The anticancer activity of 3- and 10-bromofascaplysins is mediated by caspase-8, -9, -3-dependent apoptosis

Cancer-preventive and cytotoxic activities of 3- and 10-bromofascaplysins ( 1 and 2) are mediated, at least in part, through the induction of caspase-dependent apoptosis. 3- and 10-Bromofascaplysins was previously found to possess cytotoxic activity. In this study, we investigated their cancer preve...

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Published in:Bioorganic & medicinal chemistry 2010-06, Vol.18 (11), p.3834-3840
Main Authors: Kuzmich, Alexandra S., Fedorov, Sergey N., Shastina, Valeria V., Shubina, Larisa K., Radchenko, Oleg S., Balaneva, Nadezda N., Zhidkov, Maxim E., Park, Joo-In, Kwak, Jong Y., Stonik, Valentin A.
Format: Article
Language:English
Subjects:
3- and 10-Bromofascaplysins
Animals
Antineoplastic Agents - pharmacology
Apoptosis
Apoptosis - drug effects
Cancer preventive
Caspase 3 - metabolism
Caspase 8 - metabolism
Caspase 9 - metabolism
Caspases - metabolism
Cell Line
Cell Line, Tumor
Cell Survival - drug effects
Humans
Mice
Mitochondria - metabolism
p53, AP-1 nuclear factors
Permeability - drug effects
Skin - cytology
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Summary:Cancer-preventive and cytotoxic activities of 3- and 10-bromofascaplysins ( 1 and 2) are mediated, at least in part, through the induction of caspase-dependent apoptosis. 3- and 10-Bromofascaplysins was previously found to possess cytotoxic activity. In this study, we investigated their cancer preventive and proapoptotic properties. These effects were tested on mouse skin epidermal JB6 P + Cl41 cell line, its stable transfectants, and human tumor HL-60, THP-1, SNU-C4, SK-MEL-28, DLD-1, MDA-MB-231, and HeLa cells using a variety of assessments, including a cell viability (MTS) assay, flow cytometry, anchorage-independent soft agar assay, luciferase assay, mitochondrial permeability assay, and Western blotting. 3- and 10-Bromofascaplysins were effective at submicromolar concentrations as the anticancer agents, which exerted their action, at least in part, through the induction of caspase-8, -9, -3-dependent apoptosis.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2010.04.043