(-)-Gossypol enhances the anticancer activity of epirubicin via downregulating survivin in hepatocellular carcinoma

Chem Biol Interact. 2022 Sep 1:364:110060. doi: 10.1016/j.cbi.2022.110060. Epub 2022 Jul 22.

Abstract

Epirubicin (EPI)-based transarterial chemoembolization is an effective therapy for advanced hepatocellular carcinoma (HCC). However, EPI-induced survivin expression limits its tumor-killing potential in HCC. Interestingly, (-)-gossypol ((-)-Gsp), a male contraceptive, suppresses various malignancies. More importantly, (-)-Gsp also holds promise for enhancing the antitumor effects of chemotherapy in numerous cancer types. In the present study, we demonstrated for the first time that (-)-Gsp-sensitized EPI inhibited cell growth and induced apoptosis of HCC cells in vitro. Furthermore, (-)-Gsp sensitized EPI by attenuating the EPI-elevated survivin protein levels. Mechanistic studies showed that EPI stimulated survivin protein synthesis by promoting translation initiation, which was alleviated by (-)-Gsp mainly through suppressing the AKT-4EBP1/p70S6K-survivin and ERK-4EBP1-survivin pathways. HCC xenograft experiments in nude mice also showed that (-)-Gsp treatment acted synergistically with EPI to repress xenograft tumor growth. Overall, our proof-of-concept results may pave the way for novel strategies for the treatment of HCC based on the combination of EPI and (-)-Gsp.

Keywords: (−)-Gossypol; Epirubicin; Hepatocellular carcinoma; Sensitization; Survivin.

MeSH terms

  • Animals
  • Apoptosis
  • Carcinoma, Hepatocellular* / pathology
  • Cell Line, Tumor
  • Chemoembolization, Therapeutic*
  • Epirubicin / pharmacology
  • Epirubicin / therapeutic use
  • Gossypol*
  • Humans
  • Inhibitor of Apoptosis Proteins / metabolism
  • Liver Neoplasms* / metabolism
  • Male
  • Mice
  • Mice, Nude
  • Survivin
  • Xenograft Model Antitumor Assays

Substances

  • Inhibitor of Apoptosis Proteins
  • Survivin
  • Epirubicin
  • Gossypol