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Peer-reviewedCC BY 4.0Molecules

Coumarin–Ferulic Acid Hybrid Mediates HT-29-Selective Growth Inhibition and Proteomic Profiling

  • Sucheewin Krobthong1
  • Meng Chieh Yang1
  • Pattarawit Rukthong2,3
  • Satsawat Visansirikul4,5
  • Kittisak Sripha4,5
  • Arnatchai Maiuthed1,6
6 affiliations
  1. 1Centre of Biopharmaceutical Science for Healthy Ageing, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
  2. 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Srinakharinwirot University, Ongkharak, Nakhonnayok 25120, Thailand
  3. 3Center for Excellence in Plant and Herbal Innovation Research, Strategic Wisdom and Research Institute, Srinakharinwirot University, Nakornnayok 26120, Thailand
  4. 4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mahidol University, Si Ayutthaya Rd, Bangkok 10400, Thailand
  5. 5Unit of Compound Library for Drug Discovery, Mahidol University, Bangkok 10400, Thailand
  6. 6Department of Pharmacology, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
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Abstract

Coumarin-based molecular hybrids provide a framework for examining how structural changes influence cellular responses. This study compared four hybrids and three reference compounds across ten human cancer cell lines, with the lead hybrid also tested in non-cancerous Beas-2B cells, followed by functional assays and quantitative expression proteomics in HT-29 cells. Of 70 compound–cell-line combinations, the ferulic ester hybrid (FEC) was the only compound to yield a reproducibly measurable IC50 within the primary screening range, reaching 42.8 ± 4.7 µM in HT-29 cells. Replacing the ferulic moiety or the ester linkage reduced activity within this series. HCT116 cells did not reach 50% inhibition at up to 100 µM. Basal PPARγ abundance did not consistently explain sensitivity across the panel. FEC reduced metabolic activity and colony formation, whereas annexin V/propidium iodide analysis showed a smaller apoptotic response. Proteomics identified coordinated decreases in DNA replication and translation proteins and a modest increase in endoplasmic reticulum protein-folding enzymes. These findings support a structure-dependent and cell-context-dependent antiproliferative response despite moderate potency.

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Cite

BibTeXRIS
BibTeX
@article{krobthong2026coumarinferulic,
  title = {{Coumarin–Ferulic Acid Hybrid Mediates HT-29-Selective Growth Inhibition and Proteomic Profiling}},
  author = {Sucheewin Krobthong and Meng Chieh Yang and Pattarawit Rukthong and Satsawat Visansirikul and Kittisak Sripha and Arnatchai Maiuthed},
  journal = {Molecules},
  year = {2026},
  month = oct,
  doi = {10.3390/molecules31203729},
  url = {https://www.mdpi.com/1420-3049/31/20/3729},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - Coumarin–Ferulic Acid Hybrid Mediates HT-29-Selective Growth Inhibition and Proteomic Profiling
AU  - Sucheewin Krobthong
AU  - Meng Chieh Yang
AU  - Pattarawit Rukthong
AU  - Satsawat Visansirikul
AU  - Kittisak Sripha
AU  - Arnatchai Maiuthed
PY  - 2026
DA  - 2026/10/01
JO  - Molecules
DO  - 10.3390/molecules31203729
UR  - https://www.mdpi.com/1420-3049/31/20/3729
AB  - Coumarin-based molecular hybrids provide a framework for examining how structural changes influence cellular responses. This study compared four hybrids and three reference compounds across ten human cancer cell lines, with the lead hybrid also tested in non-cancerous Beas-2B cells, followed by functional assays and quantitative expression proteomics in HT-29 cells. Of 70 compound–cell-line combinations, the ferulic ester hybrid (FEC) was the only compound to yield a reproducibly measurable IC50 within the primary screening range, reaching 42.8 ± 4.7 µM in HT-29 cells. Replacing the ferulic moiety or the ester linkage reduced activity within this series. HCT116 cells did not reach 50% inhibition at up to 100 µM. Basal PPARγ abundance did not consistently explain sensitivity across the panel. FEC reduced metabolic activity and colony formation, whereas annexin V/propidium iodide analysis showed a smaller apoptotic response. Proteomics identified coordinated decreases in DNA replication and translation proteins and a modest increase in endoplasmic reticulum protein-folding enzymes. These findings support a structure-dependent and cell-context-dependent antiproliferative response despite moderate potency.
SN  - 1420-3049
ER  -