Jiaogulan (Gynostemma pentaphyllum) is a traditional Chinese medicinal herb that has been widely used in food and supplemental products. In the last 20 years, extensive research has been conducted to investigate the medicinal prospects of jiaogulan, and in this regard, more than 200 compounds have been isolated with various medicinal properties such as anticancer, anti-obesity, anti-inflammation, and antioxidation. In respect of potential benefits, jiaogulan market is likely growing, and various food items comprised of jiaogulan (beverage, sport drinks, cola, beer, tea, bread, and noodles) have been commercialized in the United States of America, China, and other Asian countries. More recently, there has been growing interest in the prebiotic potential of jiaogulan, especially at the interface of the gut microbiota. This review focuses on the prebiotic and therapeutic aspects of saponins and polysaccharides of jiaogulan tea by summarizing the literature on cancer, obesity, antioxidant activity, and immune-modulatory properties.