Background:
Natural plant metabolites and their semisynthetic derivatives have been used for years in
cancer therapy. Xanthones are oxygenated heterocyclic compounds produced as secondary metabolites by higher
plants, fungi or lichens. Xanthone core may serve as a template in the synthesis of many derivatives that have broad
biological activities.
Objective:
This study synthesized a series of 17 new xanthones, and their anticancer potential was also evaluated.
Methods:
The anticancer potential was evaluated in vitro using a highly invasive T24 cancer cell line. Direct cytotoxic
effects of the xanthones were established by IC50 estimation based on XTT assay.
Results:
5 compounds of the total 17 showed significant cytotoxicity toward the studied cancer cultures and were
submitted to further detailed analysis, including studies examining their influence on gelatinase A and B expression,
as well as on the cancer cells migration and adhesion to an extracellular matrix. These analyses were carried out on
five human tumor cell lines: A2780 (ovarian cancer), A549 (lung cancer), HeLa (cervical cancer), Hep G2 (liver
cancer), and T24 (urinary bladder cancer). All the compounds, especially 4, showed promising anticancer activity:
they exhibited significant cytotoxicity towards all the evaluated cell lines, including MCF-7 breast cancer, and
hindered migration-motility activity of cancer cells demonstrating more potent activity than α-mangostin which
served as a reference xanthone.
Conclusion:
These results suggest that our xanthone derivatives may be further analyzed in order to include them in
cancer treatment protocols.
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