Trichosanthin (TCS) is a type I ribosome-inactivating protein that is isolated from the root tubers of the Chinese medicinal herb Trichosanthes kirilowii Maximowicz. TCS has been used as an abortifacient for 1,500 years in China because of its high toxicity on trophoblasts. Over the past 20 years, TCS has been the subject of much research because of its potential antitumor activities. Many reports have revealed that TCS is cytotoxic in a variety of tumor cell lines in vitro and in vivo. Monoclonal antibody-conjugated TCS could enhance its antitumor efficacy; thus, TCS is considered to be a potential biological agent for cancer treatment. TCS is able to inhibit protein synthesis and consequently induce necrosis. Recent studies have demonstrated that TCS does indeed induce apoptosis in several tumor cell lines. Although TCS-induced apoptosis of tumor cell lines is now well known, the underlying mechanisms remain to be elucidated. The purpose of this review was to investigate the effects of TCS and its possible mechanisms of action, based on published literature and the results of our own studies. Anat Rec, 2010. © 2010 Wiley-Liss, Inc.