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Oxymatrine is a kind of alkaloid extracted from traditional Chinese herb Sophora flavescens Ait. It has been proved to exert various biological activities such as anti-angiogenesis, proliferation-inhibiting, apoptosis-promoting, analgesic-strengthening, and anti-metastasis. The biological activities are related with inhibition of angiogenesis-associated factors, regulation of related signaling pathway and protein expression, synergistic effects with chemotherapy drug, cell cycle arrest and inhibition of voltage-activated K+ channel. In this review, we summarize the recent investigations of oxymatrine in cancer therapy so as to provide references for further study and clinical therapy.