H2valdien3 arrests the cell cycle and induces apoptosis of gastric cancer.

Despite significant advances in the diagnosis and treatment of gastric cancer (GC), its incidence and mortality remain high worldwide. Therefore, finding new anticancer drugs or treatment strategies for GC is crucial. The valdien ligand, which is not soluble in water, has demonstrated potential anticancer effects on cancer. This study highlights a water-soluble derivative of the H2valdien ligand derivatives, named H2valdien3, which can inhibit the proliferation of GC by arresting the cell cycle and inducing apoptosis. Initially, the inhibitory effects and cytotoxicity of H2valdien3 on the growth of AGS and MKN45 cells were evaluated using MTT assays. Microscopic observations revealed that H2valdien3-treated AGS and MKN45 cells exhibited deteriorated morphology. Hoechst fluorescent staining and flow cytometry results further demonstrated that H2valdien3 promotes apoptosis and arrests the cell cycle in GC cells. Additionally, the anticancer mechanism of H2valdien3 was found to involve the β-catenin/c-myc pathway. In vivo experiments showed that H2valdien3 inhibited GC proliferation without significantly affecting the weight of the mice. These findings suggest that the transformed H2valdien3 has potential anticancer properties with minimal side effects for GC treatment.