Synthesis and Anticancer Activity Evaluation of Hydrolyzed Derivatives of Saponins.

To increase the antitumor activity of ginsenosides and acetylsalicylic acid, acid hydrolysis products of saponin were used as raw materials to be combined with salicylic acid to obtain ginsenoside salicylic acid derivatives. All derivatives were assessed for anti-cancer activity. A total of 20 target compounds were designed and synthesized. The cytotoxic activity on five cancer cell lines, including human colon cancer (HT-29), gastric cancer (BGC-823), cervical cancer (Hela), human breast cancer (MCF-7), human lung cancer cells (A549), and two normal cancer cell lines (human gastric epithelial cells (GES-1), and human ovarian epithelial cells (IOSE144)) was evaluated following treatment with the compounds. The results showed that all compounds inhibited the growth of cancer cells. Compounds , , , , , and showed strong anticancer activity. For MCF-7 cells, compound showed the strongest inhibitory activity, IC = 2.56 ± 0.09 μM. In the cytotoxicity test, all compounds showed low toxicity or no toxicity (IC > 100 μM). In addition, a cell cycle distribution assay and wound healing assay demonstrated that compound specifically inhibited MCF-7 proliferation and migration ability. Our results indicate that compound represents a promising compound for further cancer studies.