• 대한화장품학회지
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• 제29권1호
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• pp.151-167
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• 2003

Melanin biosynthesis is a human defense mechanism to protect skin from UV irradiation and also determines colors of hair and skin. However, as a interest on skin-whitening increases, researches to prevent pigmentation and hypersynthesis of melanin in skin are being actively in progress. Active components used as a whitening agent in cosmeceuticals are kojic acid, arbutin, vitamin C and hydroquinone. However, until now, because comparison researches among them in the aspect of both melanin formation and cellular toxicity have not been performed, we can't exactly estimate merits and defects of them as a whitening agent. To this end, we performed experiments to compare their effects on cell viability and melanin formation. As a first step, in vitro tyrosinase inhibition assay was done. While kojic acid and hydroquinone showed strong inhibition activities(their IC$\_$50/s are all < 100uM), arbutin and vitamin C showed weak activities. IC$\_$50/s of arbutin and vitamin C are 100uM and 400∼500uM, respectively. In B16BL6 melanoma cells, like in vitro tyrosinase inhibition assay, arbutin and kojic acid showed more strong inhibition effect on melanin synthesis than vitamin C. And unlike arbutin, vitamin C and kojic acid induced cell death at high concentration. Although arbutin showed no cytotoxicity, it has side effect to induce morphological change at high concentration.. In this paper, we suggest both kojic acid and arbutin have stronger ability to inhibit melanogenesis than vitamin C. And they also have side effect, that is, kojic acid induces cell death like vitamin C and arbutin changes cell morphology respectively.

• Journal of Applied Biological Chemistry
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• 제58권3호
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• pp.266-271
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• 2015

최근에는 hyper-pigmentation에 대한 제품 개발을 위해 melanogenesis의 경로에 대한 이해를 위해 많은 노력을 하고 있다. 이에 따라 본 연구에서는 만형자(Vitex rotundifolia)의 depigmentation에 대한 효과를 조사하였다. B16F10 mouse melanoma cell을 이용하여 tyrosinase, MITF, TRP-1, TRP-2 그리고 melanin synthesis의 저해를 확인하였고, 만형자 ethyl acetate 분획물(VR-EA)을 처리하였을 때 농도의존적으로 감소한다는 것을 알 수 있었다. 특히, VR-EA는 tyrosinase와 TRP-1의 경우 각각 53.2, 88.4%의 저해율을 보여 미백에 있어서 효과적인 활성을 보여주었다. 따라서 만형자는 melanin synthesis를 효과적으로 막아주어 미백소재로서 활용 가능성이 충분하다고 사료된다.

• Journal of Ginseng Research
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• 제45권5호
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• pp.555-564
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• 2021

Background: Ginsenosides of Panax ginseng are used to enhance skin health and beauty. The present study aimed to investigate the potential use of ginsenoside Rf (Rf) from Panax ginseng as a new anti-pigmentation agent. Methods: The anti-melanogenic effects of Rf were explored. The transcriptional activity of the cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) and the expression levels of tyrosinase, microphthalmia-associated transcription factor (MITF), and tyrosinase-related proteins (Tyrps) were evaluated in melanocytes and UV-irradiated ex vivo human skin. Results: Rf significantly inhibited Forskolin (FSK) or UV-stimulated melanogenesis. Consistently, cellular tyrosinase activity and levels of MITF, tyrosinase, and Tyrps were downregulated. Furthermore, Rf suppressed MITF promoter activity, which was stimulated by FSK or CREB-regulated transcription coactivator 3 (CRTC3) overexpression. Increased CREB phosphorylation and protein kinase A (PKA) activity induced by FSK were also mitigated in the presence of Rf. Conclusion: Rf can be used as a reliable anti-pigmentation agent, which has a scientifically confirmed and reproducible action mechanism, via inhibition of CREB/MITF pathway.

• Natural Product Sciences
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• 제29권2호
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• pp.59-66
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• 2023

The anti-melanogenic activity of 259 actinomycete strains was tested, and based on the results for the inhibition of mushroom tyrosinase activity and the reduction in melanin content, Micromonospora sp. JCS1 and JCS7 were selected as the strains with the highest anti-melanogenic potential. The activity-guided fractionation of extracts from JCS1 and JCS7 led to the isolation of the dipeptides cyclo(ʟ-Phenyl alanine (Phe)-ʟ-Proline (Pro)) (1) and cyclo(ʟ-Tryptophan (Trp)-ʟ-Proline (Pro)) (2). These two compounds were tested for their inhibition of mushroom tyrosinase by monitoring ʟ-DOPA levels and melanin production. Cyclo(ʟ-Phe-ʟ-Pro) (1) and cyclo(ʟ-Trp-ʟ-Pro) (2) were thus confirmed to have the potential for use in functional whitening cosmetics containing actinomycete-derived secondary metabolites.

• Journal of Photoscience
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• 제5권4호
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• pp.163-167
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• 1998

Candida albcans growth inhibition experiments were carried out to determine the photoxicity of new monofunctional psoralen derivatives, PzPs and HMPzPs, as well as well known 8-MOP an d5-MOP. Although 8-MOP and 5-MOP showed distince photoxicity, PzPs and HMPzPs did not inhibit the growth of Candida albicans strain indicating that PzPs derivatives were not good candidate for the treatment of psoriasis. However, vitili해 could be treated by PzPs derivatives without severe phototosicity because psoralens are known to treat vitiligo by stimulating melanogenesis on skin.

• 대한화장품학회지
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• 제37권4호
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• pp.319-326
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• 2011

니겔라 사티바(Nigella sativa Linn.) 오일의 미백 효능을 확인하기 위하여 니겔라 사티바 오일 및 오일에서 분리된 유효성분들을 버섯 타이로시네이즈 효소, B16 멜라노마 세포를 이용하여 멜라닌 생성에 관련된 다양한 실험을 실시하였다. B16-F10 멜라노마 세포를 이용한 멜라닌 저해 활성시험 결과에서 니겔라 사티바 오일은 10 mg/mL의 농도에서 약 86 %의 멜라닌 생성을 억제하였으며, RT-PCR과 Western blot을 통한 멜라닌 생성 기작에 대한 영향을 조사한결과, 멜라닌 합성의 주요 단백질인 타이로시네이즈 발현 저해효과가 우수하게 나타났다. 또한, tyrosinase related protein-1 (TRP-1) 및 tyrosinase related protein-2 (TRP-2)의 발현이 억제되는 것을 확인하였다. 따라서, 니겔라 사티바오일은 멜라닌 생합성 저해 효과뿐만 아니라, 멜라닌 합성에 필수적인 효소(타이로시네이즈, TRP-1, TRP-2)의 발현저해를 통해 미백 효과를 나타내는 것으로 확인되었으며, 이에 따라 니겔라 사티바 오일은 멜라닌 생합성을 저해하는미백 소재로 활용할 수 있을 것으로 사료된다.

• 생약학회지
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• 제34권2호통권133호
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• pp.156-160
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• 2003

$NF-{\kappa}B$ (nuclear factor-kappa B) plays a particularly central role in epidermal biology. It has been established that ultraviolet radiation (UVR) is one of the mechanisms to induce the activation of $NF-{\kappa}B$ in human skin. We previously demonstrated that melanogenic inhibitors may act through the inhibition of $NF-{\kappa}B$ activation in keratinocytes. In order to find another type of melanogenic inhibitors of $NF-{\kappa}B$ activation, various kinds of the extracts from crude drugs $(30\;{\mu}g/ml)$ were preincubated with transfectant HaCaT cells for 3 hrs and then UVR $(60\;mj/cm^2)$ was irradiated. UVR-exposed cells were incubated for another 6 hrs to measure the $NF-{\kappa}B$ activity. $NF-{\kappa}B$ activation was measured with the secreatory alkaline phosphates (SEAP) reporter gene assay using a fluorescence detection method. Among natural products, Lycium chinense, Acanthopanax senticosus, Angelica koreana, Kalopanax pictus and Asparagus cochinchinensis were the most potent inhibitors of $NF-{\kappa}B$ activation by UVR. These observations suggest that some crude drugs might act partially through the modulation of the synthesis of melanotrophic factors to decrease melanogenesis in keratinocytes.

• Biomolecules & Therapeutics
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• 제24권1호
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• pp.85-93
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• 2016

We already reported that genetically engineered resveratrol-enriched rice (RR) showed to down-regulate skin melanogenesis. To be developed to increase the bioactivity of RR using calli from plants, RR was adopted for mass production using plant tissue culture technologies. In addition, high-pressure homogenization (HPH) was used to increase the biocompatibility and penetration of the calli from RR into the skin. We aimed to develop anti-melanogenic agents incorporating calli of RR (cRR) and nanoparticles by high-pressure homogenization, examining the synergistic effects on the inhibition of UVB-induced hyperpigmentation. Depigmentation was observed following topical application of micro-cRR, nano-calli of normal rice (cNR), and nano-cRR to ultraviolet B (UVB)-stimulated hyperpigmented guinea pig dorsal skin. Colorimetric analysis, tyrosinase immunostaining, and Fontana-Masson staining for UVB-promoted melanin were performed. Nano-cRR inhibited changes in the melanin color index caused by UVB-promoted hyperpigmentation, and demonstrated stronger anti-melanogenic potential than micro-cRR. In epidermal skin, nano-cRR repressed UVB-promoted melanin granules, thereby suppressing hyperpigmentation. The UVB-enhanced, highly expressed tyrosinase in the basal layer of the epidermis was inhibited by nano-cRR more prominently than by micro-cRR and nano-cNR. The anti-melanogenic potency of nano-cRR also depended on pH and particle size. Nano-cRR shows promising potential to regulate skin pigmentation following UVB exposure.

• 대한화장품학회지
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• 제36권3호
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• pp.207-213
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• 2010

본 연구는 미생물에 의한 골담초(Caragana sinica Rehder) 발효 추출물의 항산화 효과 및 피부 미백 효능에 관한 연구로 골담초에 S. cerevisiae KCTC 7913를 첨가하여 발효를 통해 얻어진 발효 추출물을 B16F10 멜라닌 세포에 처리한 결과, 농도의존적으로 멜라닌 생성 억제 효능이 증가한 것으로 확인하였으며, 추출물 내 유효 성분인 resveratrol의 함량이 발효 전의 추출물에 비해 증가함을 확인하였다. 멜라닌 생성 과정의 주요 단백질인 tyrosinase의 활성 억제 또한 골담초 추출물에 비해 골담초 발효 추출물의 효능이 우수함을 확인하였으며, 골담초 발효 추출물의 피부 자극 또한 일어나지 않는 것으로 확인되어 피부에 안전한 화장품 원료로서의 사용이 가능할 것으로 사료된다.

• 한국축산식품학회지
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• 제35권5호
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• pp.707-713
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• 2015

Royal jelly has been widely used as a health supplement worldwide. However, royal jelly has been implicated in allergic reactions, and we developed a water-soluble royal jelly (WSRJ) without the allergy inducing protein. In this study, we aimed to identify the anti-melanogenic efficacy of WSRJ. B16F1 melanoma cells were first treated with 10 nM α-melanocyte stimulating hormone (α-MSH) and then with various doses of WSRJ. In addition, we investigated the mRNA and protein expression of melanogenesis-related genes such as tyrosinase, tyrosinase related protein-1 (TRP-1) and TRP-2 by reverse transcription-polymerase chain reaction and western blotting. WSRJ directly inhibited tyrosinase and cellular tyrosinase activity, which decreased melanin synthesis in α-MSH stimulated B16F1 melanoma cells a level comparable to that observed with arbutin. WSRJ decreased the mRNA and protein expressions of tyrosinase, TRP-1, and TRP-2, which was comparable to that observed with arbutin. WSRJ has strong anti-melanogenic activity, which invoice direct inhibition of tyrosinase enzyme activity and suppression of expression of melanogenesis related genes. Results from this study suggests that WSRJ is a potential candidate for the treatment of skin pigmentation.