Barleria prionitis Linn. (Family: Acanthaceae) is a well-known perennial, Ayurvedic herb distributed in the tropical Asia, Africa and Yemen. The whole plant or its specific parts (leaf, stem, root, bark and flower) has been utilized for treatment of toothache, catarrhal affections, whooping cough, inflammations, glandular swellings, urinary infection, jaundice, fever, gastrointestinal disorders and as diuretic and tonic. A wide range of phytochemical constituents including balarenone, pipataline prionisides, barlerinoside, verbascoside, shanzhiside methyl ester, barlerin, acetylbarlerin, lupulinoside, scutellarein have been isolated from the different parts of this plant. Extracts and isolated phytochemicals from this plant have been found to posses wide range of pharmacological include antimicrobial, anthelmintic, antifertility, antioxidant, antidiabetic, anti-inflammatory, anti-arthritic, cytoprotective, hepatoprotective, diuretic, antidiarrhoeal, enzyme inhibitory and anti-nociceptive activities without any toxic effects. So, in this review attempt has being made to highlight the traditional uses, phytochemistry, pharmacology and toxicity of this plant.