期刊
FITOTERAPIA
卷 137, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.fitote.2019.104279
关键词
25-OH-PPD; Anti-tumor activity; Structure modification; Apoptosis
资金
- National Key R&D Program of China [2017YFC1702302]
- Technology Platform of Industrialization Chromatographic Preparation for Standard Extract of Traditional Chinese Medicine [2010ZX09401-304-105B]
- Liaoning (FGW) Engineering Technology Research Center for industrial chromatographic preparation of natural innovative drugs materials [2017-1007]
- Natural Science Foundation of Jilin Province [20160101218JC]
20(R)-25-hydroxyprotopanaxadiol (25-OH-PPD) is a natural compound showing a variety of anti-tumor effects. In an attempt to search for a new anti-cancer compound with higher antitumor activities, we designed and synthesized a series of 25-OH-PPD derivatives. Cytotoxicity assay of these derivatives towards MCF-7, A549, U87, HO-8901, Hela cancer cell lines and normal IOSE144 cell lines were tested by MTF assay. Results showed that compared with compound 25-OH-PPD, Compounds 4, 5, 6, 10, 11 showed strong anticancer activity, and all compounds showed low toxicity or no toxicity for normal cells. In particular, compound 6 exhibited the best anti-tumor activity in all cancer cell lines (MCF-7, A549, U87, HO-8901, and Hela) with IC50 values of 5.04 mu M, 1.36 mu M, 3.24 mu M, 3.47 mu M, 4.57 mu M, respectively. Among the five cell lines, all the compounds showed strong inhibition on A549 cells. Further studies showed that Compound 6 significantly inhibited the proliferation of A549 cells by inducing apoptosis. Our results indicate that Compound 6 is a potential anticancer inhibitor and provides a theoretical basis for further research.
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