4.7 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 11, Pages 3834-3840

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.04.043

Keywords

3-and 10-Bromofascaplysins; Cancer preventive; p53, AP-1 nuclear factors; Apoptosis

Funding

  1. Leading Russian Science Schools [2813.2008.4]
  2. Presidium of RAS
  3. FEB RAS [09-III-A-05-146, 09-III-B-05-155]
  4. Korean government through the Medical Research Center for Cancer Molecular Therapy at Dong-A University [R13-2002-044-04001-0]
  5. National Research Foundation of Korea [R13-2002-044-04001-0] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)

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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. (C) 2010 Elsevier Ltd. All rights reserved.

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