High density lipoprotein (HDL) can transfer cholesterol from foam cells to the liver and metabolize it into bile and excreted into intestinal tract, finally exhaust out of body, then it produces an anti-atherosclerosis effect, which is called HDL's reverse cholesterol transport (RCT). Therefore, how to increase the concentration of HDL and promote the function of HDL to give full play to its anti-atherosclerosis function are becoming a research hotspot in recent years. However, studies have shown that simple elevation of HDLC level has no significant clinical effect, revealing the complexity of HDL function. Therefore, it is necessary to systematically review the molecular structure, synthesis and metabolism of HDL, and re-recognize the molecular biological basis of its RCT function, so as to provide theoretical support for further research on the RCT function of HDL.