Background: Like the impressive biological properties of embelin, its chemical
aspects have raised the interest of scientists in the field as well. A detailed understanding
of the chemistry of embelin is necessary to fully exploit it medicinally.
Methods: Search for embelin isolation and its chemical modifications was carried out using
web-based literature searching tools such as Pubmed and Scifinder. Pertinent literature
is covered up to 2016. Structures of bioactive embelin derivatives are provided.
Results: Pure embelin, obtained from Embelia ribes
berries extraction or by total synthesis,
was applied for a number of biological assays. Semi-synthetic and total synthetic approaches
led to new high affinity embelin-derived inhibitors of crucial protein targets and
to new embelin derivatives with improved pharmacological properties (e.g.
, with better
water-solubility or as applications for drug carrier systems).
Conclusion: This review provides a summary of the rich chemistry of embelin and the
latest developments in the field of optimized (semi-)synthetic embelin derivatives including
their biological activities.