In this book, the author provides expert analysis on naturally occurring iridoids, their chemistry and their distribution in plants and insects. Particular attention is given to the pharmacology of iridoids and their prospective applications in pharmaceutical and agricultural industries. Iridoids are found in a wide variety of plants and some insects, and they are structurally derived from monoterpenoid natural products. In the first two chapters of this book, the author describes the iridoids classification, occurrence and distribution in plants and insects. The following chapters cover different chromatographic and spectroscopic techniques that can be used to identify and quantify iridoids in herbal formulations, and also the biosynthesis of iridoids, in which the reader will discover a metabolomics and transcriptomics analysis to identify the genes involved in the biosynthesis. The final chapters provide insights on several pharmacological activities of iridoids, their physiological role in insects, pharmacokinetics in mammals, insects and microorganisms, and their applications in medicine and agriculture. This book will engage students and researchers interested in the chemistry of natural products, and it will also appeal to medicinal chemists and practitioners working in the design of new herbal drugs with bioactive pure iridoids.
This book provides a concise introduction to pericyclic and photochemical reactions for organic synthesis. In the first part about pericyclic reactions, the author explains electrocyclic reactions, cycloaddition reactions, sigmatropic rearrangements, and group transfer reactions. The second part on photochemistry is dedicated to photochemical reactions of a variety of compound classes, including alkenes, dienes, and polyenes, carbonyl compounds, and aromatic compounds. Additionally, photofragmentation reactions are described in a dedicated chapter. The last chapter gives an outlook on applications of photochemistry and natural photochemical phenomena. Both parts start with a comprehensive presentation of the general principles of the pericyclic and photochemical reactions. All chapters are rich in examples, which help illustrate the explained principles and establish ties to results and trends in recent research. Additionally, each chapter offers exercises for students, and solutions to the problems are provided in a separate appendix. This book nicely illustrates the utility of pericyclic and photochemical reactions and provides students and researchers with the tools to apply them routinely for an efficient synthesis of complex organic molecules. It will therefore appeal to advanced undergraduate students, graduate and postgraduate students, and even to practitioners and scientists in the field of organic synthesis. The rich examples and exercises will also make it a versatile tool for teachers and lecturers.
The Ca+2-dependent mammalian Proprotein Convertase Subtilisin Kexins (PCSKs) or Proprotein/ Prohormone Convertases (PCs) are a family of endoproteases that play critical roles not only in normal development and metabolism but also in various physiological and pathological conditions. These were initiated by the proteolytic processing of large inactive proproteins into their shorter bioactive mature forms by the PCSK enzymes. These events take place in a highly selective, orchestrated, and stepwise manner. Among the various proprotein substrates of PCSK enzymes, particularly important are the precursor growth factors that include proPDGF-A, B, proIGF-1, 2 and proVEGF-C because of their strong implications in neoplasia initiation, progression, and metastasis. As a result of these findings, PCSK enzymes, particularly furin or PCSK3, became a major target for possible interventions of cancer via the use of their selective inhibitors. Significant progress has been accomplished in the development of peptide and protein-based PCSK inhibitors. However, non-peptide PCSK9 inhibitors are more preferable because of their drug-like and other characteristics. So far, a few non-peptide inhibitors of PCSK enzymes of various types of chemical structures have been described in the literature. These include (i) Carbocyclic compounds of diterpene and streptamine class. (ii) Nitrogen (N)-based heterocyclic compounds of various types and chemical structures such as (a) pyrrolidine bis piperazines, (b) Cu/Zn chelating terpyridine derivatives; (iii) Oxygen (O)-based Heterocyclic compounds of varying types of chemical structures such as (a) Flavonoids, (b) Coumarins of simple and dimeric types, (c) Quinonoids, (d) Iridoids; (iv) Aromatic compounds such as (a) Aryl guanidino and amidino derivatives, (b) Naphthyl fluorescein derivative, and (c) Phenyl Arsonic acids; and (v) C2-symmetrical aromatic azo-compounds. When measured against a small peptidyl-MCA fluorogenic substrate, these inhibitors displayed IC50 values ranging from nM to μM. A number of these inhibitors exhibited significant anti-PCSK activity when tested in ex vivo or cell culture conditions. This article provides an overall review of all non-peptide PCSK inhibitors so far reported in the literature along with those we identified recently for the first time and not yet published. The potential implications of these molecules as biochemical, therapeutical, or clinical agents will also be discussed.
This book provides a concise introduction to pericyclic and photochemical reactions for organic synthesis. In the first part about pericyclic reactions, the author explains electrocyclic reactions, cycloaddition reactions, sigmatropic rearrangements, and group transfer reactions. The second part on photochemistry is dedicated to photochemical reactions of a variety of compound classes, including alkenes, dienes, and polyenes, carbonyl compounds, and aromatic compounds. Additionally, photofragmentation reactions are described in a dedicated chapter. The last chapter gives an outlook on applications of photochemistry and natural photochemical phenomena. Both parts start with a comprehensive presentation of the general principles of the pericyclic and photochemical reactions. All chapters are rich in examples, which help illustrate the explained principles and establish ties to results and trends in recent research. Additionally, each chapter offers exercises for students, and solutions to the problems are provided in a separate appendix. This book nicely illustrates the utility of pericyclic and photochemical reactions and provides students and researchers with the tools to apply them routinely for an efficient synthesis of complex organic molecules. It will therefore appeal to advanced undergraduate students, graduate and postgraduate students, and even to practitioners and scientists in the field of organic synthesis. The rich examples and exercises will also make it a versatile tool for teachers and lecturers.
In this book, the author provides expert analysis on naturally occurring iridoids, their chemistry and their distribution in plants and insects. Particular attention is given to the pharmacology of iridoids and their prospective applications in pharmaceutical and agricultural industries. Iridoids are found in a wide variety of plants and some insects, and they are structurally derived from monoterpenoid natural products. In the first two chapters of this book, the author describes the iridoids classification, occurrence and distribution in plants and insects. The following chapters cover different chromatographic and spectroscopic techniques that can be used to identify and quantify iridoids in herbal formulations, and also the biosynthesis of iridoids, in which the reader will discover a metabolomics and transcriptomics analysis to identify the genes involved in the biosynthesis. The final chapters provide insights on several pharmacological activities of iridoids, their physiological role in insects, pharmacokinetics in mammals, insects and microorganisms, and their applications in medicine and agriculture. This book will engage students and researchers interested in the chemistry of natural products, and it will also appeal to medicinal chemists and practitioners working in the design of new herbal drugs with bioactive pure iridoids.
The Ca+2-dependent mammalian Proprotein Convertase Subtilisin Kexins (PCSKs) or Proprotein/ Prohormone Convertases (PCs) are a family of endoproteases that play critical roles not only in normal development and metabolism but also in various physiological and pathological conditions. These were initiated by the proteolytic processing of large inactive proproteins into their shorter bioactive mature forms by the PCSK enzymes. These events take place in a highly selective, orchestrated, and stepwise manner. Among the various proprotein substrates of PCSK enzymes, particularly important are the precursor growth factors that include proPDGF-A, B, proIGF-1, 2 and proVEGF-C because of their strong implications in neoplasia initiation, progression, and metastasis. As a result of these findings, PCSK enzymes, particularly furin or PCSK3, became a major target for possible interventions of cancer via the use of their selective inhibitors. Significant progress has been accomplished in the development of peptide and protein-based PCSK inhibitors. However, non-peptide PCSK9 inhibitors are more preferable because of their drug-like and other characteristics. So far, a few non-peptide inhibitors of PCSK enzymes of various types of chemical structures have been described in the literature. These include (i) Carbocyclic compounds of diterpene and streptamine class. (ii) Nitrogen (N)-based heterocyclic compounds of various types and chemical structures such as (a) pyrrolidine bis piperazines, (b) Cu/Zn chelating terpyridine derivatives; (iii) Oxygen (O)-based Heterocyclic compounds of varying types of chemical structures such as (a) Flavonoids, (b) Coumarins of simple and dimeric types, (c) Quinonoids, (d) Iridoids; (iv) Aromatic compounds such as (a) Aryl guanidino and amidino derivatives, (b) Naphthyl fluorescein derivative, and (c) Phenyl Arsonic acids; and (v) C2-symmetrical aromatic azo-compounds. When measured against a small peptidyl-MCA fluorogenic substrate, these inhibitors displayed IC50 values ranging from nM to ?M. A number of these inhibitors exhibited significant anti-PCSK activity when tested in ex vivo or cell culture conditions. This article provides an overall review of all non-peptide PCSK inhibitors so far reported in the literature along with those we identified recently for the first time and not yet published. The potential implications of these molecules as biochemical, therapeutical, or clinical agents will also be discussed. Table of Contents: Introduction / Historical Perspectives / Class of PCSK Inhibitors / Comparative Analyses of Peptide and Non-peptide Inhibitors / Class of Non-peptide Inhibitors of PCSKs / Comparison of Activities of Non-peptide Inhibitors of PCSK Enzymes / Blockade of Proprotein Processing by Non-peptide PCSK Inhibitors in Cellular Models / Animal Study with Non-peptide PCSK Inhibitors / Future Perspectives of Non-peptide PCSK Inhibitors and Concluding Remarks / Acknowledgments / References
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