3-Butylidenephthalide is a gamma-lactone isolated from Angelica sinensis, which is used to treat anemia and gynecological dysfunction in traditional Chinese medicine. 3-Butylidenephthalide is a natural liposoluble compound with a low molecular weight that possesses multiple pharmacological activities, such as reducing injury and fibrosis in the liver and neuroprotective activity. 3-Butylidenephthalide exerts cytotoxic or inhibitory effects on various cancers, including brain, lung, colon, prostate, and liver cancers.