人体内的二酰甘油酰基转移酶是催化三酰甘油最终合成的关键酶,其基因缺失或酶活受抑时,机体不会因高脂饮食而发生肥胖,且对胰岛素的敏感性增强,因此该酶可作为肥胖和糖尿病治疗药物的靶点。综述二酰甘油酰基转移酶的功能研究以及天然来源和合成的二酰甘油酰基转移酶抑制剂的药理活性和构效关系。 Diacylglycerol acyltransferase in the human body is the key enzyme that catalyzes the final synthesis of triacylglycerol. When the gene is deleted or the enzyme activity is inhibited, the body will not be obese due to the high-fat diet and the insulin sensitivity will be enhanced. This enzyme can be used as a target for the treatment of obesity and diabetes. The function of diacylglycerol acyltransferase and the pharmacological activity and structure-activity relationship of natural and synthetic diacylglycerol acyltransferase inhibitors were reviewed.