• 한국약용작물학회:학술대회논문집
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• 2011.04a
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• pp.262-263
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• 2011

• Biomolecules & Therapeutics
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• v.21 no.5
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• pp.343-348
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• 2013

We investigated the inhibitory effects of hesperidin on melanogenesis. To find melanosome transport inhibitor from natural products, we collected the structural information of natural products from Korea Food and Drug Administration (KFDA) and performed pharmacophore-based in silico screening for Rab27A and melanophilin (MLPH). Hesperidin did not inhibit melanin production in B16F10 murine melanoma cells stimulated with ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH), and also did not affect the catalytic activity of tyrosinase. But, hesperidin inhibited melanosome transport in melanocyte and showed skin lightening effect in pigmented reconstructed epidermis model. Therefore, we suggest that hesperidin is a useful inhibitor of melanosome transport and it might be applied to whitening agent.

• Journal of Microbiology and Biotechnology
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• v.12 no.2
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• pp.286-291
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• 2002

Histone deacetylase I (HDAC1) works as one of the components in a nucleosome remodeling (NuRD) complex that consists of several proteins, including metastasis-associated protein 1 (MTA1). Since the protein-protein interaction of HDAC1 and MTA1 would appear to be important for both the integrity and functionality of the HDAC1 complex, the interruption of the HDAC1 and MTA1 interaction may be an efficient way to regulate the biological function of the HDAC1 complex. Based on this idea, a yeast two-hybrid system was constructed with HDAC1 and MTA1 expressing vectors in the DNA binding and activation domains, respectively. To verify the efficiency of the assay system, 3,500 microbial metabolite libraries were tested using the paper disc method, and KB0699 was found to inhibit the HDAC1 and MTA1 interaction without any toxicity to the wild-type yeast. Furthermore, KB0699 blocked the interaction of HDAC1 and MTA1 in an in vitro GST pull down assay and induced morphological changes in B16/BL6 melanoma cells, indicating the interruption of the HDAC1 complex function. Accordingly, these results demonstrated that the yeast assay strain developed in this study could be a valuable tool for the isolation of a HDAC1 complex disruptor.

• Microbiology and Biotechnology Letters
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• v.23 no.6
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• pp.641-646
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• 1995

During the screening of inhibitors of melanin biosynthesis from microbial secondary metabolites, a fungal strain MR304 which was capable of producing high level of an inhibitor was selected. Based on taxonomic studies, this fungus could be classified as Trichoderma harzianum. The active compound (MR304-1) was purified from culture broth by Diaion HP-20 column chromatography, ethylacetate extraction, Sephadex LH-20 column chromatographv and HPLC. The inhibitor was identified as 3-(1,5-dihvdroxy-3-isocyanocyclopent-(E)-3-envl)prop-2-enoate by spectroscopic methods of UV, ESIMS, $^{1}$H-NMR, $^{13}$C-NMR, NOE, HMQC and HMBC. MR304-1 showed strong mushroom tyrosinase inhibitory activity with IC$_{50}$ value of 0.25 $\mu $g/ml. It inhibited melanin biosynthesis with 15 mm inhibition zone at 30 $\mu $g/paper disc in Streptomyces bikiniensis, a bacterium used as an indicator organism in this work. It also inhibited melanin biosynthesis in B16 melanoma cells with a niinimum inhibitory concentration of 0.05 $\mu $g/ml.

• 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.

• YAKHAK HOEJI
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• v.44 no.6
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• pp.607-612
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• 2000

Generally, antitumor drugs have strong toxicity and result in damage in normal cells. Previously, lectin has been reported as a tumor cell specific binding protein and tannin as an antitumor substance. In this study, we investigated antitumor activity of lectin-conjugated ellagitannin and used praecoxin A as an ellagitannin source. We injected mouse melanoma cell, B16-F10, on right the femoral region of C57BL/6 mouse. After 10 hours later, first treatment with praecoxin A, lectin-praecoxin A mixiture and lectin-conjugated praecoxin A was carried and followed by injection i.m. every 48 hours. Praecoxin A extended the life of mice up to 14.8% in comparison with the negative control group at 5 mg/kg dose. The life extending ratio of Lectin-praecoxin A mixture was 26.1% at 5 mg/kg dose, and the life extending ratio of lectin-conjugated praecoxin A was 28.7% at 5 mg/kg dose. On the basis of these findings, we suggest that antitumor activities of lectin-praecoxin A mixiture and lectin-conjugated praecoxin A on survival are better than that of praecoxin A.

• Journal of Physiology & Pathology in Korean Medicine
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• v.17 no.5
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• pp.1288-1292
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• 2003

This study was carried out to evaluate cytotoxic effects of Houttuynia cordata T/sub HUNB/ extracts on A549 (lung cancer), MDA-MB231 (breast cancer), SNU-C4 (colon cancer) and B16 (mouse melanoma) cell lines. We have determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay. The 150 ㎍/㎖ concentration of methanol extract (63.81 %) of Houttuynia cordata T/sub HUNB/ was shown significantly antitoxic activity on A549 cell lines. The order of cytotoxicity fractions of methanol from Houttuynia cordata T/sub HUNB/ extracts against cancer cell lines in vitro is as follows : hexane fraction layer > chloroform fraction layer > ethyl acetate fraction layer > buthanol fraction layer > water fraction layer. These results suggest that the hexane fraction of methanol extract from Houttuynia cordata T/sub HUNB/ extract may be a valuable choice for the development of antitumor agents.

• Korean Journal of Pharmacognosy
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• v.36 no.4 s.143
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• pp.273-277
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• 2005

In mammalian melanocytes, melanin synthesis is controlled by tyrosinase, the key enzyme in the pigment synthesis. In this study, to develop a new whitening agent, we have investigated the antioxidant and the inhibitory effect of Artemisia anomala extract on tyrosinase activity and melanigenesis in the B16/F1 melanoma cells. The inhibition ratio of tyrosinase activity of butanol fraction from A. anomala was higher than that of arbutin ($97.5{\pm}0.5%$ at the concentration of 2 mg/ml). The butanol fraction was shown 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 butanol fraction ($25.0{\pm}3%$ at the concentration of $200\;{\mu}g/ml$). From these results, we suggest that the A. anomala extract might be used to be a potential agent for skin whitening.

• 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.

• Journal of the Korean Chemical Society
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• v.67 no.2
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• pp.137-144
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• 2023

In this study were evaluated the whitening and anti-oxidative activities from the extracts of Sorbus alnifolia branches, and identified the chemical structures of the active ingredients. In the whitening tests using α-MSH stimulated B16F10 melanoma cells, the 70% ethanol extract and n-butanol (n-BuOH) fractions concentration-dependently inhibited cellular melanogenesis and intracellular tyrosinase activities without causing cell toxicity. The total polyphenol content of n-BuOH and ethyl acetate (EtOAc) fractions were measured to be respectively 241.1 ± 1.1 and 222.9 ± 2.4 (mg/g GAE), and the total flavonoid content of EtOAc fraction was 75.3 ± 2.0 (mg/g QE). Upon anti-oxidant studies with DPPH and ABTS⁺ radicals, potent radical scavenging activities were observed in the EtOAc and n-BuOH fractions. Moreover, in the study of cell protection efficacy using HaCaT keratinocytes damaged by H₂O₂, the EtOAc and n-BuOH fractions showed a very positive results on prevention of oxidative stress. Phytochemical studies for this extract resulted in the isolation of four compounds; 2-oxopomolic acid (1), euscaphic acid (2), epi-catechin (3), prunasin (4). These results suggested that the extract of S. alnifolia branches containing compounds 1-4 as natural ingredients could be used as whitening and anti-oxidant ingredients in cosmetic formulations.