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Background <p>Recent studies have highlighted the pharmaceutical potential of lichen extracts, particularly with respect to their anticancer properties. Lichens, symbiotic organisms composed of fungi and algae or cyanobacteria, have long been utilized in traditional medicine. Accumulating evidence from recent investigations further supports the potential therapeutic applications of lichen-derived compounds in a variety of diseases, including cancer.</p> Objective <p>The study aimed to investigate the anticancer activity of himantormione B, a newly identified secondary metabolite isolated from the Antarctic lichen <i>Himantormia lugubris</i>, in the human colorectal cancer cell lines HCT116 and HT-29.</p> Methods <p>Cell viability was assessed using an MTS assay in MRC-5, HCT116, and HT-29 cells. Quantitative reverse transcription–polymerase chain reaction (qRT–PCR) and immunoblot analyses were performed to evaluate the expression levels of apoptosis-related genes, including <i>BAX</i>, <i>BCL2</i>, <i>PUMA</i>, and <i>CASP3</i>. To further investigate the apoptotic effects of himantormione B in HCT116 and HT-29 cells, cells were stained with Annexin V–FITC and propidium iodide (PI), followed by flow cytometric analysis (FACS). In addition, in silico ADMET analyses were conducted to determine whether himantormione B exhibits favorable drug-like properties and promising pharmacological potential.</p> Results <p>Based on our results, himantormione B exerted a significant cytotoxic effect on colorectal cancer cells compared with MRC-5 normal fibroblasts. Moreover, himantormione B induced apoptosis in a concentration-dependent manner by modulating the expression of apoptosis-related genes, including <i>BAX</i>, <i>BCL-2</i>, <i>PUMA</i>, and <i>CASP3</i>. Specifically, treatment with himantormione B significantly downregulated the expression of the anti-apoptotic gene <i>BCL-2</i>, while concomitantly upregulating the expression of the pro-apoptotic genes <i>BAX</i> and <i>PUMA</i>. In agreement with the flow cytometric analysis demonstrating himantormione B-induced apoptosis, we further observed a dose-dependent increase in cleaved caspase-3 levels. Given that caspase-3 is a key executioner caspase that promotes apoptotic progression and suppresses cell survival, these findings collectively indicate that himantormione B induces apoptosis via activation of the intrinsic apoptotic signaling pathway.</p> Conclusion <p>Taken together, the present study provides a comprehensive evaluation of the anticancer activity of himantormione B in colorectal cancer, highlighting its potential as a promising therapeutic candidate for targeted treatment strategies.</p>

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Anticancer activity of himantormione B: a new depsidone from the Antarctic lichen Himantormia lugubris, in colorectal cancer

  • 期刊论文

  • 发表日期：

    2026年3月31日

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  • Hae-Jung Chae,
  • Min-Ji Shin,
  • Man Hyung Koo,
  • Jong Bae Seo,
  • Ui Joung Youn,
  • Sung-Suk Suh

摘要

Background

Recent studies have highlighted the pharmaceutical potential of lichen extracts, particularly with respect to their anticancer properties. Lichens, symbiotic organisms composed of fungi and algae or cyanobacteria, have long been utilized in traditional medicine. Accumulating evidence from recent investigations further supports the potential therapeutic applications of lichen-derived compounds in a variety of diseases, including cancer.

Objective

The study aimed to investigate the anticancer activity of himantormione B, a newly identified secondary metabolite isolated from the Antarctic lichen Himantormia lugubris, in the human colorectal cancer cell lines HCT116 and HT-29.

Methods

Cell viability was assessed using an MTS assay in MRC-5, HCT116, and HT-29 cells. Quantitative reverse transcription–polymerase chain reaction (qRT–PCR) and immunoblot analyses were performed to evaluate the expression levels of apoptosis-related genes, including BAX, BCL2, PUMA, and CASP3. To further investigate the apoptotic effects of himantormione B in HCT116 and HT-29 cells, cells were stained with Annexin V–FITC and propidium iodide (PI), followed by flow cytometric analysis (FACS). In addition, in silico ADMET analyses were conducted to determine whether himantormione B exhibits favorable drug-like properties and promising pharmacological potential.

Results

Based on our results, himantormione B exerted a significant cytotoxic effect on colorectal cancer cells compared with MRC-5 normal fibroblasts. Moreover, himantormione B induced apoptosis in a concentration-dependent manner by modulating the expression of apoptosis-related genes, including BAX, BCL-2, PUMA, and CASP3. Specifically, treatment with himantormione B significantly downregulated the expression of the anti-apoptotic gene BCL-2, while concomitantly upregulating the expression of the pro-apoptotic genes BAX and PUMA. In agreement with the flow cytometric analysis demonstrating himantormione B-induced apoptosis, we further observed a dose-dependent increase in cleaved caspase-3 levels. Given that caspase-3 is a key executioner caspase that promotes apoptotic progression and suppresses cell survival, these findings collectively indicate that himantormione B induces apoptosis via activation of the intrinsic apoptotic signaling pathway.

Conclusion

Taken together, the present study provides a comprehensive evaluation of the anticancer activity of himantormione B in colorectal cancer, highlighting its potential as a promising therapeutic candidate for targeted treatment strategies.