Betulinic acid-induced mitochondria-dependent cell death is counterbalanced by an autophagic salvage response

Cell Death Dis. 2014 Apr 10;5(4):e1169. doi: 10.1038/cddis.2014.139.

Abstract

Betulinic acid (BetA) is a plant-derived pentacyclic triterpenoid that exerts potent anti-cancer effects in vitro and in vivo. It was shown to induce apoptosis via a direct effect on mitochondria. This is largely independent of proapoptotic BAK and BAX, but can be inhibited by cyclosporin A (CsA), an inhibitor of the permeability transition (PT) pore. Here we show that blocking apoptosis with general caspase inhibitors did not prevent cell death, indicating that alternative, caspase-independent cell death pathways were activated. BetA did not induce necroptosis, but we observed a strong induction of autophagy in several cancer cell lines. Autophagy was functional as shown by enhanced flux and degradation of long-lived proteins. BetA-induced autophagy could be blocked, just like apoptosis, with CsA, suggesting that autophagy is activated as a response to the mitochondrial damage inflicted by BetA. As both a survival and cell death role have been attributed to autophagy, autophagy-deficient tumor cells and mouse embryo fibroblasts were analyzed to determine the role of autophagy in BetA-induced cell death. This clearly established BetA-induced autophagy as a survival mechanism and indicates that BetA utilizes an as yet-undefined mechanism to kill cancer cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Autophagy / drug effects*
  • Betulinic Acid
  • Cell Line, Tumor
  • Cyclosporine / pharmacology
  • Humans
  • Mice
  • Mitochondria / drug effects
  • Mitochondria / metabolism*
  • Necrosis
  • Pentacyclic Triterpenes
  • Signal Transduction / drug effects
  • Triterpenes / pharmacology*

Substances

  • Pentacyclic Triterpenes
  • Triterpenes
  • Cyclosporine
  • Betulinic Acid