Chlorogenic acid (CGA), a natural hydroxycinnamic phenolic acid, is widely found in coffee, Eucommia ulmoides leaves and potatoes. Numerous studies have highlighted that CGA exhibits diverse bioactivities, including antibacterial, anti-inflammatory, and antioxidant properties, making it valuable in pharmaceuticals, health foods, and industrial applications. Notably, its anti-tumor efficacy has garnered substantial research attention, with its activity validated in both in vitro and in vivo studies. Therefore, CGA has been recognized by the China Food and Drug Administration (CFDA) as a potential natural anticancer agent, demonstrating great promise for cancer treatment. This review discusses the physicochemical properties, botanical sources, pharmacokinetic characteristics, biosynthesis, and derivatives of CGA. Notably, it provides the first comprehensive analysis of the latest research progress on the anti-tumor effects of CGA from the perspective of multiple anti-tumor mechanisms, including its regulation of cell differentiation, induction of ferroptosis, and modulation of the tumor microenvironment (TME), and presents the first systematic evaluation of its applications in combination therapy. Notably, such combinations can reduce the monotherapy dosages, minimize toxicity, and enhance efficacy, highlighting the significant research value of CGA in cancer treatment. Finally, the article explores the critical scientific challenges confronting CGA in clinical oncology, including bioavailability and target specificity, while proposing future directions for translational research.
Qin et al. (Thu,) studied this question.