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Chemopreventive Effects of Synthetic C-substituted Diindolylmethanes Originating From Cruciferous Vegetables in Human Oral Cancer Cells

Chemopreventive Effects of Synthetic C-substituted Diindolylmethanes Originating From Cruciferous Vegetables in Human Oral Cancer Cells

Ji-Ae Shin, Jung-Hyun Shim, Eun-Sun Choi, Dae-Ho Leem, Ki Han Kwon, Syng-Ook Lee, Stephen Safe, Nam-Pyo Cho, Sung-Dae Cho

Eur J Cancer Prev. 2011 Sep;20(5):417-25.

PMID: 21597379

Abstract:

Diindolylmethane (DIM), an isothiocyanate found in cruciferous vegetables, has been shown to have cancer chemopreventive effects. A series of synthetic C-substituted DIMs (C-DIMs) analogs was developed, including DIM-C-pPhtBu and DIM-C-pPhC6H5, which exhibited better inhibitory activity in cancer cells than DIM. This study examined the effects of C-DIMs on the growth of human oral cancer cells. DIM-C-pPhtBu and DIM-C-pPhC6H5 decreased the number of viable KB cells and induced caspase-dependent apoptosis. The apoptotic cell death was accompanied by a change in Bax/Bcl-2 ratio and damage to mitochondrial membrane potential through the induction of death receptor 5 and the cleavage of Bid and caspase 8. Studies on the mechanism of action showed that the apoptotic cell death induced by DIM-C-pPhtBu and DIM-C-pPhC6H5 was mediated by endoplasmic reticulum stress. In addition, C-DIMs inhibited cell proliferation and induced PARP cleavage through death receptor 5 and CHOP in HEp-2 and HN22 cells. This provides the first evidence that synthetic C-DIMs originating from cruciferous vegetables induce apoptosis in human oral cancer cells through the endoplasmic reticulum stress pathway.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP94944806	DIM-C-pPhtBu		94944-80-6	Price

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