Plant-based drug discovery has drawn the attention of researchers, especially the one used as traditional medicines. Centella asiatica is traditional Ayurveda medicine widely used in India and across Asia for treating a variety of diseases. The aerial parts and roots are used for medicinal purpose, and its chemical constituents have wide therapeutic applications in areas of antimicrobial, anti-inflammatory, anticancer, neuroprotective, antioxidant, and wound healing activities. Many of its uses have been proven scientifically, and bioactive ingredients have been validated. In this review, we have done a critical evaluation of available literature looking for the pharmacological importance of C. asiatica. Further studies will be helpful to discover more bioactive compounds their exact mode of actions.