Higher fungi are characterised by the production of macroscopic fruiting bo
dies to generate and to distribute their spores. These fruiting bodies are
under constant threat of other organisms feeding on them. As a consequence
these organisms developed a number of strategies for protection, one of the
m is the production of toxins. The fungal subdivision Basidiomycotina produ
ce toxic sesquiterpenes many of them are derived from the protoilludane ske
leton. This skeleton is transformed and rearranged to a large number of com
pounds. Some of these sesquiterpenes show interesting biological properties
which may be attractive for medicinal chemistry.
The overview describes the different types of bioactive fungal sesquiterpen
es derived from humulene known to date in Basidiomycotina and their formati
on. The metabolites are discussed according to their sesquiterpene skeleton
and the different metabolites are compared. Where available biological act
ivities concerning antifungal, antibacterial, cytotoxic and enzyme inhibiti
on data are given. Special attention was paid for the different activities
of these metabolites and the attempts made to use them in medicinal chemist
ry. The question whether metabolites produced for the self-protection of fu
ngi can be used for pharmaceutical applications for humans will be adressed
and discussed.