The present invention provides a method of treating or preventing hyperlipidemia in a subject in need thereof. Such method includes, specifically, administrating to the subject a therapeutically effective amount of a caffeamide derivative. The present invention also provides a pharmaceutical composition containing, primarily, the caffeamide derivative. The method and pharmaceutical composition of the present invention can effectively and significantly lower the high-fat diet-induced body weight gain and absolute visceral fat weight as well as the concentration of triglycerides and free fatty acids in blood, and levels of total lipid and triacylglycerol in liver tissue. In addition, the caffeamide of the present invention also reduces size of adipocyte, hepatocellular ballooning phenomenon, and liver steatosis. Through promotion of phosphorylation of 5′ adenosine monophosphate-activated protein kinase (AMPK) in muscle and liver, the caffeamide derivatives of the present invention is suitable for ameliorating or remedying hyperlipidemia.
