ReferenceID 563

The antitumor natural compound falcarindiol promotes cancer cell death by inducing endoplasmic reticulum stress

Cell Death Dis

Falcarindiol (FAD) is a natural polyyne with various beneficial biological activities. We show here that FAD preferentially kills colon cancer cells but not normal colon epithelial cells. Furthermore, FAD inhibits tumor

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Reference Id
563
Evidence Id
17153
Core Evidence Id
17153
Source Reference Id
1111
Herb2 Reference Id
HBREF001863
Subject Paper Key
HBIN026343_22914324
Pubmed Id
22914324
Doi
10.1038/cddis.2012.122
Paper Title
The antitumor natural compound falcarindiol promotes cancer cell death by inducing endoplasmic reticulum stress
Paper Abstract
Falcarindiol (FAD) is a natural polyyne with various beneficial biological activities. We show here that FAD preferentially kills colon cancer cells but not normal colon epithelial cells. Furthermore, FAD inhibits tumor growth in a xenograft tumor model and exhibits strong synergistic killing of cancer cells with 5-fluorouracil, an approved cancer chemotherapeutic drug. We demonstrate that FAD-induced cell death is mediated by induction of endoplasmic reticulum (ER) stress and activation of the unfolded protein response (UPR). Decreasing the level of ER stress, either by overexpressing the ER chaperone protein glucose-regulated protein 78 (GRP78) or by knockout of components of the UPR pathway, reduces FAD-induced apoptosis. In contrast, increasing the level of ER stress by knocking down GRP78 potentiates FAD-induced apoptosis. Finally, FAD-induced ER stress and apoptosis is correlated with the accumulation of ubiquitinated proteins, suggesting that FAD functions at least in part by interfering with proteasome function, leading to the accumulation of unfolded protein and induction of ER stress. Consistent with this, inhibition of protein synthesis by cycloheximide significantly decreases the accumulation of ubiquitinated proteins and blocks FAD-induced ER stress and cell death. Taken together, our study shows that FAD is a potential new anticancer agent that exerts its activity through inducing ER stress and apoptosis.
Journal
Cell Death Dis
Publish Year
2012
Experiment Subject
colon cancer cells
Experiment Type
Cell Experiment
Phenotype Related
Paper Title Cn
Paper Title En
The antitumor natural compound falcarindiol promotes cancer cell death by inducing endoplasmic reticulum stress
Bilingual Status
semi_complete