Pityriacitrin is a natural marine alkaloid with a typical β-carboline scaffold, and which has
been demonstrated to exhibit diverse biological functions. The special structural features for pityriacitrin
lead to the increasing research interest and the emergence of versatile derivatives, and many
pityriacitrin analogues have been isolated or synthesized over the past decades. The structural diversity
and evolved biological activity of these natural alkaloids can offer opportunities for the development
of highly potential novel drugs with a new mechanism of action, and therefore, the aim of this
brief review is to describe the discovery, synthesis, and biological properties of natural pityriacitrin
and its derivatives, as well as the isolation source.