The use of herbal or natural medicines for the treatment of various disorders has a long and extensive history. Many of these herbal medicines are finding their way onto the world market as alternatives to prescribed drugs currently available to treat various disorders/ailments. Hyperlipidemia contributes significantly in the manifestation and development of atherosclerosis and coronary heart disease (CHD). Hyperlipidemia prevalence continued to increase annually, requiring the development of drugs capable of lowering blood lipids to reduce mortality and morbidity due to cardiovascular complications. Although synthetic lipid-lowering drugs are useful in treating hyperlipidemia, there are number of adverse effects. So, the current interest has stimulated the search for new lipid-lowering agents with minimal side effects from natural sources. The purpose of this review is to highlight the current antihyperlipidemic drugs and their targets, the natural hypolipidemic agents and their mechanisms of action as well as experimental models of assessments.