Pharmacognosy

A.Y. 2021/2022
8
Max ECTS
64
Overall hours
SSD
BIO/15
Language
Italian
Learning objectives
The main objective of the course is to provide knowledge on the pharmacological activity of synthetic or natural drugs. Taking into consideration the complexity of botanicals, the course will define the parts of plant used for their pharmacological activity and the active principles responsible for it. Moreover, the course will provide the theoretical basis of pharmacokinetic and pharmacodynamic, examining the main neurotransmitter systems and the effects of active principles of specific natural drugs on these targets.
Expected learning outcomes
At the end of the course, students are expected to know and understand principles underlying concepts of pharmacokinetic and pharmacodynamic, applying this knowledge to the comprehension of the effects of the active principles from natural or synthetic source and their molecular target. In particular, students will be able to know and understand the main mechanisms of action of drugs, their relationship with the endogenous systems, the aspects which influence variability of active principles in the drug, and factors able to affect safety and/or efficacy (quality of botanicals).
Course syllabus and organization

Linea AK

Responsible
Lesson period
year
More specific information on the delivery modes of training activities for academic year 2021-2022 will be provided over the coming months, based on the evolution of the public health situation.
Course syllabus
Main classes of pharmacological target;
Principle of pharmacodynamic, agonist (full, partial and inverse) antagonists and allosteric ligands;
Drug-receptor interaction theories;

Principle of pharmacokinetic (ADME and main pharmacokinetic parameters);

The principal neurotransmitters: the adrenergic, cholinergic, dopaminergic, serotoninergic, gabaergic, glutamatergic, histaminergic systems. In addition the arachidonic acid system and their drugs;

General pharmacognosy, phitocomplex and the principal natural drugs: alkaloids, phenols, cardiac glycosides, vanilloids, essential oils, laxatives;
Plant biotechnologies;
Drugs of abuse.
Prerequisites for admission
Subjects taught in the following preparatory courses are mandatory:
Animal Biology and Plant Biology
Human Anatomy and Physiology

It is suggested to have, at least, attended the course of Biochemistry
Teaching methods
64 oral seminars
Teaching Resources
Clementi, Fumagalli - General an molecular Pharmacology, ed Wiley
Capasso, DePasquale, Grandolini, Mascolo: FARMACOGNOSIA (2° ediz.)
Ed Springer 2010
Slide provided by the teacher in digital format on the ARIEL web site
Assessment methods and Criteria
The exam will consist of two parts: first part a written multiple choice questionary consisting of 15 questions (correct answer: +1 point; wrong answer: -0.5 point; no answer given: 0 point) will be utilized. Test is considered passed with a minimum score of 9.
Time allowed 15 min.

Second part is an oral exam with 30/30 vote
BIO/15 - PHARMACEUTICAL BIOLOGY - University credits: 8
Lessons: 64 hours
Professor: Rovati Gianenrico

Linea LZ

Responsible
Lesson period
year
The Course "Pharmacognosy" is offered during both the first and the second teaching semesters. More specific informations on the delivery modes of training activities for the academic year 2021-22 will be provided over the coming months, based on the evolution of the public health situation. If the COVID-19 emergency will not allow face-to-face teaching, lessons will be provided using Teams following the regular schedule of the Course. Written tests, if carried out remotely, will use Moodle + Safe Exam Browser, with audio/video monitoring using Zoom Cloud Meetings. Updated informations about the beginning and the conduct of the Course can be found on the Board of the Ariel site of the Course.
Course syllabus
Introduction and definitions of interest in Pharmacology and Pharmacognosy.
Sustainability for the use of drugs obtained from natural sources. The phases of the research. Pharmacovigilance. Introduction to Pharmacoeconomics and definition of shadow costs.
Biological membrane crossing, Routes of administration, absorption and bioavailability of active principles. First-pass effect. Absorption kinetics. Transporters and drug absorption: P-gl and MRPs. Factors affection drug absorption.
Drug distribution and Kp. Apparent distribution volume. Plasma protein binding. Factors affecting drug distribution.
Drug metabolism. Inhibition and induction of drug metabolic enzymes. Enterohepatic recirculation. Factors affecting drug metabolism and variability in the response to drugs. Pharmacogenetics and pharmacogenomics: polymorphisms affecting drug metabolism and activity.
Drug elimination. Drug renal excretion. Tubular secretion and reabsorption. Renal clearance. Transporters and other factors affecting drug elimination.
Plasmatic drug concentration: Pharmacokinetics. Systemic clearance. Plasmatic half-life. Clearance, plasmatic half-life, elimination rate constant and distribution volume relationship. Single and multiple dosing. Steady state plasmatic concentration. Therapeutic window and therapeutic ratio. Saturation kinetics. Therapeutic regimen corrections. Individual variations in response to drugs and drug interactions.
Proteins as drug targets. Enzymes, Transporters, Receptors. Channel receptors, G-protein-coupled receptors, enzymatic activity-coupled receptors. Enzyme inhibition. Voltage-gated channels. ATP-dependent pumps and exchangers.
Transporters and their role in drug absorption and elimination. Examples of drugs affecting transporters activity.
Ligand activated channels. Nicotinic and GABA receptors.
Tyrosin kinase receptors and signal transduction.
Seven transmembrane domains receptors and major transduction mechanisms (heteromeric G-proteins, adenylyl-cyclase, phospholipases C and D, small G-proteins).
Nuclear receptors. Hormone responsive elements.
Occupation theory of receptors. Dose-response curves, EC50 and Kd. Drug potency and efficacy. Reversible and irreversible antagonists. Dose-Ratio. Partial agonists. Reserve of receptors. Inverse agonists.
Protein phosphorylation and control of biological functions. Kinases and phosphatases.
Intracellular calcium-ion concentrations. Ca-channels, pumps and transporters. Ca-binding proteins.
Definition of natural drugs, variability of active principles, secondary metabolism and its physiological function, balsamic time, preservation of vegetable and animal drugs,
Quality control, standardization. Elements of chemical-physical analysis.
Powders, extracts, tinctures and essences.
Classification of vegetable drugs. Alkaloids.
Autonomic nervous system and somatic nervous system. Anatomical and functional arrangement of the autonomic nervous system. Actions mediated by the sympathetic and parasympathetic nervous system.
Catecholaminergic transmission: organization, biochemistry and function of the synapse, adrenaline and noradrenaline, alpha- and beta-adrenergic receptors, agonists and antagonists. Introduction to dopaminergic transmission. Dopaminergic receptors. Vegetable drugs active on the catecholaminergic transmission (Ephedra sinica, Erythroxylum coca, Catha edulis, Yohimbe).
Cholinergic transmission: organization, biochemistry and function of the cholinergic synapse, nicotinic and muscarinic receptors, agonists and antagonists, acetylcholin-esterase inhibitors. Neuromuscular junction blockers and curare. Vegetable drugs active on the cholinergic transmission (Atropa belladonna, Datura stramonium, Hyosciamus niger, Pilocarpus jaborandi, Physostigma venenosum, Nicotiana tabacum, Areca cathecu, Lobelia inflata, Hemlock)
Elements of neuropeptidergic transmission. Opioid neuropeptides and their receptors. Papaver somniferum. Substance P: Capsicum.
Antitumor drugs (Vinca spp, Taxus spp, Podophyllum peltatum, Camptotheca acuminata). Colchicum.
Xanthine-based drugs: Coffea spp., Thea spp, Theobroma cacao, Cola acuminata.
Chinolinic-based drugs (Chinchona). Nux vomica. Ipecac.
Introduction to serotoninergic transmission. Serotoninergic receptors. Vegetable drugs active on the serotoninergic transmission (Claviceps purpurea, Psilocybe mexicana, Lophophora williamsii, Mimosa hostilis).
Salvia divinorum.
Histamine: distribution and pathophysiologic role. Rubia Tibetica.
Elements of lipidergic transmission. Endocannabinoids. Cannabis sativa.
Lipidic autacoids: arachionic acid metabolites and PAF. Vegetable drugs affecting lipidic autacoids (Glycyrrhiza glabra, Ginkgo biloba).
Reactive oxygen species (ROS): Mechanisms of ROS-induced damage. Antioxidant drugs: Polyphenols-based drugs. Flavonoids and citroflavonoids. Propolis, Passiflora incarnata, Echinacea spp. Coumarins-based drugs (Sweet clover, Kella). Lignan- and neolignane-based drugs (Milk Thistle). Antocian-based drugs (Blueberry). Tannins-based drugs (Hamamelis virginiana, Aleppo's gall). Floroglucinols-based drugs (Hops, St. John's-wort).
Anthraquinonic glycoside-based drugs (Aloe spp, Rhamnus spp, Cassia spp, Rheum spp). Cyanogenic glycoside-based drugs (Common laurel, Prunus spp). Sulphated glycoside-based drugs (Black mustard, Garlic). Phenolic glicosyde-based drugs (Salix alba). Saponin glycosides-based drugs (Horse-chestnut, Milkwort, Butcher's broom, common Ivy, Primrose, Panax ginseng, Centella asiatica, Common Marigold, Eleutherococcum). Digitalic glycoside-based drugs (Digitalis spp, Strophantus spp, Urginea maritima, Nerium oleander, Lily of the valley, Adonis vernalis)
Lipid-based drugs: oils (coconut oil, almond oil, castor oil, olive oil, peanut oil, fish oil) and waxes (lanolin). Pharmacological activities of polyunsaturated fatty acids.
Carbohydrate-based drugs (honey, manna ash, dextran ,cyclodextrins, starchs, gums, Malva silvestris, Aloe spp).
Terpenes-based drugs. Essential Oils (Lavender, Oreganon, Mint, Eucalyptus, Turmeric, Lemon balm, Ginger, Chamomile, Feverfew, Valeriana officinalis, Hawthorn). Oleoresins (Myrrh). Carotenoids (Vitamin A, Lycopene; Annatto, Saffron).
Prerequisites for admission
Subjects taught in preparatory courses are mandatory.
Teaching methods
Frontal lesson and Q&A.
Teaching Resources
Farmacologia generale e molecolare. F. Clementi e G. Fumagalli. IV edition
UTET, Milano
Goodman & Gilman: Le Basi Farmacologiche della Terapia; Il Manuale. Brunton, Parker, Blumenthal, Buxton. II edition, Zanichelli, Milano
Farmacognosia. F. Capasso, R. De Pasquale, G. Grandolini, N. Mascolo.
Casa editrice Springer, Milano
Slides available at the Course official web site:
https://asalaflz.ariel.ctu.unimi.it
Assessment methods and Criteria
Knowledge will be assessed with a written test, carried out directly on computers located in IT classrooms, accessed using username and password of the institutional email. The test is structured in two sections: the first section is a multiple choice test with 15 questions in 20 minutes, and the second part proposes 4 open questions that can be discussed in an hour. A passing score for first section is mandatory in order to seat in the second section of the test, that takes place immediately after the first one. Scoring of the first part is generated automatically assigning 1 point for each correct answer, -0.5 for each wrong answer, while no answer is scored 0. The test is passed with a score of 9 or above. Scoring of the first section accounts for 30% of the final score.
8-9 test sessions are scheduled during the Academic Year, according to the avalability of IT classrooms.
BIO/15 - PHARMACEUTICAL BIOLOGY - University credits: 8
Lessons: 64 hours
Professor: Sala Angelo
Educational website(s)
Professor(s)
Reception:
Wednesday from 10.30 am, upon appointment by writing to the institutional email
Via Balzaretti 9 or using Zoom Cloud Meetings videoconference