Abstract
To increase the antitumor activity of ginsenosides and acetylsalicylic acid, acid hydrolysis products of Panaxnotoginseng 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 1a, 3a, 7a, 1b, 2b, 3b and 8b showed strong anticancer activity. For MCF-7 cells, compound 3b 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 3b specifically inhibited MCF-7 proliferation and migration ability. Our results indicate that compound 3b represents a promising compound for further cancer studies.
Highlights
Panaxnotoginseng is the ginseng plant of the genus Araliaceae
“Shenyi Capsule”, a new type of anti-cancer drug, was listed in 2003, and the main component of this drug is ginsenoside-Rg3. This provides an important opportunity for the full utilization and development of ginseng plants into medicinal resources
We have proven that ginsenosides and their derivatives from ginseng, American ginseng, and Panaxnotoginseng have anti-tumor activity [8]
Summary
Panaxnotoginseng is the ginseng plant of the genus Araliaceae. In modern scientific research, the main active ingredients of Panaxnotoginseng are ginsenosides [1]. “Shenyi Capsule”, a new type of anti-cancer drug, was listed in 2003, and the main component of this drug is ginsenoside-Rg3. This provides an important opportunity for the full utilization and development of ginseng plants into medicinal resources. We have proven that ginsenosides and their derivatives from ginseng, American ginseng, and Panaxnotoginseng have anti-tumor activity [8]. These include a series of studies on 25-methoxyprotopanaxadiol (25-OCH3 -PPD, AD-1), 25-hydroxyprotopanaxadiol (25-OH-PPD, AD-2), panaxadiol (PD), and their homologs. New structure-activity relationships produced by changes to these compounds is a hot topic, including structural modifications of dammarane derivatives [9]
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