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Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells

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2011
Authors
Kommera, Harish
Kaluđerović, Goran N.
Kalbitz, Jutta
Paschke, Reinhard
Article (Published version)
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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 acid
Source:
Investigational New Drugs, 2011, 29, 2, 266-272
Publisher:
  • 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

WoS: 000287248100008

Scopus: 2-s2.0-79955594006
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/3411
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IHTM

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