Synthesis of Water-soluble Porphyrin-dendron Conjugates for Targeted Photodynamic Therapy PDF Download
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Author: Francesca Bryden
Publisher:
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Category :
Languages : en
Pages :
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Author: Francesca Bryden
Publisher:
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Category :
Languages : en
Pages :
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Author: Katriann Arja
Publisher: Linköping University Electronic Press
ISBN: 9176852555
Category :
Languages : en
Pages : 105
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Organic compounds that interact both with certain biological targets and display specific photophysical properties can be utilized as molecular tools to visualize and possibly effect disease related processes taking place in living organisms. In this regard, porphyrins are a class of naturally occurring molecules that possess intriguingly interesting photophysical properties where they can act as luminescent probes by emitting detectable light, as well as photosensitizers in the light mediated therapy called photodynamic therapy. In this thesis, the porphyrin structure has been synthetically combined with other molecule classes to achieve compounds with desirable multimodal characteristics. Firstly, luminescent conjugated oligothiophenes (LCOs) that have extensively, and with great success, been utilized as fluorescent ligands for amyloid formations, have been conjugated to porphyrins to render oligothiophene porphyrin hybrids (OTPHs) comprising two optically active modalities. When applied as fluorescent amyloidophilic dyes for visualization of amyloid-? (A?), one of the pathological hallmarks in Alzheimer’s disease, an enhanced optical assignment of distinct aggregated forms of A? was afforded. Thus, properly functionalized OTPHs could give us more information about pathological processes underlying devastating disorders, such as Alzheimer’s disease. In addition, the OTPHs can be associated with synthetic peptides inducing peptide folding into certain three-dimensional helical structures giving rise to novel optically active materials. Secondly, this thesis also embraces porphyrins’ potential as photosensitizers in photodynamic therapy to kill cancer cells. Grounded on the prerequisites for an optimal photosensitizer, we designed porphyrin-based conjugates equipped with common carbohydrates for improved cancer cell selectivity and with a fluorinated glucose derivative, 2-fluoro 2-deoxy glucose, for advantageous metabolism in cancer cells. Furthermore, incorporation of a radioisotopic fluorine-18 atom into the glycoporphyrins could give the means for diagnostic use of the conjugates in positron emission tomography (PET). In order to tether together the above-mentioned molecular moieties in a controlled fashion, we developed a robust synthetic strategy for asymmetrical functionalization of porphyrin core. The method involves chlorosulfonation of this otherwise inert tetrapyrrolic structure, followed by alkynylation. Parallelly to amide coupling reactions, copper(I)-catalyzed alkyne azide cycloaddition is used for fast and high-yielding late-stage conjugations. Overall, this thesis demonstrates how combining different molecular moieties in synthetic organic chemistry yields novel molecules with combined and improved multimodal properties for biological and medicinal applications, guided by the design-by-function methodology.
Author: Ravindra K Pandey
Publisher: World Scientific
ISBN: 9814719668
Category : Science
Languages : en
Pages : 563
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The main objective of this book is to present the recent applications of photodynamic therapy (PDT) in treating cancer and other diseases. The limitations associated with current PDT agents, and the synthetic designs that have been used in various laboratories are also discussed. The utility of certain tumor-avid agent for cancer imaging (fluorescence, PET, MRI) is also summarized. The book also includes the use of delivery vehicles, including nanoparticles in improving the tumor-specificity of the desired agents. The book is basically focused on the translational approach of drug development. By providing certain specific examples, a clear concept of moving a 'product' from the bench to bed-side is also discussed.To have a clear concept of drug development the book is divided in three parts — Medicinal Chemistry, Mechanistic and Clinical studies. Each part includes the contributions from the leading scientists with extensive experience in the respective field. The handbook is assembled by renowned scientists Dr Dougherty, known as the father of PDT, Dr Kessel, well known for his contributions on mechanism of PDT and Dr Pandey for his inventions in developing improved agents for PDT and cancer-imaging.
Author: Joseph Earl Bradshaw
Publisher:
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Category :
Languages : en
Pages :
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Photodynamic therapy (PDT) agents are light-activated materials used for localized disease treatment. Porphyrins are classic representations of photosensitive agents. Identified by their large, planar molecular structure, porphyrins are centrally composed of four pyrrole rings. Through this project, the starting material, H2TPPC, a tetra-carboxylic acid porphyrin, was first synthesized and later modified through the addition of the amine, morpholin-2-ylmethanol. This multi-step synthesis resulted in the highly water-soluble porphyrin product H2TPP-MorphMeOH. Following this synthesis, the compound was purified using liquid chromatography, and then structurally identified and classified using infrared (IR), nuclear magnetic resonance (NMR), and UV-Vis spectroscopies. Lastly, to determine its utility as a potential PDT agent, the cytotoxicity of H2TPP-MorphMeOH was determined using an MTT assay on MDA-MB-231 triple negative breast cancer cells comparing exposure and absence of white light.
Author: Catherine Shirley
Publisher:
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Category :
Languages : en
Pages :
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Photodynamic cancer therapy (PDT) is a type of treatment involving the use of light in conjunction with a photosensitive agent- a chemical or series of chemicals designed for activation when exposed to light. This research project investigated the synthesis and identification of the novel photosensitive agent, H2TPP-Pro-OH. To create the water-soluble porphyrin, (S)-(+)-prolinol was added to the tetra-carboxyl porphyrin, H2TPPC, to form the final H2TPP-Pro-OH product. This compound was then purified using syringe filtration and column chromatography, and subsequently characterized using infrared (IR), nuclear magnetic resonance (NMR), and UV-vis spectroscopies. Finally, the utility of the material as a PDT agent was determined by examining the cytotoxicity of the H2TPP-Pro-OH product was determined using MTT assay on MDA-MB-231 triple negative breast cancer cells comparing dark and light exposure.
Author: Sarita Sitaula
Publisher:
ISBN:
Category : Photochemotherapy
Languages : en
Pages : 486
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Author: Diana Samaroo
Publisher:
ISBN:
Category : Photochemotherapy
Languages : en
Pages : 406
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Author: Mingqian Tan
Publisher: World Scientific
ISBN: 981463543X
Category : Science
Languages : en
Pages : 430
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Nanomaterials offer great potential for effective tumor diagnosis and therapy combing diagnostic agents and therapeutic drugs into one platform. In this book, the most recent progress of main nanomaterials and their applications in tumor targeting theranostics is presented. It summarizes the recent advances of current principal nanomaterials in tumor theranostics, including magnetic nanomaterials, quantum dots, mesoporous silica nanoparticles, gold nanomaterials, polymeric nanosystem, carbon nanomaterials, lipopolyplex nanoparticles, microbubbles, upconversion nanomaterials and dendrimers. It will enable readers to get a more realistic understanding of both the advantages and limitations of nanomaterials for potential tumor targeting theranosis. The publication of this book will accelerate the spread of ideas that are currently trickling through the scientific literature. Also a greater understanding of the potential and challenge of nanomaterials for tumor targeting theranostics is highly anticipated for practical clinical use.
Author: Asha Kumari
Publisher: Elsevier
ISBN: 0443153493
Category : Science
Languages : en
Pages : 243
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Book Description
Sweet Biochemistry: Remembering Structures, Cycles, and Pathways by Mnemonics, Second Edition makes biochemistry lively, interesting and memorable by connecting objects, images and stories to biochemistry concepts. Here, Dr. Asha Kumari has converted cycles and difficult pathways into very simple formula and short stories and images to help readers see things in complicated cycles and better visualize biochemistry. As biochemistry is evolving steadily, with new and impactful topics, this new edition has been fully updated to include mnemonics on timely topics in biochemistry such as DNA replication, RNA, transcription, translation, and CRISPR technology, as well as fundamentals of immunity. - Provides quick, indigenous formula, mnemonics, figures, poems and short stories to absorb key concepts in biochemistry - Presents original diagrams that are easy to recall - Features simplified tables for remembering distinguishing features - Updated to address evolving topics in basic and medical biochemistry, including DNA replication, RNA transcription and translation and immunity fundamentals
Author: A Villaverde
Publisher: Academic Press
ISBN: 0124160204
Category : Medical
Languages : en
Pages : 650
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Book Description
This volume explores some of the most exciting recent advances in basic research on nanoparticles in translational science and medicine and how this knowledge is leading to advances in the various fields. This series provides a forum for discussion of new discoveries, approaches, and ideas Contributions from leading scholars and industry experts Reference guide for researchers involved in molecular biology and related fields
