Before the modern day, medicine and its pharmacopeia of synthetic drugs, there were plants and ancient civilizations knew how to use the plants strategically to treat common ailments and even life-threatening diseases. Natural plant-based remedies are used for the both acute and chronic health problems from treating common colds to control blood pressure and cholesterol. Plant medicines were the most widely used medicines in the world because of their safety and very less or no side effects. In this way, the aim of this review article was to summarize the phytochemical and medicinal information of the readily reachable plant Cardiospermum halicacabum Linn. This is commonly known as Balloon vine extensively dispersed in tropical and subtropical areas of world. The roots, leaves, stem, and seeds of this plant are employed as herbal medication. The phytochemical analysis confirmed that this herb contains flavonoids, terpenoids, tannins, saponin, protein, carbohydrates, glycosides, variety of fatty acids, and volatile esters. Due to the presence of various compounds, this plant has antibacterial, antifungal, antiparasitic, antidiarrheal, anxiolytic, antioxidant, antipyretic, antirheumatic, anticonvulsant, anti-inflammatory, and anticancinogenic activities.