Chlorophyllin is a semi-synthetic derivative of chlorophyll that is commercially used as a food additive and coloring agent. Chlorophyllin exhibits anti-angiogenic, anticancer chemotherapeutic, and chemopreventive activities. Chlorophyllin can act as a photosensitizer, inducing apoptosis and autophagy under UV light in bladder cancer cells. In vivo, chlorophyllin decreases expression of HDACs, VEGF, VEGFR2, and HIF-1α and suppresses Wnt/β-catenin signaling. In vitro, this compound decreases DNA adduct formation induced by benzo[a]pyrene. Chlorophyllin also decreases carcinogenesis, mortality, and tumor number in animal models of DBP-induced carcinogenesis.