A Mechanism for Apoptotic Effects of a Planar Catechin Analog on Cancer Cells.

Catechin is one of the representative antioxidants that shows physiological activities such as an anti-cancer effect. We have developed a chemically modified catechin analog possessing a planar structure, which shows an enhanced radical-scavenging activity as well as inhibitory effects on the proliferation and migration of cancer cells, compared to the parent (+)-catechin. In this study, the mechanism for cancer cell inhibition by the planar catechin was partly elucidated using a gastric cancer cell line. The planar catechin treatment induced an enhanced expression of an apoptotic marker, cleaved caspase-3, in addition to the mitigation of the intracellular accumulation of reactive oxygen species (ROS) and NF-κB expression. Furthermore, γH2AX, a marker of double-strand breaks in DNA, was also induced by the planar catechin treatment in a dose-dependent manner. These findings suggest that the removal of ROS by the planar catechin with a higher antioxidant ability executed NF-κB suppression and/or the planar catechin-injured DNA, leading to the induction of apoptosis in cancer cells.