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

Summary 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...

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Bibliographic Details
Published in:Investigational new drugs 2011-04, Vol.29 (2), p.266-272
Main Authors: Kommera, Harish, Kaluđerović, Goran N., Kalbitz, Jutta, Paschke, Reinhard
Format: Article
Language:English
Subjects:
Acids
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis
Apoptosis - drug effects
Cancer
Caspases - metabolism
Cell culture
Cell death
Cell Line, Tumor
Cell Survival - drug effects
Chemistry
Colorectal cancer
Cytotoxicity
DNA Fragmentation - drug effects
Drug dosages
Drug Screening Assays, Antitumor
Enzymes
Fibroblasts
Humans
Inhibitory Concentration 50
Investigations
Kinetics
Laboratories
Medicine
Medicine & Public Health
Natural products
Oncology
Penicillin
Pharmaceuticals
Pharmacology/Toxicology
Preclinical Studies
R&D
Research & development
Toxicity
Triterpenes - chemistry
Triterpenes - pharmacology
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Summary:Summary 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.
ISSN:0167-6997
1573-0646
DOI:10.1007/s10637-009-9358-x