Dihydroartemisinin is a newly defined STAT3 inhibitor that may be of multiple potential uses in cancer treatment

Abstract

Accumulating evidence from epidemiological, pharmacological and case control studies has shown that dihydroartemisinin (DHA), one of first-line antimalarial drugs recommended by World Health Organization (WHO), possesses antineoplastic activity and selective cytotoxicity to a variety of human cancer cell model systems. Although some antitumor mechanisms of DHA have been confirmed, the findings from the previous studies are insufficient to fully reveal the whole picture of tumor suppression by DHA. In a recent investigation, we demonstrated that DHA exhibits antitumor properties against a variety of human HNSCC cells both in vitro and in vivo. The underlying mechanism involves selective inhibition of Jak2/STAT3 signaling. By specific inhibition of STAT3 activation, DHA exerted the chemotherapeutic efficacy, including reduction in cell viability and migratory capability, along with induction of G1 phase cell cycle arrest and apoptosis in HNSCC cells. All of data suggested that DHA may be a potent inhibitor of STAT3 that can be potentially used to treat patients with HNSCC, as well as other human cancers harboring STAT3 activation.