stress disorder management
Abstract
25.1 Introduction to posttraumatic stress disorder (PTSD)
25.2 Cannabis
25.3 Endocannabinoid (eCB) system
25.4 Cannabis sativa as a therapeutic tool for the management of posttraumatic stress disorder
25.5 Pathophysiology for posttraumatic stress disorder
25.6 Treatments for posttraumatic stress disorder
25.7 Cannabis (marijuana) – mechanism of action for the management of posttraumatic stress disorder
25.8 Conclusion
25.9 Future perspectives
References
Chapter 26. The endocannabinoid and immunomodulatory systems of cannabis and its products
Abstract
26.1 Introduction
26.2 Phytocannabinoids: mechanism and immunity
26.3 Modulation of immune cells by cannabis components
26.4 Conclusions and future perspectives
References
Chapter 27. Catha edulis in antimicrobial drug development
Abstract
27.1 Introduction
27.2 Conclusion
References
Chapter 28. Clinical uses of cannabis and Catha edulis products
Abstract
28.1 Introduction
28.2 Evidence-based insights: a review of clinical trial data on cannabis and cannabinoids products
28.3 Side effects of cannabis and cannabinoids products during clinical trials
28.4 Clinical trials on Catha edulis
28.5 Side effects of Catha edulis during clinical trials
28.6 Interactions between the pharmacological effects of Catha edulis and Cannabis sativa
28.7 Conclusion
References
Chapter 29. Innovative cannabis products on the market
Abstract
29.1 Introduction to innovative cannabis products
29.2 Innovations in medicine and pharmaceuticals
29.3 Cannabis innovations in the health and wellness industry
29.4 Cannabis innovations in the construction industry
29.5 Cannabis innovations in textile and consumer goods industries
29.6 Cannabis innovations in finance and investment
29.7 Cannabis Innovations in research and academia
29.8 Cannabis innovations in the food industry
29.9 Complexities with cannabis innovations
29.10 Legal complexities
29.11 Future prospects of cannabis innovations
References
Chapter 30. Pesticides and disease causing contaminants in Khat and Khat products
Abstract
30.1 Background
30.2 Pesticide use in Khat and Cannabis and its toxicity to consumers
30.3 Quality control in Khat and Cannabis product formulation
30.4 Heavy metals in cannabis
30.5 Risk of carcinogenicity
30.6 Conclusion
References
Section 5: Policy and regulation on Cannabis and Khat
Chapter 31. Industrial and medical use approvals and regulations of cannabis products
Abstract
31.1 Introduction
31.2 Global legal status of cannabis
31.3 Therapeutic uses of cannabis
31.4 Pain management
31.5 Obesity
31.6 Multiple sclerosis and inflammation
31.7 Anxiety
31.8 Epilepsy
31.9 Parkinson’s and Alzheimer’s disease
31.10 Medicinal use approval and regulations
31.11 Industrial use approvals and regulations
31.12 Conclusion
Abbreviations
References
Chapter 32. Approaches in the conservation of Cannabis species and their chemical products
Abstract
32.1 Introduction
32.2 Climatic conditions in cannabis cultivation
32.3 Temperature requirements for cannabis cultivation
32.4 Rainfall and water availability for cannabis cultivation
32.5 Sunlight and photoperiodicity of cannabis growth patterns
32.6 Altitude and microclimates in cannabis cultivation
32.7 Cannabis and ecologically sustainable cultivation practices
32.8 Environmental conservation in cannabis cultivation
32.9 Biotechnology approaches in cannabis conservation
32.10 Gene collection and characterization
32.11 Development of seedbanks
32.12 Breeding and propagation
32.13 Application of bioinformatics in cannabis conservation
32.14 Conclusion
References
Chapter 33. Policy and regulation of Catha edulis product uses
Abstract
33.1 Introduction
33.2 Socioeconomic perspective
33.3 Previous attempts at regulation
33.4 Anti-khat legislations since 1971
33.5 Proposed approach to regulation
33.6 Conclusion
References
Further reading
Chapter 34. Future perspectives on the use of cannabis and Catha edulis products
Abstract
34.1 Introduction to future perspectives of cannabis and Khat products
34.2 Cannabis and Khat’s relevance to industry
34.3 The construction industry
34.4 Social well-being
34.5 Political landscape and security
34.6 Interventions for controls
34.7 Policy frameworks
34.8 Conclusion
References
Chapter 35. Dependence syndrome in Catha edulis product uses
Abstract
35.1 Introduction
35.2 Background
35.3 Conclusion
References
Index

Andrew G. Mtewa

A member of the American Chemical Society (ACS), the Phytochemistry Society of Europe (PSE), the National Organization for the Professional Advancement of Black Chemists and Chemical Engineers (NOBCChE), and an Associate Member of the Royal Society of Chemistry (RSC), Andrew is a Medicinal Chemist trained under the Wellcome Center for Anti-infectives Research (WCAiR) at the Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee in Scotland as part of his PhD studies. He also did his PhD at the Mbarara University of Science and Technology under the Pharm-Biotechnology and Traditional Medicine Centre in Uganda and attended a Phytochemistry PhD summer School at Kenya’s Egerton University on a DAAD scholarship. His main area of interest is drug design and development using medicinal chemistry aspects and various computational and synthetic techniques to obtain logical hits to leads for particular biological targets from synthetic scaffolds in various libraries, de novo as well as from natural products. He did his MSc degree in Applied Chemistry (Natural Product Chemistry). He has a passion to coach and train upcoming drug discoverers to search for drugs beyond plant extracts to compound level towards optimization. Before joining the academia, Andrew served in various portfolios including but not limited to being Quality Assurance Manager for Valid Nutrition’s therapeutic foods’ factory, assistant Quality Manager (Shifts controller) for Alliance one international tobacco processors and graduate trainee for the Japanese Tobacco International (JTI), Malawi factory. He founded Leptons Scientific consultants in 2011 and has provided consultancy services in his areas of expertise to various clients. For close to a decade now, Andrew has also been researching military strategies, security and weaponry among others. He studied intelligence analysis and is trained in H2H close combat. He has published various journal articles and book chapters with various publishers such as Elsevier and is a reviewer for various journals including Systematic Reviews, Tuberculosis and of late, the African Health Sciences among others. Apart from this book, he is also the lead editor of the book ‘Poisonous Plants and Phytochemicals in Drug Discovery’ by Wiley. Currently, Andrew is a Chemistry lecturer at the Malawi University of Science and Technology in Malawi.

Affiliations and expertise

Medicinal Chemist, Chemistry Section, Department of Applied Studies, Malawi Institute of Technology, Malawi University of Science and Technology, Malawi

Tadele Mekuriya

Tadele Mekuriya is a PhD fellow in the area of Clinical Pharmacy and Pharmacovigilance. His PhD research is in the area of Pharmacovigilance in hospitalized patients, developing and validating adverse drug-reaction risk prediction tools among the elderly population. More widely, he also works in the application of clinical pharmacy of drug agents and new chemical entities from synthetic and natural products including psychoactive agents and observe their clinical outcomes. He has 15 publications including research articles, book chapters and books. He has taught and done research at Ambo University in Ethiopia in the same field for over 5 years. Tadele is currently a Senior Lecturer of Clinical Pharmacy at Mbarara University of Science and Technology in Uganda where he is also pursuing his PhD studies.

Affiliations and expertise

Clinical Pharmacologist, Department of Pharmacy, Ambo University, Ethiopia

Paul E. Alele

Paul E. Alele is a pharmacologist and physician. He is presently an Associate Professor in the Department of Pharmacology and Therapeutics at Mbarara University of Science and Technology in Uganda. He earned a Ph.D. (Idaho) in pharmaceutical sciences and then did postdoctoral training in developmental neurobiology investigating the influence of psychostimulants such as methylphenidate on neuronal development and activity. His research involves both basic biomedical questions using animal models, and field and clinical studies comprising human participants. He has conducted research related to khat (Catha edulis), caffeine, and ethanol, and how these substances modulate seizure expression, dependence and withdrawal. He has published peer-reviewed journal articles widely in the neurosciences, ethnopharmacology and clinical aspects of pharmacology. Dr. Alele has been teaching for over twenty years and has mentored undergraduate and postgraduate student researchers and junior faculty supported by grants from the Fogarty International Center/National Institutes of Health in the U.S.

Affiliations and expertise

Physician and Pharmacologist, Department of Pharmacology, Mbarara University of Science and Technology, Uganda

John O. Igoli

John O. Igoli is a professor of organic chemistry. He obtained a PhD in organic chemistry specializing in natural products from the University of Nigeria Nsukka and had a six year postdoctoral training at the Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde Glasgow. He currently works at the Department of Chemistry, University of Agriculture, Makurdi Nigeria. His expertise is in the area of Phytochemistry, Ethnobotany and Natural products. Isolation and structural characterization of compounds from plants and other sources using chromatographic and spectroscopic methods and bioactivity studies against NTDs. He has over 150 publications centred on ethnobotanical studies, pharmacology, Phytochemistry and structure elucidation of novel bioactive compounds especially those with antikinetoplastid activities. He is avidly involved in training young scientists on the spectroscopic identification of compounds and the evaluation of plants used in traditional medicine. He is passionate about teaching and research collaboration. He has facilitated several structure elucidation, grant writing and research workshops. He is currently editing a special edition of Frontiers in pharmacology focused on drug discovery for neglected tropical diseases.

Affiliations and expertise

Natural Products Research Group, Department of Chemistry, University of Agriculture, Makurdi, Nigeria

Fanuel Lampiao

Fanuel Lampiao is a Professor of Reproductive Physiology at the College of Medicine, University of Malawi. He is the current Dean of Postgraduate Studies and Research. His research interests are on the influence of herbal extracts on various diseases which has culminated in the authorship of several scientific manuscripts, book chapters, as well as over 50 international and national conference presentations. He is the recipient of various national and international awards, grants and scholarships. Besides his contribution to the dissemination of research findings, he serves on the editorial board of leading publications and regularly performs reviews for international funding agencies and journals. His preferred work assignments are multifactorial and include the transfer of subject specific knowledge at undergraduate and postgraduate level, and solving intricate research questions

Affiliations and expertise

Dean of Postgraduate Studies and Research / Professor of Reproductive Physiology, College of Medicine, University of Malawi, Malawi

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Cannabis and Khat in Drug Discovery

The Discovery Pipeline and the Endocannabinoid System

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Andrew G. Mtewa

Tadele Mekuriya

Paul E. Alele

John O. Igoli

Fanuel Lampiao

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