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Journal Article Ahead of print 1 citation

PubMed: 42530763 DOI: 10.1007/s11010-026-05675-y

Aurone analog LYK01 exerts oxidative stress-dependent antiproliferation, G2/M arrest, apoptosis, and DNA damage of oral cancer cells involving MAPK modulation.

Mol Cell Biochem

Authors: Yan-Ning Chen, Chia-Hung Yen, Ching-Yu Yen, Ammad Ahmad Farooqi, Meng-Yang Chang, Tsu-Ming Chien, Jen-Yang Tang, Hsueh-Wei Chang

Affiliations

  • Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
  • School of Dentistry, Taipei Medical University, Taipei, 11031, Taiwan.
  • Department of Oral and Maxillofacial Surgery, Chi-Mei Medical Center, Tainan, 71004, Taiwan.
  • Department of Molecular Oncology, Institute of Biomedical and Genetic Engineering (IBGE), Islamabad, Pakistan.
  • Department of Medicinal and Applied Chemistry, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
  • School of Post-Baccalaureate Medicine, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
  • Department of Urology, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
  • Department of Urology, Kaohsiung Gangshan Hospital, Kaohsiung Medical University, Kaohsiung, 820111, Taiwan.
  • School of Post-Baccalaureate Medicine, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
  • Department of Radiation Oncology, Kaohsiung Medical University Hospital, Kaohsiung, 80708, Taiwan.
  • Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
  • Department of Biomedical Science and Environmental Biology, College of Life Science, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
  • Department of Medical Research, Kaohsiung Medical University Hospital, Kaohsiung, 80708, Taiwan.
  • Center for Cancer Research and Research Center for Molecular Medicine, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.
  • Drug Development and Value Creation Research Center, Kaohsiung Medical University, Kaohsiung, 80708, Taiwan.

Abstract

Aurones are plant flavonoids that generally exhibit oxidative stress and anticancer properties. We developed a novel aurone analog, LYK01, but its biological effects have yet to be examined, particularly in relation to its anticancer functions. In our experiment, LYK01 inhibited the proliferation of four types of oral cancer cells with limited cytotoxicity to normal oral cells, attenuated by N-acetylcysteine (NAC), demonstrating a selective ability to kill oral cancer cells. Regarding NAC pretreatment, the LYK01-induced mechanisms were confirmed to be oxidative stress-dependent. Mechanistically, LYK01 triggers G2/M arrest, oxidative stress (ROS and MitoSOX), DNA damage (γH2AX), and extrinsic caspase 8/3-based apoptosis to a greater extent in oral cancer cells than normal cells. Regarding MAPK inhibitors for p38, JNK, and ERK, LYK01-induced antiproliferation and apoptosis in oral cancer cells were attenuated. In conclusion, LYK01 exhibits preferential antiproliferative effects in oral cancer cells -mediated by oxidative stress and MAPK-associated pathways-while exhibiting limited cytotoxicity toward normal cells. These findings warrant in vivo and translational validation.

MeSH

Cells, Acetylcysteine, Stress, Physiological, Neoplasms, Oxidative Stress, Apoptosis, Mouth Neoplasms, Dna Damage