Tyrosinase Inhibitors Naturally Present in Plants and Synthetic Modifications of These Natural Products as Anti-Melanogenic Agents: A Review

Abstract

Tyrosinase is a key enzyme target to design new chemical ligands against melanogenesis. In the current review, different chemical derivatives are explored which have been used as anti-melanogenic compounds. These are different chemical compounds naturally present in plants and semi-synthetic and synthetic compounds inspired by these natural products, such as kojic acid produced by several species of fungi; arbutin—a glycosylated hydroquinone extracted from the bearberry plant; vanillin—a phenolic aldehyde extracted from the vanilla bean, etc. After enzyme inhibition screening, various chemical compounds showed different therapeutic effects as tyrosinase inhibitors with different values of the inhibition constant and IC50. We show how appropriately designed scaffolds inspired by the structures of natural compounds are used to develop novel synthetic inhibitors. We review the results of numerous studies, which could lead to the development of effective anti-tyrosinase agents with increased efficiency and safety in the near future, with many applications in the food, pharmaceutical and cosmetics industries.

Unraveling the chemical profile, antioxidant, enzyme inhibitory, cytotoxic potential of different extracts from Astragalus caraganae

“…[34] In this context, recent tendencies in the discovery of tyrosinase inhibitors derived from plants, have provided a rationale for the continued research on natural tyrosinase inhibitors. [35,36] In the present study, while all extracts showed tyrosinase inhibition (9.37-63.56 areas. As such, inhibition of cholinesterase enzymes is an effective therapeutic approach for treating Alzheimer's disease symptoms.…”

“…[ 34 ] In this context, recent tendencies in the discovery of tyrosinase inhibitors derived from plants, have provided a rationale for the continued research on natural tyrosinase inhibitors. [ 35,36 ]…”

Tetrahedral framework nucleic acid loaded with glabridin: A transdermal delivery system applicated to anti‐hyperpigmentation

“…TYR, MITF, TRP‐1 and TRP‐2 play important roles in melanin synthesis. After activation, TYR converts l ‐tyrosine into dopaquinone, which can be used in subsequent reactions to produce melanin 53–55 . During this process, factors secreted by keratinocytes bind to melanocyte receptors and initiate melanin synthesis, including cAMP stimulation 56,57 .…”

The Effects of 2′-Hydroxy-3,6′-Dimethoxychalcone on Melanogenesis and Inflammation

“…Nevertheless, arbutin is chemically unstable in its natural form and can release toxic hydroquinone when separated from hydroquinone and glucose. Kojic acid can lead to side effects such as contact dermatitis, sensitization, and erythema, and its use has been restricted due to its storage instability [32][33][34]. Consequently, there is a need to develop melanogenesis inhibitors that effectively hinder melanogenesis with fewer potential risks and side effects for humans.…”

“…In macrophages, NF-κB remains inactive in the cytoplasm when bound to IκB-α, but upon exposure to external stimuli such as LPS, it is degraded and released with the phosphorylation of IκB-α, which activates NF-κB. Subsequently, the activated NF-κB translocates from the cytoplasm to the nucleus and triggers the activation of various pro-inflammatory cytokines and pro-inflammatory transcription factors [32,33]. However, here, this phenomenon was reversed after 3,6 -DMC treatment, through which we observed that the phosphorylation of IκB-α was reduced and the degradation of IκB-α induced by LPS was inhibited in RAW 264.7 cells, resulting in the increased binding of NF-κB to IκB-α (Figure 13).…”