EICOSANOIDS
Dr Madiha Soban
Contents of the Lecture
Definition of Eicosanoids
Types of Eicosanoids
Importance of Eicosanoids
Biosynthesis of Eicosanoids
Structure & Functions of
Prostaglandin
Effects of Thromboxanes
Leukotrienes & their role
History
• Prostaglandins were discovered in
the 1930's.
• Ulf von Euler found that seminal fluid
and seminal vesicles from most animals
including man contain a substance
which causes contraction of the smooth
muscle of the uterus.
• He named this new substance
prostaglandin sincethey were originally
thought to be secreted bytheprostrategland.
EICOSANOIDS - Definition
Any of a class of compounds that
are derived from polyunsaturated
fatty acids as arachidonic acid and
are involved in cellular activities.
Example:
Prostaglandins, Leukotrienes, and
Thromboxanes
EICOSANOIDS - Types
PROSTAGLANDINS
THROMBOXANES LEUKOTRIENES LIPOXINS
They are Physiologically and
Pharmacologically active
compounds
Act as local hormones
functioning through G-Proteins
EICOSANOIDS –Importance
EICOSANOIDS - BioSynthesis
Prostaglandins
Any of a group of potent hormone like
substances that are produced in various
mammalian tissues, derived from Arachidonic
acid, and mediate a wide range of physiological
functions, such as control of blood pressure,
contraction of uterine, smooth muscle, and
modulation of inflammation
CHEMICAL STRUCTURE
All prostaglandins are considered to
be derived from the 20 C cyclic
saturated fatty acid, Prostanoic
Acid.
The five carbon ring is saturated.
All naturally occurring PGs have an
alpha- oriented OH group at C15.
Prostaglandins
PGs are not stored; precursor fatty acids are stored in
membrane as phospholipids.
Arachidonic acid is released by the action of Phospholipase A2
on phospholipids
Synthesis is catalysed by prostaglandins H synthase(PGHS).
It contains two separate enzymes (cyclo-oxygenase &
peroxidase).
PGG2 and PGH2 are formed as intermediates during synthesis
of other PGs.
Functions of Prostaglandins
Effects
on GIT
Effects
on
Inflamm
ation
Effects
on Resp
tract
Effects
on
uterus
Effects
on CVS
Functions of Prostaglandins
PGI2
Vasodilatation
Inhibits platelet aggregation
PGA and PGE class prostaglandins lower
blood pressure.
Effects
on
CVS
CVS effects
PGF2
Stimulates uterine muscles
Inducing labor
Effects
on
uterus
Functions of Prostaglandins
Effects on Uterus
PGF-Bronchoconstriction
PGE-Bronchodilator
PGE- series are used in
aerosols for relieving
vasospasm
Effects on
Respiratory
tract
Functions of Prostaglandins
Effects on Respiratory tract
• Effects on uterus
PGE2
Involved in inflammatory
response by increasing
capillary permeability.
Effects on
Inflammation
Functions of Prostaglandins
Effects on Inflammation
PGE2
suppress gastric acid
secretion and intestinal
motility and used in
treatment of acid peptic
disease
Effects
on GIT
Functions of Prostaglandins
Effects on GIT
THROMBOXANE EFFECTS
Increase platelet aggregation
Vasoconstriction
Mobilize intracellular calcium
Smooth muscle contraction
Bronchoconstriction
EICOSANOIDS FUNCTIONS
Summary of uses
Use Preparation
Abortion PgE1
Cervical ripening PgE1 / E2
Peptic ulcer PgE1
Glaucoma PgE1-Latanoprost
PPH PgI2
PDA PgE1
EFFECT OF NSAIDS
EFFECT OF NSAIDS
LEUKOTRIENES
LEUKOTRIENES
LEUKOTRIENES
Increase chemotaxis
Facilitate inflammation & allergic reactions
Contraction of smooth muscle
Bronchoconstriction
Vasoconstriction
LEUKOTRIENES
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