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Intro to D&D Midterm > Med Chem Part 1 > Flashcards

Med Chem Part 1 Flashcards

1
Q

true or false

inflammation is a normal process

A

true

it’s a normal response to noxious (harmful) stimuli that threaten the host

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2
Q

name the thing that initiates inflammation, and then the 4 steps that follow

A

-initial injury
1. histamine and prostaglandins released

  1. blood vessels dilate and clotting begins
  2. phagocytic cells attracted to the area by chemotactic factors
  3. phagocytes consume pathogen and cell debris
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3
Q

as mentioned, the initial injury is what triggers the first step of inflammation (histamine and prostaglandin release)

this initial injury can be what 5 stimuli?

A

physical stimuli
chemical stimuli
microbial stimuli
inflammatory stimuli
mitogenic stimuli

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4
Q

how are NSAIDS involved in preventing the inflammatory process?

A

they block the biosynthesis of prostaglandins from arachidonic acid
bc prostaglandins are the things responsible for pain, inflammation, and fever

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5
Q

the release of lysosomal enzymes during inflammation does what?

A

degrades the connective tissue

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6
Q

what catalyzes the conversion of arachidonic acid to prostaglandins?

A

COX (cyclooxygenase)

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7
Q

what is COX (cyclooxygenase)

A

an enzyme that catalyzes the formation of prostaglandins from arachidonic acid

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8
Q

what is the target for NSAIDS

A

COX

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9
Q

how many isoforms of COX are there?

A

3
COX-1
COX-2
COX-3

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10
Q

Where in the cell are COX enzymes located?

A

bound to the ER membrane

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11
Q

COX are ___ containing ___ enzymes

explain

A

heme containing bifunctional enzymes

bifunctional because COX possesses cyclooxygenase and peroxidase activity, BOTH of which are needed for the production of prostaglandins

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12
Q

what is the target of NSAIDS? how do they accomplish this?

A

the target of enzymes is COX activity.
they do this by competing with arachidonic acid for the COX active site

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13
Q

true or false

NSAIDS promote the synthesis of prostaglandins

A

FALSE - they inhibit.
these cause pain and inflammation and fever

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14
Q

how many active sites does COX have? what are they?

A

2
the cyclooxygenase active site and the peroxidase active site

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15
Q

explain the relationship between the 2 active sites of the COX enzyme

A

they are spacially distant but functionally intertwined

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16
Q

how is it that the cyclooxygenase active site and the peroxidase active site of COX are functionally intertwined?

A

because both pathways are needed for the production of prostaglandins

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17
Q

NSAIDS are useful for treating what?

A

acute pain and inflammation
osteoarthritis, rheumatoid arthritis
ankylosing spondylitis (arthritis that causes inflammation in spine and other areas)
painful shoulder
acute gouty arthritis
postoperative pain (in some scenarios)

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18
Q

what is the major pathway catalyzing the conversion of arachidonic acid into prostaglandins?

A

the COX (cyclooxygenase) enzyme system

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19
Q

_____ is converted into prostaglandins through the COX enzyme

A

arachidonic acid

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20
Q

explain the structure of prostaglandins. name 2 things

A

they contain a cyclopentane
they are lipophilic acids

21
Q

where are prostaglandins produced?

A

locally - at the site of tissue damage

22
Q

explain the half life of prostaglandins

A

very short - 1-5 mins

23
Q

where is arachidonic acid located?
how is it released from this location for activity?

A

arachidonic acid is located as a component of the phospholipid cell membrane.

the enzyme PLA2 (phospholipase A2) hydrolyzes the phospholipid cell membrane, releasing arachidonic acid

24
Q

as mentioned, PLA2 (phospholipase A2) is the enzyme that hydrolyzes the cell membrane to release arachidonic acid from it.

what process will increase the amount of PLA2?? What is the result of increased PLA2?

A

inflammatory cytokines like IL-1 will increase membrane bound PLA2 activity

this will in turn increase prostaglandin biosynthesis, through the increased release or arachidonic acid from the cell membrane

25
Q

where is PLA2 located?

A

some is membrane bound, like arachidonic acid

26
Q

explain the structure of a membrane phospholipid

A

glycerol + phosphatidic acid

glycerol has 3 hydroxyl groups
at 2nd hydroxyl group, arachidonic acid is attached

27
Q

what is the chemical reaction catalyzed by PLA2 that releases arachidonic acid from the cell membrane?

A

hydrolysis

28
Q

explain the structure of arachidonic acid

A

has 20 carbons
with 4 double bonds, all of which are CIS conformation
has terminal COOH (carboxylic acid group)

29
Q

as mentioned, arachidonic acid contains 4 double bonds

at which positions are they and what conformations are they?

A

all are cis
5,8,11,14

30
Q

give another name for arachidonic acid

A

eicosatetraenoic acid

31
Q

arachidonic acid is a _____ acid
what is the relative half life?

A

lipophilic acid
very short half life

32
Q

glycerol contains how many hydroxyl groups?

A

3

33
Q

explain the full pathway of arachidonic acid metabolism by COX (after arachidonic acid is released from the cell membrane)

A
  1. Arachidonic acid is converted to Prostaglandin G2 through COX activity
  2. Prostaglandin G2 is converted to Prostaglandin H2 through PEROXIDASE activity

prostaglandin H2 is a MAJOR source of bioimportant prostaglandins

  1. Tissue-specific synthase enzymes convert prostaglandin H2 into 5 major bioactive prostaglandins
34
Q

as mentioned, Prostaglandin H2 is a major source of bioimportant prostaglandins through tissue-specific synthase enzyme activity.

name these 5 makor bioactive prostaglandins.

A

PGE2
PGI2
PGD2
PGF2
TXA2

35
Q

the 5 major bioactive prostaglandins are

PGD2
PGE2
PGF2
PGI2
TXA2

how do they exert their effects in the body?

A

by interacting with their respective prostaglandin receptors. they are G-protein coupled receptors (GPCRs)

PGE2 binds EP receptor
PGD2 binds DP receptor
PGF2 binds FP receptor
PGI2 binds IP receptor
TXA2 binds TP receptor

36
Q

true or false

the 5 major bioactive prostaglandins exert their effects through binding to ligand gated ion channels

A

FALSE - through GPCRs

37
Q

how is prostaglandin G2 produced

A

through COX1 and COX2 activity conversion of arachidonic acid to prostaglandin G2

38
Q

explain in further detail the chemistry of the conversion of arachidonic acid to prostaglandin G2 (PGG2)

A

this occurs through COX1 and COX2 activity
needs 2 MOLECULAR OXYGEN**** (2O2)
Bis-oxygenation occurs to form the HIGHLY UNSTABLE PGG2

39
Q

explain in further detail the chemistry of the conversion of PGG2 to PGH2 by Peroxidase activity

A

15-OOH, through the Peroxidase activity of COX, is reduced to 15-OH to produce PGH2

essentially peroxide (H2O2) becomes hydroxide (OH)

40
Q

explain the difference between the target of NSAIDS vs acetaminophen

A

NSAIDS inhibit COX1 AND COX2 - the cyclooxygenase active site - prevents conversion of arachidonic acid to PGG2

acetaminophen inhibits the PEROXIDASE activity of COX - prevents conversion of PGG2to PGH2

41
Q

true or false

NSAIDS inhibit the conversion of PGH2 to PGG2

A

false

inhibit conversion of arachidonic acid into PGG2

42
Q

once PGG2 is converted to PGH2 through peroxidase activity, what happens to PGH2?

A

it’s converted into various major bioactive prostaglandins through different pathways

43
Q

what enzyme converts PGH2 into PGE2?

A

PG endoperoxide E isomerase

44
Q

what enzyme converts PGH2 into PGF2?

A

PG endoperoxide reductase

45
Q

What enzyme converts PGH2 into PGD2

A

Glutathione-S-transferase

46
Q

what major bioactive prostaglandin is responsible for uterine contraction

A

PGF2

47
Q

what 2 major bioactive prostaglandins are responsible for being proinflammatory, swelling, and fever?
which additionally causes allergic reactions?

A

PGE2 and PGD2

PGD2 also responsible for allergic reactions

48
Q
A

Intro to D&D Midterm (29 decks)

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