The ancient science of life known as Ayurveda offers countless potential to uncover many unexplored manuscripts that lead to effective medications. Understanding traditional medicinal plants can open up a wealth of significant bioactive phytoconstituents with numerous significant pharmacological functions. This treasure must be located based on the understanding of old Ayurveda and other traditional references. Sapindaceae family member Cardiospermum halicacabum Linn. is a rich source of phytochemicals, including tannins, saponins, phenols, flavonoids, terpenoids, alkaloids, and sterols. Many of these phytochemicals exhibit antioxidant, anxiolytic, anti-inflammatory, anti-ulcer, anti-cancer, anti-microbial, antifungal, anti-bacterial, anti-diabetic, immunomodulatory, antiviral, cardioprotective, mainly neuroprotective properties according to Ayurveda. The plants' aerial parts are rich in phenolic acids, glycosidic compounds, tannins, and sterols. Researchers and academicians are examining the pharmacognosy, phytochemistry, and other pharmacological effects of the traditional medicinal plant known as Karnasphota (Cardiospermum halicacabum Linn.), which is cited in Ayurveda as one of the neuroprotective agents. Karnasphota (Cardiospermum halicacabum Linn.) is shown to have promising therapeutic potential by the scientific evidence offered by researchers and academics, and it can be further assessed as a novel candidate for drug discovery. The current review aims to examine the potential of the underexplored herb from Ayurveda "Karnasphota" for developing and designing future medications by reviewing the existence of medicinally significant secondary metabolites, potential pharmacological importance, and its role in neuroprotection in neurodegenerative diseases.