• 약학회지
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• 제55권6호
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• pp.485-491
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• 2011

Previously, we have reported that apigenin, a natural flavonoid found in a variety of vegetables and fruits, stimulated melanogenesis through the activation of $K^+-Cl^-$-cotransport (KCC) in B16 melanoma cells. In this study we investigated the possible involvement of reactive oxygen species (ROS) in the mechanism of apigenin-induced melanogenesis in B16 cells. Apigenin elevated intracellular ROS level in a dose-dependent manner. Treatment with various inhibitors of NADPH oxidase, diphenylene iodonium (DPI), apocynin (Apo) and neopterine (NP) significantly inhibited both the generation of ROS and melanogenesis induced by apigenin. In addition these inhibitors profoundly inhibited apigenin-induced $Cl^-$-dependent $K^+$ efflux, a hallmark of KCC activity. However, the apigenin-induced ROS generation was not significantly affected by treatment with a specific KCC inhibitor R-(+)-[(2-n-butyl-6,7-dichloro-2-cyclopentyl-2,3-dihydro-1-oxo-1H-inden-5-yl)oxy]acetic acid (DIOA). These results indicate that the ROS production may be a upstream regulator of the apigenin-induced KCC stimulation, and in turn, melanogenesis in the B16 cells. Taken together, these results suggest that the NADPH oxidase-mediated ROS production may play an important role in the apigenin-induced melanogenesis in B16 cells. These results further suggest that NADPH oxidase may be a good target for the management of hyperpigmentation disorders.

• 생약학회지
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• 제36권1호통권140호
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• pp.1-8
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• 2005

To develop an whitening cosmetics, we isolated the melanogenesis inhibitors from the unripe fruits of Poncirus trifoliata (Rutaceae). Isolated compounds were identified as poncirin(l), naringin(2), bis(2-methylheptyl)phthalate(3), avenalumic acid methyl ester(4) by comparison of physical and spectral data with those reported in the literature. Among the isolated compounds, bis(2-methylheptyl)phthalate showed most potent inhibitory effect on the melanogenesis in cultured B-16 mouse melanoma cell lines$(IC_{50},\;36.8\;{\mu}M)$ compared with kojic acid$(IC_{50},\;150\;{\mu}M)$.

• Journal of Microbiology and Biotechnology
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• 제22권6호
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• pp.814-817
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• 2012

In the continued search for melanogenesis inhibitors from microbial metabolites, we found that the culture broth of Clitocybe sp. MKACC 53267 inhibited melanogenesis in B16F10 melanoma cells. The active component was purified by solvent extraction, silica gel chromatography, Sephadex LH-20 column chromatography, and finally by preparative HPLC. Its structure was determined as 5-pentyl-2-furaldehyde on the basis of the UV, NMR, and MS spectroscopic analysis. The 5-pentyl-2-furaldehyde potently inhibited melanogenesis in B16F10 cells with an $IC_{50}$ value of 8.4 ${\mu}g/ml$, without cytotoxicity.

• 한국식품과학회지
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• 제28권6호
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• pp.1089-1094
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• 1996

검은툭눈붕어를 이용하여 tyrosinase 저해제가 어체의 melanogenesis에 미치는 영향을 평가하였다. 저해제로는 glutathione, cysteine, benzoic acid를 각각 5, 5, 1 mM씩울 혼합하여 첨가한 식품첨가물 처리구, 표고버섯을 주기질로 하여 Aspergillus oryzae를 발효시켜 얻은 microbial inhibitor 처리구, 설록차, 무, 팽이버섯, red chicory 등 4종의 식물체 추출액 혼합물 처리구로 나누어 효능을 평가하였다. 검은툭눈붕어를 0.9% NaCl 용액에서 일주일간 양식하면서 stress를 가하여 비늘의 melanin 농도를 높이고 다시 민물에 담고 각 처리구의 저해제를 첨가한 용액에서 6일간 양식한 후 가슴 부위, 측선 부위 및 등지느러미의 색을 색도계로 측정하고 현미경으로 melanin을 관찰하였을 때 식품 첨가물 처리구와 microbial inhibitor 처리구의 색은 대조구보다 명도와 yellowness가 높아진 것으로 나타나 melanogenesis 억제 효과가 뚜렷하였다. 한편, 농산물 처리구의 경우에도 미약하지만 효과가 인정되었다. 저해제를 처리한 검은툭눈붕어와 대조구 붕어의 측선 부위 비늘과 등지느러미를 설취하여 현미경으로 관찰한 결과 저해제 처리구에서는 단위 면적당 melanophore의 수가 감소하고 하나의 melanophore의 크기도 작아진 것으로 나타났다.

• Journal of Microbiology and Biotechnology
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• 제19권4호
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• pp.368-371
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• 2009

In the course of screening for the melanogenesis inhibitors, aspochalasin I was isolated from solid-state culture of Aspergillus sp. Fb020460. Its structure was determined by spectroscopic analysis including mass spectroscopy and NMR analysis. Aspochalasin I potently inhibited melanogenesis in Mel-Ab cells with an $IC_{50}$ value of $22.4{\mu}M$ without cytotoxicity.

• Natural Product Sciences
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• 제17권1호
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• pp.26-32
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• 2011

Novel tyrosinase inhibitors are important for pigmentation in the skin. Following extraction of tyrosinase inhibitors from edible vegetables or fruits, we found that the Prunus persica flesh extract (PPFE) exhibited potential inhibitory activity for melanogenesis. PPFE showed tyrosinase inhibitory activity in an enzymatic assay and PPFE also significantly inhibited the melanin formation in cultured mouse melan-a cells. Moreover, real-time RT-PCR analysis revealed that the inhibition of melanin production by PPFE was closely related to marked suppression of mRNA expression of tyrosinase and tyrosinase-related protein-1 and -2 (TRP-1 and TRP-2) in melan-a cells. Further investigation found that the modulation of tyrosinase expression by PPFE was associated with the transcriptional regulation of the microphthalmia-associated transcription factor (MITF). PPFE inhibited the promoter activity of MITF and suppressed MITF mRNA expression in melan-a cells. These results indicate that PPFE down-regulates melanogenesis-associated gene expression through MITF-mediated transcriptional regulation and these events might be related to the hypopigmentary effects of PPFE.

• Journal of Microbiology and Biotechnology
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• 제17권10호
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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.

• Bulletin of the Korean Chemical Society
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• 제35권2호
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• pp.666-668
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• 2014

• 생약학회지
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• 제36권1호통권140호
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• pp.60-63
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• 2005

One sesquiterpenoid was isolated from the methanol extract of Atractylodes rhizomes which has been used as traditional medicine for diuresis and the compound was established as selina-4(14),7(11)-dien-8-one by the spectroscopic methods. The compound$(IC_{50}<10\;ppm)$ has inhibitory effects on melanogenesis in B16 mouse melanoma.

• 생약학회지
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• 제38권4호
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• pp.382-386
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• 2007

Cinnamomi Cortex (Lauraceae), the dried bark of Cinnamomum cassia BLUME, has been used as traditional Chinese medicine for its stomachic, astringent, carminative, antispasmodic, antibacterial, antifungal properties. Four compounds were isolated from the MeOH extract of Cinnamomi Cortex, and their structures were identified as trans-cinnamic acid (1), ${\beta}-sitosterol$ (2), bis(2-methylheptyl)phthalate (3), coumarin (4) by comparison of their physical and spectral data with those reported in the literature. These compounds were tested melanogenesis inhibitory effect on B-16 mouse melanoma cell lines. Among them, trans-cinnamic acid (1) showed the most potent inhibitory effect on melanogenesis with $IC_{50}$ value of $13{\mu}g/ml$. Arbutin, positive control, exhibited an $IC_{50}$ value of $29{\mu}g/ml$.