December 2016 Introduction to Pharmacognosy Pharmacognosy I Third Lecture 1 Introduction ID: 734688
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Mohammed N. Sabir December 2016
Introduction to Pharmacognosy
Pharmacognosy I – Third Lecture 1- IntroductionSlide2
11-Dec-162Some terms and abbreviations used during your study in pharmacognosy…- Natural Products (NPs) - Phytochemistry- Primary Metabolites - Secondary Metabolites- Biotechnology - Building blocks- Crude drugs - Quality Control (QC)
Pharmacognosy I – Third
Lecture 1- IntroductionSlide3
11-Dec-163Aims of the course- Descriptive study of selected medicinal plants
- Highlight the role of Natural Products (NPs) in
medicine
- The biosynthetic pathways of NPs
Pharmacognosy I – Third
Lecture 1- IntroductionSlide4
11-Dec-164 Pharmacognosy I – Third Lecture 1- Introduction
Aims of the course
- Studying Crude drugs
- Methods for isolation of NPs from crude materials
(physicochemical investigation)Slide5
11-Dec-165Course objectives
Understand crude drugs, its classification and factors affect its storage and quality control.
A good understanding of the extraction, separation and isolation of natural products including chromatographic methods
.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide6
11-Dec-166Course objectives
Understand secondary metabolic
pathways and its necessity in the production of their metabolites.
Know the mechanisms underlying the biochemical reactions that take place in secondary metabolism.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide7
11-Dec-167Be able to categorize and recognize the classes of natural products.Have enough information on the medicinal uses, mechanism of action, toxicities and the chemistry of the studied topics.
Course objectives
Pharmacognosy I – Third
Lecture 1- IntroductionSlide8
Course contents- Introduction- Value of NPs- Physicochemical investigation for NPs
- Secondary
metabolism- General biosynthetic pathways for secondary
metabolism
11-Dec-16
8
Pharmacognosy I – Third
Lecture 1- IntroductionSlide9
Course contents- Drug discovery- Glycosides
- Terpenoids
- Steroids and steroid biosynthesis inhibitors-
Polyphenolics (tannins, flavonoids and lignans
)
- Coumarins and chromones
11-Dec-16
9
Pharmacognosy I – Third
Lecture 1- IntroductionSlide10
11-Dec-1610Reading List and References
Key references
Useful referencesJournals and reviews (internet)
1. James
E. Robbers,
Marilyn
K.
Speedie
, Varro E. Tyler, (1996). Pharmacognosy and
Pharmacobiotechnology
. First edition, Williams and Wilkins a Waverly company.
1.
Dewick
P. M., (1998). Medicinal Natural Products a Biosynthetic Approach. First edition, Springer, India.
1. Botanical
Medicine in Clinical Practice. A collection of newly approved literatures. (2008). Edited by Ronald R. Watson, Victor R.
Preedy
. Arizona Cancer
Centre,
University of Arizona, USA. Department of Nutrition and Diabetics, king's College London, UK.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide11
11-Dec-1611Key references
2. Trease
and EvansW
. Charles, Pharmacognosy,
(
2002).
Fifteenth
edition
.
W.B.
Saunders
Edinburgh
London
,
New
York,
Philadelphia
,
St
Louis
,
Sydney,
Toronto
.
Useful references
2.
Bhat
S.V.,
Nagasampagi
B. A., and
Sivakumar
M., (2007). Chemistry of Natural Products. First edition. Springer,
Narosa
. India.
Journals and reviews (internet)
2.
Otto
Sticher
. (2008). Natural product isolation. Natural Product Reports,
Pharmacognosy I – Third
Lecture 1- IntroductionSlide12
11-Dec-16123. Saxena P.B. (2007). Chemistry of Alkaloids. First edition. Discovery Publishing House.
3. Cannell
J. P. Richard, (1998). Natural Products Isolation. First edition, Glaxo
Wellcome Research & Development, Stevenage, Herts, UK. Humana Press, Totowa New Jersey.
Robert K. Murray, Daryl K.
Granner
, Peter A. Mayes, Victor W.
Rodwell
. (2003). Harper's Illustrated Biochemistry. Twenty sixth edition.
Mc
Graw
Hill.
4.
Eberhard
Teuscher
, (2006). Medicinal Spices, A Handbook of Culinary Herbs, Spices, Spice Mixtures. First edition.
Medpharm
Scientific publishers
Stuttgart.
5.
Joule
J. A., and Mills K. (2002). Heterocyclic Chemistry. Fourth edition. Blackwell Science.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide13
11-Dec-16135. Chevallei A. (2005). Alternative Medicine, Treatment by Herbal Products and Medicinal Plants. First edition. International Academia.
6.
Chaudhuri Debabrata,
Kar D. Kumar, and Halder
Soma. (2008). A Handbook of Plant Biosynthetic Pathways. First edition. NCBA.
7. James
R. Hanson, Natural Products. (2003) . The secondary Metabolites. The Royal Society of Chemistry, Cambridge, UK
Pharmacognosy I – Third
Lecture 1- IntroductionSlide14
11-Dec-16146. Bertram G. Katzung, Anthony J. Trevor, Susan B. Masters. Basic and Clinical pharmacology (2009), by 11
th edition, McGraw-Hill
8. Pretsch
E., Buhlmann P., and
Affolter C. (2000). Structure determination of organic compounds. First edition. Springer.
9.
Satyajit
D.
Sarker
,
Zahid
Latif
, and Alexander I.
Gray
(2006), Natural Products Isolation, SECOND EDITION, Humana Press, Totowa New Jersey
10. Allen
M.
Schoffstall
, Barbara A. Gaddis, and Melvin L.
Druelinger
. (2004).
Microscale
and
Miniscale
Organic Chemistry Laboratory Experiments. 2
nd
Edition. McGraw Hill, New York
Pharmacognosy I – Third
Lecture 1- IntroductionSlide15
Further readings…11-Dec-1615
Pharmacognosy I – Third
Lecture 1- IntroductionSlide16
11-Dec-1616Further readings…
Pharmacognosy I – Third
Lecture 1- IntroductionSlide17
11-Dec-1617
Further readings…
Pharmacognosy I – Third
Lecture 1- IntroductionSlide18
11-Dec-1618
Further readings…
Pharmacognosy I – Third
Lecture 1- IntroductionSlide19
11-Dec-1619 Pharmacognosy I – Third Lecture 1- IntroductionSlide20
11-Dec-1620Course overview
The course provides the fundamental
information on pharmacognosy as a leading subject to understand drug-derived from natural sources including important biologically active medicines like:-
terpenoids, glycosides, volatile
oils, tannins, steroids,
flavonoids
, and
coumarins.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide21
11-Dec-1621The course also studies the origin of these natural products, the processes used for their extraction, separation, isolation and characterization as well as the biosynthetic routes that lead for the formation of these natural products.
Pharmacognosy I – Third Lecture 1- IntroductionSlide22
11-Dec-1622The biologic activities of these agents are discussed including their mechanism of action, clinical uses, toxicities, and the active constituents that are responsible for the biologic action. Pharmacognosy I – Third Lecture 1- IntroductionSlide23
11-Dec-1623Structural modifications to produce semisynthetic products are also discussed if any. Pharmacognosy I – Third Lecture 1- IntroductionSlide24
11-Dec-1624Lecture overviewDefinition
Historical Aspects
Disciplines to understand pharmacognosyDevelopment of medicinal chemistry
Value of natural products
Pharmacognosy I – Third
Lecture 1- IntroductionSlide25
11-Dec-1625Lecture overviewExamples
Crude drug and classification systems
Physicochemical investigation of natural productsSummary &
conclusion
Pharmacognosy I – Third
Lecture 1- IntroductionSlide26
11-Dec-1626Introduction to Pharmacognosy…
Pharmacognosy
studies all aspects of medications (drugs) derived form natural sources including (
Plants, Micro Organisms, Marine products, Insects and Animals). Pharmacognosy I – Third
Lecture 1- IntroductionSlide27
11-Dec-1627Introduction to Pharmacognosy…
It also concerns the biochemical pathways
that are involved in the biosynthesis of these drugs
(drug discovery). Pharmacognosy I – Third
Lecture 1- IntroductionSlide28
11-Dec-1628Introduction to Pharmacognosy…
and the techniques involved for their
isolation from the crude materials (Isolation)
Pharmacognosy I – Third Lecture 1- IntroductionSlide29
11-Dec-1629Introduction to Pharmacognosy…
The chemical modification to approach more effective and less toxic
product and their pharmacological properties (drug design). Pharmacognosy I – Third
Lecture 1- IntroductionSlide30
11-Dec-1630Introduction to Pharmacognosy…
All the physical and chemical characterizations of these agents as well (Identification).
Pharmacognosy I – Third Lecture 1- IntroductionSlide31
11-Dec-1631 Pharmacognosy I – Third Lecture 1- Introduction
Introduction to
Pharmacognosy…
So…
In addition to studying drugs derived from NPs,Slide32
11-Dec-1632 Pharmacognosy I – Third Lecture 1- Introduction
Introduction to
Pharmacognosy…
It is a drug discovery involving; isolation, drug design and identification techniques.Slide33
11-Dec-1633Biotechnology [recombinant DNA technology (rDNA
)], has opened new perspectives in pharmacognosy…
Pharmacognosy I – Third Lecture 1- IntroductionSlide34
11-Dec-1634This is achieved through production of chemical entities or drugs by tissue cultures via genetic engineering (this needs a good understanding of enzymology).
Pharmacognosy I – Third
Lecture 1- IntroductionSlide35
11-Dec-1635Biotechnology is applied to:- 1- Increase the yield of the drugAs in
Taxol (an anticancer agent).
Pharmacognosy I – Third
Lecture 1- IntroductionSlide36
11-Dec-16362- Modification on the secondary metabolite through genetic engineering to obtain less toxic and more effective drug as well as enhance drug delivery (ex: Antibiotics, antivirals and anticancers). Pharmacognosy I – Third Lecture 1- IntroductionSlide37
11-Dec-16373- It also provide methods for production of many drugs that cannot be synthesized by chemical synthesis:- Pharmacognosy I – Third Lecture 1- IntroductionSlide38
11-Dec-1638Insulin form E. coli.Tissue plasminogen activator [t-PA] from melanoma cell lines.
Human serum albumin (HSA) from
E. coli. Pharmacognosy I – Third
Lecture 1- IntroductionSlide39
11-Dec-1639- Development of vaccines:
Separation of a pure antigen
using a specific
monoclonal antibody
.
b) Synthesis of an antigen with the help of a
cloned
gene
.
c) Synthesis of
peptides
to be used as vaccines.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide40
11-Dec-1640Biotechnology and drug discovery… Pharmacognosy I – Third Lecture 1- IntroductionSlide41
11-Dec-1641Cell and tissue culture can be obtained from many plant species, M.Os., animals or human.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide42
11-Dec-1642In such In vitro culture, each cell has all the genes necessary for all the functions of a living organism, including secondary metabolism.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide43
11-Dec-1643
Pharmacognosy I – Third
Lecture 1- IntroductionSlide44
11-Dec-1644 Pharmacognosy I – Third Lecture 1- IntroductionSlide45
11-Dec-1645
KS: ketosynthase
MAT: malonyl-acetyl transferase
DH: dehydratase KR: ketoreductase
ACP: acyl carrier protein
The biosynthetic pathway for the fungal
polyketide
6-methylsalicylic acid (6-MSA)
. 6-MSA is assembled from four
ketide
units (one acetate and three
malonates
).
Extension
, carrying out different levels of reductive processing at each stage.
(
Staunton and Weismann,
Nat. Prod. Rep
., 2001, 18, 380–416
)
Pharmacognosy I – Third
Lecture 1- IntroductionSlide46
11-Dec-1646
KS
:
ketoacyl
synthase
AT
: acyl
transferase
DH
:
dehydratase
ER
:
enoyl
reductase
ACP
: acyl carrying protein
Pharmacognosy I – Third
Lecture 1- IntroductionSlide47
Historical aspects -Papyrus
Ebersc (1600 B.C.)
11-Dec-16
47
Pharmacognosy I – Third
Lecture 1- IntroductionSlide48
-Greek pharmaco-botanist in the first century A.D. (Pedanios Dioscorides) and “
materia medica
”
11-Dec-16
48
Pharmacognosy I – Third
Lecture 1- IntroductionSlide49
Li Shih Chen and published in 1596 A.D., listed more than 2000 drugs of natural origin. About 5000 native medicinal herbs are used in China today
11-Dec-16
49
Pharmacognosy I – Third Lecture 1- IntroductionSlide50
11-Dec-1650A collection of hymns predating 1000 B.C., included more than 1000 healing herbs, many of which continue to be used in Ayurvedic medicine (Hindu traditional medicine).
Pharmacognosy I – Third
Lecture 1- IntroductionSlide51
The Unani (Islamic Medicine) has contribution in this field by (Avicenna 890-1037 A.D.), he collected his knowledge about medicinal plants in the
Kitab-Al-Shifa’a
.
11-Dec-16
51
Pharmacognosy I – Third
Lecture 1- IntroductionSlide52
The word Pharmacognosy formed from two Greek words pharmakon (drug) and gnosis (knowledge), this title was introduced by C.A. Seydler, a German medical student, who used
Analytica
pharmacognostica for his dissertation in 1815.11-Dec-1652
Pharmacognosy I – Third
Lecture 1- IntroductionSlide53
However, recent historical research has found an earlier usage of “Pharmacognosis”. J.A. Schmidt used that title in his Lehrbuch der Materia
medica, published in Vienna in 1811, to describe the study of medicinal plants and their properties.
11-Dec-1653
Pharmacognosy I – Third Lecture 1- IntroductionSlide54
A complete understanding of medicinal plants involves a number of disciplines including:-Commerce.Botany.
Horticulture.
Chemistry.
Enzymology.Genetics.
Quality control.
Pharmacology.
11-Dec-16
54
Pharmacognosy I – Third
Lecture 1- IntroductionSlide55
The use of modern isolation techniques and pharmacological testing procedures means that new plant drugs usually fined their way into medicine as purified substances rather than in the form of galenical preparations.11-Dec-16
55 Pharmacognosy I – Third
Lecture 1- IntroductionSlide56
Advances in synthetic chemistry and production of drugs with more complicated chemical structure has opened a new field which is known as Pharmaceutical and Medicinal Chemistry11-Dec-1656 Pharmacognosy I – Third
Lecture 1- IntroductionSlide57
Pharmacology; studying drug actions and effects.Medicinal Chemistry; the studying the chemical aspects of drugs, their design, synthesis and mechanism of actions on molecular level.Pharmacognosy
; dealing with medicines derived from natural sources.
11-Dec-1657
Pharmacognosy I – Third
Lecture 1- IntroductionSlide58
11-Dec-1658
Pharmacognosy I – Third
Lecture 1- IntroductionSlide59
Value of natural drugs productsRole of compounds that are derived from natural sources could be summarized as follows
:-11-Dec-16
59 Pharmacognosy I – Third
Lecture 1- IntroductionSlide60
11-Dec-1660Value of natural drugs products
They provide a number of extremely useful drugs that are difficult, if not impossible, to be produced commercially by synthetic means, like:
Pharmacognosy I – Third Lecture 1- IntroductionSlide61
11-Dec-1661alkaloids of opium poppy, ergot, and Solanaceous plants; the
cardiotonic glycosides of digitalis; most of the antibiotics; and all of the serums, vaccines, and related products.
Pharmacognosy I – Third Lecture 1- IntroductionSlide62
Natural sources also supply basic compounds (templates) that may be modified slightly to render them more effective or less toxic.11-Dec-16
62
Pharmacognosy I – Third Lecture 1- IntroductionSlide63
11-Dec-1663Examples:-The modification of morphine molecule to codeine, and modification of podophyllotoxin to
teniposide.
Pharmacognosy I – Third Lecture 1- IntroductionSlide64
The utility of natural products as (prototypes) or models for synthetic drugs possessing physiologic activities similar to the originals,11-Dec-16
64
Pharmacognosy I – Third Lecture 1- IntroductionSlide65
11-Dec-1665Examples:--Procaine and similar local anesthetics.
-Dicoumarol
and other oral anticoagulant (warfarin). Pharmacognosy I – Third
Lecture 1- IntroductionSlide66
As (precursors) of significant drugs; some natural products contain compounds that demonstrate little or no activity themselves but upon modification by chemical or biological means; they will be converted to
potent drugs…11-Dec-16
66 Pharmacognosy I – Third
Lecture 1- IntroductionSlide67
11-Dec-1667But these agents are not easily obtained by other methods like: Pharmacognosy I – Third
Lecture 1- IntroductionSlide68
11-Dec-1668Taxol which may be synthesized from bactin
III, which occur in the leaves of Pacific Yew.
Whereas taxol it self is found only in the bark of scarce Pacific
Yew.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide69
11-Dec-1669Bactin IIITaxol
Pharmacognosy I – Third
Lecture 1- IntroductionSlide70
(Fig. 1)
Below
are examples of some drugs that are derived from natural sources, their semisynthetic and their
prototypes
11-Dec-16
70
Pharmacognosy I – Third
Lecture 1- IntroductionSlide71
11-Dec-1671Crude drugsAre NPs that has not been advanced in value or improved in condition by any process or treatment beyond that which is essential for its proper packing and prevention from deterioration. Pharmacognosy I – Third
Lecture 1- IntroductionSlide72
11-Dec-1672Classification of crude drugs1. Alphabetical classification; Pharmacognosy I – Third
Lecture 1- IntroductionSlide73
Merits: • It is easy and quick to use • There is no repetition of entries and is devoid of confusion. • In this system location, tracing and addition of drug entries is easy.
Alphabetical classification
11-Dec-1673 Pharmacognosy I – Third
Lecture 1- IntroductionSlide74
11-Dec-1674Demerits:There is no relationship between previous and successive drug entries.
Examples: Acacia, Benzoin, Cinchona, Dill, Ergot, Fennel, Gentian, Hyoscyamus
, Ipecacuanha, Jalap, Kurchi,
Liquorice, Mints, Nuxvomica, Opium,
Podophyllum,
Quassia
,
Rauwolfia
,
Senna
,
Vasaka
, Wool fat, Yellow bees wax,
Zeodary
.
Alphabetical classification
Pharmacognosy I – Third
Lecture 1- IntroductionSlide75
11-Dec-1675Classification of crude drugs2. Morphological classification; - Organized (Solid) Wood, leaves, bark…etc.
- Non-organized (Liquid) Waxes, gums, resins, etc.
Pharmacognosy I – Third Lecture 1- IntroductionSlide76
Unorganized Drugs. Dried latex– Opium, Papain Dried Juice– Aloe, Kino Dried extracts– Agar, Alginate, Black catechu, Pale catechu,
Pectin, Waxes - Beeswax, Spermaceti, Carnauba wax
Gums – Acacia, Guar Gum, Indian Gum, Sterculia, Tragacenth. Resins– Asafoetida, Benzoin, Colophony, copaiba Guaiacum, Guggul
, Mastic, Coal tar, Tar, Tolu balsam,
Storax, Sandarac.
11-Dec-16
76
Pharmacognosy I – Third
Lecture 1- IntroductionSlide77
11-Dec-1677Unorganized Drugs. Volatile oil– Turpentine, Anise, Coriander, Peppermint, Rosemary, Sandalwood, Cinnamon, Lemon, Caraway, Dill, Clove, Eucalyptus, Nutmeg, Camphor.
Fixed oils and Fats– Arachis, Castor,
Chalmoogra, Coconut, Cotton seed, Linseed, Olive, Sesame, Almond, Theobroma, Cod-liver, Halibut liver, Kokum butter.
Animal Products – Bees wax, Cantharides, Cod-liver oil, Gelatin, Halibut liver oil, Honey, Shark liver oil, shellac, Spermaceti wax, wool fat, musk, Lactose. Fossil organism and Minerals– Bentonite
, Kaolin, Kiesslguhr
, Talc.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide78
11-Dec-1678Classification of crude drugs3. Taxonomic classification; - More advanced
Pharmacognosy I – Third Lecture 1- IntroductionSlide79
Taxonomic classificationPlant Kingdom Thallophyta Pteridophyta Gymnosperm Angiosperm
Phyllum
Order Family Drugs
11-Dec-1679
Pharmacognosy I – Third
Lecture 1- IntroductionSlide80
11-Dec-1680Classification of crude drugs4. Pharmacological classification; - Advanced, depends on biological actions of the
plant.
Pharmacognosy I – Third Lecture 1- IntroductionSlide81
Pharmacological Classification Anticancer Anti-inflammatory Antiamoebic
Antiasthmatic Anthelminthic
Antispasmodic Astringent Analgesic Bitter tonic
Carminatives Purgatives Expectorant
Cardiotonic
Tranquilizers
Vinca
,
Podophyllum
,
Taxus
Colchicum, Turmeric
Ipecac root,
Kurchi
bark
Ephedra, Lobelia
Male fern,
Quassia
wood
Datura
,
Hyoscyamus
Catechu
Opium, poppy
Quassia
wood,
Nux
-vomica, Gentian
Coriander, fennel, clove, peppermint
Senna
, Rhubarb
Tulsi
, Balsam of
Tolu
,
Vasaka
Digitalis,
Squill
,
Strophanthus
Rauwolfia
Roots
Classification of Drugs based on Pharmacological action
Pharmacological Action
Drug
11-Dec-16
81
Pharmacognosy I – Third
Lecture 1- IntroductionSlide82
11-Dec-1682Classification of crude drugs5. Chemical classification; - Doesn’t show species or genus.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide83
Chemical Classification
Carbohydrates
Glycosides
TanninsVolatile oils and Terpenoids
Lipids
Resins
Alkaloids
Proteins
Vitamins
11-Dec-16
83
Pharmacognosy I – Third
Lecture 1- IntroductionSlide84
11-Dec-1684Classification of crude drugs6. Chemotaxonomic classification; - Needs a lot of time to recognize the plant, it depends on taxa and secondary metabolites.
Pharmacognosy I – Third
Lecture 1- IntroductionSlide85
Chemotaxonomic Classification This system of classification relies on the chemical similarity of a taxon i.e. it is based on the existence of relationship between constituents in various plants. 11-Dec-16
85
Pharmacognosy I – Third Lecture 1- IntroductionSlide86
11-Dec-1686Classification of crude drugsTaxonomic classification is more applied, since it depends on the genetics and morphological features of the plant. Pharmacognosy I – Third Lecture 1- IntroductionSlide87
11-Dec-1687Secondary metabolism and natural products- Secondary metabolites and building blocks…Natural products (NPs) and their chemistry…
Importance of NPs in modern medicine…
Pharmacognosy I – Third Lecture 1- IntroductionSlide88
11-Dec-1688Secondary metabolism and natural products- The scope of pharmacognosy in modern medicine…
Pharmacognosy I – Third Lecture 1- IntroductionSlide89
11-Dec-1689Natural products in drug discovery… Pharmacognosy I – Third Lecture 1- IntroductionSlide90
11-Dec-1690- Lecture review…- Next lecture topics… Pharmacognosy I – Third Lecture 1- IntroductionSlide91
Thank You11-Dec-1691 Pharmacognosy I – Third
Lecture 1- Introduction