Title:Chlorogenic Acid Derivatives: Structural Modifications, Drug Design, and
Biological Activities: A Review
Volume: 24
Issue: 7
Author(s): Shima Joneidi, Seyedeh Roya Alizadeh*Mohammad Ali Ebrahimzadeh*
Affiliation:
- Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences Research Center, Mazandaran
University of Medical Sciences, Sari, Iran
- Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences Research Center, Mazandaran
University of Medical Sciences, Sari, Iran
Keywords:
Chlorogenic acid, polyphenol, biological activity, drug design, SAR, anti-oxidant activity, synthetic methods.
Abstract:
Background: Phenolic acids have recently gained considerable attention because of their
numerous practical, biological, and pharmacological benefits. Various polyphenolic compounds are
widely distributed in plant sources. Flavonoids and phenolic acids are the two main polyphenolic
compounds that many plants contain abundant polyphenols. Chlorogenic acid, one of the most abundant
phenolic acids, has various biological activities, but it is chemically unstable and degrades into
other compounds or different enzymatic processes.
Methods: In this review, we have studied many publications about CA and its derivatives. CA derivatives
were classified into three categories in terms of structure and determined each part’s effects on
the body. The biological evaluations, structure-activity relationship, and mechanism of action of CA
derivatives were investigated. The search databases for this review were ScienceDirect, Scopus, Pub-
Med and google scholar.
Results: Many studies have reported that CA derivatives have demonstrated several biological effects,
including anti-oxidant, anti-inflammatory, anti-microbes, anti-mutation, anti-carcinogenic, anti-viral,
anti-hypercholesterolemia, anti-hypertensive, anti-bacterial, and hypoglycemic actions. The synthesis
of new stable CA derivatives can enhance its metabolic stability and biological activity.
Conclusion: The present study represented different synthetic methods and biological activities of CA
derivatives. These compounds showed high antioxidant activity across a wide range of biological effects.
Our goal was to help other researchers design and develop stable analogs of CA for the improvement
of its metabolic stability and the promotion of its biological activity.