文档介绍：Antiatherosclerotic Agents抗动脉粥样硬化药
Lipid Core
lumen
neointima
Formation of Atherosclerotic Plaques
LDL
Therapeutic Strategies
Regulation of lipid
Antioxidation
Protection of arterial endothelium
Others:
Cholesterol
Cholesteryl esters(CE)
Triglycerides(TG)
Phospholipids
+
apopoprotein
Lipoprotein
血浆脂蛋白的结构
(载脂蛋白)
(游离胆固醇)
(磷脂)
(甘油三酯)
(胆固醇酯)
非极性脂类核心
Cholesterol and Triglyceride Metabolism
De Novo Cholesterol Biosynthesis
Liver synthesizes 2/3 of cholesterol made by the body. The rate limiting enzyme is 3-hydroxyl 3-methyl glutaryl (HMG)-CoA reductase.
Bile acids are synthesized from cholesterol in the liver, released into the intestine and reabsorbed in the jejunum and ileum
Classification of hyperlipoproteinemia and drug treatment
Type lipoprotein Ch TG AS risk drug treatment
elevated
I CM + +++ none
IIa LDL ++ high HMG-CoA reductase inhibitors

IIb LDL+VLDL +++ ++ high fibrates, HMG-CoARI
III IDL ++ ++ moderate fibrates,
IV VLDL + ++ moderate fibrates,
V CM+VLDL + ++ none
Lipoprotein Disorders
OR:
HDL concentration<normal
VLDL
LDL
IDL
concentration>normal
Regulators of lipoproteins’ levels
1. Competitive inhibitors of HMG-CoA (3-hydroxy-3-methylglutaryl-coenzyme A) reductase:
lovastatin (洛伐他汀),
mevastatin(美伐他汀),
pravastatin (普伐他汀),
simvastatin (辛伐他汀),
fluvastatin (氟伐他汀).