Dyslipidemia is a key risk factor for cardiovascular diseases, which are a major cause of morbidity and mortality worldwide. However, despite the advancement of the treatment and prevention of dyslipidemia, medications used to treat dyslipidemia are limited to chemical drugs. Herbal medicine, as an alternative treatment, has a long history of usage and provides more treatment options, and related studies have revealed intervention targets for dyslipidemia. Four lipid-lowering mechanisms of herbal medicines have been proposed and are discussed in this paper. These mechanisms are the inhibition of cholesterol absorption in enterocytes, reduction of cholesterol synthesis, elevation of reverse cholesterol transport, and promotion of cholesterol excretion in the liver. This review elaborates on the underlying molecular pathways involved in plasma lipid balance via bioactive compounds from herbal medicines.