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Indoloquinolizidine Derivatives as Novel and Potent Apoptosis Inducers and Cell‐Cycle Blockers
Author(s) -
Wehner Frank,
NörenMüller Andrea,
Müller Oliver,
ReisCorrêa Ivan,
Giannis Athanassios,
Waldmann Herbert
Publication year - 2008
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200700558
Subject(s) - hela , apoptosis , cell sorting , microbiology and biotechnology , cell cycle , cell growth , cell , mtt assay , programmed cell death , chemistry , necrosis , inducer , biology , flow cytometry , biochemistry , gene , genetics
A collection of approximately 11 000 natural‐product derived and inspired compounds was screened for potential apoptosis inducers in the human tumour cell lines HepG2 (liver), HeLa (cervix) and MCF‐7 (breast) by means of MTT and ATP‐luminescence assays, automated cell counting, caspase 3/7 assay as well as by fluorescence activated cell sorting (FACS) analysis. A group of seven indoloquinolizidine derivatives was identified that exhibited IC 50 values for cell proliferation as low as 2 μmol L −1 , with no major necrosis of cells detectable. At the same time, an increase in the rate of apoptosis of up to 600 % relative to the reference level was observed. FACS analysis indicated that these effects are related to an arrest of cells in the G 2 M phase of the cell cycle.