Siraitia grosvenorii (Swingle) C. Jeffrey, a perennial vine of the Cucurbitaceae family, is a unique medicine food homology species from China. S. grosvenorii can be used as a natural sweetener in the food industry and as a traditional medicine for moistening the lungs, quenching a cough, smoothing the intestines, and relieving constipation. Additionally, the fruits, roots, stems, and leaves of S. grosvenorii are rich in active ingredients, and have pharmacological effects such as immune regulation, hypoglycemia, and antioxidant, hepatoprotective, and antitumor effects, etc. Therefore, S. grosvenorii has broad application prospects in the pharmaceutical industry. This paper reviews the bioactive components, pharmacological effects, and extraction methods of S. grosvenorii, summarizes them, and proposes their future development directions. This current overview highlights the value of S. grosvenorii. By documenting the comprehensive information of S. grosvenorii, the review aims to provide the appropriate guidelines for its future in-depth development and the utilization of S. grosvenorii resources for their roles as active ingredient (triterpenoids, flavonoids, and polysaccharides, etc.) sources in the food industry and in the development of functional foods.