Subcellular Localization and Activity of Gambogic Acid

Gianni Guizzunti, Ayse Batova, Oraphin Chantarasriwong, Marianna Dakanali, Emmanuel A. Theodorakis

Research output: Contribution to journalArticlepeer-review

20 Scopus citations


The natural product gambogic acid (GA) has shown significant potential as an anticancer agent as it is able to induce apoptosis in multiple tumor cell lines, including multidrug-resistant cell lines, as well as displaying antitumor activity in animal models. Despite the fact that GA has entered phase I clinical trials, the primary cellular target and mode of action of this compound remain unclear, although many proteins have been shown to be affected by it. By thorough analysis of several cellular organelles, at both the morphological and functional levels, we demonstrate that the primary effect of GA is at the mitochondria. We found that GA induces mitochondrial damage within minutes of incubation at low-micromolar concentrations. Moreover, a fluorescent derivative of GA was able to localize specifically to the mitochondria and was displaced from these organelles after competition with unlabeled GA. These findings indicate that GA directly targets the mitochondria to induce the intrinsic pathway of apoptosis, and thus represents a new member of the mitocans.

Original languageEnglish (US)
Pages (from-to)1191-1198
Number of pages8
Issue number8
StatePublished - May 2012


  • Apoptosis
  • Caged Garcinia xanthone
  • Membranes
  • Mitocan
  • Mitochondria

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Organic Chemistry


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