1'-Acetoxychavicol acetate (ACA) is found in the rhizomes or seeds of Alpinia galanga and Alpinia conchigera, which are used as traditional spices in cooking and traditional medicines in Southeast Asia. ACA possesses numerous medicinal properties. Those include anticancer, anti-obesity, antiallergy, antimicrobial, antidiabetic, gastroprotective, and anti-inflammatory activities. ACA is also observed to exhibit antidementia activity. Recent studies have demonstrated that combining ACA with other substances results in synergistic anticancer effects. The structural factors which regulates the activity of ACA include: (1) the acetyl group at position 1', (2) the acetyl group at position 4, and (3) the unsaturated double bond between positions 2' and 3'. ACA induces the activation of AMPK, which regulates the signal transduction pathways, and has an important role for the prevention of diseases, including cancer, obesity, hyperlipidemia, diabetes, and neurodegenerative disorders. Such findings suggest that AMPK has a central role in different pharmacological functions of ACA, and ACA is useful for the prevention of life-threatening diseases. However, more studies should be performed to evaluate the clinical effects of ACA and to better understand its potential.