Wehner Frank, Nören-Müller Andrea, Müller Oliver, Reis-Corrêa Ivan, Giannis Athanassios, Waldmann Herbert
Department of Systemic Cell Biology, Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.
Chembiochem. 2008 Feb 15;9(3):401-5. doi: 10.1002/cbic.200700558.
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 mumol 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.
通过MTT和ATP发光测定、自动细胞计数、半胱天冬酶3/7测定以及荧光激活细胞分选（FACS）分析，对大约11000种天然产物衍生及受其启发的化合物进行了筛选，以寻找在人肝癌细胞系HepG2（肝脏）、宫颈癌HeLa细胞系和乳腺癌MCF - 7细胞系中潜在的凋亡诱导剂。鉴定出一组七种吲哚喹嗪衍生物，其细胞增殖的IC(50)值低至2 μmol L(-1)，未检测到明显的细胞坏死。同时，观察到相对于参考水平，细胞凋亡率增加高达600%。FACS分析表明，这些效应与细胞周期G(2)M期的细胞停滞有关。
