Embelin is a naturally occurring para-benzoquinone isolated from Embelia ribes (Burm. f.)
of the Myrsinaceae family, and contains two carbonyl groups, a methine group and two hydroxyl
groups. With embelin as the lead compound, more than one hundred derivatives have been reported.
Embelin is well known for its ability to antagonize the X-linked inhibitor of apoptosis protein (XIAP)
with an IC50 value of 4.1 μM. The potential of embelin and its derivatives in the treatment of various
cancers has been extensively studied. In addition, these compounds display a variety of other biological
effects: antimicrobial, antioxidant, analgesic, anti-inflammatory, anxiolytic and antifertility activity.
This paper reviews the recent progress in the synthesis and biological activity of embelin and its derivatives.
Their cellular mechanisms of action and prospects in the research and development of new
drugs are also discussed.