PHARMACOGNOSY AND PLANT CHEMISTRY

Lecture
Pharmacognosy is defined as the study of crude 5. Galen – described the
drugs obtained from plants, animals, & mineral method of preparing
and their constituent. It was derived from the formula containing plant
Greek word, “Gignosco” or “Gignoso” and animal drugs.

 Simultaneous application of various

scientific disciplines with the object
of acquiring knowledge of drug Pharmakon – Drug
from every point of view – Gignosco or Gignoso – to acquire knowledge
Fluckinger of Ayurveda (Ayur – life; Veda – study )
 An applied science that deals with Crr. Anotheus Seydler
the biologic, biochemical and Johann Adam Schmidt – failed to have copyright
economic features of natural drugs Susrata Samhita
and their constituents – Tyler
1. Pepper
1. C.A Seydler (1815) – coined the term 2. Ricinus
from pharmakon and gnosis in his 3. Castor Oil
doctoral thesis Analecta 4. Valerian
Pharmacognostica. 5. Lily
2. J. A Schmidt (1811) – first person to
coined the term or use the term on his De Materia Medica
book Lehrbuch der materia medica,
which described the study of medicinal 1. Belladona
plants and their properties. 2. Ergot
3. Aloe
HISTORY OF PHARMACOGNOSY 4. Hyoscyamus
5. Colchicum
Ancient Podophyllum, Rhubarb, 6. Opium
China Ginseng, Stramonium.
Cinnamon bark and Ephedra Galen
Ancient Ebers Papyrus – a collection of
Egypt 800 prescription and mentioning  Father of Pharmaceutical compounding
700 drugs.  Galenicals (most famous: Cold cream)
Ancient Ayurveda – refers to traditional
India medicine of ancient India. Solubility – important factor to consider in
Susrata Samhita - most important extraction
writing in Ayurveda
Ancient 1. Hippocrates – father of PHARMACY IN ANCIENT
Greece medicine and is famous BABYLONIANS
and for his oath now  Apothecary (drugstore)
Rome administered doctors.  2600 BC priest, physician and
2. Aristotle pharmacist (all on one)
3. Theoprastus
 GREEKS – HIPPOCRATES – “Father
4. Dioscorides – describe
600 medicinal plants in of Medicine” showed in writing and
his work, “De materia practices the fundamental of scientific
medica” of which some method of research.
mention plants are even
PHARMACY IN ANCIENT CHINA
used today.
  Shen Nung (2000 BC) – “Father of  Paracelsus – most important advocate of
Chinese Medicine” chemically prepared drugs from crude
o Pen Ts’ao Kang Mu 365 drugs plant and mineral substances
(herbs, barks and roots)  Doctrine signature – God had placed the
sign on healing substances indicating
PAPYRUS EBERS
their usage against disease
 EGYPTIAN MEDICINE (300 BC) –
George Ebers “Papyrus ebers” (1500 SCHEELE – GREATEST
BC) 800 prescriptions, 700 drugs PHYTOCHEMIST
 German Egyptologist and novelist,  Carl Wilhelm Scheele – Unicorn
discovered the Egyptian medical apothecary in Gothenburg
papyrus, of ca 1550 BCE  Discovered oxygen, chlorine, prussic
acid, tartaric acid, tungsten,
THEOPHRASTUS molybdenum, glycerin, nitroglycerin
 Father of Botany and other organic compounds.
 Dealing with medicinal qualities and  Isolated citric acid from lemon juice
peculiarities of herbs 
DIOSCORIDES – MATERIA MEDICA SERTURNER – FIRST OF THE
 Pedanios Dioscorides – recorded the ALKALOID CHEMISTS
observed promulgated excellent rules in  Friedrich Wilhelm Adam Serturner –
the collection of drugs, their storage and morphine (alkaloids)
use
LEHRBUCH DER MATERIA MEDICA
 Greek physician – pharmaco-botanist 78
A.D.  Written by Johann Adam Schmidt (1759
 Author of De Materia Medica – an – 1809)
organized pharmaceutical and medical ANALECTA PHARMACOGNOSTICA
knowledge that gives information
pertaining to about 600 drugs and their  Pharmacognosy appears again in 1815
usage. in a small work by Chr. Aenostheus
Seydler
CLADIUS GALEN – DRUG 
COMPOUNDER
PHARMACOGNOSY CAN BE DIVIDED
 Greek physician pharmacist
INTO:
 Introduced the principles of preparing
and compounding medicines from plants
and animals – Galenicals 1. Medical Ethnobotany – the study of the
 Originators – formula of cold cream traditional use of plants for medicinal
 Pharmaceutical preparation “Shotgun purposes
prescription” 2. Ethnopharmacology – the study of the
pharmacological qualities of traditional
medicinal substances
PARACELSUS – GREAT ALCHEMIST 3. Phytotherapy – the medicinal use of
 Aureolus Phillipus Theoprastus plant extracts
Bombastus von Hohenheim 4. Phytochemistry – the study of chemicals
derived from plants

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 2. Marc – undissolved
PHYTOCHEMISTRY portion of the
extraction process
 The study of composition of plant 3. Extractive - - product
principle, their extraction, biosynthesis of extraction
and identification (Solvent + Dissolved
substances)
DEFINITION OF TERMS
4. Extract – substance
Natural  Substances found in nature remain after
Substance that comprises the plants or separating or
animal parts or secretions. removing the
Synthetic  Substances that are menstruum from
substance synthesized in the laboratory extractives.
by either of the two methods:
 Total synthesis – complete Indigenous  Growing in their native
synthetic process plant countries or specific locality.
Naturalized  Grown in foreign land
Example: Total synthesis of plants other than their native homes
Camphor (Vinyl chloride + or in different locality.
Cyclopentadiene)
DRUG EXTRACTION PROCESS
 Semi-synthetic – not
 The general accepted method of
entirely a synthetic process
obtaining the plant principle/s
but a chemical modification
of a natural product SOLVENT/MENSTRUA (MENSTRUUM)
 A liquid/s that is employed in the
Example: Semi-synthesis of extraction process to remove/obtain
Camphor (modify a natural the plant principle/s
camphor from camphor tree)
Crude drugs  Vegetable or animal drugs GEOGRAPHIC SOURCE/HABITAT
that consist of natural  The region in which the plant or
substances that have animal yielding the drug grows
undergone only the process CULTIVATED PLANTS
of collection and drying.  These are medicinal plants that have
been propagated for many centuries
 Crude – used in relation to
natural products that has not
been in advanced in value or DECOCTION
improved in condition.  Is a process of boiling vegetable
Derivatives  Product of extraction substances with water to extract the
(extractives) process which contains the soluble principles
chief constituent of the drug. INFUSION
Extraction  A process of removing  Is a process in which vegetable
only those substances that drugs are extracted of their water-
can be dissolved in the liquid soluble constituents by steeping or
or liquid mixture referred to drenching them in water
as solvent (menstruum). DIGESTION
 Is a form of maceration in which
1. Menstruum – liquid gentle heat (40-60oC) is applied to
or solvent the drug menstruum mixture and

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 maintained throughout the positive cocci and bacilli and is used
extraction to increase the solvent
for mild to moderate, upper and
powers of the menstruum
lower respiratory tract infections.
Natural products Cephalosporins from
 They are chemical compound or Cephalosporium acremonium is an
substances produced by a living
organism that originate from nature antibacterial agents.
and have pharmacological and
biological activity.
 Natural products are produced as 2. Marine Natural Products
metabolites that are intermediates or  The first active compounds to be
end products in the pathways of
primary and secondary metabolism. isolated from marine species were
Natural Products may include the spongouridine and spongothymidine
whole organism (plant, organism)
part of an organism an extract or from Carribean sponge Cryptotheca
crude exudates of an organism crypta in 1950s. These compounds
isolated pure compound.
are nucleotides with potent
Natural products can be divided into broad anticancer and antiviral activities.
categories namely:
 Another example is an anti-tumor
(i) Microbial: e.g. Cephalosporins – compound called discodermolide
Cephalosporium acremonium.
(ii) Plants: e.g. Paclitaxel – Taxus brevifolia isolated from marine sponge
(iii) Marine: e.g. Discodermolide – Discodermia Discodermia dissoluta. It has similar
dissoluta
(iv) Animal: e.g. Epibatidine – African clawed activity as Paclitaxol® but with
frog. better water solubility. A
combination therapy of the two
drugs is effective in reduction of
1. Natural Products from Microbes
certain tumor growths.
 Exploitation of microbes as source
of drug candidates began in earnest
after the discovery of Penicillin
3. Natural Products from Animal Source
from the fungus, Penicillium
 venoms and toxins from snakes,
notatum. Potentially active
spiders, scorpions, and insects are
compounds or drugs have been
extremely potent because they often
discovered such as the macrolide
have very specific interactions with
erythromycin from
a macromolecular target in the body.
Saccharopolyspora erythraea is an
 Animals have yielded new natural
antibacterial drug that has broad
chemical entities. For example, a
spectrum activities against gram-

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 series of antibiotic peptides was  1820 quinine
extracted from the skin of the alkaloids
African clawed frog. Epibatidine cinchona
obtained from the skin of an officinalis
Ecuadorian poison frog is ten times 21first century
more potent than morphine.  ACTM
Teprotide (pry-trp-pro-arg-glu-ile- Artemisia
pro-pro), extracted from Brazilian annua
viper, has led to the development of Natural products of plant origin used for
cilazapril and captopril, which are medicinal purposes are also called herbal
effective against hypertension. Cod- medicines.
liver oil from fresh liver of Gadus Herbal medicine is defined as, use of
morhua used as oil, or source of herbs, herbal materials, herbal preparations and
vitamins, honey from Apis mellifera finished herbal products to treat and manage
used respiratory problems. diseases. Herbal medicine has been employed by
man for centuries as a remedy for various
4. Plant Natural Products diseases and is thought to be due to the history
th
During the 19 century a range of drugs was of qualified success, reasonable science, its
isolated: affordability, its accessibility and long-standing
 1805 morphine- cultural and spiritual values.
class of drugs
called opiods
(poppy plants
Papaver
somniferum)
 1817 emetine- Example of herbal plant with medicinal
alkaloid use include;
(Psychotria 1. Thymus serphyllum is
ipecacuanha) commonly used locally for
 1819 strychnine various purposes such as
alkaloid antiseptic, anti-helminthic,
(Strychnos nux- carminative (flatulence relieve)
vomica Linn) and expectorant.
pesticide

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 2. Crossopteryx febrifuga Benth
(family Rubiaceae) preparations
have been used traditionally for Uses of natural products
treating septic wounds, 1. Sold as health foods and food
respiratory infections, fever, supplements
dysentery, pain and malaria.  Example are:
3. Morphine, from opium poppy  Stevia derived from Stevia
(Papaver somniferum), used as rebaudiana is 30 times sweeter than
an analgesic. sugar. Since the active ingredient
4. Digoxin and other digitalis possesses zero calories, this plant
glycosides, from foxglove may be useful for people with
(Digitalis spp.), used to treat diabetes, hypoglycemia.
heartfailure.  Xylitol is also used as a diabetic
5. Taxol, from the Pacific yew sweetener and is seen as beneficial
(Taxus brevifolia), for dental health by reducing caries
6. vincristine (Catharanthus to a third in regular use.
rosea) used as an anticancer  Green, black, and white teas are all
treatment and derived from Camellia sinensis, an
7. quinine, from Cinchona bark evergreen shrub of the Theaceae
(Cinchona spp.),used in the family.
treatment of malaria. 2. Spices are used for flavoring and for
preserving foods, particularly meat
Traditional system of medicine can be products. They also possess
classified into three: antimicrobial properties.
 Common spices include:
1. Traditional scholarly medical systems: have  Cinnamon
documented knowledge, pharmacopoeias for  Pepper
doctors and institutions for training doctors  cloves
2. Traditional medical knowledge (Folk  nutmeg
medicine): orally transmitted and associated  cumin
with households, communities and ethnic  ginger
groups.
3. Shamanistic medicine: have strong spiritual 3. Pharmaceutical medicine: Natural
element and is applied by special practitioners. products and their derivatives are an

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 invaluable source not only of lead Natural products from both plants and
compounds( a chemical compound that animals are used as fibers, chemicals,
shows promise as a treatment for a insecticides, fibers and dyes.
diseases and may lead to the
development of new drug) for Why pharmacognosy ?
pharmaceutical development but also o For the purposes of drug discovery and
therapeutic agents themselves. understanding how dietary supplements
 Example: morphine from opium work.
poppies (Papaver somniferum) still o The development and use of analytical
provides an important source of opiate methods for quality control of natural
analgesics and a starting material products in the market place.
forcodeine synthesis. o The study of the use of traditional
remedies by native cultures.
4. Cosmetic preparation; there is high o The microscopic evaluation and species
demand in use of natural products as verification of medicinal or
ingredients in cosmetics or use of economically important natural
natural cosmetics example Aloe vera, products.
roses( rose oil are rich in vitamin C), o The use of natural products for specific
lavender, jojoba, chamoline, tea tree, agricultural purposes, such as natural
egg oil, avocado, coconut oil, emu oil, pesticides or insect antifeedants.
honey, beeswax, rose mary and basil. o Assessing safety and functional
5. Production of biofuels as alternative and properties of compounds found in novel
renewable energy sources e. g biodiesel foods or food ingredients and consumer
derived from vegetable oil (castor oil, products.
jatropa, palm oil, peanut, soyabean and o The cosmetic application of natural
cotton) and animal fats (bovine fat and compounds or extracts.
swine fat). o The study and manipulation of genetic
biosynthetic pathways for the purpose of
6. Source of income: trade in medicinal
enhancing the production of natural
plants is a huge. Roughly half of all
compounds, or producing novel
approved prescription drugs are natural
compounds.
products, mostly from plants and
microbial sources, their semi-synthetic SCOPE OF PHARMACOGNOSY
derivatives or fully synthetic analogs.
1. Medicine
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 2. Bulk Drugs  Simpliest method; arranged in
3. Food Supplement alphabetical order; employed in
4. Pharmaceutical necessities dictionaries, pharmacopoeias,
5. Pesticides monographs and reference books; uses
6. Tissue culture biotechnology 7. Latin, English and Vernacular/Local;
Engineering Easy and quick to use.
 No repetition of entries
“Simultaneous application of various disciplines   Avoid confusion
with the object of acquiring knowledge of drugs   Location and tracing is easy
from every point of view.” – Friedrich August
Fluckiger  No relationship/correlation among
plants.


CLASSIFICATION OF CRUDE DRUGS TAXONOMIC

ORGANIZED DRUGS  Arranged by Kingdoms; based on

phylogeny (Natural relationship of
 Consist of cellular organization in the plants among other organism)
form of anatomical features and consist  Helpful for studying evolutionary
mostly of crude drugs from plant development
sources.  No relationship/correlation among
 Mostly from plant sources plants*
 Example are:  Crude drugs are grouped based on the
o Cinchona bark natural relationship or phylogeny
o Sandal wood, Quassia wood
o Senna leaves, Digitalis leaves  Umbellifereae Family –
o Rauvolfia roots, etc includes cremocard fruits (anise,
fennel, caraway)
UNORGANIZED DRUGS
 Solanaceae Family – includes
 do not have morphological or plants yielding capsule/berry-
anatomical organization as such and like fruits(belladonna,
comes directly in the market but their hyocyamus, stramonium)
ultimate source remains, plant, animals
or minerals.  Labiateae Family – include
 Plant, mineral and animal sources - drugs possessing square stems,
Examples are: opposite leaves (peppermint,
 Beeswax from Honeycomb of spearmint, thyme)
bees
 spermacetti from head cavities MORPHOLOGICAL
of whale
 Plant Exudates such as Gums  Crude drugs are grouped according to
(Xanthan Gum, tragacanth) the part of the plant or animal
 Plant latex ( opium)
represented; such as roots, leaves,
organs, glands

 Arranged by morphology or external

ALPHABETICAL
characteristics of plants; answers the

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 question “Which part of the plant was
used?” Labiatae Lamiaceae
 Helpful in identifying and detecting
adulteration Compositae Asteraceae
 Convenient for practical study especially
if the chemical structure isn’t Guttiferae Clusiaceae
understood
 No correlation of chemical constituent
with therapeutic action CHEMICAL/BIOGENETIC
 Repetition of plants
 Depends upon the most important
PHARMACOLOGICAL/THERAPEUTIC constituent arranged by carbohydrates,
proteins, tannins, saponins etc
 According to  Popular for phytochemical students
pharmacological/therapeutic effect; most  Ambiguous arise when particular drugs
relevant classification and follow possess a lot of constituents ( must
method choose the most abundant one as main
 Used for suggesting substitute if drug classification)
isn’t available
 Plants with different actions are
classified separately in multiple groups
 Example: Cinchona bark both have PREPARATION OF CRUDE DRUGS FOR
antimalarial and antiarrhythmic effect COMMERCIAL MARKET
 Crude drugs are grouped based on the
similarity of therapeutic effects, 1. COLLECTION
regardless of morphology, taxonomy or
chemical relation. Examples are:  Most important step next to Cultivation
 Cascara sagrada, Senna,  Always ensures a true natural sources &
Podophyllum, Castor oil – affect reliable product.
the intestinal tract  Drugs should be collected when they
 Digitalis, Strophantus, Squill – contain maximum amount of
constituents in highly scientific manner.
affect the cardiac muscle
 The most advantageous time for
collection is the time when
PLANT NOMENCLATURE AND  The part of the plant constitutes
TAXONOMY the drug is highest in its content
of active content of active
principles
OLD FAMILY NEW FAMILY
NAME NAME  When the plant material will dry
to give the maximum quantity
Graminae Poaceae and appearance
Factors that affects the amount of Constituent
Palmae Arecaceae
present:
Cruciferae Brassicaceae 1. Season
 Example: Rhubarbs – Best harvested during
Leguminosae Fabaceae summer because during winter, it doesn’t
contain anthraquinine(active form; cathartic)
Umbilliferae Apiaceae instead, it contains anthranol (inactive form)

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 2. Age of plant – amount and proportion of   Benefits:
constituent are affected 1. a) Inhibits partially enzymatic
 Example: Young peppermint has reactions
pulegone while matured peppermint has 2. b) Facilitates pulverizing or
menthol and menthone grinding of crude drugs.
3. Time (Day/Night)   Types of Drying
 Example: Contained secondary metabolites 1. Natural Drying (Sun Drying)
vary from day and night due to the plant’s 2. Direct Sun Drying – Contents
transpiration and expiration. Plants release more are stable to high temperature
water during the day and release less amount of and sunlight.
water during the night 3. Shed – Preferred if natural color
 In general: Leaves are best harvested before and volatile principles of drugs
flowering season or when the photosynthesis is are to be retained
active or as the flowers are beginning to open or 4. Artificial Drying
when fully expanded. Flowers before it 5. Tray dryers – Suitable for drugs
blooms/pollination process or before they are which do not contain volatile
fully expanded. Underground plants ( rhizomes) oils and are quite stable to heat
when its aerial part dies( after the vegetation or which needs deactivation of
process have ceased) such as carrots, onions and enzymes are dried in this
gingers. Roots after the vegetation process has method. Examples: Belladonna
begun roots, Cinchona bark, Tea and
 Some fruits are collected after full maturity Raspberry leaves, Gums
or right after ripening . Seeds when mature ad 6. Vacuum dryers – Suitable for
fully ripened fruits. drugs which are sensitive to
 Most barks are collected at spring season higher temperature. Examples:
 Most ideal time in collection of Active Tannic acid and Digitalis leaves
constituents is when the desired constituent is at 7. Spray dryers – Suitable for
its highest or the time that could give its highly sensitive drugs to
maximum quality. atmospheric conditions and also
to temperature of vacuum
drying. Examples: Papaya latex,
2. HARVESTING Pectin and tannins
 Its purpose are
 Important operation in cultivation
technology and the important point in 1. Removal of sufficient moisture,
this process is the type of drug to be to ensure good keeping qualities
harvested 2. To prevent mold growth,
 The mode of harvesting varies with each enzymatic action; bacterial
drug produced and with the action, chemical or other
pharmaceutic requirements of each drug possible changes
 Manual vs Mechanical labor 3. “Fixes” the constituents
 By hand labor – requires 4. Facilitates grinding and milling
“skillful” selection of plant parts 5. Converts the drug into a more
 With the use of mechanical convenient form for commercial
devices handling
3. DRYING

 Consist of removal of sufficient

moisture content of crude drugs, so as to 4. CURING
improve its quality and make it resistant
to the growth of microorganisms.

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  special drying process that enhances the celsius or drying the
properties of the plants active drug thoroughly
ingredients  Fumigation of large lots
 Examples: of crude drugs with
1. a) Vanilla via Sweating Process methyl bromide, carbon
2. b) Cascara Sagrada (Cathartic) disulfide, hydrocyanic
via maceration with Magnesium
acid
Oxide for 1 year to reduce its
 Addition of few drops
active components into its
reduced forms since it’s less of CHCL3 , and CCl4
irritating  For storage, the ideal temperature is just
above freezing. The warehouse or other
5. GARBLING ( Final step in preparation) place of storage should be as cool as
possible (2-8 Celsius)
 Consist of removal of foreign organic
matter (extraneous matter) such as other EVALUATION OF CRUDE DRUGS
plant parts, dirt, and added adulterants.
 Why remove adulterans? To provide  ensures the identity of a drug and
quality . determines the quality and purity of
 This step is carried: drugs.
 After the drug has been dried
 Before the drug is labeled or 1. Organoleptic Evaluation
packaged  refers to the method of analysis like color,
odor, taste, size, shape, and special features  A
6. PACKAGING, STORAGE AND study that uses organs or senses
PREPARATION
2. Microscopic Evaluation
 PACKAGING of drugs depends on their  Identification of small fragments of crude or
final deposition. It is customary to powdered herbs and detection of adulterants, as
choose the type of packaging that well as identification of plant by characteristics
provides ample protection to the drugs tissue features
and gives economy of space.
 PROPER STORAGE AND 3. Chemical Evaluation
PRESERVATION are of important  includes qualitative and quantitative chemical
factors in maintaining a high degree of tests, chemical assays, and instrumental analysis
quality of the drugs.  Titration is applied
 All drugs should be preserved in a well-  Qualitative: Identification tests for various
closed and filled containers, stored in phytochemicals present
the premises which are water-proof, fire-  Quantitative: Acid value,saponification,ester
proof, and rodent proof. Drugs must also value
be protected from insects and molds
attacks. 4. Physical Evaluation
 Factors to be considered:  often used to determine the physical property
o For destruction/prevention of of the crude drugs
insect-contamination: insect 
attacks prevention Solubility,Specificgravity,Opticalrotation,viscosi
 Exposure of the drug to ty,refractiveindex,MPandwatercontent 5.
a temperature of 65 Biological Evaluation

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 plant or extract can be evaluated by various
biological methods to determine
pharmacological activity, potency, and toxicity. BIOASSAY
 Uses in vivo(using animals)and vitro(using Glucagon Cat
membranes)studies Atropine Cat
Oxytocin Chicken
Parathyroid hormone Dog
ASSAY ON LIVING ANIMALS Insulin Rabbit
 Bacteria such as Salmonella typhosa Tubocurarine Rabbit
and Micrococcos pyrogenes, are a Digoxin Pigeon
means of determining the phenol
coefficient or antiseptic value of
certain drugs
 Rats or Mice
o Rat – line test is employed
for the assay of vitamin D
preparation, etc.
o Mice – test animal in the
safety test for Rabies
vaccine
 Guinea pigs
o They are used to test the
toxicity and antigenicity of
biological products such as
Diphteria toxin and Tetanus
toxoid.
o They are also employed to
determine oxytoxic activity
of Vasopressin injection and
similar compounds
 Pigeons – utilized in the assay of
Digitalis
 Cats – used in drugs with depressor
activity, assay of Glucagon for
injection, mydriatic drugs such as
atropine
 Rabbits – used in determining the
presence of pyrogens in parenteral
solution of the antibiotic, and testing
of ophthalmic preparations
 Dogs – are utilized in assaying
Veratrum viride preparation
HUMANS
 Valuable as a means of noting the
activity of drugs

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