• 약학회지
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• 제43권1호
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• pp.28-32
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• 1999

Four derivatives of kojic acid were synthesized and their inhibitory activities against tyrosinase were evaluated. The C-2 hydroxymethyl and C-7 hydroxyl of kojic acid were replaced by carboxylate and amine, respectively. These derivatives were coupled to L-phenylalanine, producing two amide compounds. The carboxylate derivative (3), its amide compound (5), and the amine derivative (7) were weak inhibitors. The amide compound (9) where amine derivative (7) coupled to L-phenylalanine showed strong inhibitory activity ($IC_{50}=24.6{\;}{\mu}M$) comparable to kojic acid.

• 생약학회지
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• 제45권2호
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• pp.141-146
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• 2014

In this study, we investigated on antioxidative activities and tyrosinase inhibitory activities of methanol extract and its fractions from roots of Arctium lappa. The total phenolic compound and flavonoid content of the ethylacetate fraction was found to be 818.29 mg/g and 360.59 mg/g as the highest content. In the measurement of DPPH radical scavenging ability and tyrosinase inhibitory activity, the ethylacetate fraction was higher than the other fractions and the extract. In addition, comparative analysis of phenolic compounds by liquid chromatography-mass spectrometry (MS)/MS system under the multiple-reaction monitoring (MRM) with negative-ion electrospray ionization mode. The main phenolic compounds in the extract and fractions of roots from Arctium lappa were cynarin and chlorogenic acid. The main phenolic compound of the ethylacetate fraction was cynarin. n-Butanol fraction had a significantly higher chlorogenic acid content than other samples. In conclusion, DPPH radical scavenging ability and tyrosinase inhibitory activity of the cynarin-riched ethylacetate fraction showed the highest activity.

• Fisheries and Aquatic Sciences
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• 제21권11호
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• pp.35.1-35.7
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• 2018

Background: The aim of this study was to investigate the in vitro inhibitory effects of Fucofuroeckol-A isolated from Eisenia bicyclis against tyrosinase activity and 3-isobutyl-1-methylxanthine (IBMX)-induced melanin biosynthesis in B16F10 melanoma cells. Result: Among the ethanolic (EtOH) extract of E. bicyclis and its organic solvent fractions, the ethyl acetate (EtOAc) soluble fraction showed a noticeable inhibitory effect on mushroom tyrosinase with an $IC_{50}$ value of $37.6{\pm}0.1{\mu}g/mL$. Repeated column chromatography of the active EtOAc fraction resulted in the isolation of Fucofuroeckol-A. It evidenced more potent tyrosinase inhibitory effect with an $IC_{50}$ value of $11.4{\pm}1.4{\mu}M$ than arbutin ($IC_{50}=1076.6{\pm}44.3{\mu}M$), which was used as a positive control. Lineweaver-Burk plots suggest that Fucofuroeckol-A plays as a noncompetitive inhibitor against tyrosinase. Furthermore, we have evaluated the inhibitory effects of Fucofuroeckol-A on IBMX-induced melanin formation in B16F10 melanoma cells. Fucofuroeckol-A ($12.5-100{\mu}M$) exhibited a significant inhibition of melanin production in the melanoma cells. Conclusion: In the present study, we suggested that Fucofuroeckol-A might prove possibility as a novel inhibitor of melanin biosynthesis in cosmetic applications.

• Journal of Applied Biological Chemistry
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• 제54권2호
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• pp.108-113
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• 2011

황백 추출물의 tyrosinase 억제효과를 검토한 결과 60% 에탄올추출물에서 25% 정도의 억제효과를 나타내었으며, melanoma세포(B16F10)에서의 멜라닌 생합성을 측정한 결과 31.2%의 저해활성을 나타내어 멜라닌생성억제효과가 있음을 알 수 있었다. 황백추출물에서 tyrosinase저해 활성물질을 정제하고자 Sephadex LH-20과 MCI-gel CHP-20 open column을 이용하여 용출한 결과 순수하게 정제된 활성물질을 얻을 수 있었으며, 정제물질을 구조 동정한 결과 미백물질은 obacunone으로 동정되었다. 정제된 obacunone은 35.1%의 저해활성을 나타내어 미백 활성이 비교적 우수함을 확인할 수 있었으며, 황백추출물로부터 분리한 미백물질을 이용한 미백 화장품을 제조하여 관능평가를 한 결과 우수한 평가를 받았다. 미백화장품의 안정성 검사를 위해 pH, 점도 및 복소탄성률의 변화를 측정하였으나 저장기간 60일 동안 큰 변화를 나타내지 않았다. 또한 온도변화, 인공 및 자연광에 의한 변화, 온도순환에 의한 변화 및 냉 해동순환(Freeze & Thaw cycling)에 따른 변화들 살펴본 결과 저장 60일 동안 모든 조건에서 상의 분리와 변색, 변취 등의 변화 없이 안정성을 나타내었다.

• 한국자원식물학회지
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• 제34권4호
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• pp.368-376
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• 2021

흰민들레 추출물에서 분리한 taraxinic acid, dihydrotaraxinic acid 및 luteolin를 대상으로 화장품의 미백 소재로서의 이용 가능성을 조사하였다. In vitro tyrosinase 저해 활성은 100 ㎍/mL에서 대조군인 ascorbic acid는 42% 저해 활성을 보였으며, luteolin은 48%, taraxinic acid는 29%, 그리고 dihydrotaraxinic acid는 18%를 보여 luteolin이 가장 높게 나타냈다. Taraxinic acid와 dihydrotaraxinic acid는 100 ㎍/mL 이하의 조건에서 B16BL6 멜라닌 형성 세포의 생존율에 영향을 미치지 않았으나, luteolin은 강한 세포 독성을 나타냈다. Taraxinic acid와 dihydrotaraxinic acid가 세포 생존율에 영향을 미치지 않는 농도 범위(10, 50, 100 ㎍/mL)에서 B16BL6 세포 내 멜라닌 생합성 및 tyrosinase 활성을 확인한 결과 농도 의존적으로 억제하는 것으로 확인되었다. 특히 taraxinic acid는 tyrosinase inhibitor로 알려진 arbutin보다 뛰어난 저해 활성을 나타내어, 천연 기능성 미백 화장품 원료로 사용 가능성이 기대된다.

• 한방안이비인후피부과학회지
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• 제28권1호
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• pp.11-22
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• 2015

Objective : Siegesbeckia Herba can treat various skin disease by expelling wind and removing dampness and clearing away heat and toxic material effects. This study was designed to investigate effects of Siegesbeckia Herba Extracts(SHE) on skin elasticity and whitening using B16F10 cell lines. Method : In this experiment, We observed effect of SHE on cell viability, inhibition of melanin synthesis and inhibitory effect on tyrosinase and elastase. Results : 1. SHE treated group showed decreased cell viability rates significantly compared with non-treated group. More than SHE $250{\mu}g/ml$, $500{\mu}g/ml$ and $1,000{\mu}g/ml$ of treated groups were lower levels of melanin synthesis respectively. 2. SHE significantly showed tyrosinase inhibitory activity in vitro, SHE increased tyrosinase inhibitory activity and elastase inhibitory activity in B16F10 cells, and tyrosinase inhibitory activity in vitro. 3. Tyrosinase inhibitory activity and elastase inhibitory activity in B16F10 cells, tyrosinase inhibitory activity in vitro were not accepted statistical significance compared with non-treated group. 4. SHE treated group showed increased SOD-like activity rates significantly compared with non-treated group. More than SHE $250{\mu}g/ml$, $500{\mu}g/ml$ and $1,000{\mu}g/ml$ of treated groups were lower levels of melanin synthesis respectively. Conclusion : These results suggest that SHE can inhibit melanin synthesis and tyrosinase inhibtory activity. So, We suggest that SHE can be maintained skin whitening.

• Advances in Traditional Medicine
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• 제1권2호
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• pp.6-13
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• 2000

Melanin is specifically produced in melanocytes. The pathway for melanin biosynthesis is mainly controlled by tyrosinase. To estimate the inhibitory effect of melanin biosynthesis from 31 medicinal plants extracts, we tested the inhibitory effects of the tyrosinase promoter on B16 mouse melanoma cells. The result of this study demonstrated that Mori Radicis Cortex and Castena Fractus extracts only in tested medicinal plant extracts have high inhibitory effects on tyrosinase promoters with very low cytotoxicity on B16 mouse melanoma cells. Therefore, extracts of Mori Radicis Cortex and Castena Fractus were evaluated as very effective negative regulators of tyrosinase gene expression.

• Natural Product Sciences
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• 제17권3호
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• pp.198-201
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• 2011

Tyrosinase is one of the important enzymes in the mammalian melanin synthesis. In the process of melanin synthesis, tyrosine is oxidized to DOPA (3,4-dihydroxyphenylalanine), and DOPA is further oxidized to dopaquinone. Tyrosinase is an enzyme catalyzing this oxidation of tyrosine, so chemicals that inhibit the activity of tyrosinase can be used as skin whitening agents. In this study, we isolated five constituents from the 80% MeOH extract of Morus bombycis cortex by bioactivity-guided fractionation. We performed mushroom tyrosinase inhibition assay. As a result, 7,2',4'-trihydroxyflavanone (1), 2',4',2,4,-tetrahydroxychalcone (2), and oxyresveratrol (3) showed the more potent inhibitory effect compared to kojic acid, a well-known skin whitening agent with antityrosinase effect. Moracinoside M (4) and moracin M-3'-O-${\beta}$-D-glucopyranoside (5) also showed the moderate tyrosinase inhibitory activities.

• 한방안이비인후피부과학회지
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• 제16권2호
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• pp.96-118
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• 2003

The effect of Glycyrrhizae Radix water extract, known as depigmenting agent, on melanin biosynthesis was investigated in cellular level by using B16 mouse melanoma cells. The inhibitory effect of Glycyrrhizae Radix water extract on melanogenesis was determined by mushroom tyrosinase assay traditionally using in vitro screening test. To determine whether Glycyrrhizae Radix water extract suppress melanin synthesis in cellular level, B16 mouse melanoma cells were cultured in the presence of different concentrations of Glycyrrhizae Radix water extract. Effects on cell proliferation, melanin biosynthesis, tyrosinase activity, DOPAchrome tautomerase activity, and expression level of mRNA for tyrosinase were examined. The maximum concentration of Glycyrrhizae Radix water extract that was not inhibitory to growth of the cells was 2 mgml. At that concentration, melanin synthesis was significantly inhibited without cytotoxicity after 5 days, compared with untreated cells. The treatment with Glycyrrhizae Radix water extract reduced tyrosinase and DOPAchrome tautomerase activity in a dose-dependent manner. However, the treatment with Glycyrrhizae Radix water extract did not affect significantly mRNA levels for tyrosinase. These results suggest that the inhibitory effect of Glycyrrhizae Radix water extract on melanogenesis is correlated with the suppression of tyrosinase and DOPAchrome tautomerase activity more than altering mRNA levels of tyrosinase.

• 대한한방피부미용학회지
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• 제1권1호
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• pp.91-97
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• 2005

(1) Objectives: To discover natural skin-lightening agents, we have evaluated the inhibitory activity of EtOH extracts from 20 medicinal plants against mushroom tyrosinase. (2) Methods: Tyrosinase activity was determined by the dopachrome method using L-tyrosine as the substrates. (3) Results: Of the plant extracts tested, the extracts of 4 plants, Albizzia julibrissin, Curcuma longa, Anethum graveolens and Sophora flavescens, exhibited potent inhibitory activity (> 50%) in mushroom tyrosinase assay. Four plant extract, extracts of Agrimonia pilosa, Paeonia moutan, Magnolia obovata and Eugenia caryophyllata also showed relatively strong inhibitory (> 40%) against mushroom tyrosinase. (4) Conclusion: These active medicinal plants may be useful for the development of skin-whitening agents. Since the active medicinal plants may contain effective tyrosinase inhibitors even more than kojic acid, further study to identify the active constituents from the plants is expected.