Indoloquinolizidine derivatives as novel and potent apoptosis inducers and cell-cycle blockers

Chembiochem : a European Journal of Chemical Biology
Frank WehnerHerbert Waldmann

Abstract

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.

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Citations

Apr 11, 2009·Chembiochem : a European Journal of Chemical Biology·Thilo WaltherHans-Dieter Arndt
Mar 15, 2012·Chemistry : a European Journal·Andrea OlmosPatrick Pale
May 21, 2010·Accounts of Chemical Research·Robin S Bon, Herbert Waldmann

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Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis