Auraptene is a monoterpene coumarin originally found in Citrus species. Auraptene exhibits anti-inflammatory, neuroprotective, anti-parasitic, antihypertensive, anti-diabetic, and chemopreventive activities. Auraptene inhibits growth of species of Leishmania, decreases mean arterial pressure, binds estrogen receptors, inhibits ACAT, and induces phase II metabolizing enzymes. Auraptene also inhibits LPS-induced COX-2 expression, loss of body weight, activation of microglia and astrocytes, and brain inflammation in animal models of cerebral ischemia. Additionally, auraptene activates PPARα, improving high fat diet-induced hyperglycemia and alterations in glucose tolerance. This compound also decreases expression of cyclin D1 and delays tumor formation in animal models of mammary carcinogenesis.