CHIMICA FARMACEUTICA - ANALISI CHIMICO-TOSSICOLOGICA DELLE PIANTE OFFCINALI E DEI PRODOTTI NUTRACEUTICI
Academic Year 2020/2021 - 2° Year - Curriculum Scienze Erboristiche e dei Prodotti Nutraceutici- Medicinal Chemistry: Loredana SALERNO
- ANALISI CHIMICO-TOSSICOLOGICA DELLE PIANTE OFFICINALI E DEI PRODOTTI NUTRACEUTICI: Salvatore GUCCIONE
Scientific field: CHIM/08 - Pharmaceutical chemistry
Taught classes: 84 hours
Laboratories: 36 hours
Term / Semester: 1° and 2°
Learning Objectives
- Medicinal Chemistry
Knowledge and understanding
The course aims to provide students with the tools to study the fundamental concepts that characterize Pharmaceutical Chemistry
Applying knowledge and understanding
The student acquires knowledge of the strategies used for the discovery and design of new active ingredients, of the steps necessary for the development of these drugs and for their development as medicaments. In addition, he will have knowledge of the moments of the action of the drugs, from administration to elimination and of the conditioning properties of the drug-two-phase interaction. The student will have knowledge of selected classes of drugs and will understand how they interact with neurotransmitter receptors, with intracellular receptors, with enzymes and with ion channels, deepening their mechanisms of action, chemical-pharmaceutical and toxicological properties, and structure-activity relationships
EXPECTED LEARNING RESULTS
The student will know and understand the issues related to the design, the mechanism of action at the molecular level, drug-receptor interactions, toxicity, metabolism and structure-activity relationships of the classes of drugs examined, in particular those of origin natural - ANALISI CHIMICO-TOSSICOLOGICA DELLE PIANTE OFFICINALI E DEI PRODOTTI NUTRACEUTICI
This course introduces the principles of analytical chemistry and provides how these principles are applied in the analysis of plants active principles and nutraceuticals.
The aim of this course is to provide students with a broad understanding of the principles and applications of analytical chemistry. Students are first provided with an introduction into sample collection and preparation, analytical measurements and statistical treatment of data that can be obtained from a variety of analytical methods compehensive of the basic instrumental methods of chemical analysis. This course will cover important titrimetric methods: acid-base, complexometric and redox titrations, as titrimetric techniques still play an important role in the modern analytical laboratory, to a large extent because many titrations can be fully automated.The students will also be introduced to basic separation techniques, e.g. solvent extraction and ion-exchange including chromatography. The teaching offers the basic knowledge for the assessment of some analytical methods suitable for the analysis of the active principles present in medicinal plants, phytoderivatives and nutraceuticals and to carry out the quality control of the herbal products, according to the certification standards of the quality systems.
On successful completion of the course students will be able to:
1. Describe and compare a range of analytical chemistry methods and explain the underlying theoretical principles.
2. Employ a variety of analytical and instrumental methods to prepare, separate and quantify active principles and neutraceticals.
3. Apply the scientific process, including statistical treatment of data, in the conduct and reporting of chemical analysis.
4. Work safely and competently in an analytical laboratory setting.
Course Structure
- Medicinal Chemistry
The course will be held mainly through lectures. During the lessons the student will be asked to actively participate in the discussion on the topics presented and in particular in case studies. Classroom exercises on exam methods will be proposed during the course.
Should teaching be carried out in mixed mode or remotely, it may be necessary to introduce changes with respect to previous statements, in line with the programme planned and outlined in the syllabus.
Learning assessment may also be carried out on line, should the conditions require it.
- ANALISI CHIMICO-TOSSICOLOGICA DELLE PIANTE OFFICINALI E DEI PRODOTTI NUTRACEUTICI
Frontal Lessons.
Theory is brought to practice in the laboratory if possible or through videos.
According to "Regolamento Didattico di Ateneo (R.D.A.) i.e. University Didactic Regulations attendance of both lessons and laboratory training is mandatory.
Should teaching be carried out in mixed mode or remotely, it may be necessary to introduce changes with respect to previous statements, in line with the programme planned and outlined in the syllabus.
Learning assessment may also be carried out on line, should the conditions require it.
Detailed Course Content
- Medicinal Chemistry
GENERAL PART
Definition and objectives of Pharmaceutical Chemistry, history and evolution. Discovery of drugs from natural products. Definition of drug. Different ways to classify drugs. ATC classification of drugs. Nomenclature of drugs. Stages of drug action: pharmaceutical, pharmacokinetics, pharmacodynamics. Pharmacokinetics: absorption, metabolism (phase I and phase II), distribution and elimination of a drug. Pharmacodynamics: Drug targets. Molecular drug-target interaction: description of the different chemical bonds involved in the interaction. Receptors: G protein coupled receptors, receptors with intrinsic enzymatic activity, ion channels ligand-gated and voltage-gated. Enzymes and enzymatic inhibition, competitive and non-competitive inhibitors. Nucleic acids. Lipids. Carbohydrates. Discovery, design and development of drugs. Optimization of interaction with the target. Optimization of target access. Prodrugs and Softdrugs. The introduction of drugs on the market.
SYSTEMATIC PART
Examples of drugs derived from natural substances (the following examples will be integrated in class).
OPIOID ANALGESICS. Introduction. Morphine: structure and properties, structure-activity relationships. Opioid receptors, development of morphine analogues, agonists, antagonists.
ANTICANCER. General information on neoplastic diseases and therapeutic approaches, classification of anticancer drugs. Plant-based anticancer drugs - ANALISI CHIMICO-TOSSICOLOGICA DELLE PIANTE OFFICINALI E DEI PRODOTTI NUTRACEUTICI
1. Measurements, Statistics
2. Sample Preparation
3. Acid-Base Equilibria and Titrations
4. Complexation Equilibria and Titrations, EDTA titration
5. Redox Chemistry and Titrations
6. Electroanalytical Methods: electrolysis and electrodeposition coulometry, polarography
7. Spectrophotometry: fundamentals and applications, absorption and emission of radiation, spectra, Beer's law relationship between absorption and concentration, instruments for UV-visible spectrophotometry, choosing a spectrophotometric method, techniques of spectrophotometric determination
8. Atomic Spectroscopy: atomic absorption spectroscopy, flame emission spectroscopy, plasma and electric discharge spectroscopy
9.Separation: Precipitation, Solvent extraction, Ion-exchange
10. Chromatography: principles of chromatograhy, gas chromatography, liquid chromatography
Textbook Information
- Medicinal Chemistry
G. L. Patrick – Introduzione alla Chimica Farmaceutica- EdiSES
W.O. Foye- Principi di chimica farmaceutica- Piccin
- ANALISI CHIMICO-TOSSICOLOGICA DELLE PIANTE OFFICINALI E DEI PRODOTTI NUTRACEUTICI
1)Daniel C Harris,
QUANTITATIVA 2017, ZANICHELLI;
2) Renato Cozzi , Pierpaolo Protti , Tarcisio Ruaro Elementi di chimica analitica strumentale Terza edizione 2020, ZANICHELLI;3)Luisa Mannina, Maria Daglia Alberto Ritieni, La chimica e gli alimenti nutrienti e aspetti nutraceutici, Casa Editrice Ambrosiana. Distribuzione esclusiva Zanichelli, 2019.
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