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

Authorized Users Only
2011
Authors
Kommera, Harish
Kaluđerović, Goran N.
Kalbitz, Jutta
Paschke, Reinhard
Article (Published version)
Metadata
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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
Funding / 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
[ Google Scholar ]
53
42
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/3411
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
TY  - JOUR
AU  - Kommera, Harish
AU  - Kaluđerović, Goran N.
AU  - Kalbitz, Jutta
AU  - Paschke, Reinhard
PY  - 2011
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/3411
AB  - 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.
PB  - Netherlands : Springer
T2  - Investigational  New Drugs
T1  - Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells
VL  - 29
IS  - 2
SP  - 266
EP  - 272
DO  - 10.1007/s10637-009-9358-x
ER  - 
@article{
author = "Kommera, Harish and Kaluđerović, Goran N. and Kalbitz, Jutta and Paschke, Reinhard",
year = "2011",
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.",
publisher = "Netherlands : Springer",
journal = "Investigational  New Drugs",
title = "Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells",
volume = "29",
number = "2",
pages = "266-272",
doi = "10.1007/s10637-009-9358-x"
}
Kommera, H., Kaluđerović, G. N., Kalbitz, J.,& Paschke, R.. (2011). Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells. in Investigational  New Drugs
Netherlands : Springer., 29(2), 266-272.
https://doi.org/10.1007/s10637-009-9358-x
Kommera H, Kaluđerović GN, Kalbitz J, Paschke R. Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells. in Investigational  New Drugs. 2011;29(2):266-272.
doi:10.1007/s10637-009-9358-x .
Kommera, Harish, Kaluđerović, Goran N., Kalbitz, Jutta, Paschke, Reinhard, "Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells" in Investigational  New Drugs, 29, no. 2 (2011):266-272,
https://doi.org/10.1007/s10637-009-9358-x . .

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