Abstract: Artemisinic acid (AA) and dihydroartemisinic acid (DHAA) were isolated from Artemisia annua L., and were used as key precursors for the synthesis of artemisinin. AA and DHAA can be obtained through plant extraction, chemical synthesis, or biosynthesis. Due to their activities in inhibiting melanin, lowering fat, anti-inflammatory, and anti-glycation, AA and DHAA have attracted increasing attention in the field of medicine and cosmetics. This article reviews recent research progress in the preparation, structural modification, and evaluation of biological activity of AA and DHAA, aiming to provide systematic literature support and future research directions for the semi-synthesis of artemisinin from AA and DHAA, the direct utilization of AA and DHAA, and the development and utilization of its structural modifications.