Chlorogenic acid (5-O-caffeoylquinic acid) is a phenolic compound from the hydroxycinnamic acid family. This polyphenol possesses many health-promoting properties, most of them related to the treatment of metabolic syndrome, including anti-oxidant, anti-inflammatory, antilipidemic, antidiabetic, and antihypertensive activities. The first part of this review will discuss the role of chlorogenic acid as a nutraceutical for the prevention and treatment of metabolic syndrome and associated disorders, including in vivo studies, clinical trials, and mechanisms of action. The second part of the review will be dealing with the role of chlorogenic acid as a food additive. Chlorogenic acid has shown antimicrobial activity against a wide range of organisms, including bacteria, yeasts, molds, viruses, and amoebas. These antimicrobial properties can be useful for the food industry in its constant search for new and natural molecules for the preservation of food products. In addition, chlorogenic acid has antioxidant activity, particularly against lipid oxidation; protective properties against degradation of other bioactive compounds present in food, and prebiotic activity. The combination of these properties makes chlorogenic acid an excellent candidate for the formulation of dietary supplements and functional foods.

Chlorogenic acid is a well-known nutraceutical, but it is extensively metabolized by the body. More valuable information can be obtained from its metabolites. Dihydrocaffeic acid is a metabolite of chlorogenic acid and has shown antioxidant, cardioprotective, and neuroprotective effects; however, information about its anticancer activity is very scarce. Therefore, the main objective of this study was to determine the anticancer potential of dihydrocaffeic acid. The cancer cell lines used were MCF-7, Hep-G2, PC-3, and HCT-116, while HDFa was used as healthy cells. The cytotoxic concentrations to kill 50%, 75%, and 90% of the cells (CC₅₀, CC₇₅, CC₉₀) were determined using the MTS assay. Dihydrocaffeic acid was significantly more cytotoxic for most cancer cell lines, including MCF-7, PC-3, and HCT-116, compared with HDFa; however, Hep-G2 was significantly more resistant than HDFa. Dihydrocaffeic acid is a potential candidate for cancer prevention and treatment. The mechanism of action remains to be elucidated.

Nutraceutical combinations that act synergistically could be a powerful solution against colon cancer, which is the second deadliest malignancy worldwide. In this study, curcumin (C), sulforaphane (S), and dihydrocaffeic acid (D, a chlorogenic acid metabolite) were evaluated, individually and in different combinations, over the viability of HT-29 and Caco-2 colon cancer cells, and compared against healthy fetal human colon (FHC) cells. The cytotoxic concentrations to kill 50%, 75%, and 90% of the cells (CC₅₀, CC₇₅, and CC₉₀) were obtained, using the MTS assay. Synergistic, additive, and antagonistic effects were determined by using the combination index (CI) method. The 1:1 combination of S and D exerted synergistic effects against HT-29 at 90% cytotoxicity level (doses 90:90 µM), whereas CD(1:4) was synergistic at all cytotoxicity levels (9:36–34:136 µM) and CD(9:2) at 90% (108:24 µM) against Caco-2 cells. SD(1:1) was significantly more cytotoxic for cancer cells than healthy cells, while CD(1:4) and CD(9:2) were similarly or more cytotoxic for healthy cells. Therefore, the SD(1:1) combination was chosen as the best. A model explaining SD(1:1) synergy is proposed. SD(1:1) can be used as a basis to develop advanced food products for the prevention/co-treatment of colon cancer.