• 제목/요약/키워드: inhibition of melanin

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Di-acetyl-nor-aporphines: Novel molecules and a novel mechanism to inhibit melanogenesis

  • Lintner, Karl;Peschard, Olivier;Leroux, Richard;Mondon, Philippe;Lamy, Francois
    • Proceedings of the SCSK Conference
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    • 2003.09a
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    • pp.268-284
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    • 2003
  • Nor-aporphine derivatives have been discovered which interfere with the flux of Calcium into and out of the cell interior. It has been shown that adrenergic antagonists that block the Calcium exchange lead to an inhibition of Protein kinase C activity, thus blocking tyrosinase activation. Di-acetyl-dimethoxy-methyl-nor-aporphine is a semi-synthetic molecule of natural origin with very high potency. On B16 melanocytes as well as in normal human melanocytes the decrease in melanin synthesis reaches -50% at a level of 40 ppm in the culture medium. On a molar concentration basis, this is 50 to 70 times stronger than Kojic acid inhibition. Yet, the cell viability is not affected. Reversibility studies show that after washing out of the active compound, melanogenesis returns to normal levels. Possible mechanisms of the activity are discussed. Tests carried out on SkinEthic(R) three-dimensional models of the epidermis and in vivo clinical studies on Asian population confirm the strong inhibition of melanogenesis. Safety evaluation of these molecules, on the other hand, demonstrates good skin tolerance and absence of toxicity.

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The Development of Whitening Cosmetic Ingredient Having Activity of Melanin Degradation (멜라닌 분해능을 지닌 미백용 기능성 화장품원료의 개발)

  • Kang, Whan-Koo;Hwang, Sun-Duk;Kim, Hyoung-Sik;Jeung, Jong-Sik;Lee, Bheong-Uk
    • KSBB Journal
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    • v.22 no.1
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    • pp.7-15
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    • 2007
  • Extensive research was carried out for inhibition of melanin formation as development of whitening cosmetic ingredients. But degradation of melanin itself was not intensively pursued as development of cosmetics. In this study, novel melanin degradation enzyme was developed and characterized. Also this enzyme production process was optimized and formulation was tried using micro encapsulation technique.

Tyrosinase inhibitory effect of gentisic acid derivatives

  • Lee, Yeon-Jung;Yoon, Sung-Il;Kim, Jung-Sun;Lee, Chi-Ho;Kim, Dae-Duk
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.294.2-295
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    • 2003
  • Gentisic acid, a skin-whitening agent, is known to possess tyrosinase inhibition activity. In order to develop an effective skin-whitening agent, hydroquinone derivatives in which the carboxylic acid moiety of gentisic acid was replaced with various functional groups, were selected and evaluated for their ability to inhibit tyrosinase activity as well as to inhibit melanin release. (omitted)

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Comparison of whitening effect of Rubus coreanus fruit according to maturity (성숙도에 따른 복분자 열매의 미백 활성 비교)

  • Park, Jeong-Yong;Lee, Ji Yeon;Seo, Kyung Hye;Jang, Gwi Young;Lee, Seung Eun;Ji, Yun-Jeong;Kim, Hyung Don
    • Journal of Nutrition and Health
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    • v.53 no.2
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    • pp.121-128
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    • 2020
  • Purpose: The Rubus coreanus fruit (RF) is an important traditional medicinal herb having antioxidant, anti-inflammatory, and immunoregulatory properties. These activities are known to change dramatically, depending on maturity of the RF. It is presumed that change of functional components, such as flavonoids, tannins, phenolic acids, triterpenoids and organic acids in RF, affect the various bioactivities. This study aimed to confirm changes in the anti-melanogenic effects of RF based on maturity, and to identify the bioactive compounds responsible. Methods: The cell viability of mature RF (MRF) and immature RF (IRF) extracts was investigated using B16F10 cells. To compare the anti-melanogenic effect of MRF and IRF extracts, we first assessed the melanin content. High-performance liquid chromatography analysis was performed to evaluate changes in the level of ellagic acid according to maturity of the RF. In addition, tyrosinase inhibitory activity of both extracts was examined. Results: MRF and IRF extracts (50-200 ㎍/mL) do not affect the cell viability of B16F10 melanoma cells. IRF extract more effectively inhibited melanin synthesis than MRF extract. The content of ellagic acid in IRF extract was higher than that obtained in MRF extract. Furthermore, greater inhibition of tyrosinase activity was observed after exposure to IRF extract than MRF extract. A positive correlation was determined between ellagic acid content and tyrosinase inhibitory activity, and a negative correlation was obtained between ellagic acid content and melanin content. Taken together, our results indicate that ellagic acid is one of the major bioactive compounds of RF that imparts a whitening effect. Conclusion: Our results indicate that ellagic acid in MRF and IRF extracts affect the anti-melanogenesis effect through inhibition of tyrosinase activity. Therefore, the ellagic acid rich IRF has greater potential for application as a natural and functional cosmetic material.

Anti-inflammatory and whitening effects of ginseng complex as a cosmetic material (화장품소재로서의 인삼복합물의 항염증 및 미백효능 검증)

  • Jang, Young-Ah
    • Journal of the Korean Applied Science and Technology
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    • v.35 no.2
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    • pp.325-335
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    • 2018
  • This study is for checking the possibility of ginseng complex as cosmetic materials. For this we carried out biological active evaluation about anti-inflammatory and whitening effects by using ethanol extract of ginseng complex. Samples were prepared by extracting 70% ethanol from each of Panax ginseng C. A. Meyer (A), Phellinus linteus (B) and Pinus rigida Mill. (C), and mixing them at a ratio of (A) 1 : (B) 1 : (C) 0.5. In order to evaluate the anti-inflammatory effects of the samples in macrophages (RAW 264.7 cells), MTT assay was used to evaluate the toxicity of the samples and the inhibitory activity of nitric oxide production and the expression levels of inflammation-related proteins and genes. To evaluate the whitening effect of the samples in melanoma (B16F10 cell), MTT assay was used to evaluate the toxicity of the sample, cellular tyrosinase inhibition, and melanin contents. The inhibitory activity of nitric oxide in the LPS-induced RAW 264.7 cells was 71.2% at $25{\mu}g/mL$ concentration and western blot analysis showed that the expression of iNOS and COX-2 protein decreased in a concentration-dependent manner. Inhibition of tyrosinase activity showed 36.8% inhibition at $50{\mu}g/mL$ concentration of ginseng complex and inhibition of melanin contents showed 47.8% inhibition at $50{\mu}g/mL$ concentration. From the results of the experiment, it was confirmed that the ginseng complex had excellent anti-inflammatory and whitening effect and could be used as a safe natural cosmetic material in the future.

Study on Skin Care Properties of Milk Kefir Whey

  • Chen, Ming-Ju;Liu, J.R.;Sheu, J.F.;Lin, C.W.;Chuang, C.L.
    • Asian-Australasian Journal of Animal Sciences
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    • v.19 no.6
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    • pp.905-908
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    • 2006
  • The purpose of this research was to study the effects of kefir whey (kefir whey, peptides, lactic acid) on skin care properties including skin lightening effect and acne treatment. The final aim was to develop a new cosmetic product and enhance the value of dairy products. The results of skin lightening tests showed that all three kefir whey components (kefir whey, peptides and lactic acid) had inhibitory ability against melanin synthesis. Furthermore, copper chelating analysis demonstrated that both kefir whey and kefir whey peptides could chelate the copper in tyrosinase, which might explain the mechanism of inhibition. The ability for acne treatment indicated that lactic acid level higher than 60 mg/ml could inhibit the growth of Propionibacterium acne, whereas no inhibition was found with other components.

Development of Whitenin Agents by Synthesis of Polyhydroxy Aromatic Compounds

  • Hyun-Ho Lee;You
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.23 no.3
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    • pp.86-91
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    • 1997
  • Some natural polyhydroxy aromatic compounds have inhibitory activity against tyrosinase, key enzyme for formation of melanin pigment. We examined the structure-activity relationship of the natural polyhydrowy aromatic compounds and synthesized a number of new derivetives through various methods. Skin lightening effects of these compounds were examined through inhibition of mushroom tyrosinase and inhibitory of melanogenesis on B-16 melanoma cells. These new compounds showed strong inhibitory activity against tyrosinase. Good lightening effects sue to inhibition of melanogenesis were observed from several resorcinol and pyrogallol derivatives. In toxicological tests such as skin primary irritation and sensitization, the above compounds were sufficiently safe for cosmetic use.

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Inhibition of Aqueous Extract from Amomum xanthioides on ${\alpha}$-melnocyte Stimulating Hormone Induced Melanogenesis in B16F10 Cell (사인의 열수 추출물이 B16F10 흑색종세포의 멜라닌형성에 미치는 영향)

  • Lee, Soo-Jin;Ye, Jeong-Sook;Choi, Yung-Hyun;Lee, Yong-Tae;Chung, Kyung-Tae;Jeong, Seong-Yun;Choi, Byung-Tae
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.21 no.1
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    • pp.50-53
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    • 2007
  • To develope skin-whitening or therapeutic agents against hyperpigmentation, aqueous extract from Amomum xanthioides (AEAX) was evaluated for melanogenesis inhibitory activity in B16F10 melanoma cell. The treatment with AEAX at the 0.5 and 1.0 mg/ml level significantly inhibits the biosynthesis of melanin compared with untreated control. The AEAX-treated cells at the 1.0 mg/ml level were more efficient than commercial arbutin at 0.1 mg/ml. The tyrosinase activity also significantly decreased in AEAX-treated cells at the 0.5 and 1.0 mg/ml level. The Western analyses confirmed the significantly decreased expression of tyrosinase and tyrosinase-related protein-1 by AEAX treatment. These results indicate that AEAX may contribute to the inhibition of melanin biosynthesis through regulating tyrosinase activity and expression and serve as a new candidate in the design of new skin-whitening or therapeutic agents.

Antioxidant Activities and Whitening Effect from Lindera obtusiloba BL. Extract (생강나무 추출물의 항산화 활성과 미백효과)

  • Bang, Chae-Young;Won, Eun-Kyung;Park, Kuen-Woo;Lee, Gwang-Won;Choung, Se-Young
    • YAKHAK HOEJI
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    • v.52 no.5
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    • pp.355-360
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    • 2008
  • In this study we investigated antioxidant activity of against several free radicals and skin whitening effect of 70% ethanol extract (leaf extracts and branch/stem mixed) of Lindera obtusiloba BL. Antioxidant activity was assessed by DPPH, superoxide radical and hydroxyl radical assays. The Lindera obtusiloba BL. extract had antioxidant activity dose dependently with an ${IC}_{50}$ value of 243.14 and 181.10 ${\mu}g$/ml for DPPH, 165.77 and >1500 ${\mu}g$/ml for non-enzymatic system of superoxide radical assay, 35.47 and >100 ${\mu}g$/ml for enzymatic system of superoxide radical assay, 1.21 mg/ml for hydroxyl radical assay. In addition we tested tyrosinase inhibition activity and melanin contents on B16 melanoma F10. B16 melanoma cell was treated by such sample as 1, 5, 10 and 50 ${\mu}g$/ml for 72 hr and tyrosinase inhibition was tested. Melanogenesis was inhibited to 22% at the dose of 50 ${\mu}g$/ml and tyrosinase was inhibited to 45.2% at the same dose. In conclusion Lindera obtusiloba BL had potent antioxidant activity and inhibitory activity of tyrosinase and melanin formation. It could be developed as the health functional food and functional cosmetic resources.