Pharmacognosy
A.Y. 2020/2021
Learning objectives
The main objective of the course is to give information on the pharmacological activity of synthetic or natural drugs. Taking into consideration the complexity of botanicals, the course will consider the parts of plant used for the pharmacological activity and their active principles, analyzing in detail the structure-activity relationship and the biosynthetic pathways of active components. Moreover, the course will consider the theoretical basis of pharmacokinetic and pharmacodynamic, considering the main neurotransmitters, acetylcholine, GABA, biogenic amines etc. and the effects of botanicals 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).
Lesson period: Activity scheduled over several sessions (see Course syllabus and organization section for more detailed information).
Assessment methods: Esame
Assessment result: voto verbalizzato in trentesimi
Single course
This course cannot be attended as a single course. Please check our list of single courses to find the ones available for enrolment.
Course syllabus and organization
Linea AK
Lesson period
year
During the emergency teaching phase, the course program and the reference material will not change.
If classroom lessons will not be allowed, lessons will be implemented on line by synchronous lesson through the Microsoft Teams platform. The schedule and criteria for attending face-to-face lessons will be published in due time on the Ariel website along with any updates related to the Covid-19 emergency
If classroom lessons will not be allowed, lessons will be implemented on line by synchronous lesson through the Microsoft Teams platform. The schedule and criteria for attending face-to-face lessons will be published in due time on the Ariel website along with any updates related to the Covid-19 emergency
Course syllabus
Main classes of pharmacological target;
Principle of pharmacodynamic;
Principle of pharmacokinetic;
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.
Principle of pharmacodynamic;
Principle of pharmacokinetic;
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.
Prerequisites for admission
Subjects taught in the preparatory courses are mandatory. 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
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 multiple choice theory test consisting of fifteen questions. Test is considered passed with a minimum of ten corrected answers.
Second part is an oral exam with 30/30 vote
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 provided during both the first and the second teaching semesters. If the COVID-19 emergency will not allow face-to-face teaching, lessons will be provided using Zoom 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. 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. The phases of the research. Pharmacovigilance Introduction to pharmacoeconomics.
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. 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.
Neurotransmitters, hormones and receptors. Drug-receptor interactions. Definition of intrinsic activity, agonism, inverse agonism, antagonism, potency, efficacy.
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 and regulation of gene transcription. Mechanism of action of glucocorticoids.
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 and capsaicin.
Elements of lipidergic transmission. Endocannabinoids. Cannabis sativa.
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.
Inflammation and autacoids. Nitric oxide. Reactive oxygen species (ROS): formation and elimination. Mechanisms of ROS-induced damage. Antioxidant drugs: polyphenols-based drugs (Artichoke, Java tea, Sweet clover, Wild celery, Kella, Milk Thistle, Citrus spp, Propolis, Passiflora incarnata, Achillea, Equisetum, Echinacea spp, Blueberry, tannins, Hamamelis virginiana, Krameria); fluroglucinols-based drugs (Hops, St. John's-wort).
Introduction to serotoninergic transmission. Serotoninergic receptors. Vegetable drugs active on the serotoninergic transmission (Claviceps purpurea, Psilocybe mexicana, Lophophora williamsii, Mimosa hostilis).
Salvia divinorum.
Lipidic autacoids: arachionic acid metabolites and PAF. Vegetable drugs affecting lipidic autacoids (Glycyrrhiza glabra, Ginkgo biloba).
Glycosides-based drugs: anthraquinone, cyanogenic, sulphated, saponin, coumarin and digitalic glycosides (Aloe spp, Rhamnus spp, Cassia spp, Rheum spp, Common laurel, Prunus spp, Black mustard, Garlic, Mead wort, Salix alba, Bearberry, Horse-chestnut, Milkwort, Butcher's broom, common Ivy, Primrose, Panax ginseng, Centella asiatica, Common Marigold, Eleutherococcum, 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, cyclodextrin, starch, gum arabic, tragacanth, karaya e guar, Althea officinalis, Malva silvestris, Linum usitatissimum, dextran).
Terpenes-based drugs. Essential Oils (Lavender, Oreganon, Mint, Eucalyptus, Niaouli, Grand Wormwood, Turmeric, Lemon balm, Ginger, Chamomile, Feverfew, Valeriana officinalis, Black Horehound, Rosemary, Thyme, Hawthorn, Sage). Oleoresins (Myrrh, Turpentine). Balms.
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. 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.
Neurotransmitters, hormones and receptors. Drug-receptor interactions. Definition of intrinsic activity, agonism, inverse agonism, antagonism, potency, efficacy.
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 and regulation of gene transcription. Mechanism of action of glucocorticoids.
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 and capsaicin.
Elements of lipidergic transmission. Endocannabinoids. Cannabis sativa.
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.
Inflammation and autacoids. Nitric oxide. Reactive oxygen species (ROS): formation and elimination. Mechanisms of ROS-induced damage. Antioxidant drugs: polyphenols-based drugs (Artichoke, Java tea, Sweet clover, Wild celery, Kella, Milk Thistle, Citrus spp, Propolis, Passiflora incarnata, Achillea, Equisetum, Echinacea spp, Blueberry, tannins, Hamamelis virginiana, Krameria); fluroglucinols-based drugs (Hops, St. John's-wort).
Introduction to serotoninergic transmission. Serotoninergic receptors. Vegetable drugs active on the serotoninergic transmission (Claviceps purpurea, Psilocybe mexicana, Lophophora williamsii, Mimosa hostilis).
Salvia divinorum.
Lipidic autacoids: arachionic acid metabolites and PAF. Vegetable drugs affecting lipidic autacoids (Glycyrrhiza glabra, Ginkgo biloba).
Glycosides-based drugs: anthraquinone, cyanogenic, sulphated, saponin, coumarin and digitalic glycosides (Aloe spp, Rhamnus spp, Cassia spp, Rheum spp, Common laurel, Prunus spp, Black mustard, Garlic, Mead wort, Salix alba, Bearberry, Horse-chestnut, Milkwort, Butcher's broom, common Ivy, Primrose, Panax ginseng, Centella asiatica, Common Marigold, Eleutherococcum, 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, cyclodextrin, starch, gum arabic, tragacanth, karaya e guar, Althea officinalis, Malva silvestris, Linum usitatissimum, dextran).
Terpenes-based drugs. Essential Oils (Lavender, Oreganon, Mint, Eucalyptus, Niaouli, Grand Wormwood, Turmeric, Lemon balm, Ginger, Chamomile, Feverfew, Valeriana officinalis, Black Horehound, Rosemary, Thyme, Hawthorn, Sage). Oleoresins (Myrrh, Turpentine). Balms.
Prerequisites for admission
Subjects taught in preparatory courses are mandatory.
Teaching methods
Frontal lesson and open discussion.
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://asalaf.ariel.ctu.unimi.it
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://asalaf.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.
8-9 test sessions are scheduled during the Academic Year, according to the avalability of IT classrooms.
Professor(s)
Reception:
Tuesday from 10.30 am, upon arrangement by writing to the institutional email
Via Balzaretti 9 or using Zoom Cloud Meetings videoconference