BASIC INTRODUCTION TO Pharmacognosy BY Dr. SARTAJ BEGUM
What is Pharmacognosy ? Is a science which deals with the study of crude medicine in substances obtained from natural sources mainly plant and animal. Crude medicine; are drugs which are from plant or animal not processed (no any addition to add potency ) The word "Pharmacognosy" derived from the Greek words " Pharmakon ” –a drug, or medicine " gignosis ” –to acquire knowledge of
It deals with scientific study of structural, physical, chemical and sensory characters of crude drug obtained from plan t, animal and mineral source s . Therefore:Pharmacognosy is “an applied science that deals with the biological, biochemical and economic features of natural crude drugs and their active constituents (derivatives)”.
Pharmacognosy does not include the study of synthetic drugs. Pharmacognosy is NOT identical to Medicinal Chemistry and/or Pharmacology but utilizes their methods. Studies drugs from plants, animals and minerals E.g.: Digitalis leaf & its glycosides ( digitoxin ) Rauwolfia root & its alklaoids (reserpine) Thyroid gland & its extracted hormone (thyroxin)
Pharmacognosy is not confined to plants BUT also investigates biodynamic compounds in animals, marine organisms, fungi, and micro-organisms NOTE: Natural drug constituents which have been prepared synthetically (e.g. ephedrine, vanillin, caffeine, codeine, menthol, penicillin) BOTH natural and synthetic substances are considered a definite part of pharmacognosy .
6 Pharmacognosy “derived from the Greek Pharmacon , a drug, and Gignosis which means acquire knowledge. Pharmacognosy is the study of crude drugs obtained from plants, animals and mineral kingdom Crude drugs : Are those natural products such as plants or part of plants, extracts and exudates which are not pure compounds and used in medicine
historical development of pharmacognosy Pharmacognosy is regarded as the mother of all science. History of pharmacognosy represents the history of pharmacy & medicine. Pharmacognosy had its origin in the health-related activities of the most primitive human race of the remote past. The early man sought to alleviate his sufferings of illness & injuries by using plants. 7
History of pharmacognosy----- They acquired knowledge of medicinal properties of plants in the following way: By guesswork or trial & error While searching for food By superficial resemblance between the plant parts & the affected organs, that is, by examining the “Signature of Nature”. By observing other animals instinctive discrimination between toxic & palatable plants By accidental discovery (SERENDIPITY) 8
History of pharmacognosy----- By a combination of all these means the ancient people acquired a considerable volume of knowledge about drugs. In course of time a group of people emerged in each community who acquired expertise in collecting, testing & using medicinal plants for treating diseases. These people later became known as `Medicine Men'. The Medicine Men monopolized the knowledge of drugs and hide that knowledge in some mysterious incantations. 9
History of pharmacognosy----- They transferred this secret knowledge only to their trusted predecessors of the successive generations, who gradually increased the volume of knowledge about drugs and their uses. Initially the transfer of the acquired knowledge from generation to generation used to be done verbally by the use of signs & symbols. As civilization progressed, transfer and recording of the knowledge were done in writing. 10
History of pharmacognosy----- The use of plants, plant extracts or pure chemicals isolated form natural products to treat disease is a therapeutic modality, which has stood the test of time even if much of the science behind such therapy is still in its infancy. Indeed today many pharmacological classes of drugs include a natural product prototype. 11
HISTORICAL DEVELOPMENT OF PHARMACOGNOS Y With increase of knowledge of drugs, the volume of works also increased a lot and it become impossible for one person to manage them properly . Thus at this point pharmacy and medicine started to develop along two separate paths One group specialized in diagnosing the disease and prescribing the drug known as phyisician or doctors The other group specialized in collection , processing ,preparation and collection of medicaments knows as pharmacist,.
HISTORICAL DEVELOPMENT OF PHARMACOGNOS Y From the earliest times man and animals have had to distinguish from those plants which are poisonous and those which are not. While pharmacognosy is mainly concerned with natural occurring substances having a medicinal action, it is not entirely limited to such substances only but also to natural, synthetic fibers and the surgical dressings prepared from them . Also includes the study of other materials used in pharmacy, such as flavoring agents, suspending agents, disintegrants, filtering and support media etc.
HISTORICAL DEVELOPMENT OF PHARMACOGNOS Y Other fields which have natural associations with the subject are those of poisonous and hallucinogenic plants, raw materials for production of oral contraceptives, allergens, herbicides and insecticides . Pharmacognosy is closely related to both botany and plant chemistry, being particularly concerned with the description and identification of drugs both in whole state, powder form and with their history, commerce, collection, preparation, evaluation, preservation and storage. Undoubtedly the plant kingdom still holds many species of plants containing substances of medicinal value which have not yet be discovered.
HISTORICAL DEVELOPMENT OF PHARMACOGNOS Y As a result of Modern isolation and pharmacological testing procedures, new plant drugs usually find their way into medicine as purified substances rather than in the form of older galenical preparation . Thus , there came to be three basic disciplines devoted to drugs ; Pharmacology – This dealt with drug actions and effects . Pharmacognosy – covering all information on medicines from natural sources i.e. plants, animals and microorganisms. Medicinal chemistry – the science of synthetic drugs.
Naturally occurring substances having a medicinal action: Surgical dressings prepared from natural fibres Flavourings and suspending agents Disintegrants Filtering and support media Other associated fields: Poisonous and hallucinogenic plants Raw materials for production of oral contraceptives Allergens Herbicides and insecticides 16
Pharmacognosy is related to: Botany Ethnobotany Marine biology Microbiology Herbal medicine Chemistry ( phytochemistry ) Pharmacology Pharmaceutics 17
Why do we need plants? Source of drug molecules Most drugs can be synthesised Still more economical to use the plant Papaver opium -> morphine, codeine (strong medicinal pain) Ergot fungus –> ergotamine (headache), ergometrine (direct action on uterine muscle) 18
19 Digitalis foxglove -> digoxin (acts on cardiac muscle)
2. Source of complex molecules that can be modified to medicinal compounds Examples: Dioscera yam: molecule -> steroids Soya: saponins -> steroids 20
3. Source of toxic molecules To study the way the body responds to their pharmacological use Investigating pharmacological mechanisms picrotoxin – nerve conduction 21
Conclusion Natural products very important to medicine Exist in range of structures that one wouldn’t think of synthesizing Can act as templates for new drug development Untapped reservoir of new compounds 22
Introduction to Natural Products A brief history of natural products in medicine Value of natural drug products Production of natural drug products The role of natural products in drug discovery General principles of botany: morphology and systematics
I. The history of natural products in medicine A great proportion of the natural products used as drugs The study of drugs used by traditional healers is an important object of pharmacognostical research Sumerians and Akkadians (3 rd millennium BC)
Egyptians ( Ebers papyrus , 1550 BC)
Authors of antiquity Hippocrates (460-377 BC) “The Father of Medicine”
The Islamic era Ibn Altabari (770 850) ” فردوس الحكمه“
Ibn Sina (980-1037) ”القانون في الطب“
Ibn Albitar (1148-1197) ”الجامع لمفردات الأدوية والأغذية“
The era of European exploration overseas (16 th and 17 th century)
The 18 th century, Pharmacognosy Johann Adam (1759-1809) Linnaeus (naming and classifying plants) At the end of the 18 th century, crude drugs were still being used as powders, simple extracts, or tinctures
The era of pure compounds (In 1803, a new era in the history of medicine) Isolation of morphine from opium Strychnine ( 1817 ) Quinine and caffeine ( 1820 ) Nicotine ( 1828 ) Atropine ( 1833 ) Cocaine ( 1855 )
In the 19 th century, the chemical structures of many of the isolated compounds were determined In the 20 th century, the discovery of important drugs from the animal kingdom, particularly hormones and vitamins. Microorganisms have become a very important source of drugs
Crude Drugs Also,means any product that has not been advanced in value or improved in condition by grinding, chipping, crushing, distilling , evaporating , extracting, artificial mixing with other substance or by any other process or treatment beyond what is essential to its proper packing and the prevention of decay or deterioration pending manufacture. 36
Today, Crude drugs are rarely used as therapeutic agents; more often their chief principles (derivatives or extractives which contains active constituents) are separated by various means. Sources of Crude Drugs: Plant sources , e.g. Senna,Digitalis,Datura , Cascara, Cinchona, Clove, Opium, etc. Animal sources , e.g. cochineal, cantharidin , honey, cod liver oil, musk, thyroxin, etc. Mineral sources , e.g . talc, kaolin, kieselguhr, etc. 37
What is a Natural Product? A natural product is a substance obtained from a natural source. 1 . A crude drug , e.g. Senna , Cascara, Cinchona, etc.. 2. A galenical preparation of a crude drug, e.g. extracts and tinctures, etc.. 3. A pure compound , e.g. morphine, atropine, digoxin, etc.. 4. A semithynthetic product, e.g. etoposide , teniposide , hyoscine butyl bromide etc.. 38
39 Uses of Natural products: As drugs for the treatment of a wide range of diseases, e.g. morphine, atropine, digoxin, hormones, antibiotics, etc .. As pharmaceutical aids in pharmaceutical industry e.g. suspending & emulsifying agents, suppository bases, binders, sweetening & colouring agents, etc..
Uses of Natural products: In cosmetics as flavouring & colouring agents, etc. In culture media for the propagation of micro-organisms in microbiology laboratories & biotechnology. General uses e.g. in food industries: as dusting powders, as indicators and in perfumery. 40
Definitions Pharmacognosy : It is the science of biogenic or nature-derived pharmaceuticals and poisons Crude drugs : It is used for those natural products such as plants or part of plants, extracts and exudates which are not pure compounds
Ethnobotany : It is a broad term referring to the study of plants by humans Ethnomedicine : It refers to the use of plants by humans as medicine Traditional medicine : It is the sum total of all non-mainstream medical practices, usually excluding so called “western” medicine
Natural products: they can be Entire organism (plant, animal, organism) Part of an organism (a leaf or flower of a plant, an isolated gland or other organ of an animal) An extract or an exudate of an organism Isolated pure compounds
Types of drugs derived from plants Herbal drugs, derived from specific parts of a medicinal plant Compounds isolated from nature Nutraceuticals, or “functional foods”
II. Value of natural products Compounds from natural sources play four significant roles in modern medicine: They provide a number of extremely useful drugs that are difficult, if not impossible, to produce commercially by synthetic means Natural sources also supply basic compounds that may be modified slightly to render them more effective or less toxic
3. Their utility as prototypes or models for synthetic drugs possessing physiologic activities similar to the originals
4. Some natural products contain compounds that demonstrate little or no activity themselves but which can be modified by chemical or biological methods to produce potent drugs not easily obtained by other methods Baccatin III Taxol
III. Production of natural drug products Collection (wild) Cultivation (commercial), collection, harvesting, drying, garbling, packaging, storage and preservation e.g. ginseng, ginkgo, peppermint Fermentation (Recombinant DNA technology or Genetically engineered drugs) Cell-culture techniques Microbial transformation Biologics (prepared from the blood of animals)
IV. The role of natural products in drug discovery Combinatorial chemistry High-throughput screening of natural products Combinatorial biosynthesis Ethnopharmacology
V. General principles of botany: morphology and systematics How to define a pharmaceutical plant-derived drug from the botanical point of view ? a botanical drug is a product that is either: Derived from a plant and transformed into a drug by drying certain plant parts, or sometimes the whole plant, or Obtained from a plant, but no longer retains the structure of the plant or its organs and contains a complex mixture of biogenic compounds (e.g. fatty and essential oils, gums, resins, balms)
isolated pure natural products are thus not “botanical drugs”, but rather chemically defined drugs derived from nature. the following plant organs are the most important, with the Latin name that is used, for example in international trade, in parentheses: Aerial parts or herb ( herba ) Leaf ( folia ) Flower ( flos ) Fruit ( fructus ) Bark ( cortex ) Root ( radix ) Rhizome ( rhizoma ) Bulb ( bulbus )
The large majority of botanical drugs in current use are derived from leaves or aerial parts. A plant-derived drug should be defined not only in terms of the species from which it is obtained but also the plant part that is used to produce the dried product. Thus, a drug is considered to be adulterated if the wrong plant parts are included (e.g. aerial parts instead of leaves )
Taxonomy It is the science of naming organisms and their correct integration into the existing system of nomenclature The names of species are given in binomial form: the first part of the name indicates the wider taxonomic group, the genus ; the second part of the name is the species .
Papaver somniferum L. Species : somniferum , here meaning ‘ sleep-producing’ Genus : Papaver (a group of species, in this case poppies, which are closely related) Family : Papaveraceae (a group of genera sharing certain traits) L.: indicates the botanist who provided the first scientific description of the species and who assigned the botanical name
Morphology of higher plants 1 . Flower It is the essential reproductive organ of a plant. For an inexperienced observer, two characteristics of a flower are particularly noteworthy: the size and the color Although the flowers are of great botanical importance, they are only a minor source of drugs used in phytotherapy or pharmacy e.g. chamomile , Matricaria recutita L. ( Asteraceae )
2. Fruit and seed The lower plants, such as algae, mosses and ferns, do not produce seeds Gymnosperm and Angiosperm Gymnosperm : they are characterized by seeds that are not covered by a secondary outer protective layer, but only by the testa – the seed’s outer layer Angiosperm : the seeds are covered with a specialized organ (the carpels) which in turn develop into the pericarp.
Drugs from the fruit thus have to be derived from an angiosperm species Fruits and seeds have yielded important phytotherapeutic products, including: Fruit Caraway, Carum carvi L. ( Umbelliferae ) Seed (white) mustard, Sinapis alba L. ( Brassicaceae )
3. Leaves The function of the leaves, as collectors of the sun’s energy and its assimilation, results in their typical general anatomy with a petiole (stem) and a lamina (blade) A key characteristic of a species is the way in which the leaves are arranged on the stem, they may be: Alternate Distichous Opposite Decussate Whorled
The form and size of leaves are essential characteristics e.g. oval, oblong, obovate, rounded, linear, lanceolate, elliptic, spatulate , cordate, hastate or tendril The margin of the leaf is another characteristic feature e.g. entire, serrate, dentate, sinuate, ciliate or spinose
Numerous drugs contain leaf material as the main component. e.g. Deadly nightshade, Atropa belladonna L. ( Solanaceae )
4. Bark The bark as an outer protective layer frequently accumulates biologically active substances e.g. Red cinchona, Cinchona succirubra L. ( Rubiaceae ) No stem-derived drug is currently of major importance
5. Rhizome and root drugs Underground organs of only a few species have yielded pharmaceutically important drugs e.g. Sarsaparilla , Smilax regelii ( Smilacaceae ) Korean ginseng, Panax ginseng ( Araliaceae ) 6. The bulbs and exudates Garlic, Allium sativum L. ( Liliaceae ) Aloe vera L. ( Asphodelaceae )