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Book Synthesis  in Vitro Characterization and Applications of Novel 8 aminoquinoline Fluorescent Probes

Download or read book Synthesis in Vitro Characterization and Applications of Novel 8 aminoquinoline Fluorescent Probes written by Adonis C. McQueen and published by . This book was released on 2017 with total page 103 pages. Available in PDF, EPUB and Kindle. Book excerpt: ABSTRACT: Malaria is a parasitic disease that is caused by the plasmodium parasite. Plasmodium infection has affected man for thousands of years. With advances in drug discovery over the past century, malaria has evolved to possess resistance to most mainline therapeutics. This war of drug discovery vs plasmodium evolution continues to be fought to this very day, with attempts to eradicate malaria worldwide. Frontline treatments such as chloroquine, artemisinin, and atovaquone/proguanil have all seen parasitic resistance in strains of P. vivax as well as P. falciparum. While plasmodium possesses resistance to most classes of anti-malarials, the 8-aminoquinoline (8-AQ) class has seen minimal resistance development. 8-AQs have been shown to be effective against erythrocytic and exo-erythrocytic forms of plasmodium, and are often given in combination with a blood schizonticide such as chloroquine or artemisinin. These combinations clear all forms of plasmodium infection. With 8-AQs unique set of anti-malarial properties and the advent of increased drug resistance to other drugs, much research is being done to understand 8-AQs mechanism of action and toxicity. 8-AQ use is limited due to inducing extreme hemolytic anemia in those with glucose-6-phosphate dehydrogenase (G6PD) deficiency. Primaquine is the only 8-AQ molecule available on the market with tafenoquine, an analog primaquine, currently in phase III clinical trials. It is believed that if the mechanism of action and toxicity of the 8-AQs are understood, then we can create new generation anti-malarials that will maintain the unique action of 8-AQs while reducing their toxicity. Studies have shown that 8-AQ mechanism of action has been attributed to the generation of unstable metabolites that induce ROS production in the parasite, as well as mitochondrial swelling. While there is some evidence suggesting molecular targets of 8-AQs, the actual target is still unknown. When 8-AQs is given in combination with chloroquine, a synergistic effect is observed. While chloroquine has no activity against liver stages, it still somehow potentiates primaquines activity in those stages. This mechanism of synergy in liver stages is not well understood, and its understanding can give us increased understanding of basic plasmodium biology in the liver. Additionally, more information about the mechanisms of action vii of both chloroquine and primaquine could be elucidated. Tagging drugs with fluorescent probes is a technique that can give much information about the drugs pharmacological activity in vitro, and sometimes in vivo as well. Such an approach has been used for various disease states such as HIV and cancer. Malaria is no exception; fluorescent probes of artemisinin and chloroquine have been used to examine resistance mechanisms to both molecules. In addition to 8-AQs, there are other older antimalarials that have received attention recently due to increases in resistance. Menoctone, a hydroxynapthoquinone that subsequently lead to the discovery of atovaquone, has recently gained increased attention because of its similarities to atovaquone. Research surrounding menoctone was abandoned due to the discovery of more efficacious compounds. Similar to 8-AQs, understanding the mechanisms of action and resistance to menoctone could give us much more information about plasmodium responses to this class of compounds. This understanding could potentially lead to the discovery of novel therapeutics. To understand mechanisms of action and synergy of 8-AQs, we report the creation of novel fluorescent probes of the 8-AQ molecules primaquine and tafenoquine. The organic synthesis was designed and characterization was confirmed by NMR and high resolution mass spectra, and the fluorescent properties were examined using absorbance and steady-state emission experiments. We found that the anti-malarial, anti-leishmaniasis, and cytotoxic properties of these novel probes were similar to the parent compounds. These probes localized in the cytoplasm of infected parasites in vitro. We also attempted to view their localization in liver stage infection, and investigated the synergistic combination of 8-AQs with chloroquine and quinine. Menoctone resistance was induced in vivo to determine mechanisms of resistance. Cross resistance to atovaquone was observed, and the mutation responsible for resistance was also found.

Book Synthesis and Characterization of Novel Fluorescent Sensors Based on Terpyridine  Benzoxazole and Benzothiazole Chromophores

Download or read book Synthesis and Characterization of Novel Fluorescent Sensors Based on Terpyridine Benzoxazole and Benzothiazole Chromophores written by Xiaoman Bi and published by . This book was released on 2017 with total page 173 pages. Available in PDF, EPUB and Kindle. Book excerpt: Over the past few decades, there has been significant interest in developing fluorescent probes, because they are useful tools for biological studies. As effective analytical techniques, fluorescent probes utilize distinct advantages offered by fluorescence detection in terms of sensitivity, selectivity, and fast response time. When fluorescent probes interact selectively with target molecules, ions or biological specimens, they can generate large optical responses. Since most ions or molecules, such as Zn2+, Ca2+, or pyrophosphate ion (PPi), are non-fluorescent, chemosensors having analyte binding-triggered fluorescence are appealing in many fields, like analytical chemistry, clinical biochemistry, medicine, and environmental science.This dissertation is devoted to the design, synthesis, and characterization of novel fluorescent sensors for Zn2+ and its associated applications. Chapter II of this dissertation presents several novel terpyridine-based fluorescent sensors with different substituents affecting the electronic and steric nature of the terpyridine (tpy) fluorophore. Sensors are designed to establish the correlation between sensor structure and its photophysical properties. Low temperature fluorescence is used to evaluate the essential role of intramolecular charge transfer (ICT) in zinc binding-induced fluorescence changes. The tpy molecular fragment has a relatively large [pi]-conjugated system which enables the potential [pi-pi] interaction between two tpy platforms and affects the fluorescence of tpy ligands. Chapter III introduces a dimeric tpy ligand containing two tpy fragments connected via a meta-phenylene unit. The detailed spectroscopic study shows that this ligand displays an attractive fluorescence turn-on, in sharp contrast to mono(tpy) ligand that shows fluorescence quenching upon binding Zn2+. The result suggests the existence of delicate structural influences on fluorescence of tpy derivatives.Chapter IV is devoted to 2-(2'-hydroxyphenyl)-1,3-benzoxazole (HBO) and 2-(2'-hydroxyphenyl)-1,3-benzothiazole (HBT) derivatives featured with a structural potential of excited-state intramolecular proton transfer (ESIPT). The study reveals additional information on the binding of HBO or HBT to metal cations, which aids the sensor design for Zn2+ and PPi detection. The molecular design aims to realize ESIPT process control upon complexation with an analyte. Chapter V is devoted to the synthesis of bis(HBO) derivatives which bind Zn2+ selectively and emit near-infrared (NIR) fluorescence as a consequence of metal ion binding-induced ESIPT turn-on. Preliminary cell stain experiment was conducted and indicated the potential biological applications.

Book Synthesis and Characterization of Fluorescent Peptide dendron Hybrids

Download or read book Synthesis and Characterization of Fluorescent Peptide dendron Hybrids written by Deirdre Reneé Zwilling and published by . This book was released on 2009 with total page 70 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Book Synthesis and Characterization of Fluorescent Molecular Rotors

Download or read book Synthesis and Characterization of Fluorescent Molecular Rotors written by Jamie Yen-Ka Lam and published by . This book was released on 2020 with total page 155 pages. Available in PDF, EPUB and Kindle. Book excerpt: Small molecule fluorescent probes provide a non-invasive way to obtain accurate microviscosity measurements for biological analyses, especially when bulk measurements are not feasible. A family of push-pull fluorescent dyes, inspired by the benzothiazole motif of Thioflavin T, are reported, along with preliminary data on their use for visualizing long-range bacterial signaling and binding affinities for amyloids. By altering the [pi]-wire through increased conjugation and heteroatom substitution, a red-shifted ThT analogue was successfully synthesized. Synthetic analogues of previously reported fluorescent probes were also synthesized. Increasing the [pi]-wire from phenyl to naphthyl induced a bathochromic shift. It was also observed that switching from an ester to an amide altered photophysical properties in both sets of analogues. There was a slight hypsochromic shift due to the amide, likely attributed to the slight decrease in electron-withdrawing character of the acceptor group. Moreover, the emission intensity of the FRET donor decreased in the amide ratiometric system as compared to that of its ester counterpart, potentially indicating an enhancement of energy transfer between the donor and acceptor pair. These studies point towards ways to optimize the chemical structures of various fluorescent probes for specific applications.

Book Index Medicus

Download or read book Index Medicus written by and published by . This book was released on 2004 with total page 2160 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vols. for 1963- include as pt. 2 of the Jan. issue: Medical subject headings.

Book Cumulated Index Medicus

Download or read book Cumulated Index Medicus written by and published by . This book was released on 2000 with total page 1836 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Book Microbiology Abstracts

Download or read book Microbiology Abstracts written by and published by . This book was released on 1990 with total page 882 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Book The Chemistry and Application of Dyes

Download or read book The Chemistry and Application of Dyes written by David R. Waring and published by Springer Science & Business Media. This book was released on 2013-11-11 with total page 423 pages. Available in PDF, EPUB and Kindle. Book excerpt: It is particularly appropriate that a volume concerned with dye chemistry should be included in the series Topics in Applied Chemistry. The development of the dye industry has been inexorably linked not only with the development of the chemical industry but also with organic chemistry itself since the middle of the last century. The position of dye chemistry at the forefront of chemical 1945 and more markedly so during the last advance has declined somewhat since 15 years, with pharmaceutical and medicinal chemistry assuming an increasingly prominent position. Nevertheless, dye production still accounts for a significant portion of the business of most major chemical companies. The field of dye chemistry has stimulated the publication of many books over the years but surprisingly few have concentrated on or even included the practical aspects of dye synthesis and application. Thus, the present volume is designed to fulfill that need and provide the reader with an account of advances in dye chemistry, concentrating on more recent work and giving, in a single volume, synthetic detail and methods of application of the most important classes, information which will be invaluable to both student and research chemist alike.

Book Direct Synthesis of Metal Complexes

Download or read book Direct Synthesis of Metal Complexes written by B.I. Kharisov and published by Elsevier. This book was released on 2018-04-19 with total page 470 pages. Available in PDF, EPUB and Kindle. Book excerpt: Direct Synthesis of Metal Complexes provides in-depth coverage of the direct synthesis of coordination and organometallic compounds. The work is primarily organized by methods, but also covers highly relevant complexes, such as metal-polymer coordination compounds. This updated reference discusses recent developments in cryosynthesis, electrosynthesis, and tribosynthesis (popular as it doesn’t require organic solvents), with special attention paid to ‘greener’ methodologies and approaches. Additionally, the book describes physical methods of zero-valent metal interaction with organic matter, including sputtering, ultrasonic treatment and synthesis in ionic liquids. The book presents completely new content as a follow-up to the 1999 Elsevier Science publication Direct Synthesis of Coordination and Organometallic Compounds that was edited by Dr. Garnovskii and Dr. Kharisov. Covers current methods and techniques of metal interactions with organic media leading to metal chelates, adducts, di- and polymetallic complexes, metal-containing macrocycles, supported coordination compounds (i.e., metal complexes on carbon nanotubes), and more Describes reactivities of distinct forms of elemental metals (powders, sheets, nanoparticles (including a host of less-common metal nanostructures) with organic phase (liquid, solid and gaseous) and water Includes experimental procedures, with examples of direct synthesis, at the end of each chapter

Book Fluorescent and Luminescent Probes for Biological Activity

Download or read book Fluorescent and Luminescent Probes for Biological Activity written by W. T. Mason and published by Elsevier. This book was released on 1999-04-16 with total page 697 pages. Available in PDF, EPUB and Kindle. Book excerpt: The use of fluorescent and luminescent probes to measure biological function has increased dramatically since publication of the First Edition due to their improved speed, safety, and power of analytical approach. This eagerly awaited Second Edition, also edited by Bill Mason, contains 19 new chapters and over two thirds new material, and is a must for all life scientists using optical probes. The contents include discussion of new optical methodologies for detection of proteins, DNA and other molecules, as well as probes for ions, receptors, cellular components, and gene expression. Emerging and advanced technologies for probe detection such as confocal laser scanning microscopy are also covered. This book will be essential for those embarking on work in the field or using new methods to enhance their research. TOPICS COVERED: * Single and multiphoton confocal microscopy * Applications of green fluorescent protein and chemiluminescent reporters to gene expression studies * Applications of new optical probes for imaging proteins in gels * Probes and detection technologies for imaging membrane potential in live cells * Use of optical probes to detect microorganisms * Raman and confocal raman microspectroscopy * Fluorescence lifetime imaging microscopy * Digital CCD cameras and their application in biological microscopy

Book Chemical Abstracts

Download or read book Chemical Abstracts written by and published by . This book was released on 2002 with total page 2800 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Book Metals in Cells

    Book Details:
  • Author : Valeria Culotta
  • Publisher : John Wiley & Sons
  • Release : 2016-03-16
  • ISBN : 1118636864
  • Pages : 608 pages

Download or read book Metals in Cells written by Valeria Culotta and published by John Wiley & Sons. This book was released on 2016-03-16 with total page 608 pages. Available in PDF, EPUB and Kindle. Book excerpt: Over the last three decades a lot of research on the role of metals in biochemistry and medicine has been done. As a result many structures of biomolecules with metals have been characterized and medicinal chemistry studied the effects of metal containing drugs. This new book (from the EIBC Book Series) covers recent advances made by top researchers in the field of metals in cells [the “metallome”] and include: regulated metal ion uptake and trafficking, sensing of metals within cells and across tissues, and identification of the vast cellular factors designed to orchestrate assembly of metal cofactor sites while minimizing toxic side reactions of metals. In addition, it features aspects of metals in disease, including the role of metals in neuro-degeneration, liver disease, and inflammation, as a way to highlight the detrimental effects of mishandling of metal trafficking and response to "foreign" metals. With the breadth of our recently acquired understanding of metals in cells, a book that features key aspects of cellular handling of inorganic elements is both timely and important. At this point in our understanding, it is worthwhile to step back and take an expansive view of how far our understanding has come, while also highlighting how much we still do not know. The content from this book will publish online, as part of EIBC in December 2013, find out more about the Encyclopedia of Inorganic and Bioinorganic Chemistry, the essential online resource for researchers and students working in all areas of inorganic and bioinorganic chemistry.

Book Plant derived Natural Products

Download or read book Plant derived Natural Products written by Anne E. Osbourn and published by Springer Science & Business Media. This book was released on 2009-07-07 with total page 588 pages. Available in PDF, EPUB and Kindle. Book excerpt: Plants produce a huge array of natural products (secondary metabolites). These compounds have important ecological functions, providing protection against attack by herbivores and microbes and serving as attractants for pollinators and seed-dispersing agents. They may also contribute to competition and invasiveness by suppressing the growth of neighboring plant species (a phenomenon known as allelopathy). Humans exploit natural products as sources of drugs, flavoring agents, fragrances and for a wide range of other applications. Rapid progress has been made in recent years in understanding natural product synthesis, regulation and function and the evolution of metabolic diversity. It is timely to bring this information together with contemporary advances in chemistry, plant biology, ecology, agronomy and human health to provide a comprehensive guide to plant-derived natural products. Plant-derived natural products: synthesis, function and application provides an informative and accessible overview of the different facets of the field, ranging from an introduction to the different classes of natural products through developments in natural product chemistry and biology to ecological interactions and the significance of plant-derived natural products for humans. In the final section of the book a series of chapters on new trends covers metabolic engineering, genome-wide approaches, the metabolic consequences of genetic modification, developments in traditional medicines and nutraceuticals, natural products as leads for drug discovery and novel non-food crops.

Book Handbook of Smart Materials in Analytical Chemistry

Download or read book Handbook of Smart Materials in Analytical Chemistry written by Miguel de la Guardia and published by John Wiley & Sons. This book was released on 2019-01-22 with total page 931 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive guide to smart materials and how they are used in sample preparation, analytical processes, and applications This comprehensive, two-volume handbook provides detailed information on the present state of new materials tailored for selective sample preparation and the legal frame and environmental side effects of the use of smart materials for sample preparation in analytical chemistry, as well as their use in the analytical processes and applications. It covers both methodological and applied analytical aspects, relating to the development and application of new materials for solid-phase extraction (SPE) and solid-phase microextraction (SPME), their use in the different steps and techniques of the analytical process, and their application in specific fields such as water, food, air, pharmaceuticals, clinical sciences and forensics. Every chapter in Handbook of Smart Materials in Analytical Chemistry is written by experts in the field to provide a comprehensive picture of the present state of this key area of analytical sciences and to summarize current applications and research literature in a critical way. Volume 1 covers New Materials for Sample Preparation and Analysis. Volume 2 handles Analytical Processes and Applications. Focuses on the development and applications of smart materials in analytical chemistry Covers both, methodological and applied analytical aspects, for the development of new materials and their use in the different steps and techniques of the analytical process and their application in specific fields Features applications in key areas including water, air, environment, pharma, food, forensic, and clinical Presents the available tools for the use of new materials suitable to aid recognition process to the sample preparation and analysis A key resource for analytical chemists, applied laboratories, and instrument companies Handbook of Smart Materials in Analytical Chemistry, 2V Set is an excellent reference book for specialists and advanced students in the areas of analytical chemistry, including both research and application environments.

Book Ternary Quantum Dots

Download or read book Ternary Quantum Dots written by Oluwatobi Samuel Oluwafemi and published by Woodhead Publishing. This book was released on 2021-07-02 with total page 282 pages. Available in PDF, EPUB and Kindle. Book excerpt: Ternary Quantum Dots: Synthesis, Properties, and Applications reviews the latest advances in ternary (I-III-VI) chalcopyrite quantum dots (QDs), along with their synthesis, properties and applications. Sections address the fundamental key concepts of ternary quantum dots, progress in synthesis strategies (i.e., organic and aqueous synthesis), and characterization methods (i.e., transmission electron microscopy, dynamic light scattering, etc.). Properties of ternary quantum dots are comprehensively reviewed, including optical, chemical and physical properties. The factors and mechanisms of the cytotoxicity of ternary quantum dot-based nanomaterials are also described. Since ternary chalcopyrite quantum dots are less toxic and more environmentally benign than conventional binary II-VI chalcogenide quantum dots, they are being investigated to replace conventional quantum dots in a range of applications. Thus, this book reviews QDs in various applications, such as solar cells, photocatalytic, sensors and bio-applications. Reviews fundamental concepts of ternary quantum dots and quantum dot-nanocomposites including the most relevant synthesis strategies, key properties, and characterization techniques Delves into the cytotoxicity of quantum dots looking at the factors and mechanisms that influence cytotoxicity including demonstration of cytotoxicity assays for in vitro and in vivo tests Touches on the many applications of ternary quantum dots including biomedical applications, applications in solar cells, sensing applications, and photocatalytic applications