• Korean Journal of Korean Medical Institute of Dermatology and Aesthetics
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• v.1 no.1
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• pp.91-97
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• 2005

(1) Objectives: To discover natural skin-lightening agents, we have evaluated the inhibitory activity of EtOH extracts from 20 medicinal plants against mushroom tyrosinase. (2) Methods: Tyrosinase activity was determined by the dopachrome method using L-tyrosine as the substrates. (3) Results: Of the plant extracts tested, the extracts of 4 plants, Albizzia julibrissin, Curcuma longa, Anethum graveolens and Sophora flavescens, exhibited potent inhibitory activity (> 50%) in mushroom tyrosinase assay. Four plant extract, extracts of Agrimonia pilosa, Paeonia moutan, Magnolia obovata and Eugenia caryophyllata also showed relatively strong inhibitory (> 40%) against mushroom tyrosinase. (4) Conclusion: These active medicinal plants may be useful for the development of skin-whitening agents. Since the active medicinal plants may contain effective tyrosinase inhibitors even more than kojic acid, further study to identify the active constituents from the plants is expected.

• KSBB Journal
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• v.31 no.3
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• pp.151-157
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• 2016

The purpose of the present research was to investigate the physiological activities of the thermal treated eggplant on the skin. Five minute of thermal treatment at $100^{\circ}C$ had the highest polyphenol content of eggplant. However, below and over 5 min of thermal treatment time, they did not increase. When water and ethanol extracts were used, the maximum DPPH radical scavenging activities were obtained, 66.3 and 62.8%, respectively. Among various extracts, the acetone extract gave the highest cosmetic activity. Especially, when acetone extract (15.0 mg/mL) was used, the maximum inhibition activities of tyrosinase, elastase, and collagenase were obtained, 83.4, 78.2 and 62.5%, respectively. These results suggest the anti-wrinkle and whitening and effects of acetone extract were excellent. Therefore, it is should be considered as a promising candidate for novel cosmetic agents.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.44 no.1
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• pp.73-79
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• 2018

The primary cilium protrudes from the cell body like a bio-antenna that has many receptors, channels and signaling molecules to sense and response to external stimuli. The external environment such as ultraviolet irradiation, temperature, humidity, gravity and shear stress always influences skin. Skin responds to external stimuli and differentiates by making melanin, collagen and horny layer. Ciliogenesis participates in developmental processes of skin, such as keratinocyte differentiation and hair formation. And it was reported that skin pigmentation was inhibited when ciliogenesis was induced by sonic hedgehog-smoothened-GLI2 signaling. When skin is exposed to ultraviolet irradiation, alpha-melanocyte stimulating hormones (${\alpha}$-MSH) increase melanin synthesis through activation of the cAMP pathway in melanocytes. We observed that ${\alpha}$-MSH and cAMP production inducers inhibited ciliogenesis of melanocytes. Therefore, we thought that regulation of ciliogenesis is potential candidate target for the development of agents to treat undesirable hyperpigmentation of skin. As a result, we found out that an ethanol extract of Glycyrrhiza glabra (EGG) root and 3,4,5-trimethoxy cinnamate thymol ester (TCTE, Melasolv) significantly inhibit melanin synthesis of normal human melanocyte by inducing primary cilium formation. This study proposed new theory to regulate skin pigmentation and cosmetic components for skin whitening.

• Korean Journal of Pharmacognosy
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• v.33 no.4 s.131
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• pp.399-403
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• 2002

Three melanogenesis inhibitors were isolated from the roots and rhizomes of Veratrum nigrum L. and were identified as (3S,20S,25S)-22,26-iminocholesta-5,22(N)-dien-3-ol (verazine), (3S,2OR,25S)-22,26-iminocholesta-5,22(N)-dien-3-ol (epi-verazine) and (3R,23R)-14,15,16,17- tetradehydroveratraman-3,23-diol (veratramine) on the basis of their spectroscopic data. It was turned out that these compounds did not directly inhibit tyrosinase activity, the key enzyme responsible for the formation of melanin pigment while these compounds showed strong inhibition on the melanogenesis in B16 F1 mouse melanoma $(IC_{50}<1\;{\mu}g/ml)$. Due to the strong inhibitory activity and safety compared to current whitening agents such as arbutin, kojic acid and AHA, the compound can be a good candidate for new skin whitening agents.

• Journal of Mushroom
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• v.19 no.3
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• pp.150-159
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• 2021

Anti-melanogenesis and skin anti-wrinkle effects of methanol (ME) and hot water (HE) extracts from the fruiting bodies of Ganoderma applanatum were investigated in this study. The total phenolic contents of the ME and HE of the mushroom were 11.68 and 3.15 ㎍ GAEs/mg, respectively, whereas the total flavonoid contents of the ME and HE were 21.82 and 2.69 ㎍ QEs/mg, respectively. The survival rate of B16-F10 murine melanoma cells treated with 750 ㎍ ME and HE were 83.46% and 85.54%, respectively, thereby suggesting that mushroom extracts were slightly cytotoxic at the tested concentration. The in vitro tyrosinase inhibition by ME (83.15%) and HE (83.44%) was significantly lower than that of kojic acid (99.61%), the positive control, at 2.0 mg/mL. Although the inhibition of cellular melanin synthesis in B16-F10 melanoma cells by 2.0 mg/mL of ME (50.24%) and HE (51.24%) was lower than that of arbutin (64.84%), the inhibition by both ME and HE was higher than 50%. Collagenase inhibition by HE was comparable to 2.0 mg/mL epigallocatechin (EGCG), the positive control; however, elastase inhibition by ME and HE was lower than that of EGCG at the concentration tested. The results showed that the fruiting bodies of G. applanatum had good anti-tyrosinase, good anti-collagenase, and moderate anti-elastase activities, which might be useful for developing novel skin-whitening and anti-wrinkle agents.

• YAKHAK HOEJI
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• v.51 no.5
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• pp.350-354
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• 2007

Taurine has been shown to be tissue-protective against oxidant-induced injury and is a powerful regulator of the immune system. However, there is no study on the antimelanogenic effect of taurine. In this study, we investigated the whitening effect of taurine in B16F10 mouse melanoma cells. Cell viability was measured by MTT assay. We examined melanin contents and tyrosinase activity according to time and concentration. Extracellular signal regulated kinase (ERK) is an important regulator of melanogenesis. It has been reported that activated ERK induced microphthalmia associated transcription factor (MITF) phosphorylation and its subsequent degradation and thus reduced melanin synthesis. In our B16F10 cell culture system, taurine led to decrease melanin contents by 21% at 48 hr. We then observed taurine effects on ERK-P, MITF and tyrosinase by Western blot. ERK was activated at 18 hr and 24 hr, whereas MITF reduced. We could not observe any differences in the levels of tyrosinase. These results suggested that taurine inhibited melanogenesis by ERK signal pathway via MITF degradation. We expect that taurine has potential skin whitening agents in cosmetics.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.31 no.1 s.49
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• pp.91-96
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• 2005

Holographic quantitative structure-toxicity relationships (HQSTR) of alkyl-3,4-dihydroxybenzoate (A) and N-alkyl-3,4-dihydroxybenzamide (B) derivatives were analyzed and discussed. The HQSTR model X for the skin sensitivity showed the best predictability based on the cross-validated $r^2_{cv}.$ ($q^2 = 0.744$), non cross-validated, and conventional coefficient ($r^2_{ncv}.$=0.978). The relationships between melanogenesis inhibitory activities and skin sensitization of compounds have a tendency to a reciprocal proportion. Therefore, the more higher melanogenesis inhibitory activities of compounds were, the more lower skin sensitization of compounds became. The side chain, C1 ${\~}$ C3 part of R1-substituents in (A) and (B) did not exhibit any contribution to skin sensitization. Particularly, it is reveals that the skin sensitization of ester (A) were slightly lower (A < B) than that of amide (B) and melanogenesis Inhibitory activities of (A) were slightly higher (A > B) than that of (B). It is founded that the alkyl-3,4-dihydroxybenzoate derivatives (A) were an ideal compound as an ingredient of whitening agents.

• KSBB Journal
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• v.28 no.2
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• pp.137-145
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• 2013

In order to develop new skin whitening agents, we prepared the $CH_2Cl_2$ layer (NGC) and BuOH layer (NGB) of 75% EtOH extract of the Nelumbinis nucifera Gaertner. We measured their tyrosinase inhibitory activity in vitro and melanin synthesis inhibitory activity in B16-F1 melanoma cells. They did not show inhibitory activity against mushroom tyrosinase but showed melanin synthesis inhibitory activity in a dose-dependent manner. In a melanin synthesis inhibition assay, NGC and NGB suppressed melanin production up to 52% and 46% at a concentration of $100{\mu}g/mL$, respectively. To elucidate the mechanism of the inhibitory effects of NGC and NGB on melanogenesis, we measured the expression of melanogenesis-related proteins by western blot assay. As a result, NGC suppressed the expression of tyrosinase, tyrosinase related protein 1 (TRP-1), tyrosinase related protein 2 (TRP-2), phosphorylated cAMP responsive element binding (p-CREB) protein, and microphthalmia associated transcription factor (MITF). And NGB inhibited the protein expression of tyrosinase and MITF, but had no significant effect on TRP-1, TRP-2, and p-CREB expression. Moreover, NGB increased the expression of phosphorylated extracellular signal-regulated kinase (p-ERK). In addition, we examined the inhibitory effect on the glycosylation of tyrosinase. As a result, NGC and NGB inhibited the activity of ${\alpha}$-glucosidase in vitro and the glycosylation of tyrosinase in B16-F1 melanoma cells. From these results, we concluded that NGC and NGB could be used as active ingredients for skin whitening.

• YAKHAK HOEJI
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• v.52 no.3
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• pp.165-171
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• 2008

To develop effective skin whitening agents, we tested natural herbal extracts for their melanogenic inhibitory activities. Sedum samentosum was selected for its inhibitory effect on melanogenesis in B16 melanoma cells. Ethanolic extract of S. samentosum (SSE) was evaluated for antioxidative effect and tyrosinase inhibitory activity of melanogenesis. We investigated the changes in protein level and mRNA level of tyrosinase, tyrosinase related protein (TRP)-1 and TRP-2 by using western blotting and RT-PCR, respectively. SSE showed scavenging activities of free radicals and reactive oxygen species (ROS) with the $IC_{50}$ of 342.7 $\mug/ml$ against 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and 64.69 $\mug/ml$ against superoxide radicals in the xanthine/xanthine oxidase system, respectively. SSE treatment suppressed the biosynthesis of melanin up to 46% and reduced tyrosinase activity up to 51% at 100 $\mug/ml$ in B16 melanoma cells. The tyrosinase activity and tyrosinase expression in B16 melanoma cells were reduced in a dose-dependent manner by SSE. Also, SSE was able to significantly inhibit tyrosinase and TRP-1 expression in mRNA level. These results suggest that SSE inhibited melanin production which may be dependent on tyrosinase activity and expression in B16 melanoma cells, and an effective whitening agent for the skin.

• YAKHAK HOEJI
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• v.41 no.4
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• pp.456-461
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• 1997

Tyrosinase is known to accelerate the melanin polymer biosynthesis in melanocyte, so tyrosinase inhibitors hinder the melanin polymer biosynthesis and are useful not only for th e material used in cosmetics as skin-whitening agents but also as the remedy for disturbances in pigmentation. During our search for new melanin biosynthesis inhibitors from natural sources, 130 higher plants were tested for the inhibitory effect against tyrosinase activity by the mushroom tyrosinase assay. Among them, Carex humilis ($IC_{50}$, 10vg/ml), Sophora flavescence ($IC_{50},\;20{\sim}50{mu}g/ml$) and Styrax japonica ($IC_{50},\;10{\mu}g/ml$) inhibited the tyrosinase activity strongly.