Design, Synthesis, and Cell Lines Studies of Oleanolic Acid—Hydrogen Sulfide Donor Hybrids
Source abstract
Abstract
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.
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Research context
OpenAlex topics: Natural product bioactivities and synthesis · Genomics, phytochemicals, and oxidative stress · Synthesis and biological activity
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
Affiliations
Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng 475004, China
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