Abstract

ABSTRACT 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.

Highlights

  • Chlorogenic acid is a well-known nutraceutical widely spread in plant foods

  • Chlorogenic acid is extensively metabolized by the human body (Olthof et al, 2003), which may diminish or nullify its in vitro anticancer activity, while the benefits found in vivo may be caused not by the compound itself but by its metabolites

  • The different sensitivities of the cell lines towards dihydrocaffeic acid could be due to the different genetic profiles of each cell line, which can lead to variations in the rate at which the compound is metabolized, expression of detoxifying enzymes, and the efficacy of the efflux systems (Papi et al, 2013)

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Summary

Introduction

Chlorogenic acid is a well-known nutraceutical widely spread in plant foods. This phenolic compound, from the family of hydroxycinnamic acids, possesses many beneficial properties for health, including antioxidant, antidiabetic, antihypertensive, and antiobesity activities (Santana-Gálvez et al, 2017). Some in vitro studies have reported antiproliferative and cytotoxic activity of chlorogenic acid against human breast (Deka et al, 2017), lung (Yamagata et al, 2018), colon (Hou et al, 2017), bone (Zhang et al, 2019), and kidney cancer cells Chlorogenic acid is extensively metabolized by the human body (Olthof et al, 2003), which may diminish or nullify its in vitro anticancer activity, while the benefits found in vivo may be caused not by the compound itself but by its metabolites. More valuable information about the anticancer potential of chlorogenic acid can be obtained from its metabolites

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