The genus Ilex (Aquifoliaceae) was reviewed for its chemical constituents and pharmacological significance including traditional uses. The structure-activity relationship for various compounds was illustrated to understand the mechanism of a particular activity. The genus has been known for its numerous biological activities like antioxidant, antimicrobial, cytotoxic, anti-platelet aggregation, anti-inflammatory etc. Most of the plants of this genus are rich sources of triterpenoids and saponins. Besides, these plants also contain flavonoids, alkaloids, anthocyanins and other phenolics in minute quantity. The bioactive constituents or plants extracts themselves, in the form of herbal drugs from this genus, have been validated for the treatment of various diseases and these would be used as a new formulation for the novel drugs discovery in pharmaceutical industries.
Keywords: Ilex; aquifoliaceae, triterpenoids, saponins, cytotoxic, antioxidant, CNS stimulants, mate tree, flavonoids, bioactive constituents.