PMID: 16712455 [PubMed - indexed for MEDLINE]
[iii] Honda T, Liby KT, Su
X, Sundararajan C, Honda Y, Suh N, Risingsong R, Williams CR, Royce DB, Sporn
MB, Gribble GW. Related Articles, Links Design,
synthesis, and anti-inflammatory activity both in vitro and in vivo of new
betulinic acid analogues having an enone functionality in ring A.
Bioorg
Med Chem Lett. 2006 Dec 15;16(24):6306-9. Epub 2006 Sep 25.
PMID: 16996735 [PubMed - in process]
PMID: 16996735 [PubMed - in process]
Broad
in vitro efficacy of plant-derived betulinic acid against cell lines derived
from the most prevalent human cancer types.
Laboratory for Experimental Oncology and
Radiobiology (LEXOR), Center for Experimental and Molecular Medicine, Academic
Medical Center (AMC), Meibergdreef 9, 1105 AZ Amsterdam , The Netherlands .
Betulinic acid (BA) is a widely available
plant-derived triterpene with reported activity against cancer cells of
neuroectodermal origin and leukaemias .
Treatment with BA was shown to protect mice against transplanted human melanoma
and led to tumor regression. In contrast, cells from healthy tissues were
resistant to BA and toxic side-effects in animals were absent. These
findings have raised interest in the chemotherapeutical anti-cancer potential
of BA. A comprehensive assessment of the efficacy of BA against the clinically
most important cancer types is currently lacking. Therefore, we tested the in vitro sensitivity of
broad cell line panels derived from lung, colorectal, breast, prostate and
cervical cancer, which are the prevalent cancer types characterized with
highest mortalities in woman and men. Multiple assays were used
in order to allow a reliable assessment of anti-cancer efficacy of BA. After
48h of treatment with BA, cell viability as assessed with MTT and cell death as
measured with propidium iodide exclusion showed clear differences in
sensitivity between cell lines. However, in all cell lines tested colony
formation was completely halted at remarkably equal BA concentrations that are
likely attainable in vivo. Our
results substantiate the possible application of BA as a chemotherapeutic agent
for the most prevalent human cancer types.
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