The prospection of unusual sources and undiscovered habitats is valuable
in natural product research. Indeed, the fungi kingdom has received special attention
since its ability to produce novel and intriguing secondary metabolites with various biological uses. Among secondary metabolites, alkaloid-derived structures present a
wide range of bioactivities, including antineurodegenerative, antidepressive, anxiolytic,
anti-inflammatory, cytotoxic, and insecticidal properties. Furthermore, various
studies showed particular properties of those alkaloids in reducing nicotine addiction
and alcohol dependence. Alkaloids are categorized into several groups based on their
heterocyclic ring system and biosynthetic precursor, such as indole, isoxazoles, and
muscarine. Therefore, this chapter focuses on those fungi’s bioactive alkaloids with
emphasis on pharmacokinetics as well as the current analytical approaches for
extraction and compound identification. Furthermore, the main biological activities
and action mechanisms of these fungus alkaloids will also be discussed.