Pharmacognosy Lec #1 PDF

Pharmacognosy I PHA3114147 Assist. Prof. Şule Nur KARAVUŞ Istanbul Medipol University, Faculty of Pharmacy, Department of Pharmacognosy [email protected]  - Jean Bruneton Pharmacognosy: Phytochemistry,...

Pharmacognosy I PHA3114147 Assist. Prof. Şule Nur KARAVUŞ Istanbul Medipol University, Faculty of Pharmacy, Department of Pharmacognosy [email protected]  - Jean Bruneton Pharmacognosy: Phytochemistry, Medicinal Plants - Trease and Evans' Pharmacognosy - Pharmacognosy Fundamentals, Applications and Strategy S. Badal - The Science of Flavonoids Erich Grotewold - Fundamentals of Pharmacognosy and Phytotherapy E. Williamson, Michael Heinrich, Joanne Barnes, Simon Gibbons Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1 Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  DEFINITION PHARMACOGNOSY Pharmacognosy is the branch of science that studies bioactive compounds obtained from biological sources such as plants, animals, microorganisms and marine products or raw drug materials used as drug excipients. ‘’The study of biologically active natural products’’ Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  DEFINITION PHARMACOGNOSY - The word “Pharmacognosy” was first used in a work entitled “Lehrbuch der Materia Medica” by an Austrian physician Johann Adam Schmidt (Beethoven's doctor) in 1811, and then by Anotheus Seydler in 1815. - Treatment with herbs and the use of herbs are as old as human history. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  HISTORY of PHARMACOGNOSY Early Documentation of Medicinal Plants - Mesopotamian ∼ 2.600 B.C.E. - Egyptian ∼ 1.800 B.C.E. - Chinese ∼ 1.100 B.C.E. - Indian ∼ 1000 B.C.E. - Greek and Roman ∼ 500 B.C.E Dark ages ∼ 400-1100 C.E. - Avicenna coordinated all medical knowledge everything that was avaliable to him at the time - Published a compendium The Canon of Medicine (5 volume) Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  HISTORY of PHARMACOGNOSY - The use of plants for medicinal purposes started long before any form of record. - Most of the knowlege has been passaged down the generations - The first written documentation of drugs obtained from natural products dates as far back as to the Sumerians and Akkadians (BC 3000) - Ebers Papyrus (Ancient Egypt about 1550 BC); 110 pages and 2289 lines, about 700 herbal, animal and mineral drogs are mentioned. - Egyptian hieroglyphics (Museum in Vienna) Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  HISTORY of PHARMACOGNOSY Materia Medica B.C. 1 - Dioscorides (Greek physician) was a physician in the armies of Neron and Vespasien and traveled to Eastern countries and Anatolia with these armies. - Consists of 5 books - Provides information on about 500 medicinal plants (as well as animal and inorganic medicines) - Mostly Anatolian medicinal plants. - The oldest known copy is the one known as the "Vienna Codex (Codex Vindobonensis)," kept in the Austrian National Library. - Based on Discorides observations, he gave information about their use, effects and purity analysis. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1 Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  HISTORY of PHARMACOGNOSY The Canon of Medicine (al-Qānūn fī al-ṭibb) - Translated into Latin by Gerard of Cremona in the 12th century and remained part of the standard curriculum for medical students until the late 17th century. - The Canon of Medicine is organized into five books as follows: - Book 1 General medical principles; covers the basic principles of medicine; - Book 2 Materia medica; lists approximately 800 individual drugs of plant, animal and mineral origin; - Book 3 Special pathology; discusses the diseases of individual organs; - Book 4 Diseases involving more than one member; discusses medical conditions that affect the entire body, such as fevers and poisons; - Book 5 Formulary; deals with the preparation of about 650 remedies of diverse components (Antidotarium). It contains some very complex medicines, including preparations of theriacs, electuaries, syrups, medicinal oils, pills and ointments, etc. The book concludes with a short collection of formulations against some diseases. Avicenna (Ibn-i Sina) - Ibn Sina was born in Bukhara (present-day Uzbekistan) in 980 and died in Hamadan (present-day Iran) in 1037. - Ibn Sina was referred to in the Latin West as princeps medicorum (prince of physicians). Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1 Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Development of Pyhtochemistry - Developments in chemistry during the latter part of the 18th century led not only to the synthesis of new drugs but also to the purification of plant extracts used as medicines. - 1805 Sertürner reports isolation of morphine from Papaver somniferum commercilized by E. Merck in Darmstadt in 1826 - This invention of Sertürner can be considered as the beginning of isolattion active compounds from plants. - British organic chemist Robert Robinson (1886–1975) discovered the molecular structure of morphine. He was awarded the Nobel Prize in Chemistry in 1947. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Development of Pyhtochemistry - 1820 Pelletier & Caventou – Quinine from Cinchona species - 1821 Pelletier & Caventou – Caffeine from Coffee arabica and Camelia sinensis Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Development of Pyhtochemistry Digitalis and Dr. William Withering - In 1775, Doctor William Withering identified the plant that carries the active substance in an herbal mixture used for the treatment of edema as Digitalis purpurea, using the microscopic diagnosis method. - Microscopic diagnosis of herbal drugs started with this work of Dr. Withering. - In 1997, it was found by microscopic method that the cause of poisoning caused by an herbal mixture preparation containing 14 herbs was Digitalis lanata, which was added to the mixture by mistake. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Bioprospecting - Bioprospecting is defined as a systematic and organized search for useful products derived from bioresources including plants, microorganisms, animals, etc., that can be developed further for commercialization and overall benefits of the society. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  DROG or DRUG - Definitions - Herbal Drog; They are parts of medicinal plants used for medicinal purposes (Flower, leaves or roots). - Medicinal plant: It was defined by the World Health Organization (WHO) in 1980 as “plant varieties that can be curative or preventive of diseases with one or more organs or can be the precursor of any chemical-pharmaceutical synthesis”. - Phytotherapy: Treatment with herbs. - Phytotherapeutic is the general name given to products (medical tea, herbal medicine, etc.) prepared from drugs used in the treatment (phytotherapy) with herbal drugs. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  DROG or DRUG - Definitions - Active substances: (galantamine, pilocarpine, ephedrine, digoxin, taxol, atropine, etc.) obtained from medicinal plants and prepared in a pharmaceutical form and at a certain dose are not considered herbal medicines! - Food supplements: They are products for which the daily intake dose is determined by being prepared as tablets, capsules, disposable powder packs and other forms of plant and animal origin substances that have nutritional or physiological effects in order to supplement normal nutrition. - Nutraceuticals: Products that contain much higher amounts of a component of a food that are considered biologically effective. Lycopene, which is the effective component of tomato, resveratrol in grape seed, EGCG (epigallocatechin gallate), which is the effective component of green tea, and isoflavones obtained from soybeans are considered nutraceuticals. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Standardization of herbal preparations While preparing herbal preparations; The same plant and the same process may produce different results. - The effect of the herbal preparation; growing conditions of the plant, the collection time, the drying and storage methods, the preparation method and the standardization methods used. - Existing analytical methods were not sufficient to accurately determine the amount of active compounds in the herbal preparation. - Sometimes the effective compound was unknown. - In Scandinavia, England and America, most herbal preparations have been removed from the drug lists. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Factors affecting the structure (qualitative) and/or amount of active substances in Medicinal Plants: 1) Growing conditions *Soil selection should be made in accordance with the type of plant, for example; While Lavandula spicata does not grow well in wet and calcareous soils, Mentha piperita grows very well. *Preparation of the soil; the soil is plowed and fertilized. The crop yield in the field increases as the tilled soil holds better water. *Climate: temperature, light and rain 2) Collection time *The structure (qualitative) and/or amount of the active substances carried by medicinal plants may change according to the seasons and even according to different time periods during the day. Alkaloid biosynthesis in Papaver somniferum begins with thebaine, which first converts to codeine and then to morphine. *The amount of codeine in P. somniferum latex reaches its highest level at noon. 3) Drying: method, time and temperature The drying process stops the enzymatic reactions in the plant and prevents the decomposition or change of the active substances, as the water contained in the plant is largely removed without qualitative and quantitative changes in the active ingredients. Some plant materials need to be shredded or peeled (eg Liquiritiae radix) before drying, which is difficult to do after drying. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Factors affecting the structure (qualitative) and/or amount of active substances in Medicinal Plants: 4) Storage of the dried material The dried material should be stored in a cool, dry and dark place so that it is not affected by moisture (hydrolysis, enzyme reactions and microorganism), heat (polymerization, decomposition, microorganism) and light. The material can be stored in a paper bag, cloth bag, cardboard box, tin can or glass jar. 5) Stabilization of plant material Enzymes inactivated by drying are activated again when the material absorbs moisture and is exposed to heat. Enzymes must be destroyed (stabilization of the material) in order to stop the enzyme activities that continue after the plant is harvested. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Factors affecting the structure (qualitative) and/or amount of active substances in Medicinal Plants: Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Rules of Collection of Plants 1. Leaves; It should be collected when the plant is blooming. 2. Flowers; It should be collected before fully opening or in buds. 3. Underground parts; After drying the aerial parts of the plant. 4. Shells; The shells should be collected after shedding its leaves. 5. Fruit or seeds; If there is no special record, it should be collected after ripening. 6. Leaves, flowers or aerial parts should not be collected in rainy weather (the quality will be poor as it will be difficult to dry). 7. Roots, rhizomes and tubers should be removed in rainy weather, and the shells should be collected in rainy weather. Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Modified Natural Products - Quinine change the World profound ways - Anti-malarial drug - Isolated from the bark of Cinchona officinalis Introduced: 1632 (tea of bark) – 1820 (isolated) - 1910 (1st case of drug resistance) - 1945 (Chloroquine) - 1957 (Chloroquine drug resistance) – 1977 (Mefloquine) - 1982 (Mefloquine drug resistance) - There is a drug resistance problem that’s growing Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Modified Natural Products - Prof. Youyou TU (2015 Nobel Prize) - Currently the standart of care for quinine-resistant malaria artemesinoids are to be given in combination therapy - It binds totaly different proteins n totally different way - Artemisinin metabolized into dihydroartemisinin which is active metabolite - Amenable for modification - Changes on molecule improving the drug-like properties (Artesunate orally given drug) - Millions og people that are dying each year and since 2000 after discovery of artemisinin 10 million lives have been saved Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1  Small molecules approvals from FDA over the last 40 years Antibodies and other Synthetic chemistry Vaccines (8%) inspired by nature, biologics (18%) using natural active moiety, or natural Unmodified natural product (4%) mimic (26%) Botanical mixture (1%) Totally synhetic from various discovery methods (25%) Pharmacognosy I Instructor: Sule Nur KARAVUS Fall 2024-Lecture #1 Newman, D. J., & Cragg, G. M. (2020). Natural products as sources of new drugs over the nearly four decades from 01/1981 to 09/2019. Journal of natural products, 83(3), 770-803.