• Korean Journal of Food Science and Technology
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• v.27 no.6
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• pp.891-896
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• 1995

In order to screen natural inhibitor of tyrosinase which catalyzes an enzymatic browning of some foods and in vivo synthesis of melanin, inhibitory effect of 129 edible plants and 15 chemical compounds on the in vivo melanin synthesis by mushroom tyrosinase was analyzed. Among leafy vegetables tested, radish bud, red chicory, Shepherd's purse and small green onion were found to have more than 50% tyrosinase inhibition effect in the descending order. Chinese radish and garlic in root vegetables, and nameko, shiitake and oyster mushroom in mushrooms, and teas showed also more than 50% inhibition effect. Among fruit vegetables tested, red pepper, Chinese quince and avocado were found to have more than 50% tyrosinase inhibition effect, while fruits generally showed low inhibitory effect. Medicinal plants which inhibit tyrosinase more than 50% were mume fructus>cinamomi ramulus>rubi fructus>mori cortex>biotae orientalis folium>puerariae radix, and herbs with more than 50% inhibitory effect were allspice>clove>mustard. In some chemical compounds tested, 4-hexylresorcinol, L-cysteine, glutathione, sodium bisulfite and kojic acid showed powerful inhibition effect on mushroom tyrosinase.

• Korean Journal of Food Science and Technology
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• v.33 no.6
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• pp.760-763
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• 2001

To develop a functional beverage from Korean cherry (Prunus tomentosa Thunberg), inhibition effect of ethanol extract and juice of the korean cherry on melanin systhesis and tyrosinase activity in vitro was investigated. Inhibition ratio of tyrosinase activity increased as the concentration of solid of korean cherry juice increased, and inhibition affect was high in initiation step of enzyme reaction and then gradually decreased. Inhibition ratio of tyrosinase activity was high in the 70% (v/v) ethanol extract of the cherry and the highest in the ethyl acetate fraction of the 70% (v/v) ethanol extract. Ultimatly, the amounts of functional matter (melanin synthesis inhibitor) in the cherry was highest in ethyl acetate fraction of the ethanol extract.

• Journal of Ginseng Research
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• v.39 no.3
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• pp.238-242
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• 2015

Background: Panax ginseng has been used to prolong longevity and is believed to be useful for improving skin complexion. Ginsenosides are the most active components isolated from ginseng, and ginsenoside Rg3 (G-Rg3) in particular has been demonstrated to possess antioxidative, antitumorigenic, and anti-inflammatory properties. The aim of this study was to examine the ability of G-Rg3 to inhibit melanogenesis. Methods: The effects of G-Rg3 on melanin contents and the protein levels of tyrosinase, microphthalmia-associated transcription factor (MITF), and tyrosinase-related protein 1 (TRP1) were evaluated. Melanogenesis-regulating signaling molecules such as Akt and extracellular signal-regulated kinase (ERK) were also examined to explore G-Rg3-induced antimelanogenic mechanisms. Results: G-Rg3 was found to significantly inhibit the synthesis of melanin in normal human epidermal melanocytes and B16F10 cells in a dose-dependent manner. The activity of cellular tyrosinase and the expression of MITF, tyrosinase, and TRP1 were all reduced, whereas ERK was strongly activated. PD98059 (a specific inhibitor of ERK) attenuated the G-Rg3-induced inhibition of melanin synthesis and tyrosinase activity. Conclusion: Taken together, these results showed that G-Rg3 induces the activation of ERK, which accounts for its antimelanogenic effects. G-Rg3 may be a promising safe skin-whitening agent, adding to the long list of uses of P. ginseng for the enhancement of skin beauty.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.26 no.1
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• pp.1-18
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• 2013

Objective: Recently the demands for the effective and safe depigmentative and anti-aging agents of the skin have increased due to the medical, pharmaceutical and cosmetic reasons. The purpose of this study is to investigate the MKG(Methanol Extract of Kaempferia galanga) and their dermal bioactivity properties related to cosmeceuticals such as depigmentation. Methods: We assessed inhibitory effects of MKG on melanin production in B16/F10 melanoma cells, on mushroom tyrosinase activity, effects of MKG on the expression tyrosinase, TRP-1, TRP-2, GSK-$3{\beta}$, CREB, MITF in B16/F10 melanoma cells without cytotoxicity range. Cell viability was measured by MTT assay and tyrosinase activity was assessed using by DOPA staining, western-blot analysis. We measured inhibition of melanin synthesis and tyrosinase activity by down-regulation of melanogenic enzyme expressions in ${\alpha}$-MSH induced melanogenesis B16/F10 melanoma cells. Results: MKG inhibited tyrosinase-activity, total melanin contents and dendrite out-growth. MKG inhibited melanogenesis by down-regulation of tyorsinase, TRP-1, TRP-2, CREB, and MITF in B16/F10 cells. The treatment with MKG at the 12.5, $25{\mu}g/ml$ level significantly inhibited the melanin synthesis induced ${\alpha}$-MSH in B16/F10 melanoma cells compared with untreated control. Conclusion: These results suggest that MKG inhibit melanin biosynthesis which is involved in hyper-pigmentation. So MKG is considered to be used as a whitening components reducing cytotoxicity.

• The Korean Journal of Physiology and Pharmacology
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• v.26 no.2
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• pp.113-123
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• 2022

Diarylpropionitrile (DPN), a selective agonist for estrogen receptor β (ERβ), has been reported to regulate various hormonal responses through activation of ERβ in tissues including the mammary gland and brain. However, the effect of DPN on melanogenesis independent of ERβ has not been studied. The aim of this study is to examine the possibility of anti-melanogenic effect of DPN and its underlying mechanism. Melanin contents and cellular tyrosinase activity assay indicated that DPN inhibited melanin biosynthesis in alpha-melanocyte stimulating hormone-stimulated B16F10 melanoma cell line. However, DPN had no direct influence on in vitro tyrosinase catalytic activity. On the other hand, 17β-estradiol had no effect on inhibition of melanogenesis, suggesting that the DPN-mediated suppression of melanin production was not related with estrogen signaling pathway. Immunoblotting analysis showed that DPN down-regulated the expression of microphthalmia-associated transcription factor (MITF), a central transcription factor of melanogenesis and its down-stream genes including tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2. Also, DPN attenuated the phosphorylation of protein kinase A (PKA) and cAMP-response element-binding protein (CREB). Additionally, DPN suppressed the melanin synthesis in UVB-irradiated HaCaT conditioned media culture system suggesting that DPN has potential as an anti-melanogenic activity in physiological conditions. Collectively, our data show that DPN inhibits melanogenesis via downregulation of PKA/CREB/MITF signaling pathway.

• Microbiology and Biotechnology Letters
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• v.37 no.1
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• pp.49-54
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• 2009

Rhapontin is the glycosylated stilbene compound, and comprising major component of rhubarb root extract. Rhapontin has been used as a raw material of skin-whitening cosmetics in Korea. Rhapontigenin, the aglycone of rhapontin, has been suggested to be more active than its glycosylated form. Therefore, the rhubarb root extract was treated with commercial enzyme, Pectinex to remove glycosylated moiety of rhapontin and rhapontigenin was prepared. The resulting material was analysed and identified as rhapontigenin by proton NMR and MALDI-Mass. Rhapontigenin exhibited tyrosinase inhibitory activity with an $IC_{50}$ of $126.72{\mu}g/mL$. The tyrosinase inhibitory activity of rhapontigenin was six times higher than that of rhapontin. In melanin biosynthesis inhibition assay using Streptomyces bikiniensis, rhapontigenin showed wider inhibition zone than that of rhapontin. From these results, we expect that rhapontigenin has stronger skin whitening effect than rhapontin and has advantages in cosmetic industry.

• Journal of Applied Biological Chemistry
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• v.54 no.4
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• pp.284-289
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• 2011

The extracts of Agrimonia pilosa L. were investigated for the inhibitory effect on the melanin synthesis in B16/F10 mouse melanoma cells as a functional ingredient for cosmetic products. Tyrosinase inhibition activities were 42% in A. pilosa L. 70% ethanol extract at $500{\mu}g/mL$. The protein and mRNA expression of tyrosinase, which are all skin-whitening related factors, showed that A. pilosa L. water and A. pilosa L. 70% ethanol extracts inhibited the protein bio-synthesis in B16F10 melanoma cell. Results indicate that the A. pilosa L. extracts tested in the present study have skin whitening activity and can be used as a functional ingredient for cosmetic compositions.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.23 no.3
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• pp.11-32
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• 2010

Objective : The aim of this study is to determine the effects of Dendrobii herba extract and Punica granatum extract on skin disease and skin beauty. Methods : To investigate in vitro anti-oxidant activity assay, ethanol extracts of medicinal plants tested by DPPH radical, xanthine oxidase activity. In the next experiment, to investigate anti-inflammatory activity assay, examined by relations in NO synthesis, IL-$1{\beta}$, IL-6, TNF-${\alpha}$, NF-${\kappa}B$, COX-2, MAP kinase. To study Skin wrinkle formation effect, we were examined by tyrosinase activities, melanin synthesis in MNT-1 cell. Results : 1. In an anti-oxidant test, Dendrobii and Punica granatum extract showed high radical scavenging activity. 2. In an anti-inflammatory test, Dendrobii herba and Punica granatum extract weakly inhibited the lipopolysaccharide(LPS)-induced nitric oxide(NO) release from RAW 246.7 macrophage cells. Dendrobii herba and Punica granatum extract also inhibited LPS-induced IL-$1{\beta}$ and COX-2 expressions. The inhibitory effect of Dendrobii herba and Punica granatum extract on macrophage activation were via the inhibition of NF-${\kappa}B$, evidenced by transient transfection assay. however, Dendrobii herba and Punica granatum extract did not have any effects about activation of Jun-N-terminal kinase(JNK) and inhibition of p38 MAP kinase in RAW 264.7 cells. 3. In the skin wrinkle formation assay, Dendrobii herba and Punica granatum extract weakly inhibited collagenase and elastase, however it was not statistically significant. 4. In the skin whitening assay, Dendrobii herba and Punica granatum extract weakly inhibited tyrosinase activity, however, it was not statistically significant. They did not have any effect on melanin synthesis, indicating that they could not be applicable for skin whitening. Conclusion : Dendrobii herba extract and Punica granatum extract may play a significant role in skin disease and skin beauty.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.1
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• pp.29-32
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• 2004

Inhibition of the early N-glycosylation process in the endoplasmic reticulum prevents the activation of tyrosinase, a key enzyme for melanin biosynthesis. This work aims at evaluating the increased activity of N-glycosylation inhibitors in vitro b, employing a nano-sized pH-sensitive liposome as a delivery carrier. Melexsome, a pH-sensitive nano carrier loaded with glycosylation inhibitos, was prepared by the hydration method with phospholipids and cholresterol-based amphiphiles. Inhibitory effects of Melexsome on the N-glycosylation process were evaluated by EndoH ＆ PNGaseF digestion and the western blotting. Melanin synthesis was also monitored after treatment with Melexsome Interestingly, Melexsome effectively increased the efficacy of N-glycosylation inhibitors. Melexsome was also much more efficiently translocated into the cytoplasm as observed in CLSM. These results demonstrated that the amphiphilic lipid-based pH-sensitive nano-carriers could be, used as an efficient delivery system for N-glycosylation inhibitor to enhance the effects of skin whitening cosmetics.

• Molecular & Cellular Toxicology
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• v.2 no.2
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• pp.81-88
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• 2006

Sphingolipid metabolites regulate many aspects of cell proliferation, differentiation, and apoptosis. In the present study, we have assessed the effects of the novel phytosphingosine derivative, N-acetylphytospingosine (NAPS), on the depigmentation of murine B16F10 melanoma cells, and have also attempted to identify the possible signaling pathway involved, in comparison with $C_{2}-ceramide$. NAPS and $C_{2}-ceramide$ both inhibited the growth of the B16F10 cells in a dose-dependent manner. Melanin content and tyrosinase activity were significantly reduced in response to treatment with NAPS and $C_{2}-ceramide$ at concentrations in a range between $1-5\;{\mu}M$. However, the levels of tyrosinase mRNA, as well as the levels of tyrosinase related protein-1 (TRP-1) and tyrosinase related protein-2 (TRP-2) genes and the level of tyrosinase protein remained unaffected by treatment with either NAPS or $C_{2}-ceramide$. We also attempted to determine the signaling pathway exploited by NAPS and $C_{2}-ceramide$. Interestingly, the phosphorylation of Akt/PKB at serine 473 by NAPS was reduced at the 5 minute mark, whereas $C_{2}-ceramide$ induced the phosphorylation of Akt/PKB at serine 473. Finally, Akt/PKB activity in the NAPS-treated cells was elevated in comparison with the untreated cells. LY294002, a specific PI3-K inhibitor which is located upstream of Akt/PKB, inhibited the phosphorylation of Akt/PKB, but induced an increase in melanin synthesis. These results suggest that the activation of Akt/PKB at serine 473 is related with the suppression of melanin production in the B16F10 mouse melanoma cells. Therefore, the mechanisms exploited by NAPS and $C_{2}-ceramide$ responsible for the depigmentation of B16F10 cells were concluded to involve the inhibition of melanosomal tyrosinase activity.