Introduction:
Artesunate, a derivative of
artemisinin, has
anti-malarial effects, and in recent years has also been reported to have anti-
tumor activity. However, its anti-
tumor mechanisms are not well understood. Methods: In this study, we focused on the targeting of Hsp90 by
artesunate to inhibit
tumor cell proliferation, which we examined using immunoprecipitation, a proliferation assay, flow cytometry, western blotting, a
tumor xenograft animal model, and immunohistochemistry. Furthermore, to examine the
tumor-suppressive effects of artesunatein nude mice, we used
artesunate-loaded PLGA-PEG nanoparticles. Results: The binding of
artesunate to Hsp90 was found to reduce the expression of its client
proteins AKT, ERK, p-AKT, p-ERK, and EGFR, thereby blocking the cell cycle at the G0/G1 → S stage in
lymphoma cells and inducing apoptosis. In addition, the results of
tumor xenograft experiments revealed that
artesunate reduced the expression of AKT and ERK
proteins in
tumor tissues, inhibited
tumor proliferation, and reduced
tumor size and weight. Furthermore, nanoparticle encapsulation was demonstrated to enhance the anti-
cancer activity of
artesunate. Discussion: We thus established that
artesunate inhibits the proliferation of
lymphoma cells by targeting the Hsp90
protein, and we accordingly believe that this compound has potential for development as a novelanti-
tumor drug.