Abstract：
: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 MTT 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 μM, 1.36 μM, 3.24 μM, 3.47 μM, 4.57 μM, 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.
journal_name
Fitoterapiajournal_title
Fitoterapiaauthors
Lv L,Lu J,Zhang H,Wang X,Su G,Piao H,Zhao Ydoi
10.1016/j.fitote.2019.104279subject
Has Abstractpub_date
2019-09-01 00:00:00pages
104279eissn
0367-326Xissn
1873-6971pii
S0367-326X(19)30589-1journal_volume
137pub_type
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