The formation and metastasis of tumor cells are closely related to the gene regulation. It is critical to elucidate the molecular mechanism of a compound using in cancer therapy. In this article, we reviewed the anti-cancer molecular mechanism of arsenic trioxide and artemisinin. Its anti-cancer function mainly includes: regulation of cell cycle regulatory proteins to inhibit tumor cell proliferation, cell apoptosis signal transduction pathway to promote apoptosis in tumor cells, immortalization associated genes to reduce the life of tumor cells, angiogenesis/invasion/metastasis gene to block the spread of tumor cells, promoter methylation and protein ubiquitination gene to enhance anti-oncogene expression and ubiquitin- mediated protein degradation, micro RNA to inhibit proliferation or induce apoptosis in tumor cells, DNA synthesis and repair of DNA damage and repair gene to decrease the DNA synthesis of tumor cells, signal transduction pathways of cell proliferation/apoptosis and invasion/metastasis etc., the expression of hormone receptors and so on. We indicated the problems existing in current studies and also prospected the future of using the compound to fight cancer.

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