Siraitia grosvenorii (SG), also known as Luo Han Guo or Monk fruit, boasts a significant history in food and medicine. This review delves into SG's historical role and varied applications in traditional Chinese culture, examining its phytochemical composition and the health benefits of its bioactive compounds. It further explores SG's biological activities, including antioxidant, anti-inflammatory, and antidiabetic properties and elucidates the mechanisms behind these effects. The review also highlights recent synthetic biology advances in enhancing the production of SG's bioactive compounds, presenting new opportunities for broadening their availability. Ultimately, this review emphasizes SG's value in food and medicine, showcasing its historical and cultural importance, phytochemistry, biological functions, action mechanisms, and the role of synthetic biology in its sustainable use.