The chemistry and biology of fungal meroterpenoids (2009-2019)

Org Biomol Chem. 2021 Mar 4;19(8):1644-1704. doi: 10.1039/d0ob02162h.


Fungal meroterpenoids are secondary metabolites from mixed terpene-biosynthetic origins. Their intriguing chemical structural diversification and complexity, potential bioactivities, and pharmacological significance make them attractive targets in natural product chemistry, organic synthesis, and biosynthesis. This review provides a systematic overview of the isolation, chemical structural features, biological activities, and fungal biodiversity of 1585 novel meroterpenoids from 79 genera terrestrial and marine-derived fungi including macrofungi, Basidiomycetes, in 441 research papers in 2009-2019. Based on the nonterpenoid starting moiety in their biosynthesis pathway, meroterpenoids were classified into four categories (polyketide-terpenoid, indole-, shikimate-, and miscellaneous-) with polyketide-terpenoids (mainly tetraketide-) and shikimate-terpenoids as the primary source. Basidiomycota produced 37.5% of meroterpenoids, mostly shikimate-terpenoids. The genera of Ganoderma, Penicillium, Aspergillus, and Stachybotrys are the four dominant producers. Moreover, about 56% of meroterpenoids display various pronounced bioactivities, including cytotoxicity, enzyme inhibition, antibacterial, anti-inflammatory, antiviral, antifungal activities. It's exciting that several meroterpenoids including antroquinonol and 4-acetyl antroquinonol B were developed into phase II clinically used drugs. We assume that the chemical diversity and therapeutic potential of these fungal meroterpenoids will provide biologists and medicinal chemists with a large promising sustainable treasure-trove for drug discovery.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Fungi / chemistry*
  • Humans
  • Terpenes / chemistry*
  • Terpenes / isolation & purification
  • Terpenes / pharmacology*


  • Terpenes