Repurposing antitussive benproperine phosphate against pancreatic cancer depends on autophagy arrest

Mol Oncol. 2021 Feb;15(2):725-738. doi: 10.1002/1878-0261.12854. Epub 2020 Dec 12.

Abstract

Pancreatic cancer (PC) is one of the most common human malignancies worldwide and remains a major clinical challenge. Here, we found that benproperine phosphate (BPP), a cough suppressant, showed a significant anticancer effect on PC both in vitro and in vivo via the induction of autophagy-mediated cell death. Mechanistic studies revealed that BPP triggered AMPK/mTOR-mediated autophagy initiation and disturbed Ras-related protein Rab-11A (RAB11A)-mediated autophagosome-lysosome fusion, resulting in excessive accumulation of autophagosomes. Inhibition of autophagy or overexpression of RAB11A partially reversed BPP-induced growth inhibition in PC cells, suggesting that BPP might induce lethal autophagy arrest in PC cells. In conclusion, our results identify BPP as a potent antitumor agent for PC via the induction of autophagy arrest, therefore providing a new potential therapeutic strategy for the treatment of PC.

Keywords: RAB11A; autophagy arrest; benproperine phosphate; drug repurposing; pancreatic cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antitussive Agents / pharmacology*
  • Autophagy / drug effects*
  • Benzhydryl Compounds / pharmacology*
  • Cell Line, Tumor
  • Drug Repositioning*
  • Humans
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Pancreatic Neoplasms* / drug therapy
  • Pancreatic Neoplasms* / metabolism
  • Pancreatic Neoplasms* / pathology
  • Piperidines / pharmacology*
  • Xenograft Model Antitumor Assays

Substances

  • Antitussive Agents
  • Benzhydryl Compounds
  • Piperidines
  • benproperine