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

被引：44
|
作者：
Kommera, Harish [1 ]
Kaluderovic, Goran N. [1 ,2 ]
Kalbitz, Jutta [3 ]
Paschke, Reinhard [1 ]
机构：
[1] Univ Halle Wittenberg, Biozentrum, D-06120 Halle, Germany
[2] Univ Belgrade, Inst Chem Technol & Met, Dept Chem, Belgrade 11000, Serbia
[3] BioSolut Halle GmbH, D-06120 Halle, Germany
来源：
INVESTIGATIONAL NEW DRUGS | 2011年 / 29卷 / 02期
关键词：
Betulinic acid; Betulin; Natural products; Apoptosis; Cytotoxicity; Caspase activity; NEUROECTODERMAL TUMORS; IN-VITRO; CYTOTOXICITY; ANTIMALARIAL; MITOCHONDRIA; ACTIVATION; AGENTS; LINES;
D O I：
10.1007/s10637-009-9358-x
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
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.
引用
收藏
页码：266 / 272
页数：7
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