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Anti-Xanthine Oxidase 5′-Hydroxyhericenes A–D from the Edible Mushroom Hericium erinaceus and Structure Revision of 3-[2,3-Dihydroxy-4-(hydroxymethyl)tetrahydrofuran-1-yl]-pyridine-4,5-diol

Summary

Researchers isolated new compounds from Lion’s mane mushroom (Hericium erinaceus) that can inhibit xanthine oxidase, an enzyme linked to breast cancer development. One compound called hericerin showed strong activity against a specific type of breast cancer cell (T47D cells) while being less harmful to normal cells. The study also corrected a misidentification from previous research, confirming that a compound previously thought to have a different structure was actually adenosine. These findings suggest Lion’s mane could be developed into a natural anti-cancer treatment.

Background

Hericium erinaceus is an edible mushroom known for diverse pharmaceutical applications and health-promoting effects. The mushroom contains bioactive compounds including polysaccharides, geranyl-resorcinols, and cyathane terpenoids with various biological activities. Breast cancer remains a leading cause of death worldwide, prompting the search for natural product-based therapeutic agents.

Objective

This study aimed to isolate and characterize bioactive compounds from H. erinaceus fruiting bodies and evaluate their anti-cancer and xanthine oxidase inhibitory activities. The research also sought to revise the structure of a previously misidentified natural product isolated from multiple organisms and plants.

Results

Four new compounds (5′-hydroxyhericenes A–D, 1–4) were isolated along with twelve known compounds. Compounds 1–4 inhibited xanthine oxidase with IC50 of 7.3 ± 0.6 μg/mL. Compounds 6, 9, and 10 scavenged reactive oxygen species generated by xanthine oxidase. Hericerin (13) demonstrated strong growth inhibitory activity against T47D breast cancer cells (IC50 5.9 ± 1.6 μM) and weaker activity against MDA-MB-231 cells and normal MRC-5 cells.

Conclusion

The bioactive compounds from H. erinaceus hold promise as potential anti-breast cancer agents, particularly for progesterone-sensitive cancer cells. The structure revision of compound 5 to adenosine clarifies misidentifications in previous research. The combined effects of multiple bioactive compounds in the mushroom may inhibit cancer cell growth while reducing uric acid levels and potentially suppressing metastasis.
  • Published in:ACS Omega,
  • Study Type:Natural Product Isolation and Characterization Study,
  • Source: 10.1021/acsomega.3c07792, PMID: 38075774
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