Inhibitory mechanisms of glabridin on tyrosinase

Chen, Jianmin; Yu, Xiuli; Huang, Yufeng

doi:10.1016/j.saa.2016.06.008

Cited by 87 publications

(66 citation statements)

References 37 publications

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“…Among several hormones and melanin‐inducer tested, α‐MSH‐stimulated melanocytes and keratinocytes showed higher TYR activity as compared to DOPA and 8‐MOP . Some of cells such as G361 did not have α‐MSH receptor, but melanin can be stimulated via other stimulators . Requirement of UV as melanin stimuli in G361 was differed from other cell in terms of intensity, type of UV, and its duration.…”

Section: Protocol and Assaysmentioning

confidence: 93%

“…This claim is supported by the fact that coumaric acid had tight binding affinity to the TYR catalytic site . Unlike coumaric acid and cinnamic acid, compounds, such as glabridin, a noncompetitive inhibitor, do not directly bind to the active site of TYR . Cinnamic acid and its derivatives (ie, hydroxycinnamic esters) also act as natural filters to UV‐B radiation and prevent hyperpigmentation in B16 cells .…”

Section: Depigmenting Compounds and Their Modulation On Melanogenesismentioning

confidence: 99%

“…On the other hand, fluorescence quenching method has been applied to study the interactions between depigmenting compound and TYR. The fluorescence emission spectra of TYR before and after the addition of depigmenting compound were measured at wavelengths of 290‐500 nm upon excitation at wavelength of 280 nm and recorded using F‐4600 spectrofluorophotometer …”

Section: Protocol and Assaysmentioning

confidence: 99%

“…46 Unlike coumaric acid and cinnamic acid, compounds, such as glabridin, a noncompetitive inhibitor, do not directly bind to the active site of TYR. 47 Cinnamic acid and its derivatives (ie, hydroxycinnamic esters) also act as natural filters to UV-B radiation and prevent hyperpigmentation in B16 cells. 48,49 Comparatively, acteoside, which had maximum absorption to UVB (283 nm) and UVA (335 nm), is a new potential UV-blocking agent, against UV-mediated pigmentation.…”

Section: Ta B L E 1 (Continued)mentioning

confidence: 99%

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Discovery of new depigmenting compounds and their efficacy to treat hyperpigmentation: Evidence from in vitro study

Lajis

Ariff

2019

J of Cosmetic Dermatology

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Summary Human skin pigmentation is a result of constitutive and facultative pigmentation. Facultative pigmentation is frequently stimulated by UV radiation, pharmacologic drugs, and hormones whereby leads to the development of abnormal skin hyperpigmentation. To date, many state‐of‐art depigmenting compounds have been studied using in vitro model to treat hyperpigmentation problems for cosmetic dermatological applications; little attention has been made to compare the effectiveness of these depigmenting compounds and their mode of actions. In this present article, new and recent depigmenting compounds, their melanogenic pathway targets, and modes of action are reviewed. This article compares the effectiveness of these new depigmenting compounds to modulate several melanogenesis‐regulatory enzymes and proteins such as tyrosinase (TYR), TYR‐related protein‐1 (TRP1), TYR‐related protein‐2 (TRP2), microphthalmia‐associated transcription factor (MITF), extracellular signal—regulated kinase (ERK) and N‐terminal kinases (JNK) and mitogen‐activated protein kinase p38 (p38 MAPK). Other evidences from in vitro assays such as inhibition on melanosomal transfer, proteasomes, nitric oxide, and inflammation‐induced melanogenesis are also highlighted. This article also reviews analytical techniques in different assays performed using in vitro model as well as their advantages and limitations. This article also provides an insight on recent finding and re‐examination of some protocols as well as their effectiveness and reliability in the evaluation of depigmenting compounds. Evidence and support from related patents are also incorporated in this present article to give an overview on current patented technology, latest trends, and intellectual values of some depigmenting compounds and protocols, which are rarely highlighted in the literatures.

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Section: Protocol and Assaysmentioning

confidence: 93%

Section: Depigmenting Compounds and Their Modulation On Melanogenesismentioning

confidence: 99%

Section: Protocol and Assaysmentioning

confidence: 99%

Section: Ta B L E 1 (Continued)mentioning

confidence: 99%

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Discovery of new depigmenting compounds and their efficacy to treat hyperpigmentation: Evidence from in vitro study

Lajis

Ariff

2019

J of Cosmetic Dermatology

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“…On the contrary, ascorbic acid had no significant reduction of melanin content and TYR activity relative to untreated control [61]. Glabridin, a reversible noncompetitive TYR inhibitor as demonstrated via mushroom tyrosinase assay, also had no significant inhibitory effects on melanin synthesis in zebrafish [62]. In contrast, sesamol, a bioactive lignan of Sesamum indicum , concentration-dependently inhibited melanin biosynthesis in zebrafish embryo.…”

Section: Application Of Zebrafish Modelmentioning

confidence: 99%

A Zebrafish Embryo as an Animal Model for the Treatment of Hyperpigmentation in Cosmetic Dermatology Medicine

Lajis

2018

Medicina

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For years, clinical studies involving human volunteers and several known pre-clinical in vivo models (i.e., mice, guinea pigs) have demonstrated their reliability in evaluating the effectiveness of a number of depigmenting agents. Although these models have great advantages, they also suffer from several drawbacks, especially involving ethical issues regarding experimentation. At present, a new depigmenting model using zebrafish has been proposed and demonstrated. The application of this model for screening and studying the depigmenting activity of many bioactive compounds has been given great attention in genetics, medicinal chemistry and even the cosmetic industry. Depigmenting studies using this model have been recognized as noteworthy approaches to investigating the antimelanogenic activity of bioactive compounds in vivo. This article details the current knowledge of zebrafish pigmentation and its reliability as a model for the screening and development of depigmenting agents. Several methods to quantify the antimelanogenic activity of bioactive compounds in this model, such as phenotype-based screening, melanin content, tyrosinase inhibitory activity, other related proteins and transcription genes, are reviewed. Depigmenting activity of several bioactive compounds which have been reported towards this model are compared in terms of their molecular structure and possible mode of actions. This includes patented materials with regard to the application of zebrafish as a depigmenting model, in order to give an insight of its intellectual value. At the end of this article, some limitations are highlighted and several recommendations are suggested for improvement of future studies.

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Evaluation of antityrosinase activity and mechanism, antioxidation, and UV filter properties of theaflavin

Chen

Ran

Wang

et al. 2021

Biotech and App Biochem

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Tyrosinase is a key metalloenzyme for the biosynthesis of melanin that plays a critical role in the prevention of skin damage caused by ultraviolet (UV) radiation. However, the overproduction of melanin may cause a variety of skin diseases. Due to the toxicity and inefficiency of existing tyrosinase inhibitors, it is urgent to identify safe and potent alternatives from natural sources. Theaflavin, a single-component extracted from black tea, has been found to possess a variety of pharmacological activities. Herein, the inhibition kinetics of theaflavin on tyrosinase and inhibitory mechanism were determined using spectroscopy, molecular docking, and zebrafish model. The results showed that theaflavin inhibited the diphenolase activity of tyrosinase in a reversible mixed type manner with IC 50 of 229.75 μmol/L and hindered the synthesis of melanin in zebrafish. This may be due to the formation of eight hydrogen bonds and hydrophobic effects between theaflavin and tyrosinase according to the results of molecular docking. To study the possible effects on the prevention of free radical-mediated skin cancer and photoaging caused by UV radiation, the antioxidation and UV filter properties of theaflavin were further verified. This study demonstrates that theaflavin is a potential multifunctional compound that can be used in cosmetic and medicinal products.

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Inhibitory mechanisms of glabridin on tyrosinase

Cited by 87 publications

References 37 publications

Discovery of new depigmenting compounds and their efficacy to treat hyperpigmentation: Evidence from in vitro study

Discovery of new depigmenting compounds and their efficacy to treat hyperpigmentation: Evidence from in vitro study

A Zebrafish Embryo as an Animal Model for the Treatment of Hyperpigmentation in Cosmetic Dermatology Medicine

Evaluation of antityrosinase activity and mechanism, antioxidation, and UV filter properties of theaflavin

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