Franceschini G, Maderna P, Sirtori C R
Center E. Grossi Paoletti, University of Milan, Italy.
Atherosclerosis. 1991 Jun;88(2-3):99-107. doi: 10.1016/0021-9150(91)90073-c.
Reverse cholesterol transport identifies a series of metabolic events resulting in the transport of cholesterol from peripheral tissues to the liver and plays a major role in maintaining cholesterol homeostasis in the body. High density lipoproteins (HDL) are the vehicle of cholesterol in this reverse transport, a function believed to explain the inverse correlation between plasma HDL levels and atherosclerosis. An attempt to stimulate, by the use of drugs, this transport process seems to be of great promise in the prevention and treatment of arterial disease. Only few drugs are now known that can modify the activity of the various factors involved in the process. Clofibrate reduces cholesterol esterification, but the newer fibric acids are generally ineffective as anion-exchange resins. Probucol directly increases the activity and mass of cholesteryl ester transfer protein, thus possibly improving the physiological process of cholesterol removal from tissues. The few available data on the effects of drugs on reverse cholesterol transport should stimulate the search for new agents specifically stimulating this antiatherogenic process.
胆固醇逆向转运识别出一系列导致胆固醇从外周组织转运至肝脏的代谢事件，并在维持体内胆固醇稳态方面发挥主要作用。高密度脂蛋白（HDL）是这种逆向转运中胆固醇的载体，这一功能被认为可以解释血浆HDL水平与动脉粥样硬化之间的负相关关系。通过使用药物来刺激这一转运过程，在动脉疾病的预防和治疗中似乎大有前景。目前已知只有少数药物能够改变该过程中各种相关因子的活性。氯贝丁酯可降低胆固醇酯化，但新型纤维酸类药物通常与阴离子交换树脂一样无效。普罗布考可直接增加胆固醇酯转运蛋白的活性和含量，从而可能改善从组织中清除胆固醇的生理过程。关于药物对胆固醇逆向转运影响的现有数据较少，这应促使人们寻找能特异性刺激这一抗动脉粥样硬化过程的新药物。
