Cholesterol has a much higher profile than the other lipids because of its association with heart disease. Despite its lethal re
putation with the public, cholesterol is vital to the body: it maintains proper fluidity of animal cell membranes and is the precursor of steroid hormones such as progesterone, testosterone, estradiol, and cortisol. Cholesterol is synthesized in the liver and, to a lesser extent, in other tissues. The rate of its synthesis is highly responsive to the cellular level of cholesterol. Cholesterol synthesis can be effectively blocked by a class of compounds called statins. The market of the statins is estimated at $20 billions. Explain the mechanism of action of statins.
The mechanism of action of statins begins with the inhibition of a protein called HMG-CoA reductase, allowing its substrate to accumulate in the body and promote cholesterol reduction. At that moment, a transporter called OATP (Organic Anion Transporting Polypeptides) takes statins to the epatic tissue where they will be transformed and metabolized until they are eliminated through bile. This elimination is influenced by the P-glycoprotein, which is the main cause of the efflix presented by the bili. This process can get help from other molecules like some protease inhibitors, digoxin and cyclosporine.
