Epipolythiodioxopiperazines (ETPs), characterized by a unique bridged disulfide
or polysulfide dioxopiperazine six-membered ring (namely 2,5-epipolythiopepeazine-3,6-
dione ring system), occur in a diversity of fungi. In recent years, ETPs drawn increasing
research attentions from the field of chemistry and biological due to their broad spectra of
bioactivities including antitumor, antiviral and antimicrobial activities. From this point of
view, this review summarized diverse natural sources that produce ETPs, the synthetic
chemistry of ETPs and an overview of promising bioactivities exhibited by some well
studied ETPs. The plausible biosynthetic hypotheses of ETPs and some new results on
antitumor activity of ETPs are also reviewed.
Keywords: Epipolythiodioxopiperazine, Gliotoxin, Emestrin, Sporidesmin,
Aranotin, Epicorzine, Chaetocin, Verticillin, Leptosin, Sirodesmin, Bioactivities,
Biosynthesis.
