Acanthus ilicifolius L. (Mangrove Holly, Sea Holly, Jeruju putih, Kolimulli) is a type of mangrove that has a long history of use as a traditional remedy according to the Ayurvedic and Traditional Chinese Medicine systems; hence, it is of huge importance to the people living in littoral areas because of its medicinal potentials, including as an anti-inflammatory agent, gastroprotective, anti-atherosclerotic, anti-arthritic, antioxidant, antimicrobial, anticancer, and anticoagulant. Several chemical compounds have been isolated from the plant (i.e., class of flavonoid, alkaloid, lignan, terpenoid, glycoside, steroid, phenylethanol, and coumarin). This review presents an overview of the potential pharmacology of A. ilicifolius-related sources that could be used in the future drug development.