• 대한화장품학회지
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• 제40권1호
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• pp.89-94
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• 2014

물푸레나무 수피 추출물은 주요 생활성 물질로서 esculetin과 esculin을 포함하고 있다. 이 가운데, Esculetin은 B16F10 melanoma cells에서 $IC_{50}$ value $2.8{\mu}M$의 아주 좋은 melanogenesis 억제 활성을 나타내며, 이를 통해 Melan-A cell에서 melanin 합성을 감소시킨다. 더욱이, esculetin은 mushroom tyrosinase에서도 $IC_{50}$ value $40{\mu}M$의 억제 활성을 나타내어 melanin biosynthesis를 저해한다. 위의 결과들로서, 우리는 melanogenic enzyme 활성 조절에 의해 melanin 생성을 저해하는 효과적인 피부미백 물질로서 esculetin을 제안하고자 한다.

• Journal of Microbiology and Biotechnology
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• 제30권7호
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• pp.1051-1059
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• 2020

Overproduction and accumulation of melanin in the skin will darken the skin and cause skin disorders. So far, components that can inhibit tyrosinase, a melanin synthase of melanocytes, have been developed and used as ingredients of cosmetics or pharmaceutical products. However, most of existing substances can only inhibit the biosynthesis of melanin while melanin that is already synthesized and deposited is not directly decomposed. Thus, their effects in decreasing melanin concentration in the skin are weak. To overcome the limitation of existing therapeutic agents, we started to develop a substance that could directly biodegrade melanin. We screened traditional fermented food microorganisms for their abilities to direct biodegrade melanin. As a result, we found that a kimchi-derived Pediococcus acidilactici PMC48 had a direct melanin-degrading effect. This PMC48 strain is a new strain, different from P. acidilactici strains reported so far. It not only directly degrades melanin, but also has tyrosinase-inhibiting effect. It has a direct melanin-decomposition effect. It exceeds existing melanin synthesis-inhibiting technology. It is expected to be of high value as a raw material for melanin degradation drugs and cosmetics.

• 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.

• 한국미생물·생명공학회지
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• 제23권2호
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• pp.209-213
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• 1995

During the screening of inhibitors of melanin biosynthesis from microbial secondary metabolites, a fungal strain MR-93 which was capable of producing high level of an inhibitor was selected from plant leaf. Based on taxonomic studies, the fungus could be classified as a strain of Trichoderma sp.. The active compound (MR-93D) was purified from the culture broth by Diaion HP-20 column chromatography, ethylacetate extraction, Sephadex LH-20 column chromatography and HPLC. The inhibitor was identified as 4-hydroxy-8-isocyano-l-oxaspiro[4-4]cyclonon-8-en-2- one by spectroscopic methods of UV, $^{1}$H-NMR, ESIMS and IR. MR-93D showed a strong tyrosinase inhibitory activity with 0.03 $\mu$g/m of IC$_{50}$ value. It also inhibited melanin biosynthesis with 35 mm inhibition zone at 30 $\mu$g/paper disc in Streptomyces bikiniensis, a bacterium used as an indicator organism in this work.

• 한국미생물·생명공학회지
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• 제23권6호
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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.

• 생약학회지
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• 제44권4호
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• pp.391-396
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• 2013

In this study, we investigated the effects of onion(Allium cepa L.) peel extraction aplication on UVB-induced damage of mouse skin. The male C57BL/6 weeks mice were divided into three groups; the control group(Con), the UVB irradiated group(UVB) and the group treated with onion peel extract after UVB irradiation(UVB+Onion peel). Onion peel extraction were topically treated after UVB irradiation(800 $mJ/cm^2$) to dorsal skin. We were measured TEWL, melanin value, erythema index and histological of mouse skin. In the TEWL, melanin value and erythema index observation, UVB+onion peel group were decreased then in the UVB group and 120 and 168 hr groups were similar to the control group. In the histological observation, UVB+onion peel group were indicated hyperkeratosis then in the UVB. These results showed that onion peel extract as a topical application may have preventive effect against UVB-induced skin damage. Therefore onion peel extract might be good material for UVB-damage skin care.

• 대한화장품학회지
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• 제36권3호
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• pp.193-198
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• 2010

사람의 피부색에 결정적인 영향을 미치는 멜라닌은 표피 기저층의 멜라닌형성세포(Melanocyte)에 의해 생성되어 피부 전반에 분포하고 있으며, 표피의 가장 외각인 각질층에서도 멜라닌은 존재하고 있다. 이러한 각질세포 내 멜라닌과 피부색과의 관계를 알아보고자 각질세포 내 멜라닌의 선택적 염색(Fontana-Masson method) 및 영상분석을 통한 정량적 평가법을 확립하였고, 각질세포 내 멜라닌 양과 색차계를 통한 피부색과의 상관관계를 조사하였다. 71명의 여성 피시험자를 대상으로 색차계를 이용한 피부색과 동일부위의 각질세포에 함유된 멜라닌을 정량하여 비교하였을 때, 각질 세포 내 멜라닌이 차지하는 면적을 나타내는 MCA (Melanin covering area)값이 피부색의 $L^*$값, $ITA^{\circ}$ (Individual Typology Angle)값과 비교적 높은 상관관계를 보였다(각각 r = 0.6049, r = 6651). 이러한 결과를 통해 각질세포 내 멜라닌 양이 피부색 분류의 새로운 기준이 될 수 있는 가능성을 확인했으며, MCA값에 따라 새로이 피부색을 분류하는 기준을 제시할 수 있었다. 본 실험을 통해, 각질세포 내 멜라닌 정량법의 개발과 멜라닌 양에 따른 새로운 피부색 분류 기준을 세울 수 있었으며 개발된 각질세포 내 멜라닌 정량법은 향후 새로운 in vivo 미백 평가 및 피부 색상과 관련된 여러 분야에서 매우 유용하게 이용될 수 있을 것이다.

• 한국패션뷰티학회지
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• 제4권4호
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• pp.81-86
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• 2006

Numerous novel ingredients have been introduced for the hight functionality of whitening cosmetics. Tough the preliminary research, we have found water extracts Bombyx mori have high whitening efficacy. The results of the research for the whitening effect of Bombyx Mori L. are as follow 1. Bombyx Mori L. inhibited concentration dependently the generation of melanin increased by the stimulation of $\alpha$-MSH and protoporphyrin IX, and $IC_{50}$ value was 8.3, 9.2 ${\mu}M$ respectively. 2. Melanin increased by the stimulation of $\alpha$-MSH and protoporphyrin IX was five to seven times superior in the inhibiting effect, compared with kojic acid used as positive control group. 3. Bombyx Mori L. did not have a decolorizing effect on melanin already generated. 3. Bombyx Mori L. was observed to have toxicity of over 100 ${\mu}M$ for the mouse melanoma B16 cells. Therefore, These results suggest that water extracts of Bombyx mori have inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cells in vitro.

• Bulletin of the Korean Chemical Society
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• 제34권10호
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• pp.3017-3021
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• 2013

Coumaroyl dipeptide amide, Coumaric acid-LG-$NH_2$, was prepared successfully using the solid-phase method, and its efficacy as a skin whitening agent was studied. Coumaric acid-LG-$NH_2$ was prepared with Rink-amide resin, and 96.354% of purity was obtained. Using MTT assay and LDH release assay, we found that it exhibited very low cytotoxicity. And, we found that Coumaric acid-LG-$NH_2$ inhibited tyrosinase activity dose-dependently and showed superior tyrosinase inhibitory activity to well-known whitening agent, arbutin. $IC_{50}$ value of Coumaric acid-LG-$NH_2$ was 182.4 ${\mu}M$, and $IC_{50}$ value of arbutin was 384.6 ${\mu}M$. Also, in measurement of melanin contents using B16F1 melanoma cell lines, Coumaric acid-LG-$NH_2$ reduced melanin production induced by ${\alpha}$-MSH statistically significant, and showed superior melanin inhibitory activity to p-coumaric acid or arbutin. In addition, Coumaric acid-LG-$NH_2$ reduced MC1R mRNA expression level. Thus, we concluded that MC1R pathway is the significant pathway of Coumaric acid-LG-$NH_2$, and Coumaric acid-LG-$NH_2$ has great potential to be used as novel whitening agents.

• Biomolecules & Therapeutics
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• 제26권3호
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• pp.282-289
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• 2018

Melanin is a pigment produced from tyrosine in melanocytes. Although melanin has a protective role against UVB radiation-induced damage, it is also associated with the development of melanoma and darker skin tone. Tyrosinase is a key enzyme in melanin synthesis, which regulates the rate-limiting step during conversion of tyrosine into DOPA and dopaquinone. To develop effective RNA interference therapeutics, we designed a melanin siRNA pool by applying multiple prediction programs to reduce human tyrosinase levels. First, 272 siRNAs passed the target accessibility evaluation using the RNAxs program. Then we selected 34 siRNA sequences with ${\Delta}G{\geq}-34.6kcal/mol$, i-Score value ${\geq}65$, and siRNA scales score ${\leq}30$. siRNAs were designed as 19-bp RNA duplexes with an asymmetric 3' overhang at the 3' end of the antisense strand. We tested if these siRNAs effectively reduced tyrosinase gene expression using qRT-PCR and found that 17 siRNA sequences were more effective than commercially available siRNA. Three siRNAs further tested showed an effective visual color change in MNT-1 human cells without cytotoxic effects, indicating these sequences are anti-melanogenic. Our study revealed that human tyrosinase siRNAs could be efficiently designed using multiple prediction algorithms.