Centella asiatica (CA), (also known as Centella asiatica (L.) Urb. or Indian pennywort or Gotu Kola) is native to the tropical regions of Asia and Africa and has a rich history of use in treating a wide range of ailments, including neurological, dermatological, immunological, and metabolic disorders. This plant is rich in bioactive compounds, such as pentacyclic triterpenes (notably Asiaticoside, Asiatic Acid, Madecassoside, and Madecassic Acid), flavonoids, phytosterols, and phenolic acids, which contribute significantly to its therapeutic effectiveness. The medicinal applications of CA are vast, with its chemical constituents exhibiting notable therapeutic potential in areas such as antidiabetic, antimicrobial, anti-inflammatory, anticancer, neuroprotective, antioxidant, and wound healing activities. Numerous scientific investigations have validated these applications, confirming the efficacy of its bioactive components. In this critical review, we have conducted a comprehensive analysis of the existing literature to shed light on the pharmacological significance of CA, particularly concerning diabetes and related disorders.