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

被引：0
作者：
Harish Kommera
Goran N. Kaluđerović
Jutta Kalbitz
Reinhard Paschke
机构：
[1] Martin-Luther-Universität Halle-Wittenberg,Biozentrum
[2] University of Belgrade,Department of Chemistry, Institute of Chemistry, Technology and Metallurgy
[3] BioSolutions Halle GmbH,undefined
来源：
Investigational New Drugs | 2011年 / 29卷
关键词：
Betulinic acid; Betulin; Natural products; Apoptosis; Cytotoxicity; Caspase activity;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
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.
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页码：266 / 272
页数：6
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