The Novel Autophagy Inhibitor Alpha-Hederin Promoted Paclitaxel Cytotoxicity by Increasing Reactive Oxygen Species Accumulation in Non-Small Cell Lung Cancer Cells

Int J Mol Sci. 2018 Oct 18;19(10):3221. doi: 10.3390/ijms19103221.

Abstract

Chemoresistance is a major limiting factor that impairs the outcome of non-small cell lung cancer (NSCLC) chemotherapy. Paclitaxel (Tax) induces protective autophagy in NSCLC cells, leading to the development of drug resistance. We recently identified a new autophagy inhibitor (alpha-hederin) and hypothesized that it may promote the killing effect of Tax on NSCLC cells. We found that alpha-hederin (α-Hed) could block late autophagic flux in NSCLC cells by altering lysosomal pH and inhibiting lysosomal cathepsin D maturation. Combination treatment of α-Hed and Tax synergistically reduced NSCLC cell proliferation and increased NSCLC cell apoptosis compared with treatment with α-Hed or Tax alone. Furthermore, α-Hed plus Tax enhanced the accumulation of intracellular reactive oxygen species (ROS) in NSCLC cells, while the ROS inhibitor N-acetylcysteine reversed the inhibitory effect of the combination treatment. Our findings suggest that α-Hed can increase the killing effect of Tax on NSCLC cells by promoting ROS accumulation, and that combining α-Hed with classical Tax represents a novel strategy for treating NSCLC.

Keywords: alpha-hederin; autophagy inhibition; chemotherapy; non-small cell lung cancer; paclitaxel; synergistic effect.

MeSH terms

  • Apoptosis / drug effects
  • Autophagosomes / metabolism
  • Autophagy*
  • Carcinoma, Non-Small-Cell Lung / metabolism*
  • Cathepsins / metabolism
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Humans
  • Hydrogen-Ion Concentration
  • Lung Neoplasms / metabolism*
  • Lysosomes / metabolism
  • Oleanolic Acid / analogs & derivatives*
  • Oleanolic Acid / metabolism
  • Paclitaxel / chemistry
  • Paclitaxel / pharmacology*
  • Reactive Oxygen Species / metabolism*
  • Saponins / metabolism*
  • Tubulin Modulators / chemistry
  • Tubulin Modulators / pharmacology

Substances

  • Reactive Oxygen Species
  • Saponins
  • Tubulin Modulators
  • beta-hederin
  • Oleanolic Acid
  • Cathepsins
  • Paclitaxel