(L.) Schott is a tuberous plant, also known as taro, employed as food worldwide for its renowned nutritional properties but also traditionally used in several countries for medical purposes. In this study, methanolic extracts were prepared from the corms and leaves of , subsequently fractionated via molecular exclusion chromatography (RP-HPLC) and their anti-tumor activity assessed in an in vitro model of gastric adenocarcinoma (AGS cells). Vorm extract and isolated fractions II and III affected AGS cell vitality in a dose-dependent manner through the modulation of key proteins involved in cell proliferation, apoptosis, and cell cycle processes, such as caspase 3, cyclin A, cdk2, IkBα, and ERK. To identify bioactive molecules responsible for anti-tumoral activity fractions II and III were further purified via RP-HPLC and characterized via nuclear magnetic resonance (NMR) and electrospray mass spectrometry (ESI-MS) techniques. The procedure enabled the identification of ten compounds including lignans and neolignans, some isolated for the first time in taro, uncommon megastigmane derivatives, and a gallic acid derivative. However, none of the isolated constituents showed efficacy equivalent to that of the fractions and total extract. This suggests that the whole phytocomplex has intriguing anti-tumor activity against gastric cancer.