Hepatocellular carcinoma (HCC), one of the most common malignant cancers with a low 5-year survival rate, is the third leading cause of cancer-related deaths worldwide. The finding of novel agents and strategies for the treatment of HCC is an urgent need. Sesquiterpene lactones
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Hepatocellular carcinoma (HCC), one of the most common malignant cancers with a low 5-year survival rate, is the third leading cause of cancer-related deaths worldwide. The finding of novel agents and strategies for the treatment of HCC is an urgent need. Sesquiterpene lactones (SLs) have attracted extensive attention because of their potent antitumor activity. In this study, a new series of SL derivatives (
3–
18) were synthesized using epimers
1 and
2 as parent molecules, isolated from
Sphagneticola trilobata, and evaluated for their anti-HCC activity. Furthermore, the structures of
4,
6, and
14 were confirmed by X-ray single-crystal diffraction analyses. The cytotoxic activities of
3–
18 on two HCC cell lines, including HepG2 and Huh7, were evaluated using the CCK-8 assay. Among them, compound
10 exhibited the best activity against the HepG2 and Huh7 cell lines. Further studies showed that
10 induced cell apoptosis, arrested the cell cycle at the S phase, and induced the inhibition of cell proliferation and migration in HepG2 and Huh7. In addition, absorption, distribution, metabolism, and excretion (ADME) properties prediction showed that
10 may possess the properties to be a drug candidate. Thus,
10 may be a promising lead compound for the treatment of HCC.
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