Document Detail

Small structural changes of pentacyclic lupane type triterpenoid derivatives lead to significant differences in their anticancer properties.
MedLine Citation:
PMID:  20472329     Owner:  NLM     Status:  MEDLINE    
In the present investigations five new derivatives of betulinic and betulonic acid were synthesized and the effect of this structural variations on anticancer activity was studied and discussed. The antiproliferative activity of betulinic and betulonic acid derivatives was studied against eight tumor cell lines of different histogenic origin. The derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. The apoptotic mode of cell death on colon cancer cell line HT-29 was induced by the most active compounds 5, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl (3-O-acetyl)betulinate, and 9, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl betulonate. Treatment of HT-29 cells with 5 and 9 induced apoptosis, as observed by dye exclusion test (trypan blue) and by the appearance of a typical ladder pattern in the DNA fragmentation assay and FITC annexin V assay. Cell cycle perturbations caused by compound 5 are also presented.
Harish Kommera; Goran N Kaluderović; Jutta Kalbitz; Birgit Dräger; Reinhard Paschke
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-04-27
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  45     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2010 Aug 
Date Detail:
Created Date:  2010-06-14     Completed Date:  2010-09-14     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  3346-53     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.
Biozentrum, Martin-Luther-Universität Halle-Wittenberg, Weinbergweg 22, 06120 Halle, Germany.
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MeSH Terms
Antineoplastic Agents / chemical synthesis,  chemistry*,  pharmacology*
Apoptosis / drug effects
Caspases / metabolism
Cell Cycle / drug effects
Cell Line, Tumor
Spectrum Analysis
Structure-Activity Relationship
Triterpenes / chemical synthesis,  chemistry*,  pharmacology*
Reg. No./Substance:
0/Antineoplastic Agents; 0/Triterpenes; 464-99-3/lupane; EC 3.4.22.-/Caspases

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