Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells
Abstract
In the present investigation the antiproliferative
activity of thirteen derivatives of betulinic acid and
betulin was tested against five different tumor cell lines.
The toxicity against normal human fibroblasts
(WWO70327) and the mode of cell death on HT-29
(colon cancer) as well as caspase activity induced by the
most active compounds, 9 (3-O-chloroacetylbetulinic
acid) and 15 (28-O-chloroacetylbetulin) were determined.
Investigated derivatives exerted a dose dependent antiproliferative
action at micromolar concentrations toward
target tumor cell lines. Treatment of HT-29 cells for 24 h
with 9 and 15 induced apoptosis, as observed by dye
exclusion test (trypan blue) and confirmed by the
appearance of a typical ladder pattern in the DNA
fragmentation assay.
Keywords:
Caspase activity / Cytotoxicity / Apoptosis / Natural products / Betulin / Betulinic acidSource:
Investigational New Drugs, 2011, 29, 2, 266-272Publisher:
- Netherlands : Springer
Projects:
- The authors are grateful to the Wirtschaftsministerium Sachsen-Anhalt for financial support (Antitumor drugs on the basis of natural compounds FuE 62/05).
DOI: 10.1007/s10637-009-9358-x
ISSN: 01676997; 1573-0646
PubMed: 19957199