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Chimica farmaceutica: farmaci sistemici: Lezioni del prof. Ettore Novellino

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Book Series: Phármakon ISBN: 9788868870157 Year: Volume: 1 Pages: 767 DOI: 10.6093/978-88-6887-015-7
Publisher: FedOA - Federico II University Press
Subject: Therapeutics
Added to DOAB on : 2018-06-08 13:11:19
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For thousands of years, pharmacological knowledge coming from natural remedies, has been handed down from generation to generation, without any awareness of the ways in which preparations are made to face diseases. The advent of pharmaceutical chemistry and of the modern drug industry turned that lack of awareness into a scientific knowledge that changed the destiny of the human race. The twenty-eight chapters of this book, are taken from the lectures held by Professor Ettore Novellino every year in his course “Pharmaceutical Chemistry and Toxicology 2”. The first chapters address the basic notions of drugs, homeostasis, pharmacopoeia, and receptor; then, the different pharmaceutical classes are introduced by analyzing their pharmacological and chemical aspects. In particular, the structural study of the interaction between drugs and receptors or biological enzymes gives the fundamentals to connect the chemical and stereochemical properties of a compound family, with the biological activity, a correlation better known as Quantitative Structure-Activity Relationship (QSAR). Several examples of the synthesis of some of the most historically renown drugs, provided at the end of each chapter, integrate the book.

The Molecular Aspect of Natural Secondary Metabolite Products in Health and Disease

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ISBN: 9783038971764 9783038971771 Year: Pages: 226 DOI: 10.3390/books978-3-03897-177-1 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Anthropology --- Social and Public Welfare --- Biology
Added to DOAB on : 2018-09-19 09:01:21
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ca. 200 words; this text will present the book in all promotional forms (e.g. flyers). Please describe the book in straightforward and consumer-friendly terms.[Natural secondary metabolite products, which are isolated from plants, animals, microorganisms, etc., are classified as polyketides, isoprenoids, steroids, aromatics, alkaloids, etc. Their chemical diversity and variety of biological activities have attracted the attention of chemists, biochemists, biologists, etc. This Special Issue on "The Molecular Aspect of Natural Secondary Metabolite Products in Health and Disease" is intended to offer biological active natural products as candidates and/or leads for pharmaceuticals, dietary supplements, functional foods, cosmetics, food additives, etc. The research fields of this Special Issue include natural products chemistry, phytochemistry, pharmacognosy, food chemistry, bioorganic synthetic chemistry, molecular pharmacology, molecular nutritional sciences, and other related research fields of bioactive natural secondary metabolite products. Original research and review articles on all topics in these research fields are invited. I look forward to receiving many submissions from outstanding expert on these research fields.

Biological Activity of Natural Secondary Metabolite Products

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ISBN: 9783038971740 9783038971757 Year: Pages: 466 DOI: 10.3390/books978-3-03897-175-7 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Anthropology --- Biology --- Social and Public Welfare
Added to DOAB on : 2018-09-20 12:02:36
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ca. 200 words; this text will present the book in all promotional forms (e.g. flyers). Please describe the book in straightforward and consumer-friendly terms.[Natural secondary metabolite products, which are isolated from plants, animals, microorganisms, etc., are classified as polyketides, isoprenoids, aromatics (phenylpropanoids), alkaloids, etc. Their chemical diversity and variety of biological activities have attracted the attention of chemists, biochemists, biologists, etc. The Special Issue on "Biological Activity of Natural Secondary Metabolite Products" is intended to offer biological active natural products as candidates and/or leads for pharmaceuticals, dietary supplements, functional foods, cosmetics, food additives, etc. The research fields of this Special Issue include natural products chemistry, phytochemistry, pharmacognosy, food chemistry, bioorganic synthetic chemistry, chemical biology, molecular biology, molecular pharmacology, and other related research fields of bioactive natural secondary metabolite products. Original research and review articles on all topics in these research fields are invited. I am looking forward to receiving many submissions from outstanding experts in these research fields.]

Biological Efficacy of Natural and Chemically Modified Products against Oral Inflammatory Lesions

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ISBN: 9783038979920 9783038979937 Year: Pages: 212 DOI: 10.3390/books978-3-03897-993-7 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Medicine (General) --- Therapeutics
Added to DOAB on : 2019-06-26 08:44:06
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Oral health is general health. If the oral cavity is kept healthy, the whole body is always healthy. Bacteria in the oral cavity do not stay in the oral cavity, but rather they travel throughout the body and can induce various diseases. Periodontal pathogens are involved in tooth loss. The number of remaining teeth decreases with age. People with more residual teeth can bite food well and live longer with lower incidence of dementia. There are many viruses in the oral cavity that also cause various diseases. Bacteria and viruses induce and aggravate inflammation, and therefore should be removed from the oral cavity. In the natural world, there are are many as yet undiscovered antiviral, antibacterial and anti-inflammatory substances. These natural substances, as well as chemically modified derivatives, help our oral health and lead us to more fulfilling, high quality lives. This Special Issue, entitled “Biological Efficacy of Natural and Chemically Modified Products against Oral Inflammatory Lesions”, was written by specialists from a diverse variety of fields. It serves to provide readers with up-to-date information on incidence rates in each age group, etiology and treatment of stomatitis, and to investigate the application of such treatments as oral care and cosmetic materials.

Keywords

metabolomics --- oral cell --- benzaldehyde --- eugenol --- inflammation --- cytotoxicity --- stomatitis --- recurrent aphthous stomatitis --- oral lichen planus --- CCN2 --- glucocorticoids --- alkaloids --- anti-human immunodeficiency virus (HIV) --- antiviral --- natural product --- human virus --- inflammatory disease --- stomatitis --- periodontitis --- anti-osteoclast activity --- cepharanthin --- herbal medicine --- natural product --- arachidonic acid cascade --- allergic rhinitis --- mice --- quercetin --- thioredoxin --- nasal epithelial cell --- production --- increase --- in vitro --- in vivo --- nutritionally variant streptococci --- antimicrobial susceptibilities --- oral microbiota --- infective endocarditis --- kampo formula --- traditional Japanese herbal medicine --- stomatitis --- mucositis --- Hangeshashinto --- polyphenol --- chromone --- lignin-carbohydrate complex --- alkaline extract --- Kampo medicine --- glucosyltransferase --- angiotensin II blocker --- QSAR analysis --- oral diseases --- dental application --- Chinese herbal remedies --- stomatitis --- periodontitis --- Kampo --- traditional medicine --- Jixueteng --- Juzentaihoto --- technical terms --- gargle --- tongue diagnosis --- mastic --- pathogenic factors --- quantitative structure-activity relationship --- machine learning --- random forest --- natural products --- tumour-specificity --- Kampo medicine --- constituent plant extract --- stomatitis --- oral inflammation --- quantitative structure-activity relationship (QSAR) analysis --- metabolomics

New Approaches for the Discovery of Pharmacologically-Active Natural Compounds

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ISBN: 9783039211043 9783039211050 Year: Pages: 158 DOI: 10.3390/books978-3-03921-105-0 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Medicine (General) --- Therapeutics
Added to DOAB on : 2019-08-28 11:21:27
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A major source of active compounds, natural products from different sources supply a large variety of molecules that have been approved for clinical use or used as the starting points of optimization programs. This book features nine papers (eight full articles and one review paper) written by more than 45 scientists from around the world. These papers illustrate the development and application of a broad range of computational and experimental techniques applied to natural product research. On behalf of the contributors to the book, our hope is that the research presented here contributes to advancements in the field, and encourages multidisciplinary teams, young scientists, and students to further advance in the discovery of pharmacologically-active natural compounds

G-quadruplex and Microorganisms

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ISBN: 9783039212439 9783039212446 Year: Pages: 208 DOI: 10.3390/books978-3-03921-244-6 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Medicine (General) --- Internal medicine
Added to DOAB on : 2019-12-09 11:49:15
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G-quadruplexes (G4s) are nucleic acids secondary structures that form in DNA or RNA guanine (G)-rich strands. In recent years, the presence of G4s in microorganisms has attracted increasing interest. In prokaryotes, G4 sequences have been reported in several human pathogens. Bacterial enzymes able to process G4s have been identified. In viruses, G4s have been suggested to be involved in key steps of the viral life cycle: They have been associated with the human immunodeficiency virus (HIV), herpes simplex virus 1 (HSV-1), human papilloma virus, swine pseudorabies virus, and other viruses’ genomes. New evidence shows the presence of G4s in parasitic protozoa, such as the causative agent of malaria. G4 binding proteins and mRNA G4s have been implicated in the regulation of microorganisms’ genome replication and translation. G4 ligands have been developed and tested both as tools to study the complexity of G4-mediated mechanisms in the viral life cycle and as therapeutic agents. Moreover, new techniques to study G4 folding and their interactions with proteins have been developed. This Special Issue will focus on G4s present in microorganisms, addressing all the above aspects.

Molecular Modeling in Drug Design

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ISBN: 9783038976141 Year: Pages: 220 DOI: 10.3390/books978-3-03897-615-8 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Chemistry (General) --- Science (General)
Added to DOAB on : 2019-04-05 10:34:31
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This book is a printed edition of the Special Issue Molecular Modeling in Drug Design that was published in Molecules

Keywords

hyperlipidemia --- squalene synthase (SQS) --- molecular modeling --- drug discovery --- Traditional Chinese Medicine --- molecular dynamics simulation --- biophenols --- natural compounds --- amyloid fibrils --- Alzheimer’s disease --- ligand–protofiber interactions --- adhesion --- FimH --- rational drug design --- molecular dynamics --- molecular docking --- ligand binding --- EphA2-ephrin A1 --- PPI inhibition --- interaction energy --- in silico screening --- adenosine --- boron cluster --- adenosine receptors --- AR ligands --- aggregation --- promiscuous mechanism --- human ecto-5?-nucleotidase --- virtual screening --- enzymatic assays --- turbidimetry --- dynamic light scattering --- docking --- solvent effect --- binding affinity --- scoring function --- molecular dynamics --- target-focused pharmacophore modeling --- density-based clustering --- structure-based drug design --- AutoGrid --- grid maps --- probe energies --- method development --- steered molecular dynamics --- all-atom molecular dynamics simulation --- resultant dipole moment --- mechanical stability --- protein-peptide interactions --- molecular dynamics --- proteins --- molecular recognition --- protein protein interactions --- artificial intelligence --- deep learning --- neural networks --- property prediction --- quantitative structure-activity relationship (QSAR) --- quantitative structure-property prediction (QSPR) --- de novo design --- adenosine receptor --- metadynamics --- extracellular loops --- allosterism --- molecular dynamics --- cosolvent molecular dynamics --- drug design --- fragment screening --- docking

Curcumin in Health and Disease

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ISBN: 9783039214495 9783039214501 Year: Pages: 274 DOI: 10.3390/books978-3-03921-450-1 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Science (General) --- Chemistry (General)
Added to DOAB on : 2019-12-09 11:49:15
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The plant-derived polyphenol curcumin has been used in promoting health and combating disease for thousands of years. Its therapeutic effects have been successfully utilized in Ayurvedic and Traditional Chinese Medicine in order to treat inflammatory diseases. Current results from modern biomolecular research reveal the modulatory effects of curcumin on a variety of signal transduction pathways associated with inflammation and cancer. In this context, curcumin’s antioxidant, anti-inflammatory, anti-tumorigenic, and even anti-metastatic activities are discussed. On the cellular level, the reduced activity of several transcription factors (such as NFkB or AP-1) and the suppression of inflammatory cytokines, matrix degrading enzymes, metastasis related genes and even microRNAs are reported. On functional levels, these molecular effects translate into reduced proliferative, invasive, and metastatic capacity, as well as induced tumor cell apoptosis. All these effects have been observed not only in vitro but also in animal models. In combination with anti-neoplastic drugs like Taxol, kinase inhibitors, and radiation therapy, curcumin potentiates the drugs’ therapeutic power and can protect against undesired side effects. Natural plant-derived compounds like curcumin have one significant advantage: They do not usually cause side effects. This feature qualifies curcumin for primary prevention in healthy persons with a predisposition to cancer, arteriosclerosis, or chronic inflammatory diseases. Nonetheless, curcumin is considered safe, although potential toxic effects stemming from high dosages, long-term intake, and pharmacological interactions with other compounds have yet to be assessed. This Special Issue examines in detail and updates current research on the molecular targets, protective effects, and modes of action of natural plant-derived compounds and their roles in the prevention and treatment of human diseases.

Keywords

brain ischemia --- curcumin --- Alzheimer’s disease --- neurodegeneration --- amyloid --- tau protein --- autophagy --- mitophagy --- apoptosis --- genes --- glioblastoma multiforme --- autophagy --- mitophagy --- curcumin --- chaperone-mediated autophagy --- Akt/mTOR signaling --- transmission electron microscopy --- Curcuma longa --- turmeric tuber --- Zingiberaceae --- TLC bioautography --- antimicrobial agents --- ImageJ --- TLC-MS --- hydrostatic counter-current chromatography --- centrifugal partition chromatography --- curcumin --- death receptor --- apoptosis --- curcumin --- anticancer --- structure activity relationship --- cellular pathway --- mechanism of action --- delivery system --- wound --- wound healing --- diet --- nutrition --- micronutrients --- macronutrients --- curcumin --- amino-acids --- vitamins --- minerals --- curcumin --- oxidative metabolites --- inflamm-aging --- cancer --- metabolic reprogramming --- direct protein binding --- IL-17 --- STAT3 --- SHMT2 --- ageing --- anti-cancer --- autophagy --- microbiota --- senescence --- senolytics --- curcumin --- transthyretin --- amyloidosis --- protein aggregation --- protein misfolding --- drug discovery --- curcumin --- renal cell cancer --- tumor growth --- tumor proliferation --- cell cycling --- curcumin --- reflux esophagitis --- gastroprotection --- gastric ulcer --- Helicobacter pylori --- gastric cancer --- curcumin --- complementary medicine --- cancer treatment --- supportive care --- antioxidants --- anti-inflamation --- ulcerative colitis --- Crohn’s disease --- necrotizing enterocolitis --- curcumin --- inflammatory bowel disease --- curcumin --- silica --- chitosan --- nanoparticles --- anti-tumor --- antioxidant activity --- n/a

Marine Bioactive Peptides: Structure, Function, and Therapeutic Potential

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ISBN: 9783039215324 9783039215331 Year: Pages: 442 DOI: 10.3390/books978-3-03921-533-1 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Science (General) --- Biology
Added to DOAB on : 2019-12-09 11:49:16
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This Special Issue Book, “Marine Bioactive Peptides: Structure, Function, andTherapeutic Potential"" includes up-to-date information regarding bioactivepeptides isolated from marine organisms. Marine peptides have been found invarious phyla, and their numbers have grown in recent years. These peptidesare diverse in structure and possess broad-spectrum activities that have greatpotential for medical applications. Various marine peptides are evolutionaryancient molecular factors of innate immunity that play a key role in host defense.A plethora of biological activities, including antibacterial, antifungal, antiviral,anticancer, anticoagulant, endotoxin-binding, immune-modulating, etc., makemarine peptides an attractive molecular basis for drug design. This Special IssueBook presents new results in the isolation, structural elucidation, functionalcharacterization, and therapeutic potential evaluation of peptides found inmarine organisms. Chemical synthesis and biotechnological production of marinepeptides and their mimetics is also a focus of this Special Issue Book.

Keywords

sea cucumber --- ACE-inhibitory peptide --- molecular docking --- structure-activity relationship --- plastein reaction --- Gracilariopsis lemaneiformis --- ACE-inhibitory activity --- peptide --- molecular docking --- SHRs --- prostate cancer --- Anthopleura anjunae oligopeptide --- DU-145 cells --- PI3K/AKT/mTOR signaling pathway --- cod skin --- NA-inhibitory peptide --- influenza virus --- neuraminidase --- molecular docking --- adsorption --- host defense peptide --- antimicrobial peptide --- anti-LPS factor --- host?microbe relationship --- functional diversity --- invertebrate immunity --- crustacean --- antimicrobial activity --- antimicrobial peptide --- polychaeta --- innate immunity --- BRICHOS domain --- recombinant peptide --- ?-helix --- Rana-box --- nuclear magnetic resonance (NMR) --- antimicrobial peptide --- cytotoxicity --- ?-hairpin --- polyphemusins --- tachyplesins --- cell death --- signaling pathways --- Neptunea arthritica cumingii --- multi-functional peptides --- antioxidant activity --- ACE-inhibitory activity --- anti-diabetic activity --- Arenicola marina --- antimicrobial peptides --- arenicin --- complement --- C3a --- acid-sensing ion channel --- animal models --- pain relief --- toxin --- Ugr 9-1 --- APETx2 --- hairtail (Trichiurus japonicas) --- muscle --- peptide --- antioxidant activity --- half-fin anchovy hydrolysates --- Maillard reaction products --- antibacterial peptide --- identification --- self-production of hydrogen peroxide --- membrane damage --- Perinereis aibuhitensis --- decapeptide --- lung cancer --- cell proliferation --- apoptosis --- conotoxins --- conopeptides --- computational studies --- molecular dynamics --- machine learning --- docking --- review --- drug design --- ion channels --- Conus --- conotoxin --- transcriptome sequencing --- phylogeny --- venom duct --- abalone --- peptide --- vasculogenic mimicry --- metastasis --- MMPs --- HIF-1? --- dexamethasone --- myotube atrophy --- protein synthesis --- proteolytic system --- Pyropia yezoensis peptide --- PYP15 --- QAGLSPVR --- antihypertensive effect --- Caco-2 cell monolayer --- transport routes --- oyster zinc-binding peptide --- peptide-zinc complex --- caco-2 cells --- intestinal absorption --- zinc bioavailability --- Chlorella pyrenoidosa protein hydrolysate (CPPH) --- Chlorella pyrenoidosa protein hydrolysate-calcium chelate (CPPH-Ca) --- calcium absorption --- gene expression --- gut microbiota --- cone snails --- conotoxins --- ion channels --- function --- structure --- marine peptides --- arenicin-1 --- molecular symmetry --- structure–activity relationship --- antibacterial --- cytotoxic --- chemical synthesis --- molecular dynamics --- tilapia --- HUVEC --- angiotensin II --- NF-?B --- Nrf2 --- endothelial dysfunction --- conotoxin --- cone snail --- Conus --- Conus ateralbus --- Kalloconus --- n/a

Solid-Phase Microextraction

Authors: ---
ISBN: 9783039282623 9783039282630 Year: Pages: 266 DOI: 10.3390/books978-3-03928-263-0 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Science (General) --- Chemistry (General) --- Analytical Chemistry
Added to DOAB on : 2020-04-07 23:07:08
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This book covers the most recent research activities and achievements regarding to the solid phase microextraction (SPME) technique. It is a powerful sample preparation tool that addresses the new challenges of analytical laboratories. Among others, its fundamental applications involved the sampling of volatile compounds from various matrixes. The demonstrated topics ranged from aroma characterization of various fruits, essential oils to the utilization of SPME for in-tube extraction and isolation of selected compounds from complex samples followed by state-of-the-art analytical techniques.

Keywords

mango germplasm --- volatile compound --- HS-SPME-GC-MS --- multivariate analysis --- cubeb berry --- principal component analysis (PCA) --- solid-phase microextraction (SPME) --- hydro-distillation (HD) --- simultaneous distillation/extraction (SDE) --- gas chromatography-mass spectrometry-olfactometry (GC-MS-O) --- SPME --- OH-PAHs --- gas-chromatography --- MTBSTFA --- in-tube solid-phase microextraction (IT-SPME) --- nanoliquid chromatography (nanoLC) --- contact trace analysis --- cannabis --- THC --- solid-phase microextraction --- air sampling --- air analysis --- volatile organic compounds --- COMSOL --- time-weighted average --- terpenes --- terpenoids --- headspace solid phase microextraction --- glandular source --- Monomorium chinense --- DI-SPME --- GC-MS --- Mediterranean fruit fly --- extraction solvent --- metabolites --- leave-one-solute-out (LOSO) cross-validation --- leave-one-out (LOO) cross-validation --- linear free-energy relationship (LFER) model --- membrane-coated fiber (MCF) approach --- partition coefficient --- quantitative structure-activity relationship (QSAR) --- metalworking fluid --- volatile organic compounds --- torrefaction --- waste to carbon --- biochar --- municipal solid waste --- SPME --- aromatic water --- hydrolat --- volatile compounds --- metabolic fingerprint --- eucalyptol --- SPME --- retracted SPME --- TWA SPME --- GC–MS --- on-site sampling --- air quality --- air monitoring --- VOCs --- odor --- environmental analysis --- biogenic emissions --- veraison --- viticulture --- nondestructive analysis --- wine aroma --- diffusion --- grape skin --- vacuum-assisted extraction --- solid-phase microextraction --- VOCs --- historical foods --- preserves --- volatile organic compounds (VOCs) --- bisphenol-A (BPA) --- essential oil --- drying --- SPME --- true lavender --- volatile constituents --- in-tube SPME-MS/MS --- dual ligand organic-silica hybrid monolith capillary --- amino acids --- plasma samples --- pears --- HS-SPME --- volatile compounds --- GC

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