Nuclear factor-E2-related factor 2 (Nrf2) is an important
transcription factor and plays a central role in inducible expression of many cytoprotective genes. Recent studies have reported that various
cancer cells having unrestrained Nrf2 due to its overexpression exhibit increased proliferation and resistance to
chemotherapy. Suppression of abnormal Nrf2 activation is needed for a new therapeutic approach against these
cancers. Our previous study found that
procyanidins prepared from Cinnamomi Cortex extract (CCE) have an ability to suppress Nrf2-regulated
enzyme activity and Nrf2 expression in human
lung cancer A549 cells. In the present study, we investigated the effect of CCE
procyanidins on Nrf2 activity and cell proliferation in several
cancer cells, which have normal or constitutively active Nrf2. Interestingly, CCE
procyanidin treatment selectively reduced Nrf2 expression and inhibited cell proliferation in
cancer cells that overexpress Nrf2, but these phenomena were not seen in cells with low Nrf2 expression. Moreover, transfection assay demonstrated that CCE
procyanidins had selective inhibition of activated Nrf2. These results suggest that CCE
procyanidins might be an effective
cancer therapeutic agent to selectively suppress abnormal Nrf2 activation responsible for enhanced proliferation.