Bioactive Compounds of Antrodia Fungi in Cancer Therapeutics

Antrodia species, notably Antrodia camphorata and Antrodia cinnamomea, have emerged as a rich source of chemically diverse metabolites with potent anticancer activities. These include triterpenoids such as antroquinonol, antcin A–K and eburicoic acid, benzoquinone derivatives, and high-molecular-weight polysaccharides. In vitro and in vivo studies demonstrate that these compounds induce apoptosis via both intrinsic and extrinsic pathways, arrest the cell cycle at G1/S or G2/M checkpoints, inhibit key kinases involved in survival and motility, and modulate the tumour microenvironment by downregulating matrix metalloproteinases. Moreover, certain metabolites exert epigenetic effects by reversing DNA hypermethylation of tumour suppressor genes, while others enhance ROS-mediated cytotoxicity selectively in cancer cells. Synergistic interactions with radiotherapy and conventional chemotherapeutics have also been reported, suggesting potential for combination regimens. Despite promising preclinical data, challenges remain in standardising fungal extracts, improving oral bioavailability, and conducting robust clinical trials. Continued elucidation of structure–activity relationships and advances in scalable fermentation are expected to foster translation of Antrodia-derived molecules into clinically viable cancer therapeutics.

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Bioactive Compounds of Antrodia Fungi in Cancer Therapeutics publication trend

The graph below shows the total number of articles in bioactive compounds of antrodia fungi in cancer therapeutics across all publications each year (not limited to Nature Index journals).

Technical terms

Sesquiterpene lactone: A class of terpenoid compounds characterised by a lactone ring, often responsible for modulation of signalling pathways in cancer cells.

Focal adhesion kinase (FAK): A non-receptor tyrosine kinase that regulates cell adhesion, migration and survival, frequently upregulated in tumour metastasis.

PI3K/AKT signalling pathway: A central intracellular cascade controlling cell growth, proliferation and survival, commonly dysregulated in cancer.

DNA hypermethylation: An epigenetic modification involving addition of methyl groups to cytosine residues in gene promoters, leading to transcriptional silencing of tumour suppressor genes.

CCND2 promoter: The regulatory DNA sequence upstream of the cyclin D2 gene; its methylation status influences cell-cycle progression at the G1/S checkpoint.

References

1. Review of Pharmacological Effects of Antrodia camphorata and Its Bioactive Compounds. Evidence-based Complementary and Alternative Medicine (2011).
2. Ethanol Extracts of Fruiting Bodies of Antrodia cinnamomea Suppress CL1‐5 Human Lung Adenocarcinoma Cells Migration by Inhibiting Matrix Metalloproteinase‐2/9 through ERK, JNK, p38, and PI3K/Akt Signaling Pathways. Evidence-based Complementary and Alternative Medicine (2012).
3. Antrocin Sensitizes Prostate Cancer Cells to Radiotherapy through Inhibiting PI3K/AKT and MAPK Signaling Pathways. Cancers (2018).