Copperchlorophyllin(Cu-Chl) is a chlorophyll-derived food colorant, commercially available as a complex mixture of differentchlorinmolecules. Several studies have reported great variability in the composition of the mixture as well as the presence ofporphyrinsand uncoppered chlorin derivatives. The intake of chlorophyllin and its relationship with possible health benefits have been also the subject of several studies and the results have drawn attention to the possibility that this compound may serve not just as a food colorant, but also as a potential bioactive product with antimutagenic, anticarcinogenic andantioxidant activities; however, its mechanisms of action are not yet well understood. Attaining knowledge of its mechanisms of absorption, bioavailability and consequent bioactivity is essential for the exploration of its potential health-related applications. The purpose of this paper is to present an overview of bioactivities concerning Cu-Chl and provide a discussion on the latest scientific research findings on its human health benefits.Copperchlorophyllin(Cu-Chl) is a chlorophyll-derived food colorant, commercially available as a complex mixture of differentchlorinmolecules. Several studies have reported great variability in the composition of the mixture as well as the presence ofporphyrinsand uncoppered chlorin derivatives. The intake of chlorophyllin and its relationship with possible health benefits have been also the subject of several studies and the results have drawn attention to the possibility that this compound may serve not just as a food colorant, but also as a potential bioactive product with antimutagenic, anticarcinogenic andantioxidant activities; however, its mechanisms of action are not yet well understood. Attaining knowledge of its mechanisms of absorption, bioavailability and consequent bioactivity is essential for the exploration of its potential health-related applications. The purpose of this paper is to present an overview of bioactivities concerning Cu-Chl and provide a discussion on the latest scientific research findings on its human health benefits.