Hyperlipidemia is one of the major risk factor for the development of cardiovascular disease. Hypolipidemic nutraceuticals and functional foods help improve serum lipid profiles as reducing total cholesterol, triglyceride, and low-density lipoprotein cholesterol, while elevating high-density lipoprotein cholesterol. The effectiveness of omega-3 polyunsaturated fatty acid, phytosterols, dietary fiber, and tea catechin in management of hyperlipidemia has been clearly demonstrated in epidemiological and interventional trials. Studies on mechanism reveal that they act as inhibitor or activator of critical enzyme, agonist or inhibitor of transcription factor, competitor of transporter, and sequestrant of bile acid to modulate lipid homeostasis. Hypolipidemic effects are also claimed in dietary proteins, many polyphenols, other phytochemicals, raw extract, or even whole food. This review attempts to give an overview of lipid homeostasis and summarize recent findings of hypolipidemic nutraceuticals and functional foods according to their active ingredients, focusing on the efficacy and underlying mechanisms.