Bioactive Lipids Flashcards
dereivative that has a biology effect
bioactive lipids
breakdown product of arachidonic acid
bioactive lipids
diverse physical, chemical, inflammatory and mitogenic stimuli
Help bring arachidonic acid into the cell
3 enzymes that reduce Arachiodonic acid (AA)
Cytochrome p450
LOX (Lipoxygenases)
COX (Cycloxygenases)
Cytochrome p450 breaks AA into
EETs (Epoxyeicosatrienoic acids)
LOX breaks AA into
HETEs
Leukotrienes (** Most important)
Lipoxins
COX breaks AA into
Prostanoids: such as -
Prostaglandins ()
Prostacyclin
Thromboxane ()
constitutively expressed in most cells
COX1
inducible, expression varies based on stimulus
COX2
proposed (can be inhibited in acetaminophen)
COX3
when macrophages become activated, they increase their expression of ___
COX2
Subtypes of Prostaglandins
PGE2
PGFa
PGD2
PGI1
Subtype of Thromboxane
TXA2
vasodilator produced by endothelium
PGE2
contracts longitudinal GI smooth muscle, relaxes circular GI smooth muscle
PGE2
Bronchodilator
PGE2
low concentrations enhance platelet activity, high concentrations inhibit
PGE2
vasodilator in kidney, plays a role in maintaining renal blood flow and GFR
PGE2
low concentrations cause uterine contraction, high concentrations relax
PGE2
pyrogen, can be used as an abortifacient in second trimester
PGE2
promotes inflammation
PGE2
increase bone turnover
PGE2
lowers intraocular pressure
PGE2
pro-oncogenic
PGE2
synthetic PGE2 used to ripen cervix prior to labor induction
DINOPROSTONE
synthetic PGE1 used with mifepristone (RU 486) as abortifacient
MISOPROSTOL
can be used to treat NSAID induced ulcers
MISOPROSTOL
abortion pill
MIFEPRISTONE
vasocontrictor (prostanoid subtype)
PGF2A
contracts longitudinal and circular GI smooth muscle
PGF2A
bronchoconstrictor (prostanoid subtype)
PGF2A
uterine contraction and onset (along with oxytocin) of partiurition
PGF2A
pyrogen (prostanoid subtype)
PGF2A
lower intraocular pressure
PGF2A
derivative used extensively to treat glacoma
LATANOPROST
vasodilator (prostanoid subtype)
PGI2
bronchodilator (prostanoid subtype)
PGI2
decreases uterine tone
PGI2
inhibits platelet aggregation
PGI2
used to treat severe pulmonary hypertension and as anticoagulant in dialysis machines
EPOPROSTENOL
potent vasocontrictor and bronchoconstrictor
Thromboxane A2
increase uterine tone
Thromboxane A2
platelet activator - causes thrombosis
Thromboxane A2
primary physiological effects of leukotriene pathway appear to be mediated by __ and __
LTC4 and LTD4
5-LOX inhibitor
ZILEUTON
LTD4 receptor antagonists
ZAFIRLUKAST and MONTELUKAST
primary physiological effects appear to be potent bronchoconstriction and activation of ___
leukocyte chemotaxis
decreased formation or antagonism of receptor binding are major therapeutic strategies employed in ___
asthma
decreased phospholipase A activity (decrease AA production)
cortiocsteroids
decrease COX2 synthesis
corticosteroids
nonselective vs selective COX inhibitors
NSAIDS
replace AA with dietary fatty acids
PUFA
Polyunsaturated fatty acids
prototypic nonselective
Aspirin
selective COX2
Celecoxib
causes irreversible inhibition of COX receptors
Aspirin
main COX in the stomach
COX1
side step the induced ulcers effect
COX2
what are the 2 pyrogens?
PGE2
PGF2a
Which lowers intraocular pressure?
PGE2
PGF2a
Which is a dilator?
PGE2
Which is a constrictor?
PGF2
Which contracts longitudinal GI SM but relaxes it?
PGE2
which has uterus effects but not platelet effects?
PGF2a