Gymnocladus chinensis Baillon is widely distributed in China, and its fruits have been used in the treatment of
rheumatism,
furunculosis, soreness and swelling in
traditional Chinese medicine for a long time. Few
biological components were, however, isolated. In this study, a new
triterpenoid saponin (GC-1) was extracted from the fruit of Gymnocladus chinensis Baillon and its
biological actions were investigated. The results showed that
GC-1 inhibited growth of a panel of human
cancer cell lines in vitro by 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyl tetrazolium
bromide and
sulforhodamine B assays. Furthermore,
GC-1 was demonstrated to induce apoptosis in HL-60 cells in a dose-dependent manner. By using a reporter gene assay,
nuclear factor-kappaB activity induced by
tumor necrosis factor-alpha was decreased gradually by addition of increasing concentration of
GC-1 (1-40 micromol/l). In parallel, the blockage of
nuclear factor-kappaB translocation from cytoplasm to nucleus was determined by Western blotting. This is the first study investigating the link of antiproliferative action of the compound with the inhibition of
nuclear factor-kappaB activation. The mechanism of the actions of
GC-1 might be due to the interruption of
nuclear factor-kappaB translocation in the signaling pathway, which contributes to the
chemotherapy potential.