• 한국자원식물학회지
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• 제14권1호
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• pp.32-37
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• 2001

한약재 174종으로부터 tyrosinase 저해제를 탐색하였다. 한약재는 30일간 methanol에 담가 놓은 후, 그 추출액을 제조하여 사용하였다 Tyrosinase의 활성을 측정하기 위해서는 효소 mushroom Tyrosinase와 기질 L-DOPA, phosphate buffer를 사용하였다. 탐색 결과, 한약재 174종 중 14개종이 tyrosinase를 저해 효과를 보였고, 그중 오배자 추출액이 inhibition activity가 가장 높게 나타났다.

• 약학회지
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• 제52권3호
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• pp.165-171
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• 2008

To develop effective skin whitening agents, we tested natural herbal extracts for their melanogenic inhibitory activities. Sedum samentosum was selected for its inhibitory effect on melanogenesis in B16 melanoma cells. Ethanolic extract of S. samentosum (SSE) was evaluated for antioxidative effect and tyrosinase inhibitory activity of melanogenesis. We investigated the changes in protein level and mRNA level of tyrosinase, tyrosinase related protein (TRP)-1 and TRP-2 by using western blotting and RT-PCR, respectively. SSE showed scavenging activities of free radicals and reactive oxygen species (ROS) with the $IC_{50}$ of 342.7 $\mug/ml$ against 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and 64.69 $\mug/ml$ against superoxide radicals in the xanthine/xanthine oxidase system, respectively. SSE treatment suppressed the biosynthesis of melanin up to 46% and reduced tyrosinase activity up to 51% at 100 $\mug/ml$ in B16 melanoma cells. The tyrosinase activity and tyrosinase expression in B16 melanoma cells were reduced in a dose-dependent manner by SSE. Also, SSE was able to significantly inhibit tyrosinase and TRP-1 expression in mRNA level. These results suggest that SSE inhibited melanin production which may be dependent on tyrosinase activity and expression in B16 melanoma cells, and an effective whitening agent for the skin.

• 대한화장품학회지
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• 제28권1호
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• pp.135-149
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• 2002

To date, research on the regulation of melanogenesis has focused on factors which affect tyrosinase, the rate-limiting enzyme in the melanogenic pathway, by searching for chemicals which competitively inhibit tyrosinase function. Many types of tyrosinase inhibitors have been developed, but no satisfactory results have been made clinically until now, To find a new whitening agent, which effectively inhibits melanogenesis, we synthesized several compounds and selected compounds by cell-based assay system. Finally, 3, 4, 5-trimethoxy cinnamaie thymol ester(TCTE, Melasolv) was selected and the effects of TCTE on melanogenesis were investigated. Treatment of mouse-derived melanocyte melan-a cells with TCTE results in a marked down-regulation of tyrosinase activity. 80% decrease of tyrosinase activity occurs with 30uM TCTE treatment for 72 hours without affecting cell growth. The inhibition of tyrosinase activity is dose-dependent and melanin content was also decreased to 40%. From the in vitro tyrosinase assay using cell extract, TCTE does not act as a direct inhibitor of the enzyme. Treatment of melan-a cultures with TCTE blocks the increase in tyrosinase activity by either forskolin, 3-isobutyl-1-methtyl-xanthine. TCTE decreased the expression of tyrosinase, TRP-1 without effects on TRP-2 protein expression through the down regulation of tyrosinase and TRP-1 mRNA. From the results of cAMP immunoassays, intracellular levels of the cyclin nucleotide are unaffected in cells treated with TCTE. The inhibitory effects of melanin synthesis were also shown in reconstitute human epidermis model by topical application. These findings suggest that TCTE can be used for studying the regulation of melanogenesis and depigmenting agent.

• 대한본초학회지
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• 제26권1호
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• pp.29-33
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• 2011

Objectives : This study was designed to investigate the collagen metabolism and tyrosinase activity of Angelicae Gigantis Radix extracts (AGR). Methods : The effect of AGR on type I procollagen production and collagenase activity in human normal fibroblasts HS68 after UVB (312 nm) irradiation was measured by ELISA method. The tyrosinase activity after treatment of AGR was measured. Results : Type I procollagen production was recovered by AGR in UVB damaged HS68 cells. The increased collagenase activity after UVB damage was significantly recovered by AGR and the tyrosinase activity was significantly reduced. However, the L-DOPA oxidation was not changed. Conclusion : AGR showed the anti-wrinkle effects and whitening effects in vitro. These results suggest that AGR may have potential as an anti-aging ingredient in cosmetic herbs.

• 대한약침학회지
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• 제14권1호
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• pp.51-59
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• 2011

Objectives : This study was designed to investigate the collagen metabolism and tyrosinase activity of Sipgeondaebo-tang Pharmacopuncture extracts (SP). Methods : The effect of SP on type I procollagen production and collagenase activity in human normal fibroblasts HS68 after UVB (312 nm) irradiation was measured by ELISA method. The tyrosinase activity after treatment of SP was measured as well. Results : Type I procollagen production was recovered by SP in UVB damaged HS68 cells. The increased collagenase activity after UVB damage was significantly recovered by SP. The tyrosinase activity was significantly reduced as well. However, the L-DOPA oxidation was not changed. Conclusion : SP showed the anti-wrinkle effects and whitening effects in vitro. These results suggest that SP may be a potential pharmacopuncture as an anti-aging pharmacopuncture treatments.

• Archives of Pharmacal Research
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• 제22권3호
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• pp.232-236
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• 1999

In this study, we present evidence that cotreatment of aloesin and arbutin inhibits tyrosinase activity in a synergistic manner by acting through a different action mechanism. Aloesin or arbutin similarly inhibited enzyme activity of human- and mushroom-tyrosinases with an IC50 value of 0.1 or 0.04 mM, respectively. Lineweaver-Burk plots of the enzyme kinetics data showed that aloesin inhibited tyrosinase activity noncompetitively with a Ki value of 5.3 mM, whereas arbutin did it competitively (Maeda, 1996). We then examined whether cotreatment of these agents inhibits the tyrosinase activity in a synergistic manner. The results showed that 0.01 mM aloesin in the presence of 0.03 mM arbutin inhibited activity of mushroom by 80% of the control value and the reverse was also true. The inhibitory effects were calculated to be synergistic according to the B rgi method. Taken together, we suggest that aloesin along with arbutin inhibits in synergy melanin production by combined mechanisms of noncompetitive and competitive inhibitions of tyrosinase activity.

• 약학회지
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• 제50권6호
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• pp.421-428
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• 2006

Water extracts, ethanol extracts, and juice of Cusuta japonica, C, australis, and C. chinensis were prepared, and their cytotoxicity, antioxidant activity and inhibitory effects on tyrosinase activitiy and melanin biosynthesis were estimated by using melanoma Clone M-3. From this study; the following conclusions were attained. Extracts of Cuscuta japonica, C. australis, and C. chinensis showed noticeable cytotoxicity except ethanol extracts from the stem of C. australis. A maximual cytotoxicity was observed with tile ethanol extract from the seed of C, australis (87.39%). While the ethanol extract from the seed of C. japonica (91.88%) showed the most pronounced inhibitory effect on melanin biosynthesis, the water extract from the stem of C. japonica (1.05%) possessed very little inhibitory effect. The most inhibitory effect on tyrosinase activity was observed with the water extract from the stem of C. australis (76.67%). Howeverr the water extract from the stem of C. japonica showed a very poor effect on the inhibition of tyrosinase activity All the preparations, except extracts from the seed of C. australis were able to remove reactive oxygen species (ROS) in a dose-dependent manner. The juice of C. japonica demonstrated the strongest activity (59.02%).

• 한국식품과학회지
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• 제47권6호
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• pp.785-788
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• 2015

식품 저장 중 효소적 갈변을 일으키는 타이로시네이스의 활성을 저해시킬 수 있는 LED의 파장을 구명하기 위하여 파란색, 초록색, 빨간색 LED와 형광등을 이용하여 타이로시네이스에 7일동안 조사하였다. 또한 강도에 따른 타이로시네이스의 활성을 조사하기 위하여 파란색, 초록색, 빨간색 LED를 선택하여 빛의 강도를 3단계로 구분하여 사용하였다. 파장에 따른 타이로시네이스의 활성 저해율은 형광등에서 가장 컸으며 그 다음으로 파란색 LED에서 높은 저해율을 보였다. 빨간색 LED에서는 대조구와 유사한 저해율을 보였으며 초록색 LED에서 저해율이 가장 낮았다. 상대적 빛의 강도에 따른 타이로시네이스 활성은 초록색과 빨간색 LED 조사 시 효소활성의 변화가 크지 않았고, 반면 파란색 LED에서 강도가 증가할수록 큰 저해효과를 보였다. 이러한 결과를 토대로 볼 때 여러 가지 파장의 LED 중 고강도의 파란색 LED에서 타이로시네이스에 의한 식품의 갈변을 최소화 할 수 있을 것으로 판단되며 이는 갈변 억제를 유도함으로써 과일 및 채소의 저장 중 품질을 향상시킬 수 있을 것이다.

• Journal of Applied Biological Chemistry
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• 제50권3호
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• pp.115-119
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• 2007

To discover the sources with antioxidant and tyrosinase inhibitory activities in Korean traditional medicines, 10 extract of medicinal plants were screened for their potential to scavenge stable 1,1-diphenyl-2-picryhydrazyl (DPPH) free radical, inhibit hydroxyl radical (${\cdot}OH$), total phenolic content, and inhibition of tyrosinase. The potency of DPPH radical scavenging activity was shown in the extract of Ulmus davidiana var. japonica Nakai that has a greater effect with $IC_{50}$ values of $6.49{\pm}5.43{\mu}g/mL$, than BHA ($IC_{50}=20.99{\pm}0.74{\mu}g/mL$), L-ascorbic acid $(IC_{50}=20.59{\pm}1.06{\mu}g/mL),\;and\;{\alpha}-tocopherol\;(IC_{50}=25.55{\pm}0.26{\mu}g/mL)$ as a positive control. The ${\cdot}OH$ scavenging activities were observed in the plants tested. Acanthopanax senticosus, Cirsium setiders, U. davidiana exhibited scavenging activity of more than 60% at $500{\mu}g/mL$. The scavenging activity(%) of BHA and a-tocopherol were 64.32 and 55.87% at $500{\mu}g/mL$, respectively. The total phenolic content was determined, in order to assess its effect on the extract's antioxidant activity. The total phenoic content of $33.37{\pm}0.52mg/g$ was conformed by methanolic extract of U. davidiana. The U. davidiana and Morus bombycis exhibited tyrosinase inhibitory activity with a $34.28{\pm}1.32\;and\;75.57{\pm}1.10%$, respectively. In particular, M. bombycis has stronger tyrosinase inhibitory activity than albutin with $36.48{\pm}3.56%$ as a positive control. This work showed that the inhibitory abilities of Korean medicinal plants, such as U. davidiana and M. bombycis, on DPPH free radical, inhibit hydroxyl radical (${\cdot}OH$), and inhibition of tyrosinase and total phenolic content, can be useful in the prevention and treatment of free radical-relate disease. Investigations into further isolation of inhibitory principles of U. davidiana and M. bombycis are now in progress.

• 생명과학회지
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• 제31권11호
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• pp.1019-1027
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• 2021

천연물에서 피부 미백 효능을 가진 화합물을 개발하기 위한 노력이 많이 이루어지고 있다. 꽃송이 버섯(Sparassis crispa)은 β-glucan의 함량이 건조중량의 40% 이상으로서 항암과 면역증강 효과가 있는 것으로 입증되어 약용으로도 인정받고 있다. 이 연구에서는 S. crispa β-glucan의 멜라닌 생합성 및 tyrosinase 활성억제 효능을 확인함으로써 피부 미백제로서의 활용 가능성을 평가하고자 하였다. 외부 자극제인 α-melanocyte stimulating hormone (α-MSH)와 S. crispa β-glucan (10, 100, 1,000 ㎍/ml)을 B16F1 melanoma 세포에 투여하여 멜라닌 생성량과 tyrosinase 활성도를 측정하였다. Tyrosinase, tyrosinase related protein-1 (TRP-1), TRP-2, microphthalmia-associated transcription factor (MITF)의 발현정도에 대해서는 western blot으로 분석하였다. S. crispa β-glucan을 10, 100, 1,000 ㎍/ml의 농도로 투여하였을 때 α-MSH 만 투여군에 비하여 멜라닌 생성이 각각 13.9%, 18.7%, 39.5% 감소하였다. S. crispa β-glucan을 10, 100, 1,000 ㎍/ml의 농도로 투여하였을 때 β-glucan을 투여하지않은 α-MSH 유도군에 비하여 tyrosinase 활성도는 각각 15.6%, 26.9%, 43.2% 억제되었다. 또한 tyrosinase와 TRP-1, TRP-2, MITF 단백 발현도 효과적으로 감소시켰다. 본 연구 결과에 따르면 S. crispa β-glucan은 MITF 발현을 억제함으로써 tyrosinase 발현을 감소시켜 멜라닌 생성을 억제시킨 것으로 판단된다. 따라서 S. crispa β-glucan은 미백제로서 유용하게 활용할 수 있을 것으로 생각한다.