• Journal of Applied Biological Chemistry
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• 제65권4호
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• pp.299-306
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• 2022

In this study, derivatives of trimethoxybenzene were investigated as inhibitors of melanogenesis. We examined the effects of methyl 3,4,5-trimethoxybenzoate (MTB), ethyl 3,4,5-trimethoxybenzoate (ETB), methyl 3,4,5-trimethoxycinnamate (MTC), and ethyl 3,4,5-trimethoxycinnamate (ETC). First, the inhibitory effects of these agents on melanin production were evaluated using α-melanocyte-stimulating hormone (α-MSH)-stimulated B16F10 melanoma cells. We found that all derivatives decreased α-MSH-induced melanin production in B16F10 melanoma cells; ETC showed a strong inhibitory effect at half of the concentration of the other derivatives. As tyrosinase is considered a key enzyme of melanogenesis, we also examined whether the derivatives inhibited tyrosinase activity. MTC and ETC reduced mushroom tyrosinase activity and expression levels of α-MSH-induced B16F10 cellular tyrosinase protein. Inhibitory effects of all derivatives on α-MSH-induced B16F10 cellular tyrosinase activity were shown in a dose-dependent manner. Additionally, the derivatives were exposed to diphenylpicrylhydrazyl free radical to examine their antioxidant characteristics. All derivatives showed considerable antioxidant activity, which was 2-fold higher than that of arbutin. In conclusion, the trimethoxybenzene derivatives, including MTB, ETB, MTC, and ETC exerted anti-melanogenic and antioxidant effects on α-MSH-stimulated melanogenesis, demonstrating their potential for use as novel hypopigmenting agents and antioxidants.

• Natural Product Sciences
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• 제20권1호
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• pp.33-38
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• 2014

In recent times, the demand for edible medication for the treatment of hyperpigmentation has increased significantly. Therefore, the discovery of a stable, safe and inexpansive antimelanogenic component from natural substances, such as grains, is of particular interest. The levels and activities of some metabolites and/or enzymes can be increased. In the present study, we investigated the antimelanogenic effects of water-soluble extracts from barley (BE), malt (ME) and germinated barley (GBE) in melan-a cells. The inhibitory effects of ME and GBE on melanin production were significantly greater than that of BE. Interestingly, the content of ferulic acid, the proposed active component of barley, was also higher in ME and GBE than in BE by HPLC analysis. Western blot analysis of the expression of melanogenic enzymes in melan-a cells treated with BE, ME or GBE indicated the expression of both tyrosinase and tyrosinase-related protein 2 (TRP-2) significantly decreased after treatment with BE, ME or GBE. These results suggest that besides BE, ME and GBE also inhibit melanin production most likely through suppression of tyrosinase and TRP-2 expression. ME and GBE were more efficacious at inhibiting melanin production than BE was and may also represent potential skin-whitening agents.

• 생명과학회지
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• 제23권11호
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• pp.1336-1341
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• 2013

아시아에서 한방약초로 널리 알려진 당귀 추출물의 미백활성을 알아보기 위하여 tyrosinase 저해활성을 측정한 결과 1,000 ${\mu}g/ml$의 농도에서 70% 이상의 활성을 나타내었다. 또한 당귀 추출물에 대한 멜라노마 세포(B16F10)의 세포생존율을 확인한 결과 500 ${\mu}g/ml$의 농도에서 99% 이상의 세포생존율을 확인할 수 있었다. 미백 관련 인자인 MITF, TRP-1, TRP-2 및 tyrosinase의 mRNA 발현량을 측정한 결과 50 ${\mu}g/ml$의 농도에서 각각 85.7%, 123.9%, 68.8%, 208%로 당귀 추출물을 처리하지 않은 군보다 감소하였음을 확인할 수 있었다. 이러한 연구 결과에 따라 당귀 추출물이 melanin 합성과 관련이 있는 유전자 발현의 억제효과가 있음을 확인할 수 있었으며, 미백 화장품 소재로서의 가능성을 확인하였다.

• 한국식품영양학회지
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• 제28권2호
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• pp.247-252
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• 2015

본 연구에서는 Allium 속 식물인 달래, 대파, 양파의 물 추출물에 존재하는 항산화 활성과 tyrosinase 및 elastase 저해 효과를 확인하여 화장품 자원으로 이용 가능성을 확인하고자 하였다. DPPH 라디칼 소거능의 실험에 사용한 식물 물 추출물의 $IC_{50}$은 양파($IC_{50}=19.81mg/mL$) < 달래($IC_{50}=21.50mg/mL$) < 대파($IC_{50}=137.87mg/mL$) 순으로 높았다. 그리고 ABTS 라디칼 소거능의 경우에도 양파($IC_{50}=7.67mg/mL$) < 달래($IC_{50}=8.17mg/mL$) < 대파($IC_{50}=11.88mg/mL$) 순으로 DPPH 라디칼 소거능의 결과와 일치하였다. 그리고 달래 물 추출물의 총 폴리페놀 함량을 측정한 결과, 달래 물 추출물(43.03 mg/g)이 가장 높았으며, 그 다음으로 양파(38.27 mg/g), 대파(30.01 mg/g) 순이었다. Tyrosinase의 저해 효과를 측정한 결과, 대파 물 추출물($IC_{50}=36.95mg/mL$) < 양파($IC_{50}=37.31mg/mL$) < 달래($IC_{50}=51.97mg/mL$) 순으로 대파 물 추출물이 가장 높은 저해 활성을 나타냈다. 다음, elastase의 저해 효과를 측정한 결과, 달래 물 추출물($IC_{50}=298.37$ < 대파 $IC_{50}=323.75mg/mL$) < 양파($IC_{50}=367.21mg/mL$) 순으로 달래 물 추출물이 가장 높은 저해 활성을 나타냈다. 마지막으로 가열처리에 의하여 DPPH 라디칼 소거능과 tyrosinase 저해 활성이 일반 실험군보다 더 우수하게 나타났는데, elastase 저해 활성 실험에서는 반대로 가열 처리한 실험군이 일반 실험군보다 현저한 차이로 낮게 나타났다.

• 한국약용작물학회지
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• 제19권3호
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• pp.177-184
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• 2011

This study was performed to assess the antioxidant activities and whitening effects of Agrimonia pilosa Ledeb on melanin synthesis. The whitening effects of Agrimonia pilosa Ledeb water extracts were examined by in vitro mushroom tyrosinase assay and B16BL6 melanoma cells. We assessed inhibitory effect of Agrimonia pilosa Ledeb water extract on expression of melanogenic enzyme proteins including tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2) in B16BL6 cells. Inhibitory effect of Agrimonia pilosa Ledeb onto free radical generation was determined by measuring DPPH and hydroxyl radical scavenging activitie. Our results indicated that Agrimonia pilosa Ledeb water extract effectively inhibited free radical generation. In DPPH and hydroxy radical scavenging activity, Agrimonia pilosa Ledeb water extract had a potent anti-oxidant activity in a dose-dependent manner. They significantly inhibited tyrosinase activity in vitro and in B16BL6 melanoma cells. Also, Agrimonia pilosa Ledeb suppressed the expression of tyrosinase in B16BL6 melanoma cells. These results show that Agrimonia pilosa Ledeb inhibited melanin production on the melanogenesis. The underlying mechanism of Agrimonia pilosa Ledeb on whitening activity may be due to the inhibition of tyrosinase activity. We suggest that Agrimonia pilosa Ledeb may be useful as new natural active ingredients for antioxidant and whitening cosmetics.

• 한국미생물·생명공학회지
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• 제44권1호
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• pp.1-8
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• 2016

본 연구에서는 청미래 덩굴 뿌리 추출물의 미백효과를 확인하기 위해서 tyrosinase 저해활성 및 미백관련 인자인 MITF, TRP-1, TRP-2, tyrosinase의 단백질 및 유전자 발현억제 효과를 western blot, reverse transcription-PCR 및 real time-PCR을 측정하였다. 그 결과 우수한 tyrosinase 저해활성을 확인하였고, 미백관련 인자 MITF, TRP-1, TRP-2, tyrosinase 단백질 및 유전자 발현측정에서도 4가지 인자 모두 발현이 억제됨으로써 미백 효능이 있음을 확인할 수 있었다. 따라서 청미래 덩굴 뿌리 추출물이 미백 효능을 가짐으로써 화장품 소재로 응용이 가능할 것으로 판단된다.

• 한방안이비인후피부과학회지
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• 제30권2호
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• pp.38-50
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• 2017

Objectives : This study was designed to investigate effects of Lonicera Flos Extracts(LFE) on whitening using B16F10 cell lines. Methods : In this experiment, we observed effects of LFE on cell viability, inhibitory effects of melanin synthesis, inhibitory effect on tyrosinase, tyrosinase activity, superoxide dismutase(SOD)-like activity and mRNA expression. Results : In results, more than $2000{\mu}g/ml$ of LFE treated group showed lowered cell viability rates significantly compared to albutin treated group. More than $2000{\mu}g/ml$ of LFE treated groups were lower levels of melanin synthesis. Inhibitory effects of melanin production showed in $1000{\mu}g/ml$ of LFE treated group. $1,000{\mu}g/ml$ of LFE treated group significantly suppressed tyrosinase activities in vitro. LFE and albutin treated group significantly decreased tyrosinase activity compared to non treated group. SOD-like activity of LFE treated group was lower than vitamin C treated group but increased depending on concentration. $500{\mu}g/ml$ of LFE treated group and $1,000{\mu}g/ml$ of LFE treated group was significantly increased. Tyrosinase mRNA expression of ${\alpha}$-MSH and LFE $250{\mu}g/ml$ treated group significantly decreased compared to ${\alpha}$-MSH treated group. Conclusions : These results suggest that LFE can inhibit melanin synthesis through inhibitory action on tyrosinase activity. And LFE suppressed tyrosinase activities B16F10 cells significantly. So I suggest LFE can apply to whitening.

• Biomolecules & Therapeutics
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• 제23권3호
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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.

• 생명과학회지
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• 제29권7호
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• pp.755-761
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• 2019

코직산(Kojic acid)은 생리활성물질로서 많이 알려져 있으며 antibacterial, antifungal과 같은 효능을 나타낸다. 또한 티로시나아제(tyrosinase) 억제제로서 작용하여 멜라닌 생성을 저해시키기 때문에 화장품 산업에 있어서도 미백효과를 가지는 중요한 소재로서 각광받고 있다. 본 연구에서는 독립적으로 항산화 효과를 나타내는 유도체와 코직산(Kojic acid)을 연결하여 새로운 기능성을 가지는 신규 화합물을 발굴하고자 하였으며, 클릭 반응(Click reaction)을 통해 트리아졸(triazle)로 연결하여 신규 코직산 컨쥬게이트(conjugated) 화합물을 합성하였다. 먼저 신규 코직산 컨쥬게이트(conjugated) 화합물의 티로시나아제(tyrosinase) 억제 효과에 대해서 연구한 결과 대부분의 화합물이 코직산(Kojic acid)보다 우수한 티로시나아제(tyrosinase) 억제 효과를 나타냈다. 이와 같은 결과로 미루어 보아 신규 코직산 컨쥬게이트(conjugated) 화합물은 항산화용 건강보조식품 조성물 및 항산화 소재, 노화방지 및 미백 기능을 가진 피부외용제 조성물의 유효성분으로 개발될 가능성이 매우 높다고 사료된다.

• 한국식품과학회지
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• 제51권1호
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• pp.52-57
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• 2019

본 연구는 그라비올라 잎 조다당 분획물(ALP)의 멜라닌 저해활성에 관하여 알아보기 위하여 B16F10 melanoma 세포의 세포 생존율, tyrosinase 저해활성, 멜라닌 함량, 멜라닌 생합성에 관여하는 단백질(TRP-1, TRP-2, tyrosinase, MITF 및 p-CREB)의 발현을 관찰하였다. ALP의 tyrosinase 활성 저해능을 측정하였을 때, 농도 의존적으로 감소하는 것을 알 수 있었다. 또한 B16F10 세포에 ALP를 처리하여 멜라닌 활성 저해능에 관하여 알아봤을 때, tyrosinase, 멜라닌 함량이 농도 의존적으로 줄어드는 것을 확인하였다. 또한 ALP가 미백과 관련된 TRP-1, TRP-2, tyrosinase, MITF 및 p-CREB의 단백질 발현양이 농도의존적으로 감소되는 것으로 관찰되었다. 따라서 ALP는 멜라닌 저해 활성을 효과적으로 나타낸 것으로 보아 기능성 미백 화장품 소재로서의 활용 가능성을 확인할 수 있었다.