Epigallocatechin-3-gallate (EGCG), one of the important catechins in tea, is reported to have a variety of bioactivities. However, EGCG is not fully utilized due to its poor liposolubility and stability, as well as low bioavailability. Acetylation modification of EGCG is an effective method to improve these limitations. Total acetylated epigallocatechin gallate (AcEGCG) is the fully acetylated product of EGCG. Compared to EGCG, AcEGCG has higher liposolubility, stability and bioavailability. Moreover, its physiological functions, such as anti-ultraviolet, cell damage repair and anti-cancer functions, are better than those of EGCG, suggesting a wide range of application prospects in the fields of food, medicine and chemical industry. This review will summarize recent advances in the synthesis, purification, physicochemical properties and bioactivities of AcEGCG, in order to provide a reference for further research, development and utilization of AcEGCG.