The use of legumes as functional foods has gained increasing attention for the prevention and treatment of the so called non-communicable diseases that are highly prevalent worldwide. In this regard, biotechnological approaches for the enhancement of legumes’ nutritional and functional value have been extensively employed. In the present study, the process of germination increased several parameters of mung bean (Vigna radiata L.) functionality, including extract yield, total phenolic content and in vitro antioxidant capacity. In addition, 3-day-germinated mung bean proved to be an interesting source of dietary essential minerals and exhibited a greater variety of polyphenolic compounds compared to raw mung bean. These properties resulted in enhanced cytoprotective features of the 3-day mung bean extracts against radical oxygen species in human colorectal (HT29) and monocyte (U937) cell lines. Moreover, the antiproliferative effects were tested in different colon cancer cell lines, T84 and drug-resistant HCT-18, as well as in a non-tumor colon CCD-18 line. Altogether, our results demonstrate that the germination process improves the mung bean’s nutritional value and its potential as a functional food.