Diets rich in plant polyphenols or dietary polyphenols are the subject of increasing scientific interest because of their diverse range of health benefits and medicinal uses. This book, Dietary Polyphenols in Human Diseases: Advances and Challenges in Drug Discovery, fills the gap that exists in the current knowledge by presenting the latest information in the area of polyphenol-based drug discovery research. The book focuses on the current understanding of the beneficial effects on human health of diets rich in polyphenols and/or polyphenolic compounds derived from dietary sources (plant-based foods) and their possible preventive role in the management of chronic human diseases. In addition, biochemical mechanisms involved in the antioxidative effect of dietary polyphenols along with their bioavailability, pharmacokinetic, and toxicological considerations are also discussed herein.
Key Features
- Presents health benefits and medicinal importance of dietary polyphenols having antioxidative effects and their possible preventive role against oxidative stress (OS)-induced chronic human diseases.
- Summarizes the latest understanding of the biochemical mechanism(s) involved in the antioxidative action of dietary polyphenols along with their bioavailability, pharmacokinetic, and toxicological considerations.
- Highlights novel approaches of drug discovery from dietary polyphenols through computational screening of bioactive phytochemical components.
With contributions by a global team of experts (academics, scientists, and researchers), this book is intended to be a useful resource for a wider audience, particularly those working in the area of drug discovery and development research, such as discovery scientists, pharmaceutical scientists (R&D), formulation scientists, medicinal chemists, pharmacologists, toxicologists, phytochemists, biochemists, clinicians, researchers, students, teachers, and many others.
Author(s): Mithun Rudrapal
Publisher: CRC Press
Year: 2022
Language: English
Pages: 300
City: Boca Raton
Cover
Half Title
Title Page
Copyright Page
Table of Contents
Preface
About the Editor
Contributors
1 Dietary Polyphenols, Antioxidant Effects, and Human Diseases
1.1 Introduction
1.2 Dietary Polyphenols
1.2.1 General Chemistry, Structure and Sources of Polyphenols
1.3 Dietary Polyphenols as Antioxidants
1.3.1 Antioxidant Mechanisms of Dietary Polyphenols
1.3.2 Metabolism and Bioavailability of Dietary Polyphenols
1.4 Role of Polyphenols in Human Disease Management
1.4.1 Protective Role of Dietary Polyphenols in Metabolic Syndrome (MetS)
1.4.2 Protective Role of Dietary Polyphenols in CVDs
1.4.3 Hepatoprotective Effects of Dietary Polyphenols
1.4.4 The Chemopreventive Role of Dietary Antioxidant Polyphenols
1.4.5 Protective Role of Dietary Antioxidant Polyphenols in Neurodegenerative Disorders
1.4.6 Dietary Phytochemicals in Gastrointestinal Disease and Microbial Infections
1.4.7 Interaction of Polyphenols With Gut Microbiota, Neurodegeneration and Cognition
1.4.8 Dietary Polyphenols in Arthritis and Inflammations
1.5 Future Perspectives and Conclusion
References
2 Biochemical, Molecular, Pharmacokinetic, and Toxicological Aspects of Dietary Polyphenols
2.1 Introduction
2.2 Chemistry and Biological Importance
2.2.1 Classification
2.2.2 Chemical Structure
2.2.2.1 Flavonoids
2.2.2.2 Non-Flavonoids
2.2.2.3 Polyphenol Amides
2.2.3 Medicinal Importance
2.3 Polyphenols and OS
2.3.1 Biochemistry of OS
2.3.2 Biochemical/molecular Markers as Targets for Polyphenols
2.3.3 Molecular Mechanisms of Polyphenols in OS
2.4 Anti-Inflammatory Activities
2.4.1 Regulation of NF-.B
2.4.2 Mitogen-Activated Protein Kinases (MAPKs) Regulation
2.4.3 Arachidonic Acid Regulation
2.5 Anti-Oxidant Activities
2.6 Anti-Tumor Activity
2.7 Antiaging Activities
2.8 Cardio-Protecting Effects
2.9 Neuro-Protective Effects
2.10 Pharmacokinetics Profile
2.10.1 Polyphenol Interaction With Saliva
2.10.2 Polyphenol Transit in Small Intestine
2.10.2.1 Protein Transporters Mediated Polyphenol Transit
2.10.3 Gut Microbiota-Mediated Polyphenol Transit
2.10.4 Conjugation and Nature of Metabolites
2.10.5 Plasma Transport and Lipid Structural Partitioning
2.10.6 Plasma Concentrations
2.10.7 Tissue Uptake
2.10.8 Elimination
2.11 Toxicity of the Polyphenol
2.11.1 Intestinal and Kidney Dysfunctions
2.11.2 Thyroid Dysfunction
2.11.3 Anti-Nutritional Effects
2.11.3.1 Low Iron Absorption
2.11.3.2 Low Protein Digestion Absorption
2.12 Drug Pharmacokinetics and Bioavailability
2.13 Conclusion and Future Prospective
References
3 Dietary Polyphenols in Aging, Neurological, and Cognitive Disorders
3.1 Introduction
3.1.1 Parkinson’s Disease (PD)
3.1.2 Alzheimer Disease (AD)
3.1.3 Depression
3.1.4 Schizophrenia
3.2 Bioavailability of Dietary Polyphenols
3.3 Polyphenols Beyond Blood–brain Barrier
3.4 Evidence-Based Utility of Dietary Polyphenolics in Clinical Trials
3.5 Conclusion and Future Perspective
References
4 Dietary Polyphenols in Cancer
4.1 Introduction
4.1.1 Oxidative Stress in Cancer
4.1.2 What Are Antioxidants?
4.2 Dietary Polyphenolics
4.2.1 Classification of Polyphenolics (Zhou Et Al., 2016)
4.2.1.1 Phenolic Acids
4.2.1.2 Flavonoids
4.2.1.3 Polyphenoleic Amides
4.2.1.4 Other Polyphenols
4.2.2 Potential Health Effects of Polyphenols
4.2.3 Antioxidant Activity of Polyphenols
4.2.3.1 Catechin
4.2.3.2 Lycopene
4.2.3.3 Curcumin
4.2.3.4 Resveratrol
4.2.3.5 Genistein
4.2.4 ADME Profile of Polyphenols
4.3 Polyphenols in Cancer
4.3.1 Modification of Redox Status
4.3.2 Interference With Cancer Cell Functions
4.3.2.1 Cell Cycle
4.3.2.2 Apoptosis
4.3.2.3 Invasion and Metastasis
4.3.2.4 Angiogenesis
4.4 Use of Polyphenols in Various Types of Cancer
4.4.1 Prostate Cancer
4.4.2 Colon Cancer
4.4.3 Breast Cancer
4.4.4 Lung Cancer
4.4.5 Bladder Cancer
4.4.6 Skin Cancer
4.4.7 Pancreatic Cancer
4.4.8 Leukemia
4.5 Polyphenolics in Cancer Targeted Drug Delivery Systems
4.5.1 Liposomes
4.5.2 Solid Lipid Nanoparticles
4.5.3 Nano Micelles
4.5.4 Dendrimers
4.5.5 Gold Nanoparticles
4.6 Clinical Evidence of Polyphenols
4.7 Conclusion
References
5 Dietary Polyphenols in Cardiovascular Diseases (CVDs)
5.1 Introduction
5.2 Effect of Polyphenol On Hypertension
5.2.1 Effect of Phytoestrogens On Hypertension
5.3 Polyphenols as Inhibitors of Low-Density Lipoproteins (LDL)
5.3.1 Polyphenols From Fruits and Vegetables
5.3.2 Effect of Polyphenols On Vasodilation
5.4 Conclusion
References
6 Dietary Polyphenols in Arthritis and Inflammatory Disorders
6.1 Introduction
6.2 Dietary Polyphenols Used in Treatment of Arthritis
6.2.1 Quercetin
6.2.1.1 Source
6.2.1.2 Chemistry
6.2.1.3 Pharmacology
6.2.1.4 Pharmacokinetics and Toxicity
6.2.2 Gallic Acid
6.2.2.1 Source
6.2.2.2 Chemistry
6.2.2.3 Pharmacology
6.2.2.4 Pharmacokinetics and Toxicity
6.2.3 Kaempferol
6.2.3.1 Source
6.2.3.2 Chemistry
6.2.3.3 Pharmacology
6.2.3.4 Pharmacokinetics and Toxicity
6.2.4 Naringenin
6.2.4.1 Source
6.2.4.2 Pharmacology
6.2.4.3 Pharmacokinetics and Toxicity
6.2.5 Ferulic Acid
6.2.5.1 Source
6.2.5.2 Pharmacology
6.2.5.3 Pharmacokinetics and Toxicity
6.2.6 Epigallocatechin-3-Gallate
6.2.6.1 Source
6.2.6.2 Pharmacology
6.2.6.3 Pharmacokinetics and Toxicity
6.2.7 Luteolin
6.2.7.1 Source
6.2.7.2 Pharmacology
6.2.7.3 Pharmacokinetics and Toxicity
6.2.8 Cumaric Acid
6.2.8.1 Source
6.2.8.2 Chemistry
6.2.8.3 Pharmacology
6.2.8.4 Pharmacokinetics and Toxicity
6.2.9 Chlorogenic Acid
6.2.9.1 Source
6.2.9.2 Chemistry
6.2.9.3 Pharmacology
6.2.9.4 Pharmacokinetics and Toxicity
6.2.10 Butein
6.2.10.1 Source
6.2.10.2 Pharmacology
6.2.11 Shogaol
6.2.11.1 Source
6.2.11.2 Pharmacology
6.2.11.3 Pharmacokinetics and Toxicity
6.2.12 Myricetin
6.2.12.1 Source
6.2.12.2 Pharmacology
6.2.13 6-Gingerol
6.2.13.1 Source
6.2.13.2 Pharmacology
6.2.13.3 Pharmacokinetics and Toxicity
6.2.14 Puerarin
6.2.14.1 Source
6.2.14.2 Pharmacology
6.3 Dietary Polyphenols Under Clinical Trials for the Treatment of Arthritis and Inflammatory Diseases
6.4 Conclusion and Future Perspective
References
7 Dietary Polyphenols in Diabetes
7.1 Introduction
7.2 Dietary Polyphenols
7.2.1 Structure, Classification, and Sources
7.2.2 Flavonoids
7.2.2.1 Flavonols
7.2.2.2 Flavanols
7.2.2.3 Isoflavone
7.2.2.4 Flavone
7.2.2.5 Flavanone
7.2.2.6 Anthocyanins and Anthocyanidins
7.2.3 Nonflavonoids
7.2.3.1 Phenolic Acids
7.2.3.2 Stilbenes
7.2.3.3 Lignans
7.3 The Biological and Biochemical Function of Polyphenols
7.3.1 Anti-Hypertensive Effect
7.3.2 Pro-Oxidant Activity
7.3.3 Anti-Atherosclerotic Effect
7.3.4 Anti-Metabolic Effect
7.3.5 Anti-Obesity Effect
7.3.6 Microbial Suppression Effect
7.3.7 Immunomodulatory Effect
7.3.8 Anti-Oxidant Activity
7.3.9 Anti-Cancer Effect
7.3.10 Hypoglycemic Effect
7.4 Antidiabetic Polyphenols
7.4.1 Curcumin
7.4.2 Resveratrol
7.4.3 Catechins
7.4.4 Procyanidin
7.4.5 Anthocyanidins
7.4.6 Caffeoylquinic Acids
7.4.7 Isoflavones
7.5 Antidiabetic Polyphenols in Clinical Trials and Marketed Products
7.6 Conclusion
References
8 Dietary Polyphenols in Bacterial and Fungal Infections
8.1 Introduction
8.2 Polyphenols in the Prevention of Bacterial and Fungal Infections
8.2.1 Absorption of Dietary Polyphenols
8.2.1.1 Flavonoids
8.2.1.2 Lignans
8.2.1.3 Tannins
8.2.1.4 Phenolic Acids
8.2.2 Antimicrobial Effects of Dietary Polyphenols
8.2.3 Mechanism of Action of Polyphenols On Bacteria and Fungus
8.2.3.1 Anti-Bacterial Mechanisms of Polyphenols
8.2.3.2 Antifungal Mechanisms of Polyphenols
8.2.4 Synergism
8.3 Polyphenols in Immunology
8.3.1 Role of Polyphenols in Innate and Adaptive Immunity
8.3.1.1 Effect of Polyphenols On Innate Immune System
8.3.1.2 Effect of Polyphenols On Adaptive Immune System
8.3.2 Immunobiotics and Their Interactions With Polyphenols
8.3.3 Polyphenols as Immune Boosters in Viral Infections
8.4 Implications of Food Safety Systems and Policy
8.4.1 Food Processing
8.4.2 Marketing and Regulation
8.4.3 Fortification and Supplementation
8.5 Conclusion and Future Prospective
References
9 Dietary Polyphenols in Viral Infections
9.1 Introduction
9.2 Structure and Classes of Polyphenols
9.2.1 Phenolic Acids
9.2.2 Flavonoids
9.2.3 Tannins
9.2.4 Stilbenes
9.2.5 Lignans
9.3 Significant Dietary Sources of Polyphenolic Compounds
9.4 Bioavailability and Pharmacokinetics of Polyphenols
9.5 Biological Activity of Polyphenolic Compounds
9.5.1 Antimicrobialactivity
9.5.2 Anti-SARS-CoV-2
9.5.3 Anti-HIV Activity
9.5.3.1 Anti HSV Activity
9.5.3.2 Activity Against Influenza Virus
9.5.3.3 Other Antiviral Activity of Polyphenolic Compounds
9.6 Conclusion and Future Perspectives
Acknowledgement
References
10 Dietary Polyphenols in Parasitic Diseases and Neglected Tropical Diseases (NTDs)
10.1 Introduction
10.2 Dietary Polyphenols Against Parasitic Diseases
10.2.1 Malaria
10.2.2 Dengue
10.2.3 Chikungunya
10.2.4 Leishmaniasis
10.2.5 Zika Virus
10.3 Dietary Polyphenols Against NTDs
10.3.1 Chagas Disease
10.3.2 Fascioliasis
10.3.3 Human African Trypanosomiasis
10.3.4 Leprosy
10.3.5 Lymphatic Filariasis
10.3.6 Trachoma
10.3.7 Schistosomiasis
10.4 Current Challenges and Future Scopes
10.5 Conclusions
References
11 Dietary Polyphenols for the Management of Skin Diseases and Wound Healing
11.1 Introduction
11.2 Classification and Sources of Dietary Polyphenols
11.2.1 Phenolic Acids
11.2.2 Flavonoids
11.2.3 Tannins
11.2.4 Stilbenes
11.3 Dietary Polyphenols in Skin Diseases and Wound Infections
11.3.1 Anti-Aging
11.3.2 Topical Allergies
11.3.3 Skin Cancer
11.3.4 Wound Healing
11.4 Nanocarrier-Based Delivery of Dietary Polyphenols in the Management of Skin Diseases/wound Healing
11.4.1 Lipid-Based Nanocarriers
11.4.2 Polymeric Nanoparticles
11.4.3 Nanogel
11.4.4 Hydrogel
11.4.5 Miscellaneous NPs
11.5 Conclusion
Conflicts of Interest
References
12 Dietary Polyphenols From Spices and Their Impact On Human Health
12.1 Introduction
12.2 Spices
12.2.1 Classification and Types
12.2.2 Spices in Functional Foods/culinary Preparation
12.3 Polyphenols: An Important Secondary Metabolite
12.3.2 Structure and Derivatives of Polyphenols
12.3.3 Pathways and Distribution of Polyphenols in the Spices
12.3.4 Leading Polyphenols From Spices: Analysis and Drug Discovery
12.4 Potential Mechanisms
12.4.1 Absorption and Interaction Inside the Body
12.4.2 Significant Signaling Pathways
12.5 Polyphenols and the Potential Health Effects
12.5.1 Health Assistances: Therapeutic and Pharmacological Properties
12.5.1.1 Antioxidant Activity and Their Impression On Human Health
12.5.1.2 Anti-Inflammatory Activity
12.5.1.3 Anticancer Effect
12.5.1.4 Cardio-Protective Effects
12.5.1.5 Effects Against Cognitive and Neurodegenerative Disease
12.5.1.6 Anti-Diabetic Property
12.5.2 As Dietary Supplements: Overlook for Health Benefits
12.5.3 Futuristic Approaches: Opportunities for Food and Pharmaceuticals
12.6 Conclusion and Future Prospective
Acknowledgments
Author Disclosure Statement
References
13 Dietary Polyphenols in Drug Discovery By Drug Repurposing and Computational Screening
13.1 Introduction
13.2 Structural Classification and Chemistry of Polyphenols
13.2.1 Flavonoids
13.2.2 Tannins
13.2.3 Phenolic Acids
13.2.4 Lignans
13.2.5 Stilbenes
13.3 Computational-Based Approaches for Repurposing Dietary Polyphenol
13.3.1 Virtual Screening
13.3.2 Pharmacophore Modeling
13.3.3 Molecular Docking
13.3.4 QSAR Approaches
13.3.4.1 Case Study 1
13.3.4.2 Case Study 2
13.4 Dietary Polyphenols as Leads in Drug Design and Discovery
13.4.1 Curcumin
13.4.2 Resveratrol
13.4.3 Catechins
13.4.4 Rutin
13.4.5 Quercetin
13.4.6 Kaempferol
13.5 Conclusion and Future Perspectives
References
Index
