Synthesis and Anticancer Activity Evaluation of Hydrolyzed Derivatives of Panaxnotoginseng Saponins

Abstract

To increase the antitumor activity of ginsenosides and acetylsalicylic acid, acid hydrolysis products of <i>Panaxnotoginseng</i> 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 <b>1a</b>, <b>3a</b>, <b>7a</b>, <b>1b</b>, <b>2b</b>, <b>3b</b> and <b>8b</b> showed strong anticancer activity. For MCF-7 cells, compound <b>3b</b> showed the strongest inhibitory activity, IC₅₀ = 2.56 ± 0.09 μM. In the cytotoxicity test, all compounds showed low toxicity or no toxicity (IC₅₀ > 100 μM). In addition, a cell cycle distribution assay and wound healing assay demonstrated that compound <b>3b</b> specifically inhibited MCF-7 proliferation and migration ability. Our results indicate that compound <b>3b</b> represents a promising compound for further cancer studies.