Lipid-centered applications

Question 1

what are statins

Answer 1

small-molecule drugs that inhibit the key rate-limiting and regulatory enzyme in cholesterol synthesis, HMG-CoA reductase.

Question 2

what was the first satin to be produced as a pharmaceutical was

Answer 2

Was lovastatin, a natural
molecule purified from a soil fungus.

Question 3

Describe the characteristics of lovastatin

Answer 3

1. competitive inhibitors
2. statins bind the enzyme at the active site and keep HMG-CoA from binding there.

Question 4

what does soluble fiber do?

Answer 4

Soluble fibre (such as in psyllium husks) lowers cholesterol in two ways.

Question 5

how does soluble fiber lower cholesterol

Answer 5

1. Cholesterol in the liver is used to produce bile, which goes into the intestines. In the intestines, soluble fibre reduces the reabsorbtion of bile. Therefore, more cholesterol has to be used to produce new bile.
2. Soluble fiber also reduces the absorption of dietary cholesterol.

Question 6

what happens when the cholesterol level diminish

Answer 6

1. the LDL receptors on hepatocytes go to the cell surface where they are active.
2. These LDL receptors bind LDL particles from the blood plasma and take them in = take in cholesterol.
3. the concentration of circulating LDL particles in the blood plasma decrease and the odds of atherosclerosis are reduced.

Question 7

What effect do omega-3 fatty acids have

Answer 7

known to have effects on circulatory health and
may affect other processes as well

Question 8

what are the three common omega-3 fatty acids

Answer 8

1. ALA 18:3
2. EPA 20:5
3. DHA 22:6

Question 9

What do Omega-3 fatty acid do

Answer 9

1. Incorporated into phospholipids, which in turn become integrated into cell membranes.

Question 10

what effects do omega-3 fatty acids have an cells

Answer 10

1. Membrane protein activities
2. Signalling from the membrane in the
   cell
3. Altered gene expression
4. Subsequent further altered signals

Question 11

describe omega-3 fatty acids and the cardiovascular system

Answer 11

Omega-3 fatty acids have or are expected to have multiple effects on cardiovascular risk factors, both directly and indirectly:
1. Anti-inflammatory effects
2. membrane stabilizing effects
3. Anti-thrombotic effects
4. Lipid effects
5. Plaque stabilization effects

Question 12

Where do omega-3 fatty acids naturally come from originally

Answer 12

1. EPA and DHA are natural products of microalgae and are taken in by fish, making fish a good source of these oils
2. ALA is found in plants
3. all made from algae

Question 13

Describe the earliest lipid delivery system developed for drugs.

Answer 13

1. Liposome = The earliest lipid carrier.
2. They can carry hydrophilic or
   hydrophobic drugs as cargo.
3. The phospholipid composition allows them to fuse with target cells

Question 14

what is the next generation of lipid delivery

Answer 14

lipid nanoparticles

Question 15

describe the composition of lipid nanoparticles

Answer 15

1. Non-bilayer lipid nanoparticles
2. Polyethylene glycol added for solubility
3. A tailored lipid mixture is used, including a cationic (+ charged) lipid to interaction with the (-) charged nucleic acid cargo that will be delivered to the cells

Question 16

Describe how lipid nanoparticles helped us deal with a public health challenge and provide an example

Answer 16

1. Without a lipid nanoparticle, the mRNA vaccines would not be possible. Our body would recognize it as a pathogen and destroy it.
2. mRNA is a delicate molecule prone to degradation. Without these protective lipid structures, they would not make it to the cells where they produced the COVID spike protein antigens.

Question 17

Explain whether lipid nanoparticles growing in use or falling out of favour.

Answer 17

growing!

Question 18

Describe one example of new research on lipid nanoparticles in Canada.

Answer 18

Dr. Bowen Li’s team at the University of
Toronto has developed technology to reduce off-target drug delivery by making the
nanoparticle lipid mix more targeted to a particular tissue.