| Autor: |
Fenqin Zhao, Jinyu Li, Kexin Yue, Beibei Song, Erying Sun, Xinru Cheng, Jing Ma, Lin Yan |
| Jazyk: |
angličtina |
| Rok vydání: |
2021 |
| Předmět: |
|
| Zdroj: |
Applied Sciences, Vol 11, Iss 8, p 3364 (2021) |
| Druh dokumentu: |
article |
| ISSN: |
2076-3417 |
| DOI: |
10.3390/app11083364 |
| Popis: |
In order to develop new oleanolic acid (OA) derivatives endowed with improved antitumor activities, for the first time, a number of new hybrid compounds were reported by combining OA or 3-oxooleanolic acid with appropriate H2S-donor moiety, coupled via a suitable linker. The anti-tumor evaluation indicated that they exhibited excellent anti-cancer activities against the tested cancer cell lines. Moreover, 18d with 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione moiety as H2S donor and β-alanine as the linker, showed more potent cytotoxicity against the tested cancer cell lines than OA and 3-oxooleanolic acid, especially for A549 cells. Furthermore, the preferred compound, 18d, preferentially accumulates in cancer cells (13.6 μM) over the matched normal cells LO2 (>100 μM) in vitro. The improved antitumor activity of this hybrid was probably due to its H2S-releasing capability. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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