Inhibitors and Enhancers of Melanogenesis

Taı̈eb, Alain; Cario‐André, Muriel; Briganti, Stefania; Picardo, Mauro

doi:10.1002/9783527636150.ch5

Cited by 9 publications

(7 citation statements)

References 288 publications

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“…61 The classification of tyrosinase inhibitor strenge or the IC 50 value based on the structure and mechanism of tyrosinase action is not easy due to the results of the kinetics presented with different testing system from mushroom tyrosinase, mammaliam tyrosinase, melanocytic cultures, cocultures of keralinocytes and melanocytes and in vivo application to animal skin. 62 Saponin can be found in vegetables, herbs and beans such as peas, soybeans, saponin have foaming propterties that caused by the combination between a hydrophobic and a hydrophillic parts. Health benefits of saponins are shown in many from research including protective bone loss, cholesterol reduction, anti-cancer and antibacterial.…”

Section: Phytochemical Screeningmentioning

confidence: 99%

Phytochemicals, Antioxidants and Anti-tyrosinase Analyses of Selected Ginger Plants

Rachkeeree¹,

Kantadoung²,

Puangpradub³

et al. 2020

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Background: Some of Zingeberaceae are not widely used for medicine of food, although in Thailand have been used them for many reasons about health or the diet. This study evalued the phytochemicals and anti-tyrosinase activities of 16 plant species of Alpinia, Amomum, Curcuma, Etlingera and Kaemferia (Zingiberaceae). Methods: The extractions of dried powdered rhizomes were performed using n-hexane, ethylacetate and ethanol. Percentage extract yield of the samples varied among species and solvent extracts. Chemical groups (alkaloids, flavonoids, tannins, polyphenols, steroids and terpenoids) were identified using phytochemical screening. The total phenolic contents (TPC) were analyzed using the Folin-Ciocalteu's reagent, while antioxidant activities were detected using 2,2-diphenyl-1picrylhydrazyl (DPPH) and the 2,2'-azino-bis (3-ethylbenzothizoline-6-sulphonic acid) (ABTS .+ ). The anti-tyrosinase was expressed to the half maximal inhibitory concentration (IC 50 ) value (mg/mL). Results: The ethyl acetate extract of Amomum showed the highest value of TPC. The strongest antioxidant activity were found in Amomum and Kaemferia extracts, while ethyl acetate and ethanol extracts of all samples have a better antioxidant properties than the n-hexane extracts. On the other hand, the n-hexane extracts have the highest anti-tyrosinase potential in all samples and of these, Curcuma extracts were the best group. Conclusion: Our research indicated that plants of the Zingiberaceae would be new sources of antioxidants and anti-tyrosinase for further natural product developments in cosmetics, food or nutraceuticals.

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Section: Phytochemical Screeningmentioning

confidence: 99%

Phytochemicals, Antioxidants and Anti-tyrosinase Analyses of Selected Ginger Plants

Rachkeeree¹,

Kantadoung²,

Puangpradub³

et al. 2020

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“…The overproduction of melanin causes medical problems such as postinflammatory melanoderma and melasma. . Many studies have focused on understanding the precise mechanism of melanin production because developing antimelanogenic agents is a critical goal in the clinical and cosmetic fields.…”

Section: Introductionmentioning

confidence: 99%

Novel inhibitory effect of the antidiabetic drug voglibose on melanogenesis

Bin

Seo

Yang

et al. 2013

Experimental Dermatology

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Overproduction of melanin can lead to medical disorders such as postinflammatory melanoderma and melasma. Therefore, developing antimelanogenic agents is important for both medical and cosmetic purposes. In this report, we demonstrated for the first time that the antidiabetic drug voglibose is a potent antimelanogenic agent. Voglibose is a representative antidiabetic drug possessing inhibitory activity towards human α-glucosidase; it blocked the proper N-glycan modification of tyrosinase, resulting in a dramatic reduction of the tyrosinase protein level by altering its stability and subsequently decreasing melanin production. Acarbose, another antihyperglycaemic drug that has a lower inhibitory effect on human intracellular α-glucosidase compared with voglibose, did not cause any changes in either the N-glycan modification of tyrosinase or the tyrosinase protein level, indicating that voglibose was the most efficient antimelanogenic agent among the widely used antihyperglycaemic agents. Considering that voglibose was originally selected from the valiolamine derivatives in a screen for an oral antidiabetic drug with a strong inhibitory activity towards intestinal α-glucosidase and low cell permeability, we propose an alternative strategy for screening compounds from valiolamine derivatives that show high inhibitory activity towards human intracellular α-glucosidases and high cell permeability, with the goal of obtaining antimelanogenic agents that are effective inside the cells.

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“…The inhibition of melanin biosynthesis (hypopigmentation or anti-melanogenesis) in the skin plays a critical role in protecting against various skin problems, such as spots, melasma, and freckles. Excessive production and accumulation of melanin (hyperpigmentation and melanogenesis) may cause serious skin diseases, such as skin cancer [ 1 ]. Therefore, many scientists have been trying to find a safe and effective whitening agent for cosmetic and therapeutic applications.…”

Section: Introductionmentioning

confidence: 99%

Novel Quercetin Derivative of 3,7-Dioleylquercetin Shows Less Toxicity and Highly Potent Tyrosinase Inhibition Activity

Choi

Yang

Kim

et al. 2021

IJMS

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Quercetin is a well-known plant flavonol and antioxidant; however, there has been some debate regarding the efficacy and safety of native quercetin as a skin-whitening agent via tyrosinase inhibition. Several researchers have synthesized quercetin derivatives as low-toxicity antioxidants and whitening agents. However, no suitable quercetin derivatives have been reported to date. In this study, a novel quercetin derivative was synthesized by the SN2 reaction using quercetin and oleyl bromide. The relationship between the structures and activities of quercetin derivatives as anti-melanogenic agents was assessed using in vitro enzyme kinetics, molecular docking, and quenching studies; cell line experiments; and in vivo zebrafish model studies. Novel 3,7-dioleylquercetin (OQ) exhibited a low cytotoxic concentration level at >100 µg/mL (125 µM), which is five times less toxic than native quercetin. The inhibition mechanism showed that OQ is a competitive inhibitor, similar to native quercetin. Expression of tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2), and microphthalmia-associated transcription factor was inhibited in B16F10 melanoma cell lines. mRNA transcription levels of tyrosinase, TRP-1, and TRP-2 decreased in a dose-dependent manner. Melanin formation was confirmed in the zebrafish model using quercetin derivatives. Therefore, OQ might be a valuable asset for the development of novel skin-whitening agents.

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Inhibitors and Enhancers of Melanogenesis

Cited by 9 publications

References 288 publications

Phytochemicals, Antioxidants and Anti-tyrosinase Analyses of Selected Ginger Plants

Phytochemicals, Antioxidants and Anti-tyrosinase Analyses of Selected Ginger Plants

Novel inhibitory effect of the antidiabetic drug voglibose on melanogenesis

Novel Quercetin Derivative of 3,7-Dioleylquercetin Shows Less Toxicity and Highly Potent Tyrosinase Inhibition Activity

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