The practice of plants for the deterrence and management of innumerable physiological states and diseases dates back to the history of humankind. Although many of today's medicinal yields are achieved synthetically, they are often modelled on the chemical composition of medicinal plants. In this accordance, Acanthus genus (Family Acanthaceae) has acknowledged considerable attention due to its wide range of secondary metabolites and its customary usage in Indian and Chinese system of medicine. It is worth to mention that A. ilicifolius is enormously medicinal among all the species of Acanthus genus. This plant is considered to be rich sources of steroids, triterpenoids, saponins, flavonoids, alkaloids, and tannins. Traditionally, the plant has been used for asthma, diabetes, dyspepsia, hepatitis, leprosy, neuralgia, paralysis, ringworm, skin disease, snake bite, leukemia. Toxicological investigation in mice model has showed that, the ethanolic extract of the leaves of this plant have no toxic effect up to dose of 1000 mg/kg BW, 2000 mg/kg BW dose have mild toxicity and 5000 mg/kg BW dose have caused toxic effect in some organ system like liver, heart, pancreas, lung and kidney. Different extract of this plant also exhibited Anti-inflammatory, anti-leishmanial, osteoblastic, hepatoprotective, antioxidant and anticancer activities. This review article is an endeavor to cover current expansion in phytochemical and pharmacological potential of this plant species which will be a good reference tool for investigators who wish to work on natural products.