Statins Powerful Inhibitors of Cholesterol Biosynthesis.ppt

Statins: Powerful Inhibitors of Cholesterol Biosynthesis Cholesterol: What is it?1 Two types of transportation for cholesterol In order to transport the steroid through blood, cholesterol is attached to a set of proteins called lipoproteins. There are two types of lipoproteins: high density and low density lipoproteins. HDL: High-density lipoproteins – collect cholesterol particles as they travel through blood vessels and deposits them in the liver where they are transferred to bile acids and disposed off. LDL: Low-density lipoproteins –deposits on the walls of blood vessels, and over time, builds up into cholesterol plaque and blocks blood vessels, especially arteries that feed blood to the heart. 1. The liver manufactures, secretes and removes LDL cholesterol from the body. To remove LDL cholesterol from the blood, there are special LDL receptors on the surface of liver cells. 2. LDL receptors remove LDL cholesterol particles from the blood and transport them inside the liver. A high number of active LDL receptors on the liver surfaces is necessary for the rapid removal of LDL cholesterol from the blood and low blood LDL cholesterol levels. A deficiency of LDL receptors is associated with high LDL cholesterol blood levels. Diets that are high in cholesterol diminish the activity of LDL receptors!!!! Biological Role:1 It is an important component of cell linings It helps in the digestion of lipids It is a key component in the building of hormones Initial treatment of hypercholesteraemia was directed toward limiting LDL-cholesterol levels through: The Mevanolate Pathway2 The biosynthesis of cholesterol and isoprenoids (a group of compounds responsible for cell fluidity and cell proliferation) In 1976…….. ML-236A, ML-236B, ML-236C: metabolites isolated from a fungus (Penicillium citrinum) were found to reduce serum cholesterol levels in rats. This work was done by Akira Endo, Masao Kuroda and Yoshio Tsujita a