Download or read book Computational Investigations of Cytochrome P450 Aromatase Catalysis and Biological Evaluation of Isoflavone Aromatase Inhibitors written by John C. Hackett and published by . This book was released on 2004 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Abstract: Density functional theory calculations are used to unravel the mysterious third step of aromatase catalysis. The feasibility of mechanisms in which the reduced ferrous dioxygen intermediate mediates androgen aromatization are explored and determined to be unlikely. Mechanisms for the aromatization/deformylation sequence which are initiated by 1beta-hydrogen atom abstraction by P450 Compound I are considered. 1beta-Hydrogen atom abstraction from substrates in the presence of the 2,3-enol encounters strikingly low barriers, whereas barriers for this same process are higher in the keto tautomer. Transition states for 1beta-hydrogen atom abstraction from enolized substrates in the presence of the 19-gem-diol decayed directly to the experimentally observed products. If the C19 aldehyde remains unhydrated, aromatization occurs with concomitant decarbonylation, and therefore does not support dehydration of the C19 aldehyde prior to the final catalytic step. Ab initio molecular dynamics on the confirmed that the 1beta-hydrogen atom abstraction and deformylation or decarbonylation occur in a non-synchronous, coordinated manner. These calculations support a dehydrogenase behavior of aromatase in the final catalytic step, which can be summarized by 1beta-hydrogen atom abstraction followed by gem-diol deprotonation. Aromatase, a cytochrome P450 hemoprotein that is responsible for estrogen biosynthesis by conversion of androgens into estrogens, has been an attractive target in the treatment of hormone-dependent breast cancer. There are several classes of natural products that exert potent activities in aromatase inhibition, with the flavonoids being most prominent. Previous studies have exploited flavone and flavanone scaffolds for the development of new aromatase inhibitors. In this dissertation, we describe design, synthesis, and biological evaluation of a novel series of 2-(4-pyridylmethyl)thioisoflavones as the first example of synthetic isoflavone-based aromatase inhibitors. The biological evaluation of a series of 2-azole and 2-thioazole isoflavones as potential aromatase inhibitors are described. Differences in inhibitory activity of triazole and imidazole inhibitors are rationalized with density functional theory to expose a key difference in the electronic structure of these molecules. In addition, difference binding spectra of inhibitors to immunoaffinity-purified aromatase produces classical Type II spectra consistent with coordination of the nitrogen lone pair electrons to the P450 heme.
Download or read book Directory of Graduate Research written by American Chemical Society. Committee on Professional Training and published by . This book was released on 2005 with total page 1932 pages. Available in PDF, EPUB and Kindle. Book excerpt: Faculties, publications and doctoral theses in departments or divisions of chemistry, chemical engineering, biochemistry and pharmaceutical and/or medicinal chemistry at universities in the United States and Canada.
Download or read book Autophagy in tumor and tumor microenvironment written by Sujit Kumar Bhutia and published by Springer Nature. This book was released on 2020-10-24 with total page 284 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book deals with the paradoxical role of autophagy in tumor suppression and tumor promotion in cancer cells. Autophagy plays opposing, context-dependent roles in tumors; accordingly, strategies based on inhibiting or stimulating autophagy could offer as potential cancer therapies. The book elucidates the physiological role of autophagy in modulating cancer metastasis, which is the primary cause of cancer-associated mortality. Further, it reviews its role in the differentiation, development, and activation of multiple immune cells, and its potential applications in tumor immunotherapy. In addition, it examines the effect of epigenetic modifications of autophagy-associated genes in regulating tumor growth and therapeutic response and summarizes autophagy’s role in the development of resistance to a variety of anti-cancer drugs in cancer cells. In closing, it assesses autophagy as a potential therapeutic target for cancer treatment. Given its scope, the book offers a valuable asset for all oncologists and researchers who wish to understand the potential role of autophagy in tumor biology.
Download or read book Botanical Dietary Supplements written by Gail B. Mahady and published by CRC Press. This book was released on 2001-06-01 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides reviews and details of the quality, safety and efficacy for some of the top-selling botanicals worldwide, including black cohosh, chamomile, comfrey, echinacea, garlic, ginkgo, ginseng, kava, milk thistle, St John's wort and valerian. The work was written based on a systematic review of the scientific literature from 1975-2000.;Each review includes a brief introduction, a section on quality including a definition of the crude drug, geographical distribution, and a listing of the major chemical constituents. The safety and efficacy sections summarize the medical uses, pharmacology, contraindications, warnings, precautions, adverse reactions, dose and dosage forms. The safety and efficacy sections were written for a busy health-care professional, and should enable one to ascertain which clinical uses are supported by clinical data, without having to read through all the pharmacology. Each chapter is fully referenced, enabling the reader to access further information when necessary.
Download or read book Recent Advances in Natural Products Analysis written by Seyed Mohammad Nabavi and published by Elsevier. This book was released on 2020-03-07 with total page 880 pages. Available in PDF, EPUB and Kindle. Book excerpt: Recent Advances in Natural Products Analysis is a thorough guide to the latest analytical methods used for identifying and studying bioactive phytochemicals and other natural products. Chemical compounds, such as flavonoids, alkaloids, carotenoids and saponins are examined, highlighting the many techniques for studying their properties. Each chapter is devoted to a compound category, beginning with the underlying chemical properties of the main components followed by techniques of extraction, purification and fractionation, and then techniques of identification and quantification. Biological activities, possible interactions, levels found in plants, the effects of processing, and current and potential industrial applications are also included. Focuses on the latest analytical techniques used for studying phytochemical and other biological compounds Authored and edited by the top worldwide experts in their field Discusses the current and potential applications and predicts future trends of each compound group
Download or read book Nanophytomedicine written by Sarwar Beg and published by Springer Nature. This book was released on 2020-07-27 with total page 220 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nanophytomedicine is a field that involves the application of nanomedicine-based systems to phytotherapy and phytopharmacology. This book assesses the clinical successes and failures of nanophytomedicine and also highlights emerging concepts in this field. The content is divided into three sections, the first of which describes core issues in the pharmaceuticals industry in connection with the successes, failures and prospects of nanophytomedicine. The second section highlights recent advances in phytomedicine formulation development based on nanotechnology approaches, while also discussing a variety of nanocarrier systems for the successful delivery of phytomedicines. Focusing on the clinical perspective, the third section addresses the current clinical status of nanophytomedicine as a single drug therapy or combinatorial drug therapy, pharmacovigilance, pharmacokinetics, drug interactions and toxicological profiles, while also providing concluding remarks on recent experimental findings, and considering ethical issues & regulatory challenges in nanophytomedicine. Given its scope, the book offers a valuable guide for early career researchers, young scientists, master level students, academics and industrial scientists working in various healthcare fields, e.g. the pharmaceutical and biological sciences, life sciences, biotechnology, biomedical engineering, and nanobiotechnology.
Download or read book Biotechnology and Production of Anti Cancer Compounds written by Sonia Malik and published by Springer. This book was released on 2017-04-21 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book discusses cancers and the resurgence of public interest in plant-based and herbal drugs. It also describes ways of obtaining anti-cancer drugs from plants and improving their production using biotechnological techniques. It presents methods such as cell culture, shoot and root culture, hairy root culture, purification of plant raw materials, genetic engineering, optimization of culture conditions as well as metabolic engineering with examples of successes like taxol, shikonin, ingenol mebutate and podophylotoxin. In addition, it describes the applications and limitations of large-scale production of anti-cancer compounds using biotechnological means. Lastly, it discusses future economical and eco-friendly strategies for obtaining anti-cancer compounds using biotechnology.
Download or read book Androgens and Androgen Receptor written by Chawnshang Chang and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 507 pages. Available in PDF, EPUB and Kindle. Book excerpt: Androgen Receptors is the most comprehensive and up to date volume on the topic, including discussions of the basic mechanisms of androgen-androgen receptor actions, their roles in the androgen-related diseases, and their potential clinical applications. Key topics covered include: -The discovery and cloning of the androgen receptor; -Androgen receptor coregulators; -Androgen related genes and their consensus DNA response elements; -Basic mechanism of action including functional analyses, cellular localization and phosphorylation studies; -Cross-talk to other signal transduction systems; -The recent connections of androgens to women's diseases, such as osteoporosis and ovarian cancer. This book is of interest to students, basic scientists, and clinicians as both a study guide and reference of research in the androgen field. It could also be used as an advanced level text in endocrinology, urology, OBGYN, or oncology.
Download or read book Gaseous Molecular Ions written by Eugen Illenberger and published by Springer Science & Business Media. This book was released on 1992-05-26 with total page 944 pages. Available in PDF, EPUB and Kindle. Book excerpt: Most of the matter in our solar system, and, probably, within the whole universe, exists in the form of ionized particles. On the other hand, in our natural environ ment, gaseous matter generally consists of neutral atoms and molecules. Only under certain conditions, such as within the path oflightning or in several technical devices (e. g. gas discharges, rocket engines, etc. ) will some of the atoms and molecules be ionized. It is also believed that the chemistry of the earth's troposphere predomi nantly proceeds via reactions between neutral particles. (The complex system of atmospheric chemistry will be treated in one of the forthcoming volumes to this series. ) Why, then, are ions considered so important that hundreds oflaboratories all over the world (including some of the most prestigious) are involved in research pro grams on ions, covering many different facets, from biochemistry to physics? One may obtain as many different answers as there are research groups busy in this field. There is, however, one simple, common feature which makes it attractive to work with ions: since they carry one or more net elementary charges, they can easily be gui ded, focused or separated by appropriate electric and magnetic fields, and, last but not least, they can easily be detected. Apart from these advantages, which are welcome and appreciated by the researcher, the study of molecular ions can provide insight into very fundamental aspects of the general behavior of molecules.
Download or read book Monooxygenase Peroxidase and Peroxygenase Properties and Mechanisms of Cytochrome P450 written by Eugene G. Hrycay and published by Springer. This book was released on 2015-05-22 with total page 376 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book describes in 13 chapters mechanisms of P450 used to monooxygenate substrates via the NAD(P)H/O2 pathway using its peroxidase and peroxygenase functions. P450 also utilizes peroxides, peracids, periodate and iodosobenzene to oxygenate substrates via the shunt pathway. Also described are mechanisms used in the oxidation of pharmaceuticals by CYP3A4; acyl- carbon cleavage by CYP17A1, CYP19A1 and CYP51A1; metabolism of tetrabromodiphenyl ethers and bile acids by CYP2B6 and CYP3A4; metabolism of ω-6 and ω-3 polyunsaturated fatty acids; H2O2-mediated peroxygenation of substrates using substrate misrecognition; P450 oxidative reactions using electrochemical methods; electron transfer to P450 by redox proteins; hydroxylation of 1,8-cineole by P450cin; and peroxygenation by unspecific peroxygenases using H2O2. The topics covered are relevant to P450 researchers, professors and students from a variety of disciplines ranging from pharmacology, toxicology and microbiology to chemistry.
Download or read book Herbal Medicine in India written by Saikat Sen and published by Springer Nature. This book was released on 2019-09-10 with total page 612 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book highlights the medical importance of and increasing global interest in herbal medicines, herbal health products, herbal pharmaceuticals, nutraceuticals, food supplements, herbal cosmetics, etc. It also addresses various issues that are hampering the advancement of Indian herbal medicine around the globe; these include quality concerns and quality control, pharmacovigilance, scientific investigation and validation, IPR and biopiracy, and the challenge that various indigenous systems of medicine are at risk of being lost. The book also explores the role of traditional medicine in providing new functional leads and modern approaches that can offer elegant strategies for facilitating the drug discovery process. The book also provides in-depth information on various traditional medicinal systems in India and discusses their medical importance. India has a very long history of safely using many herbal drugs. Folk medicine is also a key source of medical knowledge and plays a vital role in maintaining health in rural and remote areas. Despite its importance, this form of medicine largely remains under-investigated. Out of all the traditional medicinal systems used worldwide, Indian traditional medicine holds a unique position, as it has continued to deliver healthcare throughout the Asian subcontinent since ancient times. In addition, traditional medicine has been used to derive advanced techniques and investigate many modern drugs. Given the scope of its coverage, the book offers a valuable resource for scientists and researchers exploring traditional and herbal medicine, as well as graduate students in courses on traditional medicine, herbal medicine and pharmacy.
Download or read book Flavonoids written by Oyvind M. Andersen and published by CRC Press. This book was released on 2005-12-09 with total page 1256 pages. Available in PDF, EPUB and Kindle. Book excerpt: Advances in the flavonoid field have been nothing short of spectacular over the last 20 years. While the medical field has noticed flavonoids for their potential antioxidant, anticancer and cardioprotectant characteristics, growers and processors in plant sciences have utilized flavonoid biosynthesis and the genetic manipulation of the flavonoid pa
Download or read book Handbook of Dietary Phytochemicals written by Jianbo Xiao and published by Springer. This book was released on 2021-09-02 with total page 1953 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book summarizes recent advances in the chemistry, bioactivity, nutrition, and functional aspects of dietary phytochemicals, as well as the health and functional aspects of foods rich in phytochemicals. Consisting of forty-four chapters, it discusses the different chemical types of phytochemicals in our diets and food and presents data collected from animal or human experiments that are directly related to human health. Each chapter covers the chemistry, epidemiological study, bioavailability, bioactivity (animal experiments) function in humans and safety, as well as products on the market. Moreover, the more than 200 figures make it easy to grasp the main findings in each area.
Download or read book Trends in Breast Cancer Prevention written by Jose Russo and published by Springer. This book was released on 2016-07-14 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume, with contributions from the most recognized experts in preventive strategies in breast cancer, presents the accepted as well as the novel ideas that have been introduced for the prevention of breast cancer. There is no single preventive agent that can stop the incidence of breast cancer—the malignant disease most frequently diagnosed in women of all races and nationalities. Furthermore, its incidence around the globe is increasing in industrialized countries. The worldwide incidence of breast cancer has increased 30-40% since the 1970s, reaching an excess of 1,390,000 new cases and a mortality of more than 460,000 cases in 2015. Therefore, what is needed is the development of rational strategies for the prevention of this fatal disease.
Download or read book Encyclopedia of Molecular Pharmacology written by Stefan Offermanns and published by Springer Science & Business Media. This book was released on 2008-08-14 with total page 1515 pages. Available in PDF, EPUB and Kindle. Book excerpt: An essential text, this is a fully updated second edition of a classic, now in two volumes. It provides rapid access to information on molecular pharmacology for research scientists, clinicians and advanced students. With the A-Z format of over 2,000 entries, around 350 authors provide a complete reference to the area of molecular pharmacology. The book combines the knowledge of classic pharmacology with the more recent approach of the precise analysis of the molecular mechanisms by which drugs exert their effects. Short keyword entries define common acronyms, terms and phrases. In addition, detailed essays provide in-depth information on drugs, cellular processes, molecular targets, techniques, molecular mechanisms, and general principles.
Download or read book Carbon carbon Bond Formation written by Robert L. Augustine and published by CRC Press. This book was released on 1979-04-01 with total page 480 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Medicinal Natural Products written by Paul M. Dewick and published by John Wiley & Sons. This book was released on 2002-01-03 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: This guide covers classes of natural products in medicine, whether derived from plants, micro-organisms or animals. Structured according to biosynthetic pathway, it is written from a chemistry-based approach.
