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Upregulation of both heme oxygenase-1 and ATPase inhibitory factor 1 renders tumoricidal activity by synthetic flavonoids via depleting cellular ATP

Authors
Lee, Phil JunShin, IljinSeo, Seung-YongKim, HyoungsuKim, Hong Pyo
Issue Date
15-Oct-2014
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Chrysin derivatives; Heme oxygenase; ATPIF1; Apoptosis; Energetics
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.24, no.20, pp.4845 - 4849
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
24
Number
20
Start Page
4845
End Page
4849
URI
https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/12199
DOI
10.1016/j.bmcl.2014.08.055
ISSN
0960-894X
Abstract
Heme oxygenase-1 (HO-1) and ATPase inhibitory factor (ATPIF) 1 is often overexpressed in different types of cancer cells. Chrysin is a naturally-occurring flavonoid with antioxidant potentials, but also known to promote apoptosis. We have synthesized four chrysin derivatives and found compounds 1 and 4 remarkably upregulated the expression of HO-1, a cytoprotective enzyme. A robust expression of ATPIF1 was only seen in compound 4. Upregulation of both proteins triggers cell death in hydrogen peroxide-primed cells. Ten derivatives of compound 4 were synthesized and measured the expression of HO-1 and ATPIF1. Again, upregulation of both proteins by compound 8 killed the cells via apoptosis. To gain a physiological significance, we treated the synthetic flavonoids in colon cancer cells, HT29 and HCT116 cells and confirmed that overexpression of both HO-1 and ATPIF1 was critical for tumor cell death with an impaired mitochondrial energetics. It would provide a strategy for developing selective anti-tumor candidates. (C) 2014 Elsevier Ltd. All rights reserved.
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