• Archives of Pharmacal Research
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• v.25 no.6
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• pp.885-888
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• 2002

Four diarylheptanoids, (5R)-1,7-bis (3,4-dihydroxyphenyl)-heptane-5-O-$\beta$-D-glucoside (1), (5R)-1,7-bis (3,4-dihydroxyphenyl)-heptane-5-ol (2), oregonin (3), hirsutanonol (4), were isolated from the bark of Alnus hirsuta Turcz and its inhibitory effects on melanogenesis by measuring the melanin level and tyrosinase activity in B16 melanoma cell were examined. Melanin level and tyrosinase activity were reduced to 75 to 85% by addition of diarylheptanoids to incubation medium of the melanoma cell. On the other hand, melanin level and tyrosinase activity were reduced to 13 to 43% by the addition of diarylheptanoids to incubation medium of the melanoma cell treated with melanogenesis stimulator, $\alpha$-MSH and forskolin. These melanogenesis inhibitory effects were significantly different compared with control.

• Proceedings of the SCSK Conference
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• 2003.09b
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• pp.44-49
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• 2003

$\alpha$-MSH plays an important role in UV induced melanogenesis in human skin. It is believed to exert its effects by binding to $\alpha$-MSH receptor that in turn activates adenylate cyclase and increase melanocyte proliferation, dendricity and melanogenesis. In this study, we evaluated plant extracts showing the inhibitory activity on $\alpha$-MSH induced melanogenesis. The Cnidium officinale extracts showed high inhibitory activity on $\alpha$-MSH induced melanogenesis. It ($50{\mu}\textrm{g}$/ml) inhibited the melanin synthesis activated by $\alpha$-MSH in B-16 melanoma cells. Also, we isolated active compound from C. officinale extracts by Mass spectrophotometer, HPLC. It was identified as Senkyunolide A. It showed the same inhibitory activity as C. officinale extracts at the lower concentration. Finally, Senkyunolide A from Cnidium officinale extracts could playas $\alpha$-MSH antagonist and be used as a strong ingredient for skin whitening cosmetics.

• Biomedical Science Letters
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• v.13 no.4
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• pp.313-317
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• 2007

Melanogenesis refers to the biosynthesis of melanin pigment in melanocytes. Melanogenesis is controlled by the intra- and extracellular environments. In the present study, to develop a new whitening agent, it was investigated the antioxidant activity and the inhibitory effect of Ailanthi Radicis Cortex extract on tyrosinase activity and on melanogenesis in the B16/F1 melanoma cells. The inhibition ratio of tyrosinase activity of ethylacetate fraction from Ailanthi Radicis Cortex was higher than that of arbutin. The ethylacetate fraction showed scavenging activities of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and superoxide anion radicals in a dose dependent manner. The highest inhibitory activity of melanogenesis was also in ethylacetate fraction ($40.0{\pm}5%$ at the concentration of $400{\mu}g/ml$). This study demonstrates that the Ailanthi Radicis Cortex extract might be used to be a potential agent for skin whitening.

• Korean Journal of Plant Resources
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• v.32 no.4
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• pp.275-281
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• 2019

The pathological condition of excessive melanogenesis causing freckles, melasma, senile lentigo, pigmented acne scars, and cancer has a critical impact on the wellness of individuals. The mechanism of melanogenesis is related to the expression of melanogenic enzymes. Here, we evaluated the inhibitory effect of pine cone (Pinus densiflora) extracts on melanogenesis. P. densiflora, the Korean Red Pine, is the predominant tree species in the cool, temperate forests of northeast Asia, occurring in pure stands across Korea, Japan, and parts of northern China and Russia. P. densiflora leaves, pollen, and bark have been widely used for traditional medicine, or edible purposes. However, pine cones are rarely used as natural raw materials, although they contain many bioactive phytochemicals. The pine cone ethyl acetate fraction (PEF) showed no toxicity to B16F10 cells at a concentration of less than $100{\mu}g/mL$. PEF inhibited the expression of microphthalmiaassociated transcription factor (MITF), tyrosinase and tyrosinase-related factors in B16F10 cells treated with 3-Isobutyl1-methylxanthine (IBMX). These results suggest that pine cones can be used as an effective natural melanogenesis inhibitory agent.

• Biomolecules & Therapeutics
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• v.23 no.3
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• pp.283-289
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• 2015

The half-dried leaves of Stewartia. pseudocamellia were extracted with hot water (SPE) and partitioned with n-hexane (SPEH), dichloromethane (SPED), and ethyl acetate (SPEE) successively. SPE and SPEE showed significant inhibitory effects against melanogenesis and tyrosinase activities. By bioassay-guided isolation, ten phenolic compounds were isolated by column chromatography from SPEE. The whitening effect of the isolated compounds from SPEE were tested for the inhibitory activities against melanogenesis using B16 melanoma cells, in vitro inhibition of tyrosinase, and L-3,4-dihydorxy-indole-2-carboxylic acid (L-DOPA) auto-oxidation assay. A cytotoxic activity assay was done to examine the cellular toxicity in Raw 264.7 macrophage cells. Of the compounds isolated, gallic acid and quercetin revealed significant inhibitory activities against melanogenesis compared to arbutin. In particular, quercetin exhibited similar inhibitory activities against tyrosinase and L-DOPA oxidation without cytotoxicity. These results suggested that SPE could be used as a potential source of natural skin-whitening material in cosmetics as well as in food products.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.26 no.1
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• pp.199-212
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• 2000

A series of novel ascorbic acid derivatives, polyethoxylated ascorbic acid (PEAA) were synthesized by coupling ascorbic acid with polyethylene glycol (PEG) of two molecular weights (MW: 350 and 550) at the C-2 or C-3 hydroxyl group (2PEAA350, 3PEAA350, 2PEAA550, 3PEAA550) to increase the stability and retain the activity, as a skin whitening agent. Their stability, scavenging activity against free radical, inhibitory activity against tyroxinase and inhibitory activity of melanin synthesis in Bl6 melanoma cell of PEAAs were evaluated in viかo and compared with those of ascorbic acid and 3-O-ethyl ascorbic acid (3OEAA), a Con stable vitamin C derivative. Among PEAAs, 2PEAA350 and 2PEAA550 tad high scaveniging activity against See radical, inhibitory activity against tyrosinase and inhibitory activity if melanogenesis but low stability, 3PEAA350 had high stability and moderate scavenging activity against free radical, infibitory activity against tyrosinase and inhibitory activity of melanogenesis. The stability, scavenging activity against free radical and inhibitory activity of melanogenesis of 3PEAA350 were higher than those of 30EAA. The most stable 3PEAA350 among PEAAs was nontoxic in various toxicological tests. These results suggest that PEAA would be a good whitening agent far enhancing stability and bioavailability.

• 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.

• Journal of Microbiology and Biotechnology
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• v.17 no.10
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• pp.1585-1590
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• 2007

Although a number of melanogenesis inhibitors have recently been reported and used as cosmetic additives, none is completely satisfactory, leaving a need for novel skin-depigmenting agents. Thus, to develop a novel skin depigmenting agent from natural sources, the inhibition of melanogenesis by Chinese plants was evaluated. A methanolic extract of Nigella glandulifera Freyn was found to inhibit the melanin synthesis of murine B16F10 melanoma cells by 43.7% and exhibited a low cytotoxicity (8.1%) at a concentration of $100\;{\mu}g/ml$. Thus, to identify the melanogenesis-inhibiting mechanism, the inhibitory activity towards tyrosinase, the key enzyme of melanogenesis, was further evaluated, and the results showed inhibitory effects on the activity of intracellular tyrosinase yet not on mushroom tyrosinase. Finally, to isolate the compounds with a hypopigmenting capability, activity-guided isolation was performed, and Dioctyl phthalate identified as inhibiting melanogenesis.

• Microbiology and Biotechnology Letters
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• v.49 no.1
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• pp.24-31
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• 2021

This study aimed to investigate the melanogenesis inhibitory activity of epicatechin-3-O-gallate (ECG) isolated from Polygonum amphibium L. ECG was isolated from the ethanol extract of P. amphibium L, and its chemical structure was determined using spectroscopic methods such as LC-ESI-MS, 1D-NMR, and UV spectroscopy. ECG inhibited the melanogenesis of B16F10 cells in a dose-dependent manner. Particularly, it decreased the melanin content by 27.4% at 200 µM concentration, compared with the control, in B16F10 cells, without causing cytotoxicity. It is noteworthy that the expression of three key proteins, including tyrosinase, tyrosinase-related protein-1 (TRP-1), TRP-2, and microphthalmia-associated transcription factor (MITF), involved in melanogenesis, is significantly inhibited by ECG. The ECG isolated in this study caused the inhibition of body pigmentation and tyrosinase activity in vivo in the zebrafish model. These results suggest that the ECG isolated from P. amphibium L. is an effective anti-melanogenesis agent.

• Animal cells and systems
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• v.10 no.4
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• pp.233-236
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• 2006

For the purpose of the development of skin-whitening or therapeutic agents against hyperpigmentation, aqueous extract from Nardostachys chinensis (AENC) was evaluated for melanogenesis inhibitory activity in B16F10 melanoma cell. The treatment with AENC at the 0.2, 0.5 and 1.0 mg/ml level significantly inhibits the biosynthesis of melanin compared with untreated control. The tyrosinase activity also significantly decreased in AENC-treated cells at the 0.2 and 0.5 mg/ml level and inhibitory effects were more efficient than commercial arbutin at 0.1 mg/ml. The Western analyses confirmed the significantly decreased expression of tyrosinase and tyrosinase-related protein-2 by AENC treatment. These results indicate that AENC may contribute to the inhibition of melanin biosynthesis through regulating the expression as well as activity of tyrosinase and AENC may be useful as a new candidate in the design of new skinwhitening or therapeutic agents.