This review focuses on the major developments in
depsipeptide research since 1995.
Depsipeptides are bio-oligomers composed of hydroxy and
amino acids linked by
amide and
ester bonds. Many
depsipeptides show very promising
biological activities, including anticancer, antibacterial,
antiviral, antifungal, anti-inflammatory, and anti-clotting or anti-antherogenic properties. In this report
depsipeptides exhibiting these properties are discussed. Their isolation, structural determination, and notable structural features are discussed, but their
biological properties and therapeutic potentials are emphasized.
Depsipeptides have shown the greatest therapeutic potential as
anticancer agents. Four
depsipeptides have entered clinical trials for
cancer treatment. Among the
antiviral compounds discovered, the callipeltins and the quinoxapeptins are particularly promising due to their inhibitory activities against HIV. These compounds have the potential to be developed as
anti-AIDS drugs or to serve as lead compounds for the discovery of structurally related anti-
AIDS compounds. Antifungal compounds, such as the jaspamides, may lead to
therapies against many of the
opportunistic infections that accompany
AIDS. Anti-inflammatory compounds such as SCH217048 act as neurokinin antagonists and may lead to anti-inflammatory treatments. Some
depsipeptides such as micropeptins and
A90720A have been found to be effective
plasmin inhibitors, which have implications as treatments for
cardiovascular diseases. Compounds such as SCH58149 help control the levels of HDL and
LDL.