Betulinic acid: a new
cytotoxic compound against malignant head and neck cancer cells.
Source
Department of Otorhinolaryngology, Head and
Neck Surgery, University Hospital Vienna, Währinger Gürtel 18-20, A-1090
Vienna, Austria. dietmar.thrunher@univie.ac.at
Abstract
BACKGROUND:
A new compound, betulinic acid, has been
found to be cytotoxic against a variety of tumor cells originating from the neural crest. Its efficacy against head and
neck squamous cellular carcinoma cell lines has so far not been tested.
METHODS:
Cell numbers were assayed by automated
counting; caspase activation and programmed cell death were determined using an
antibody specific for an apoptosis-associated epitope in epithelial cells. The
expression pattern of Bcl-2 family members was assessed by Western blotting.
RESULTS:
In two HNSCC cell lines betulinic acid
induced apoptosis, which was characterized by a dose-dependent reduction in
cell numbers, emergence of apoptotic cells, and an increase in caspase
activity. Western blot analysis of the expression of various Bcl-2 family
members in betulinic acid-treated cells showed, surprisingly, a suppression of
the expression of the proapoptotic protein Bax but no changes in Mcl-1 or Bcl-2
expression.
CONCLUSION:
These data clearly demonstrate for the first
time that betulinic acid has apoptotic activity against HNSCC cells.
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