Year Semester 2 Prostaglandins Flashcards
What are prostaglandins?
Polyunsaturated, oxygenated derivatives of 3 C20 fatty acids.
What are prostaglandins classified according to?
1) ring code variants
2) number of double bonds in the side chain
What is PGE2 involved in? What is attached to its R groups?
Inflammation
- -C=O (at the top) and OH (at the bottom)
What is PGD2 involved in and what is attached to its R groups?
Immunity
- OH (at the top) and -C=O (at the bottom)
What is PGF2π involved in and what is attached to its R groups
Vasoconstriction
- 2 OH groups
What is arachidonic acid?
The major substrate used in PG synthesis
What kind of PG does arachidonic acid (AA) give rise to?
Series 2 e.g. PGE2
What kind of PG does dihomogamma-linolenic acid (DGLA) give rise to?
Series 1 e.g. PGE1
What kind of PG does eicosapentaenoic acid (EPA) give rise to?
Series 3 e.g. PGE3
What is the Omega 3 pathway?
Alpha linolenic acid β Octodeentetraenoic acid β Eicosatetraenoic acid β Eicosapentaenoic acid β Docosapentaenoic acid β Docosahexanoic acid
What is the Omega 6 pathway?
Linoleic acid β Gamma-linolenic acid β Dihomogamma-linolenic acid β Arachidonic acid β Docosatetraenoic acid β Docosapentanenoic acid
What is the Omega 9 pathway?
Oleic acid β Octadecodienoic acid β Eicosodienoic acid β Eicosotrienoic acid
What happens when COX-1 pathway is activated?
TxA2 and PGI2 control platelet aggregation and vascular tone
PGE2 is involved in cytoprotection
What happens when COX-2 pathway is activated?
pro-inflammatory PGs are synthesised
What are PGs involved in?
Fever generation Ovulation, fertilisation & parturition GI function Renal function Carcinogenesis Bone remodelling Sleep Inflammation and pain Allergy and immunity Vascular homeostasis and haemostasis
What are PG receptors and what are they linked to?
G protein coupled transmembrane receptors, they are linked to cAMP and Ca2+ signalling
What does the EP1 receptor mediate?
GI contraction and pyrexia
What does the EP2 receptor mediate?
Bronchodilation, vasodilation and GI fluid secretion
What does the EP3 receptor mediate?
GI relaxation, inhibition of gastric acid secretion, inhibition of ANS transmitters and pyrexia
What does the EP4 receptor mediate?
vasodilation, bone homeostasis & pyrexia
What are the ways in which PGs can be used therapeutically?
Substrate substitution
Enzyme inhibition
Replacement therapy
What is the role of PGE2 in cancer?
It is proliferative, too much of it isnβt good for the body. Cancer cells produce high amounts of PGE2.
What does a decrease in PGE2 lead to (terms of renal syndromes caused by the effect of NSAIDs)?
β Na retention Peripheral edema β blood pressure β weight Congestive heart failure
What does a decrease in PGI2 lead to (terms of renal syndromes caused by the effect of NSAIDs)?
Hyperkalaemia
Acute renal failure
Give examples of 2 PGFπ2
Latanoprost
Bimatoprost
What can a derivative of PGFπ2 do to intra-ocular pressure?
It can reduce intra-ocular pressure relieving the optic nerve - the allows fluid to drain freely.