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Block 5 > MBOD--Eicosanoids > Flashcards

MBOD--Eicosanoids Flashcards

1
Q

COX 1

A

cyclooxygenase; homesotatic protection and maintenance functions, expressed via constitutive expression

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2
Q

COX 2

A

functional role in pro-inflammatory and mitogenic effects; induced by TNFalpha, LPS, IL-1 and 2, EGF, and IFN gamma

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3
Q

In what path do cycloxygenases function?

A

in the PG synthesis pathways

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4
Q

Three pathways in which ArA is a substrate?

A

cycloxygenase
lipoxygenase
epoxidation (CYP450)

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5
Q

What are the 3 products of the lipoxygenase pathway?

A

leukotrienes
lipoxins
HETE

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6
Q

What is the major intermediate of the lipoxygenase pathway?

A

HPETE

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7
Q

What inhibits the lipoxygenase pathway?

A

synthesis inhibitors in asthma drugs

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8
Q

What inhibits the COX pathways?

A

NSAIDs (like ASA)

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9
Q

What are physiologic functions of eicosanoids?

A

paracrine signalers for vasoregulation, inflammation, bronchoregulation

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10
Q

Through what GPCR pathway do PGs E/D/I function?

A

Gs, so they activate adenylyl cyclase and increase cAMP/PKA/cell changes

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11
Q

Through what GPCR pathway do PGF2, TXA2, and leukotrienes function?

A

Gq: so they cleave PIP2 and IP3 releases Ca2+ from ER

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12
Q

What induces the release of eicosanoids?

A

cytokines and other hormone signals

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13
Q

What is the precursor for eicosanoid synthesis?

A

arachidonic acid, produced from phospholipids

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14
Q

What kinds of PGs do endothelial cells produce?

A

PG I/E/D to inhibit platelet aggregation

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15
Q

What catalyzes the formation of epoxides?

A

CYP 450

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16
Q

What enzyme catalyzes the formation of PGs and what is the major intermediate?

A

prostaglandin synthase; PGH2/PGG2

17
Q

What are the two catalytic functions of PG synthase and what do they each produce?

A

cycloxygenase–PGG2

peroxidase–PGH2

18
Q

What enzyme catalyzes the formation of leukotrienes, HETE, and lipoxins?

A

lipoxygenase

19
Q

What enzymes produce ArA?

A

PLA2 and DG lipase, from phospholipids and DAG respectively

20
Q

Where does glutathione come in with PG synthesis?

A

it is needed to help out the peroxidase function of PGS to convert PGH2–>PGG2

21
Q

What are the common structural features of PGs?

A

20 Carbons; 5-C ring (C8-12); 2 chains with 8 and 7 Cs each; substituent at C9 and C11; hydroxyl at C15; up 2 two double bonds in hydrocarbon chain

22
Q

What is the main physiological function of thromboxanes?

A

platelet aggregation and vasoconstriction; released at wounds

23
Q

What inhibits phospholipases?

A

Corticosteroids

24
Q

What is the basis of endometriosis?

A

estrogen tells the endometrium to grow and that causes pain and infertility; PGE2 stimulated estrogen production, both induce COX-2 so COX inhibitors like NSAIDs will help alleviate pain

25
Q

What is the effect of PGE on neurotransmission?

A

inhibits Epi release in sympathetic nerves, increase peripheral nerves’ sensitization

26
Q

What kind of activity does Acetaminophen have?

A

CNS anelgesic activity

27
Q

What is the effect of PGE in bones?

A

increases bone turnover, absorption, and formation

28
Q

What is the normal action of TXA2 on platelets, and what is the effect of inhibiting COX on TXA2?

A

normally TXA2 will promote platelet aggregation and vasoconstriction, but inhibiting it will decrease platelet aggregation and inhibit vasoconstriction; this can affect the healing process

29
Q

What is the problem with selective COX-1 or COX-2 inhibitors?

A

COX-1 will inhibit platelet aggregation, leading to GI ulcerations and poor healing; inhibiting COX-2 will prevent platelet inhibition and raise risk of clot formation

30
Q

What is the effect of PGs in the kidney?

A

COX-1 derived will promote sal excretion

COX-2 derived will maintain regular kidney filtration

31
Q

What is the role of PGE in fevers?

A

it is involved in making a fever, so NNAs lower fever by inhibiting COX path/PGE

32
Q

Epoxides play a role in…

A

vascular and myogenic tone

33
Q

Eicosatrienoic products think…

A

vasodilation

34
Q

Hydroxyeicosatetreonoic products think…

A

vascular and kidney effects that implicate it in hypertension

35
Q

Give example uses of exogenous PGE/PGF2alpha

A
  1. induce labor/uterine contraction
  2. ED
  3. Pulmonary HTN
  4. patent ductus arteriosis

Block 5 (6 decks)

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