Physalin A is one of the main active constituents of Physalis alkekengi L.var. franchetii (Mast.) Makino which possesses excellent anti-tumor and anti-inflammatory activities. Pharmacological researches showed that physalin A exerted anti-inflammatory effects via significantly inhibiting the production of nitric oxide in macrophages induced by lipopolysaccharide and its mechanism of action may be related to its inhibition of NF-κB activity by modifying IκB kinase β. Additionally, physalin A obviously inhibits the growth of melanoma, non-small cell lung cancer, prostate cancer, and liver cancer tumor cells and its anti-tumor mechanism may be related to its ability to induce tumor cell apoptosis and inhibit JAK/STAT 3 signaling. This article reviews the pharmacological effects of physalin A to provide literature references for the further development and application of physalin A.