• Genomics & Informatics
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• v.21 no.3
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• pp.43.1-43.13
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• 2023

Melanin is synthesized by tyrosinase to protect the skin from ultraviolet light. However, overproduction and accumulation of melanin can result in hyperpigmentation and skin melanoma. Tyrosinase inhibitors are commonly used in the treatment of hyperpigmentation. Natural tyrosinase inhibitors are often favoured over synthetic ones due to the potential side effects of the latter, which can include skin irritation, allergies, and other adverse reactions. Nuciferine, an alkaloid derived from Nelumbo nucifera, exhibits potent antioxidant and anti-proliferative properties. This study focused on the in silico screening of nuciferine for anti-tyrosinase activity, using kojic acid, ascorbic acid, and resorcinol as standards. The tyrosinase protein target was selected through homology modeling. The residues of the substrate binding pocket and active site pockets were identified for the purposes of grid box optimization and docking. Therefore, nuciferine is a potent natural tyrosinase inhibitor and shows promising potential for application in the treatment of hyperpigmentation and skin melanoma.

• The Korean Journal of Food And Nutrition
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• v.22 no.1
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• pp.97-102
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• 2009

In order to obtain a non-toxic and more active and stable microorganism-produced tyrosinase inhibitor, we isolated actinomycetes F-97, a producer of tyrosinase inhibitor, from soil. The aerial hyphae of this strain were gray in color with tree types. Under the microscopic examination, the isolate formed a spiral aerial spore mass with a smooth surface. The analysis of cell wall acid hydrolysate of the isolate revealed the presence of LL-diaminopimelic acid(LL-DAP). No specific sugar was detected. From these results and the cultural and physiological characteristics described in the Bergey's Manual, actinomycetes F-97 was identificated as, or best-matched to, Streptomyces aburaviensis.

• Natural Product Sciences
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• v.10 no.2
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• pp.80-84
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• 2004

Rosmarinic acid and its methyl ester, isolated from the ethyl acetate soluble fraction of the methanolic extract of Salvia miltiorrhiza Bunge (Labiatae), were found to inhibit the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with the $IC_{50}$ values of 16.8 and $21.5\;{\mu}M$, respectively. It was comparable with kojic acid, a well-known tyrosinase inhibitor, with an $IC_{50}$ of $22.4\;{\mu}M$. The inhibitory kinetics analyzed by the Lineweaver-Burk plots, were found rosmarinic acid and its methyl ester to be competitive inhibitors with $K_i\;of\;2.4{\times}10^{-5}\;and\;1.5{\times}10^{-5}\;M$, respectively.

• ALGAE
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• v.30 no.2
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• pp.163-170
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• 2015

Tyrosinase inhibitors are an important component of cosmetic products. Our previous studies have proposed that eckol isolated from the brown alga Ecklonia cava, can be explored as a tyrosinase inhibitor. However, cellular activities and mechanism of action of eckol remain unknown. Therefore, the current study analyzed the eckol binding modes using the crystal structure of Bacillus megaterium tyrosinase. The effects of eckol on melanin synthesis induced by ${\alpha}$-melanocyte stimulating hormone in B16F10 melanoma cells were also investigated. We predicted the 3D structure of tyrosinase and used a docking algorithm to simulate binding between tyrosinase and eckol. These molecular modeling studies were successful (calculated binding energy value, $-115.84kcal\;mol^{-1}$) and indicated that eckol interacts with Asn205, His208, and Arg209. Furthermore, eckol markedly inhibited tyrosinase activity and melanin synthesis in B16F10 melanoma cells. We also found that eckol decreased the expression of tyrosinase, tyrosinase-related protein (TRP) 1, and TRP2. These results indicate that eckol is a potent inhibitor of melanogenesis, and this finding may be useful for the development of novel pharmaceutical and cosmetic agents.

• The Korean Journal of Mycology
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• v.40 no.1
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• pp.60-64
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• 2012

Physiological functionalities of culture concentrates from various fungi were investigated. The culture concentrates from Saccharomyces cerevisiae Y277-3 showed the highest tyrosinase inhibitory activity of 42.7%. Among mold physiological functionalities, the culture concentrates from Aspergillus orygae CN20-3-1-4 showed the highest antioxidant activity of 15.8%. The other functionalities of fungi were very low or not detected. The intracellular tyrosinase inhibitor from Saccharomyces cerevisiae Y277-3, which showed the highest physiological functionalities was maximally produced when the strain was cultured in PD broth at $30^{\circ}C$ for 24 h.

• KSBB Journal
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• v.19 no.2
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• pp.118-124
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• 2004

Melanocytes synthesize melanin within discrete organelle termed melanosomes which are transferred to the surrounding keratinocytes and can be produced in varying sizes, numbers and densities. Skin whitening products have become increasingly popular in the past few years. The most successful natural skin whitening agents are: Arbutin, Vitamin C, Kojic acid, Mulberry, which are all tyrosinase inhibitors. In this work, melanoston, a melanogenesis inhibitor isolated from yeast was studied to understand its mechanism of melanogenesis inhibition. It was found that melanoston was not a tyrosinase inhibitor, while when melanoston was applied to the B16 melanoma cell culture media, the intracellular tyrosinase activity was decreased by more than 30％, When B16 melanoma was stimulated with ${\alpha}$-MSH, cell morphololgy was dramatically changed to have lots of dendrites on the cell membrane surface. On the other hand, B16 was treated with ${\alpha}$-MSH and melanoston, simultaneously, the change of cell morphology was not so great. This inhibition effect of melanoston was found to be related to the inhibition of intracellular activation and transportation of tyrosinase, which was observed by immunostaining of B16 melanoma using anti-tyrosinase antibody. From these results, melanoston was regarded as an inhibitor to the differentiation of melanoma cells.

• Journal of Life Science
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• v.16 no.3 s.76
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• pp.396-399
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• 2006

Crude extract prepared from sweet potato possessed inhibitory activity toward mushroom tyrosinase. The inhibitory activity was dependent upon the addition amount of sweet potato extract. After heating the sweet potato extract at $95^{\circ}C$ for 20 min, its inhibitory activity retained 37.3%. Its optimum activity was shown at pH ranges of 5.0-7.0. The tyrosinase inhibitory activity was disappeared by dialysis, which suggests the inhibitory activity of sweet potato extract is caused by some compounds of low molecular weight.

• Korean Journal of Food Science and Technology
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• v.29 no.1
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• pp.173-177
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• 1997

For the utilizing of tannins in the functional foods and natural inhibitor against browning reaction by tyrosinase in foods, inhibition effect against tyrosinase of tannins from Korean green tea was determined. Acetone extract from Korean green tea showed inhibition effect against tyrosinase. The gallocatechin compounds showed higher inhibition effect than the catechin compounds. In terms of stereo isomers, (-)-epicatechin compounds had higher inhibition effect than the (+)-catechin compounds. The monomer had higher inhibition effect than the dimer.

• Journal of Microbiology and Biotechnology
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• v.16 no.5
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• pp.667-672
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• 2006

Tyrosinase is an enzyme that catalyzes the biosynthetic pathway of melanin pigments participating in the coloring of skin, hair, and eyes, and is widely distributed in nature. The inhibitory compounds of tyrosinase have been extensively used as a cosmetic agent with a skin-whitening effect. In this paper, several plant extracts were screened using Melan-a cells for the melanin biosynthesis inhibition activity, and Idesia polycarpa was selected. A melanin biosynthesis inhibitor was isolated from I. polycarpa fruits by activity-guided fractionation, and the inhibitor was identified as 6-hydroxy-2-[[[(1-hydroxy-6-oxo-2-cyclohexenl-yl)carbonyl]oxy]methyl]phenyl$\beta$-D-glucopyranoside (idescrapin) by comparing it with reported spectral data. Idescarpin $(IC_{50}=8{\mu}g/ml)$ reduced melanin content compared with the vehicle. In addition, the inhibitory activity of idescarpin for melanin synthesis is mediated by decreasing tyrosinase protein rather than directly inhibiting the tyrosinase activity. These results suggest that idescarpin isolated from I. polycarpa fruits may be used as a skin-whitening agent.

• Bulletin of the Korean Chemical Society
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• v.32 no.4
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• pp.1241-1248
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• 2011

Three dimensional quantitative structure-activity relationships (3D-QSARs) between new thiosemicarbazone analogues (1-31) as a substrate molecule and their inhibitory activity against tyrosinase as a receptor were performed and discussed quantitatively using CoMFA (comparative molecular field analysis) and CoMSIA (comparative molecular similarity indices analysis) methods. According to the optimized CoMSIA 2 model obtained from the above procedure, inhibitory activities were mainly dependent upon H-bond acceptor favored field (36.5%) of substrate molecules. The optimized CoMSIA 2 model, with the sensitivity of the perturbation and the prediction, produced by a progressive scrambling analysis was not dependent on chance correlation. From molecular docking studies, it is supposed that the inhibitory activation of the substrate molecules against tyrosinase (PDB code: 1WX2) would not take place via uncompetitive inhibition forming a chelate between copper atoms in the active site of tyrosinase and thiosemicarbazone moieties of the substrate molecules, but via competitive inhibition based on H-bonding.