Over the past decade, herbal medicine has become an item of global importance, with both medicinal and economic implications. Widespread use of herbs throughout the globe has raised serious concerns over their quality, safety and efficacy. Thus, accurate scientific assessment has become a prerequisite for acceptance of herbal health claims. Ailanthus excelsa Roxb is a tree, indigenous to central and southern India, belongs to family Simaroubaceae is widely used in Ayurveda and evidence based phytotherapy. The tribal population uses the plant for antifertility, anthelmintic and rejuvenating purpose. Alkaloids, flavonoids, triterpenoids and bitter principles like quassinoids are reported in this plant. Several quassinoids from Simaroubaceae are designated as potent antimalarial especially against the chloroquine-resistant Plasmodium falciparum. The roots of this plant also serve as substitute for Oroxylum indicum, one of the constituents of an ayurvedic formulation Dasmularista. In the present review an attempt has been made to explore different aspects of Ailanthus excelsa.