HDAC5 stabilization by tubeimoside I suppresses cervical cancer metastasis via inhibiting H3K27ac/KPNA2 axis

Br J Cancer. 2026 Mar;134(6):881-892. doi: 10.1038/s41416-025-03328-3. Epub 2026 Jan 8.

Abstract

Background: Cervical cancer poses a significant threat to women's health, and its metastasis is one of the leading causes of cancer-related deaths. Tubeimoside I (TBMS1) is a traditional Chinese medicinal herb with anticancer properties. We previously demonstrated the anticancer effect of TBMS1 in cervical cancer by inducing autophagy-related cell death. Nevertheless, whether and how TBMS1 prevents cervical cancer metastasis remain unclear.

Methods: Wound healing, transwell assays, and a lung metastasis mouse model were used to evaluate cell metastasis. Immunoprecipitation combined with site-directed mutagenesis was used to explore ubiquitination modifications and ubiquitinated sites of histone deacetylase 5 (HDAC5). HDAC5 depletion and RNA-seq analysis were conducted to investigate the anti-metastatic mechanism of TBMS1.

Results: We show that low dose of TBMS1 inhibits cervical cancer metastasis. Mechanistically, TBMS1 binds to HDAC5 and prevents HDAC5 ubiquitination at lysine 137 and 538, leading to a decrease in proteasomal degradation of HDAC5. TBMS1-mediated HDAC5 upregulation further reduces the acetylation level of histone H3 lysine 27 (H3K27ac) and suppresses KPNA2 expression. HDAC5 depletion significantly attenuates TBMS1's anti-metastatic effect in cervical cancer.

Conclusion: Our study reveals HDAC5/H3K27ac/KPNA2 axis as the anti-metastatic mechanism of TBMS1 in cervical cancer, suggesting TBMS1 serves as a promising drug for cervical cancer treatment.

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Histone Deacetylases* / genetics
  • Histone Deacetylases* / metabolism
  • Histones* / metabolism
  • Humans
  • Lung Neoplasms* / secondary
  • Mice
  • Mice, Nude
  • Neoplasm Metastasis
  • Saponins* / pharmacology
  • Triterpenes* / pharmacology
  • Ubiquitination / drug effects
  • Uterine Cervical Neoplasms* / drug therapy
  • Uterine Cervical Neoplasms* / genetics
  • Uterine Cervical Neoplasms* / metabolism
  • Uterine Cervical Neoplasms* / pathology
  • Xenograft Model Antitumor Assays

Substances

  • Histone Deacetylases
  • Histones
  • HDAC5 protein, human
  • Triterpenes
  • tubeimoside I
  • Saponins