Lecture 4 bioactive lipids Flashcards
(24 cards)
PLA2
stimulated by calcium release, activates arachidonic acid to change into LOX or COX
arachidonic acid
all metabolites are known as eicosanoids
LOX pathway
arachidonic acid is converted into lipoxins and leukotrienes
leukotrienes
receptors are Gq coupled, eosinophils and neutrophils
COX pathway
arachidonic acid is converted into prostanoids
prostanoids
mostly Gq coupled, function depends on location
PGD2
inhibition of gastric acid secretion, coupled to Gi/Go
EP1
Gq, smooth muscle contraction (airways, GI tract)
EP2
Gs, smooth muscle relaxation, intestinal fluid secretion
EP3
Gi, inhibition gastric acid secretion, potentiation contraction (uterus)
EP4
Gs, smooth muscle relaxation
TxA2 and PGI2
control of vascular tone and platelet activation
lipoxins
annexin-1 is induced by corticosteroids, together with resolvins can stimulate GPCR
NSAIDs
prostanoid inhibitors
antipyretic effect
decrease fever
analgesic effect
pain reliever
COX1
almost expressed in all tissues, house keeping protein
COX2
sensitive to inflammatory cells, inducible isoform
COX3
splice variant from COX1 gene
aspirin
irreverisbly inhibits COX1/2. triggers lipoxins, causing inhibition of inflammation
paracetamol
weak COX inhibitor, with weak anti-inflammatory effects. No effect on GI tract
Bradykinin
locally released from mast cells during tissue damage and inflammation
prostaglandins
strongly enhance the direct action of bradykinin on the nerve terminals
misopristol
stimulates EP3 receptor causing decrease in gastric acid secretion via H2 receptor.