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<i>Ficus pumila</i> L. has been used as a functional plant for a long time in East Asia, especially its fruits, as a dietary component in Japan and parts of China. A series of bioactive compounds, including phenolic acids, flavonoids, terpenoids, alcohols, and steroids, have been extracted from the stems, leaves, flowers, and fruits of <i>Ficus pumila</i> L. Accumulated studies have demonstrated that <i>Ficus pumila</i> L. has multiple therapeutic activities, including antioxidant, anti-inflammatory, antibacterial, antitumor, hypoglycemic, and cardiovascular protective effects. Moreover, <i>Ficus pumila</i> L. has extensive applications, such as in the food industry and ecological city construction. Herein, we summarize the latest knowledge about the bioactive compounds and therapeutic activities of <i>Ficus pumila</i> L., and its applications in the food industry and ecological city construction are also discussed. We hope that this comprehensive review can attract more attention to <i>Ficus pumila</i> L. and be helpful for its further applications.