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Submit a ProposalChemistry and Biological Activities of Ivermectin
 | Edited by Rashid Ali and Shahid-ul-Islam Series: Emerging Trends in Medicinal and Pharmaceutical Chemistry Copyright: 2023 | Status: Published ISBN: 9781394166541 | Hardcover | 281 pages | 44 illustrations Price: $195 USD  |
One Line Description
The book focuses on the biological activities of ivermectin as well as the significant global utility of IVM since it was first used about 35 years ago.
Audience
Researchers, scientists, and postgraduate students working in the fields of organic synthesis, medicinal chemistry, medical science, pharmacy, biotechnology and biomedical sciences.
Researchers, scientists, and postgraduate students working in the fields of organic synthesis, medicinal chemistry, medical science, pharmacy, biotechnology and biomedical sciences.
Description
Ivermectin (IVM) is a “wonder drug” containing a 16-membered macrocyclic lactone ring system in its structure and derived from the family of avermectins. It was isolated by the fermentation of the soil microorganism Streptomyces avermitilis by Satoshi Omura in 1960 and studied by William C. Campbell in 1981, which allowed for its treatment of onchocerciasis (River Blindness) in Africa. Both scientists subsequently received the 2015 Nobel Prize in Physiology or Medicine. It was approved by the FDA in 1997 for the treatment of Strongyloidiasis and crusted scabies in AIDS patients. After that, IVM has attracted the tremendous attention of the scientific community and has been used for diverse purposes, including as an inhibitor of the causative virus (SARS-CoV-2).
The chief purpose of this volume is to focus on the chemistry and biological activities of ivermectin. The chapters have been arranged in a systematic manner, starting from the historical background and synthesis of IVM to the pharmacological and environmental aspects, followed by diverse applications. Although the usage of ivermectin for the treatment of COVID-19 remains under investigation and controversial, one of the chapters is dedicated to its use. The anti-parasitic, anti-malarial, anti-cancer, and anti-inflammatory activities of IVM are discussed in detail. The anthelminthic and insecticidal roles of IVM are briefly described and there are several cases of IVM in dermatology.
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Ivermectin (IVM) is a “wonder drug” containing a 16-membered macrocyclic lactone ring system in its structure and derived from the family of avermectins. It was isolated by the fermentation of the soil microorganism Streptomyces avermitilis by Satoshi Omura in 1960 and studied by William C. Campbell in 1981, which allowed for its treatment of onchocerciasis (River Blindness) in Africa. Both scientists subsequently received the 2015 Nobel Prize in Physiology or Medicine. It was approved by the FDA in 1997 for the treatment of Strongyloidiasis and crusted scabies in AIDS patients. After that, IVM has attracted the tremendous attention of the scientific community and has been used for diverse purposes, including as an inhibitor of the causative virus (SARS-CoV-2).
The chief purpose of this volume is to focus on the chemistry and biological activities of ivermectin. The chapters have been arranged in a systematic manner, starting from the historical background and synthesis of IVM to the pharmacological and environmental aspects, followed by diverse applications. Although the usage of ivermectin for the treatment of COVID-19 remains under investigation and controversial, one of the chapters is dedicated to its use. The anti-parasitic, anti-malarial, anti-cancer, and anti-inflammatory activities of IVM are discussed in detail. The anthelminthic and insecticidal roles of IVM are briefly described and there are several cases of IVM in dermatology.
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Author / Editor Details
Rashid Ali, PhD, is an assistant professor in the Department of Chemistry, Jamia Millia Islamia, New Delhi, India after receiving his PhD from the Indian Institute of Technology Bombay in organic and supramolecular chemistry. He has more than 50 research articles in international journals as well as multiple book chapters.
Rashid Ali, PhD, is an assistant professor in the Department of Chemistry, Jamia Millia Islamia, New Delhi, India after receiving his PhD from the Indian Institute of Technology Bombay in organic and supramolecular chemistry. He has more than 50 research articles in international journals as well as multiple book chapters.
Shahid-ul-Islam, PhD, is a Research Scientist at the Department of Textile & Fiber Engineering, Indian Institute of Technology Delhi (IIT). His areas of interest are antimicrobial coatings, green chemistry, fibers & polymers, polymeric composites and nanocomoposites, and nano-biotechnology. He has published numerous peer-reviewed research articles in journals of high repute as well as contributions to several books published by the Wiley-Scrivener imprint.
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Table of Contents
Preface
1. Introduction to Ivermectin
Aeyaz Ahmad Bhat, Atif Khurshid Wani, Tahir ul Gani Mir and Nahid Akther
1.1 Introduction
1.2 Sources and Synthesis
1.3 Pharmacological Potential of Ivermectin
1.3.1 Ivermectin in the Treatment of Cancer
1.3.1.1 Ovarian Cancer
1.3.1.2 Renal Cell Cancer
1.3.2 Ivermectin Against Viruses
1.3.3 Ivermectin in the Treatment of Bacterial Infections
1.4 Ivermectin’s Beneficial Role in Cattle
1.5 Ivermectin in the Treatment of COVID-19
1.5.1 Mode of Action
1.6 Toxicity of Ivermectin
1.6.1 Acute Toxicity
1.6.2 Developmental and Reproduction Toxicity
1.6.3 General and Safety Pharmacology
1.7 Conclusion
References
2. Historical Background of and Synthetic Approaches to Ivermectin (IVM) and its Homologues
Shakeel Alvi, Mohd Kamil Hussain and Rashid Ali
2.1 Introduction
2.1.1 Historical Background of Ivermectin
2.2 Synthetic Approaches Towards the Construction of IVM and Analogues
2.3 Biosynthesis
2.4 Chemical Synthetic Pathway
2.5 Crystal Structure
2.6 Conclusion and Outlook
Acknowledgements
References
3. Ivermectin as a Repurposed Drug for COVID-19
Hari Madhav, Mohammad Rehan, Nasimul Hoda and Ehtesham Jameel
3.1 Introduction
3.2 Symptoms of COVID-19
3.3 Repurposing of the Drugs
3.4 Repurposed Drugs for COVID-19
3.5 Repurposing of Ivermectin for COVID-19
3.6 Proposed Possible Mechanism of Action
3.7 SARS COVID-19 Clinical Studies with Ivermectin
3.8 Conclusions
3.9 Acknowledgments
References
4. Ivermectin as an Anti-Parasitic Agent
Areeba Rahman, Abdulaziz S. Alouffi, Mohammad Husain and Abdur Rub
Abbreviations
4.1 Introduction
4.2 Use of Ivermectin Against Various Human Parasitic Infections
4.2.1 Strongyloidiasis
4.2.2 Onchocerciasis
4.2.3 Lymphatic Filariasis
4.2.4 Loiasis
4.2.5 Scabies
4.2.6 Pediculosis
4.2.7 Mansonellosis
4.2.8 Ascariasis
4.2.9 Gnathostomiases
4.2.10 Leishmaniasis
4.2.11 Malaria
4.3 Mode of Action Against Various Parasites
4.4 Conclusions
4.5 Acknowledgements
References
5. Emerging Paradigm of Ivermectin and its Hybrids in Elimination of Malaria
Iram Irfan, Diksha Shahi, Mukesh C. Joshi, Shailja Singh and Mohammad Abid
5.1 Introduction
5.2 Malaria
5.2.1 World Malaria Report 2021
5.2.2 Malaria in India: Statistics and Facts
5.2.3 Providing Malaria Treatment Despite All Odds
5.2.4 Meeting the Global Goal
5.2.5 Elimination of Malaria
5.2.6 Status of Anti-Malarial Drugs
5.3 Life Cycle of Malaria
5.4 Drug Against Hepatic Malarial Stage
5.5 About Ivermectin
5.5.1 Ivermectin Against Liver Cells of Malaria Parasite
5.6 Designing and Synthesis of Ivermectin Inhibitors
5.6.1 Hybrids of Ivermectin
5.7 Conclusions
5.8 Acknowledgments
References
6. Ivermectin: A Potential Repurposed Anti-Cancer Therapeutic
Mohd Kamil Hussain, Rashid Ali, Shakir Ahamad, Mohammad Faheem Khan and Mohammad Saquib
Abbreviations
6.1 Introduction
6.2 Mechanism of Anti-Carcinogenesis
6.3 Activation of Chloride Ion Channels
6.4 Anti-Mitotic Effect and Inhibition of Angiogenesis
6.5 Inhibition of Mitochondrial Respiration
6.6 Inhibitor of Cancer Stem Cells (CSCs)
6.7 Induction of Immunogenic Cell Death (ICD)
6.8 Epigenetic Modulator
6.9 Induction PAK1-Mediated Cytostatic Autophagy
6.10 Inhibition of P-glycoprotein (P-gp)
6.11 Inhibition of Yes-Associated Protein 1 (YAP1)
6.12 Inhibition of RNA Helicase
6.13 Caspase-Dependent Apoptosis
6.14 Activation of Transcription Factor E3 (TFE3)
6.15 Inhibition of Wnt-TCF Pathway Responses
6.16 Conclusions
References
7. Ivermectin as an Anti-Inflammatory Agent
Mudasir Nabi Peerzada and Saurabh Verma
7.1 Introduction
7.2 Ant-Inflammatory Action of Ivermectin
7.3 Conclusions
Acknowledgements
References
8. Ivermectin: An Anthelminthic and Insecticide
Manisha Arora Pandit and Tarkeshwar
8.1 Introduction
8.2 Ivermectin as an Anthelmintic
8.2.1 Mode of Action
8.2.2 Ivermectin and Public Health
8.2.3 Challenges of Ivermectin Use as an Anthelminthic
8.3 Insecticidal Activity of Ivermectin
8.3.1 Mode of Action
8.3.2 Overview of Ivermectin as an Insecticide
8.3.3 Methods of Application to Animals and Plants
8.3.4 Disease Vector Control
8.3.5 Ivermectin Against Agricultural, Stored Grain Insect Pests and Other Insects
8.3.6 Ivermectin Usage in Livestock
8.3.7 Environmental Impact of Ivermectin
Conclusions
References
9. Potential Applications of Ivermectin (IVM) in Dermatology
Vikrant Jayant and Rashid Ali
9.1 Introduction
9.2 Mechanism of Action, Toxicity, and Side Effects of IVM
9.3 Motivational Approach of IVM in the Treatment of Skin
9.3.1 Anti-Bacterial Agent
9.3.2 Anti-Fungal Agent
9.3.3 Anti-Viral Agent
9.3.4 Anti-Protozoal Agent
9.4 Role of IVM with Good Anti-Parasitic Properties Against the Infection of Skin
9.4.1 Arthropods
9.4.2 Nematodes
9.5 Importance of IVM as an Anti-Cancer or Anti-Tumor Agent in Curing the Skin
9.6 Social Value of IVM in the Medical Care of Red Scrotum Syndrome (RSS)
9.7 Utility of IVM as an Anti-Inflammatory Drug in the Treatment of Skin-Related Issues
9.7.1 Allergy
9.7.2 Psoriasis or Crusted Scabies
9.7.3 Asthma
9.8 Conclusions
Acknowledgements
References
10. Antiviral Uses of Ivermectin
Shabnam Kawoosa, Rabiah Bashir, Sheeba Nazir, Zubaid-ul-Khazir Rather, Gulam Nabi Yatoo and Nisar Ahmad Khan
10.1 Introduction
10.2 Mechanism of Action of Ivermectin
10.3 Anti-Viral Effects Against Various DNA and RNA Viruses
10.3.1 RNA Viruses
10.3.1.1 COVID-19
10.3.1.2 Zika Virus
10.3.1.3 Dengue Virus
10.3.1.4 Foot-and-Mouth Disease Virus
10.3.1.5 Hendra Virus
10.3.1.6 Newcastle Virus
10.3.1.7 Avian Influenza A Virus
10.3.1.8 Human Immunodeficiency Virus Type 1
10.3.2 DNA Viruses
10.3.2.1 Equine Herpesvirus Type 1 (EHV-1)
10.3.2.2 Pseudorabies Virus (PRV)
10.3.2.3 BK Polyomavirus (BKPyV)
10.3.2.4 Porcine Circovirus 2 (PCV2)
10.4 Conclusion
References
11. Toxicology, Safety, and Environmental Aspects of Ivermectin
Ayesha Akhtar, Nasreen A. Mazumdar and Afreen Inam
11.1 Introduction
11.2 Ivermectin’s Antiparasitic Activity
11.3 Pharmacology
11.4 Adverse Effects in Humans and Animals
11.5 Ivermectin and Ectoparasites
11.5.1 Scabies
11.5.2 Pediculosis
11.5.3 Strongyloidiasis
11.5.4 Onchocerciasis
11.5.5 Lymphatic Filariasis
11.5.6 Loasis
11.6 Environmental Impact and Biodegradation of Ivermectin
11.7 Conclusion
References
Index
Back to Top
Preface
1. Introduction to Ivermectin
Aeyaz Ahmad Bhat, Atif Khurshid Wani, Tahir ul Gani Mir and Nahid Akther
1.1 Introduction
1.2 Sources and Synthesis
1.3 Pharmacological Potential of Ivermectin
1.3.1 Ivermectin in the Treatment of Cancer
1.3.1.1 Ovarian Cancer
1.3.1.2 Renal Cell Cancer
1.3.2 Ivermectin Against Viruses
1.3.3 Ivermectin in the Treatment of Bacterial Infections
1.4 Ivermectin’s Beneficial Role in Cattle
1.5 Ivermectin in the Treatment of COVID-19
1.5.1 Mode of Action
1.6 Toxicity of Ivermectin
1.6.1 Acute Toxicity
1.6.2 Developmental and Reproduction Toxicity
1.6.3 General and Safety Pharmacology
1.7 Conclusion
References
2. Historical Background of and Synthetic Approaches to Ivermectin (IVM) and its Homologues
Shakeel Alvi, Mohd Kamil Hussain and Rashid Ali
2.1 Introduction
2.1.1 Historical Background of Ivermectin
2.2 Synthetic Approaches Towards the Construction of IVM and Analogues
2.3 Biosynthesis
2.4 Chemical Synthetic Pathway
2.5 Crystal Structure
2.6 Conclusion and Outlook
Acknowledgements
References
3. Ivermectin as a Repurposed Drug for COVID-19
Hari Madhav, Mohammad Rehan, Nasimul Hoda and Ehtesham Jameel
3.1 Introduction
3.2 Symptoms of COVID-19
3.3 Repurposing of the Drugs
3.4 Repurposed Drugs for COVID-19
3.5 Repurposing of Ivermectin for COVID-19
3.6 Proposed Possible Mechanism of Action
3.7 SARS COVID-19 Clinical Studies with Ivermectin
3.8 Conclusions
3.9 Acknowledgments
References
4. Ivermectin as an Anti-Parasitic Agent
Areeba Rahman, Abdulaziz S. Alouffi, Mohammad Husain and Abdur Rub
Abbreviations
4.1 Introduction
4.2 Use of Ivermectin Against Various Human Parasitic Infections
4.2.1 Strongyloidiasis
4.2.2 Onchocerciasis
4.2.3 Lymphatic Filariasis
4.2.4 Loiasis
4.2.5 Scabies
4.2.6 Pediculosis
4.2.7 Mansonellosis
4.2.8 Ascariasis
4.2.9 Gnathostomiases
4.2.10 Leishmaniasis
4.2.11 Malaria
4.3 Mode of Action Against Various Parasites
4.4 Conclusions
4.5 Acknowledgements
References
5. Emerging Paradigm of Ivermectin and its Hybrids in Elimination of Malaria
Iram Irfan, Diksha Shahi, Mukesh C. Joshi, Shailja Singh and Mohammad Abid
5.1 Introduction
5.2 Malaria
5.2.1 World Malaria Report 2021
5.2.2 Malaria in India: Statistics and Facts
5.2.3 Providing Malaria Treatment Despite All Odds
5.2.4 Meeting the Global Goal
5.2.5 Elimination of Malaria
5.2.6 Status of Anti-Malarial Drugs
5.3 Life Cycle of Malaria
5.4 Drug Against Hepatic Malarial Stage
5.5 About Ivermectin
5.5.1 Ivermectin Against Liver Cells of Malaria Parasite
5.6 Designing and Synthesis of Ivermectin Inhibitors
5.6.1 Hybrids of Ivermectin
5.7 Conclusions
5.8 Acknowledgments
References
6. Ivermectin: A Potential Repurposed Anti-Cancer Therapeutic
Mohd Kamil Hussain, Rashid Ali, Shakir Ahamad, Mohammad Faheem Khan and Mohammad Saquib
Abbreviations
6.1 Introduction
6.2 Mechanism of Anti-Carcinogenesis
6.3 Activation of Chloride Ion Channels
6.4 Anti-Mitotic Effect and Inhibition of Angiogenesis
6.5 Inhibition of Mitochondrial Respiration
6.6 Inhibitor of Cancer Stem Cells (CSCs)
6.7 Induction of Immunogenic Cell Death (ICD)
6.8 Epigenetic Modulator
6.9 Induction PAK1-Mediated Cytostatic Autophagy
6.10 Inhibition of P-glycoprotein (P-gp)
6.11 Inhibition of Yes-Associated Protein 1 (YAP1)
6.12 Inhibition of RNA Helicase
6.13 Caspase-Dependent Apoptosis
6.14 Activation of Transcription Factor E3 (TFE3)
6.15 Inhibition of Wnt-TCF Pathway Responses
6.16 Conclusions
References
7. Ivermectin as an Anti-Inflammatory Agent
Mudasir Nabi Peerzada and Saurabh Verma
7.1 Introduction
7.2 Ant-Inflammatory Action of Ivermectin
7.3 Conclusions
Acknowledgements
References
8. Ivermectin: An Anthelminthic and Insecticide
Manisha Arora Pandit and Tarkeshwar
8.1 Introduction
8.2 Ivermectin as an Anthelmintic
8.2.1 Mode of Action
8.2.2 Ivermectin and Public Health
8.2.3 Challenges of Ivermectin Use as an Anthelminthic
8.3 Insecticidal Activity of Ivermectin
8.3.1 Mode of Action
8.3.2 Overview of Ivermectin as an Insecticide
8.3.3 Methods of Application to Animals and Plants
8.3.4 Disease Vector Control
8.3.5 Ivermectin Against Agricultural, Stored Grain Insect Pests and Other Insects
8.3.6 Ivermectin Usage in Livestock
8.3.7 Environmental Impact of Ivermectin
Conclusions
References
9. Potential Applications of Ivermectin (IVM) in Dermatology
Vikrant Jayant and Rashid Ali
9.1 Introduction
9.2 Mechanism of Action, Toxicity, and Side Effects of IVM
9.3 Motivational Approach of IVM in the Treatment of Skin
9.3.1 Anti-Bacterial Agent
9.3.2 Anti-Fungal Agent
9.3.3 Anti-Viral Agent
9.3.4 Anti-Protozoal Agent
9.4 Role of IVM with Good Anti-Parasitic Properties Against the Infection of Skin
9.4.1 Arthropods
9.4.2 Nematodes
9.5 Importance of IVM as an Anti-Cancer or Anti-Tumor Agent in Curing the Skin
9.6 Social Value of IVM in the Medical Care of Red Scrotum Syndrome (RSS)
9.7 Utility of IVM as an Anti-Inflammatory Drug in the Treatment of Skin-Related Issues
9.7.1 Allergy
9.7.2 Psoriasis or Crusted Scabies
9.7.3 Asthma
9.8 Conclusions
Acknowledgements
References
10. Antiviral Uses of Ivermectin
Shabnam Kawoosa, Rabiah Bashir, Sheeba Nazir, Zubaid-ul-Khazir Rather, Gulam Nabi Yatoo and Nisar Ahmad Khan
10.1 Introduction
10.2 Mechanism of Action of Ivermectin
10.3 Anti-Viral Effects Against Various DNA and RNA Viruses
10.3.1 RNA Viruses
10.3.1.1 COVID-19
10.3.1.2 Zika Virus
10.3.1.3 Dengue Virus
10.3.1.4 Foot-and-Mouth Disease Virus
10.3.1.5 Hendra Virus
10.3.1.6 Newcastle Virus
10.3.1.7 Avian Influenza A Virus
10.3.1.8 Human Immunodeficiency Virus Type 1
10.3.2 DNA Viruses
10.3.2.1 Equine Herpesvirus Type 1 (EHV-1)
10.3.2.2 Pseudorabies Virus (PRV)
10.3.2.3 BK Polyomavirus (BKPyV)
10.3.2.4 Porcine Circovirus 2 (PCV2)
10.4 Conclusion
References
11. Toxicology, Safety, and Environmental Aspects of Ivermectin
Ayesha Akhtar, Nasreen A. Mazumdar and Afreen Inam
11.1 Introduction
11.2 Ivermectin’s Antiparasitic Activity
11.3 Pharmacology
11.4 Adverse Effects in Humans and Animals
11.5 Ivermectin and Ectoparasites
11.5.1 Scabies
11.5.2 Pediculosis
11.5.3 Strongyloidiasis
11.5.4 Onchocerciasis
11.5.5 Lymphatic Filariasis
11.5.6 Loasis
11.6 Environmental Impact and Biodegradation of Ivermectin
11.7 Conclusion
References
Index
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