Abstract: Centratherum anthelminticum is an ethnomedicinal plant in India and a common ingredient in Ayurvedic medicine. To date, many scientific studies have been carried out, but a comprehensive review on this plant is lacking. This review aims to cover the biological activities and the active compounds derived from C. anthelminticum. Exploration of more than 40 papers available in literature (up to 20th of April 2013) revealed that the pharmacological effects of C. anthelminticum range from anti-oxidant, anti-diabetic, anti-microbial to recently found anti-cancer property. Over 120 compounds consisting of fatty acid, sterols, sesquiterpene lactones, flavonoids and carbohydrates have been identified from different parts of the plant. Many of these active compounds were derived from the seeds and have been evaluated for a variety of biological activities. Despite the encouraging results demonstrated by these studies and the traditional use as nutraceutical agent, clinical trials of C. anthelminticum extracts or derivatives are absent. Thus, a systematic documenting review would provide more insights and spur further research that would lead to production of safer and economical alternative medicine from C. anthelminthicum.