Betulin is a potent anti-tumor agent that is enhanced by cholesterol.

Betulinic Acid (BetA) and its derivatives have been extensively studied in the past for their anti-tumor effects, but relatively little is known about its precursor Betulin (BE). We found that BE induces apoptosis utilizing a similar mechanism as BetA and is prevented by cyclosporin A (CsA). BE indu...

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Main Authors: Franziska B Mullauer, Jan H Kessler, Jan Paul Medema
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2009-01-01
Series:PLoS ONE
Online Access:http://europepmc.org/articles/PMC2671171?pdf=render
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author Franziska B Mullauer
Jan H Kessler
Jan Paul Medema
author_facet Franziska B Mullauer
Jan H Kessler
Jan Paul Medema
author_sort Franziska B Mullauer
collection DOAJ
description Betulinic Acid (BetA) and its derivatives have been extensively studied in the past for their anti-tumor effects, but relatively little is known about its precursor Betulin (BE). We found that BE induces apoptosis utilizing a similar mechanism as BetA and is prevented by cyclosporin A (CsA). BE induces cell death more rapidly as compared to BetA, but to achieve similar amounts of cell death a considerably higher concentration of BE is needed. Interestingly, we observed that cholesterol sensitized cells to BE-induced apoptosis, while there was no effect of cholesterol when combined with BetA. Despite the significantly enhanced cytotoxicity, the mode of cell death was not changed as CsA completely abrogated cell death. These results indicate that BE has potent anti-tumor activity especially in combination with cholesterol.
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spelling doaj.art-ffaed2f660ef45ada4c5615ad1e62d372022-12-22T00:53:14ZengPublic Library of Science (PLoS)PLoS ONE1932-62032009-01-0144e110.1371/journal.pone.0005361Betulin is a potent anti-tumor agent that is enhanced by cholesterol.Franziska B MullauerJan H KesslerJan Paul MedemaBetulinic Acid (BetA) and its derivatives have been extensively studied in the past for their anti-tumor effects, but relatively little is known about its precursor Betulin (BE). We found that BE induces apoptosis utilizing a similar mechanism as BetA and is prevented by cyclosporin A (CsA). BE induces cell death more rapidly as compared to BetA, but to achieve similar amounts of cell death a considerably higher concentration of BE is needed. Interestingly, we observed that cholesterol sensitized cells to BE-induced apoptosis, while there was no effect of cholesterol when combined with BetA. Despite the significantly enhanced cytotoxicity, the mode of cell death was not changed as CsA completely abrogated cell death. These results indicate that BE has potent anti-tumor activity especially in combination with cholesterol.http://europepmc.org/articles/PMC2671171?pdf=render
spellingShingle Franziska B Mullauer
Jan H Kessler
Jan Paul Medema
Betulin is a potent anti-tumor agent that is enhanced by cholesterol.
PLoS ONE
title Betulin is a potent anti-tumor agent that is enhanced by cholesterol.
title_full Betulin is a potent anti-tumor agent that is enhanced by cholesterol.
title_fullStr Betulin is a potent anti-tumor agent that is enhanced by cholesterol.
title_full_unstemmed Betulin is a potent anti-tumor agent that is enhanced by cholesterol.
title_short Betulin is a potent anti-tumor agent that is enhanced by cholesterol.
title_sort betulin is a potent anti tumor agent that is enhanced by cholesterol
url http://europepmc.org/articles/PMC2671171?pdf=render
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