Biological functions of kojic acid and its derivatives in medicine, cosmetics, and food industry: Insights into health aspects

Abstract

This review traces the road leading to the demonstration of a variety of kojic acid chemical and biological properties. It illustrates the biological effects of several synthetic kojic acid derivatives. Besides the main capability of kojic acid to inhibit the activity of tyrosinase in melanin synthesis, the focus is also on antibacterial, antifungal, antiproliferative, anti-inflammatory, and other biological activities of kojic acid derivatives, which may be applicable in medicine. Kojic acid derivatives manifest antiparasitic effects and its metal complexes may serve as potential radioprotective agents. Several kojic acid derivatives exert antidiabetic therapeutic potential as nuclear peroxisome proliferator-activated receptor alpha/gamma dual agonists. Kojic acid derivatives show pancreatic lipase inhibitor properties and some of its derivatives are cognate ligands for the histamine H 3 receptor. Recently, "KojoTacrines" were reported as novel perspective preparations for the therapy of Alzheimer's disease. Kojic acid derivatives possess insecticidal or pesticidal activity, and they are powerful chelators, able to form iron(III) containing nanocomposites, as well. Toxicology and health aspects of products containing kojic acid produced by the cosmetic, health care, or food industry are summarized. Kojic acid thus represents a highly attractive molecule containing a skeleton that allows the synthesis of new kojic acid derivatives to create a novel class of effective and specific pharmaceutical preparations.

Hirsutanone Isolated from the Bark of Alnus japonica Attenuates Melanogenesis via Dual Inhibition of Tyrosinase Activity and Expression of Melanogenic Proteins

“…Tyrosinase is a key enzyme that controls melanogenesis [ 10 ]. The suppression of melanin biosynthesis can be achieved by inhibiting tyrosinase activity or reducing the protein expression of melanogenic enzymes, including tyrosinase [ 5 , 6 , 7 , 8 , 9 , 10 ]. Therefore, we examined the direct inhibitory effect of Hir on tyrosinase activity using a cell-free mushroom tyrosinase system.…”

“…These conditions can lead to a deterioration in quality of life and are clinical and cosmetic concerns worldwide. Therefore, the development of melanin production inhibitors is important for controlling hyperpigmentation, and considerable efforts have led to the discovery of many melanin inhibitors, such as hydroquinone [ 5 ], kojic acid [ 6 , 7 ], and arbutin [ 8 , 9 ].…”

Curcumin‐based bioactive heterocycles derived via multicomponent reactions

“…[96][97][98] Organic and medicinal chemistry researchers have expressed a significant deal of interest in the synthesis of kojic acid derivatives as a readily available and biologically active precursor. [99,100] Reddy et al, [101] reported InCl 3catalyzed three-component reaction of kojic acid 27, aromatic aldehydes…”

Strategies for the Enhancement of Secondary Metabolite Production via Biosynthesis Gene Cluster Regulation in Aspergillus oryzae

“…For example, kojic acid, one of the primary secondary metabolites produced by A. oryzae [26], is widely used in cosmetics as the main component of various whitening products [27]. Kojic acid and its derivatives also serve as a raw material for antibacterial, antifungal, and anti-inflammatory agents in the pharmaceutical industry [28][29][30]. Researchers have also discovered polysaccharides with anti-tumor activity [31,32], active compounds against Alzheimer's disease, antibacterial compounds [33,34], and enzyme inhibitors [35] from various A. oryzae strains.…”