• Title/Summary/Keyword: melanogenesis inhibition

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Effect of ginseng and ginsenosides on melanogenesis and their mechanism of action

  • Kim, Kwangmi
    • Journal of Ginseng Research
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    • v.39 no.1
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    • pp.1-6
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    • 2015
  • Abnormal changes in skin color induce significant cosmetic problems and affect quality of life. There are two groups of abnormal change in skin color; hyperpigmentation and hypopigmentation. Hyperpigmentation, darkening skin color by excessive pigmentation, is a major concern for Asian people with yellowe-brown skin. A variety of hypopigmenting agents have been used, but treating the hyperpigmented condition is still challenging and the results are often discouraging. Panax ginseng has been used traditionally in eastern Asia to treat various diseases, due to its immunomodulatory, neuroprotective, antioxidative, and antitumor activities. Recently, several reports have shown that extract, powder, or some constituents of ginseng could inhibit melanogenesis in vivo or in vitro. The underlying mechanisms of antimelanogenic properties in ginseng or its components include the direct inhibition of key enzymes of melanogenesis, inhibition of transcription factors or signaling pathways involved in melanogenesis, decreasing production of inducers of melanogenesis, and enhancing production of antimelanogenic factor. Although there still remain some controversial issues surrounding the antimelanogenic activity of ginseng, especially in its effect on production of proinflammatory cytokines and nitric oxide, these recent findings suggest that ginseng and its constituents might be potential candidates for novel skin whitening agents.

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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Fermented Unpolished Black Rice (Oryza sativa L.) Inhibits Melanogenesis via ERK, p38, and AKT Phosphorylation in B16F10 Melanoma Cells

  • Sangkaew, Orrarat;Yompakdee, Chulee
    • Journal of Microbiology and Biotechnology
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    • v.30 no.8
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    • pp.1184-1194
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    • 2020
  • Melanin is a major factor that darkens skin color as one of the defense systems to prevent the harmful effects of UV light. However, darkened skin from the localized or systemic accumulation of melanin is viewed in many cultures as an esthetic problem. Consequentially, searching for anti-melanogenic agents from natural sources is very popular worldwide. Previous screening of fermented rice products, obtained from various rice cultivars fermented with different sources of loog-pang (Thai traditional fermentation starter), revealed that the highest ability to reduce the melanin content in B16F10 melanoma cells was from unpolished black rice fermented with a defined starter mixture of microbes isolated from loog-pang E11. The aim of this study was to investigate the mechanism of the fermented unpolished black rice (FUBR) on the inhibition of melanogenesis in B16F10 melanoma cells. The strongest reduction of cellular melanin content was found in the FUBR sap (FUBRS). The melanin reduction activity was consistent with the significant decrease in the intracellular tyrosinase activity. The FUBRS showed no cytotoxic effect to B16F10 melanoma or Hs68 human fibroblast cell lines. It also significantly reduced the transcript and protein expression levels of tyrosinase, tyrosinase-related protein 1 (TYRP-1), TYRP-2, and microphthalmia-associated transcription factor. Furthermore, it induced a significantly increased level of phosphorylated ERK, p38 and Akt signaling pathways, which likely contributed to the negative regulation of melanogenesis. From these results, a model for the mechanism of FUBRS on melanogenesis inhibition was proposed. Moreover, these results strongly suggested that FUBRS possesses anti-melanogenesis activity with high potential for cosmeceutical application as a skin depigmenting agent.

Inhibition of Melanogenesis by Dioctyl Phthalate Isolated from Nigella glandulifera Freyn

  • Nguyen, Duc T. M.;Nguyen, Dung H.;Hwa-La, Lyun;Lee, Hyang-Bok;Shin, Jeong-Hyun;Kim, Eun-Ki
    • Journal of Microbiology and Biotechnology
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    • v.17 no.10
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    • pp.1585-1590
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    • 2007
  • Although a number of melanogenesis inhibitors have recently been reported and used as cosmetic additives, none is completely satisfactory, leaving a need for novel skin-depigmenting agents. Thus, to develop a novel skin depigmenting agent from natural sources, the inhibition of melanogenesis by Chinese plants was evaluated. A methanolic extract of Nigella glandulifera Freyn was found to inhibit the melanin synthesis of murine B16F10 melanoma cells by 43.7% and exhibited a low cytotoxicity (8.1%) at a concentration of $100\;{\mu}g/ml$. Thus, to identify the melanogenesis-inhibiting mechanism, the inhibitory activity towards tyrosinase, the key enzyme of melanogenesis, was further evaluated, and the results showed inhibitory effects on the activity of intracellular tyrosinase yet not on mushroom tyrosinase. Finally, to isolate the compounds with a hypopigmenting capability, activity-guided isolation was performed, and Dioctyl phthalate identified as inhibiting melanogenesis.

The effects of Caffeoylserotonin on inhibition of melanogenesis through the downregulation of MITF via the reduction of intracellular cAMP and acceleration of ERK activation in B16 murine melanoma cells

  • Kim, Hye-Eun;Ishihara, Atsushi;Lee, Seong-Gene
    • BMB Reports
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    • v.45 no.12
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    • pp.724-729
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    • 2012
  • In this study, we evaluated the anti-melanogenesis effects of Caffeoylserotonin (CaS) in B16 melanoma cells. Treatment with CaS reduced the melanin content and tyrosinase (TYR) activity in B16 melanoma cells in a dose-dependent manner. CaS inhibited the expression of melanogenesis-related proteins, including microphthalmia-associated transcription factor (MITF), TYR, and tyrosinase-related protein-1 (TRP-1), but not TRP-2. ${\alpha}$-MSH is known to interact with melanocortin 1 receptor (MC1R) thus activating adenylyl cyclase and increasing intracellular cyclic AMP (cAMP) levels. Furthermore, cAMP activates extracellular signal-regulated kinase 2 (ERK2) via phosphorylation, which phosphorylates MITF, thereby targeting the transcription factor to proteasomes for degradation. The CaS reduced intracellular cAMP levels to unstimulated levels and activated ERK phosphorylation within 30 min. The ERK inhibitor PD98059 abrogated the suppressive effect of CaS on ${\alpha}$-MSH-induced melanogenesis. Based on this study, the inhibitory effects of CaS on melanogenesis are derived from the downregulation of MITF signaling via the inhibition of intracellular cAMP levels, as well as acceleration of ERK activation.

Inhibitory Effect of Gardenia Fruit Extracts on Tyrosinase Activity and Melanogenesis (치자 열매 추출물의 Tyrosinase 효소활성 저해 및 Melanogenesis 억제 효과)

  • Kwak Jung-Hoon;Kim Yong-Hae;Chang Hae-Ryong;Park Chul-Woo;Han Yeong-Hwan
    • KSBB Journal
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    • v.19 no.6 s.89
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    • pp.437-440
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    • 2004
  • To determine the inhibition of tyrosinase activity and melanogenesis, gardenia fruit was extracted initially with $95\%$ ethanol (w/v), The ethanol extract was fractionated subsequently with hexane, chloroform and ethyl acetate in that order. The inhibitory effect of the ethanol extract on tyrosinase activity was higher than water extract. When 10 mg/mL of ethyl acetate fraction was applied, the inhibition ratio of tyrosinase activity was much higher ($99.7{\pm}0.1\%$) than that of arbutin. The inhibition of melanogenesis using B16F10 melanoma cell, the ethanol extract also showed higher inhibitory effect than water extract. The highest inhibitory activity of melanogenesis was also shown in ethyl acetate fraction ($89.1{\pm}1.4\%$ at the cone. of $100\;{\mu}g/mL$). These results suggests that gardenia extracts might be used to be a potential agents for whitening.

DEVELOPMENT OF NEW WHITENING AGENT. THE INHIBITORY EFFECTS OF LAGENARIA LEUCANTHA ON MELANOGENESIS AND DEPIGMENTATION EFFECT OF GOLD FISH

  • Suh, J.E.;Lee, C.W.;Cho, Y.H.;Park, S.M.
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.24 no.3
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    • pp.65-72
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    • 1998
  • In this study, we demonstrated the whitening effect of Lagenaria leucantha through the melanin biosynthesis of S bikiniensis and inhibition of melanogenesis in cultured Bl6 melanocytes. And we confirmed the whitening effect of Lagenaria leucantha through the depigmentation of gold fish in vivo. The melanogenesis of B$_{16}$ melanocytes was founded to be activated dose and time dependently by the treatment of u- MSH. When the B$_{16}$ melanocytes was treated with 200nM of $\alpha$-MSH, the morphology of melanocytes was remarkably changed. The melanin content and the synthesis of tyrosinase were strikingly increased. Lagenaria ieucantha inhibited the melanin formation stimulated by $\alpha$-MSH without affection of cell viability. However, Lagenaria leucantha didn't inhibit tyrosinase activity and showed weak suppression on the synthesis of tyrosinase. These results suggest Lagenaria leucantha might inhibit melanin formation with tyrosinase independent manner. Lagenaria ieucantha also inhibition melanin biosynthesis with 18mm inhibition zone in S.bikiniensis. To evaluate the inhibitory activity of melanogenesis of Lagenaria leucantha in vivo, we examined its effect on depigmentation of gold fish. Lagenaria ieucantha remarkably reduced the size and density of melanophores in gold fish. These results suggest that Lagenaria ieucantha can be used as a whitening agent in cosmetics.ics.s.

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Inhibitory Effects of The Flower from Abeliophyllum distichum cv. Okhwang 1 on Melanogenesis in B16 F10 Cells

  • Mi-Ji Noh;Hye-Jeong Park;So-Yeon Han;Jeong-Yong Park;Seo-Hyun Yun;Soo-Yeon Kim;Tae-Won Jang;Jae-Ho Park
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2021.04a
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    • pp.53-53
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    • 2021
  • Abeliophyllum distichum Nakai (A. distichum), endemic species of Korea, is classified according to the petals and calyx colors. Recently, A. distichum cv. Okhwang 1, which has the golden flower, designated the first official cultivar improved from A. distichum species. The study on the chloroplast genome of A. distichum cv. Okhwang 1 have been reported, but no studies on bioactivity such as antioxidant, anti-inflammatory, and anti-cancer have been progressed. This study was conducted to evaluate the inhibition on melanogenesis of the flower from A. distichum cv. Okhwang 1 (FAO). Antioxidant activity was measured using DPPH and ABTS radical scavenging assays. Inhibition effects on melanogenesis of FAO were confirmed by expression of tyrosinase-related proteins and mRNAs using immunoblotting and RT-qPCR. Tyrosinase is an enzyme that regulates both stimulation and inhibition of melanogenesis. Stimulated MITF in cellular levels increases the expressions of tyrosinase, TRP-1, and TRP-2 to induce melanogenesis. As a result, FAO inhibited the expression of MITF, followed by down-regulated tyrosinase, TRP-1, and TRP-2, which lead to inhibit melanin overproduction. In conclusion, these results indicated that FAO reduced reactive oxygen species (ROS) and markedly inhibited the expression of melanin-related factors. The present study suggested providing that FAO has the potential for development as a functional cosmetic material derived from natural.

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Effect of Ailanthi Radicis Cortex Extracts on Melanogenesis

  • Cho, Young-Ho
    • Biomedical Science Letters
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    • v.13 no.4
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    • pp.313-317
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    • 2007
  • Melanogenesis refers to the biosynthesis of melanin pigment in melanocytes. Melanogenesis is controlled by the intra- and extracellular environments. In the present study, to develop a new whitening agent, it was investigated the antioxidant activity and the inhibitory effect of Ailanthi Radicis Cortex extract on tyrosinase activity and on melanogenesis in the B16/F1 melanoma cells. The inhibition ratio of tyrosinase activity of ethylacetate fraction from Ailanthi Radicis Cortex was higher than that of arbutin. The ethylacetate fraction showed scavenging activities of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and superoxide anion radicals in a dose dependent manner. The highest inhibitory activity of melanogenesis was also in ethylacetate fraction ($40.0{\pm}5%$ at the concentration of $400{\mu}g/ml$). This study demonstrates that the Ailanthi Radicis Cortex extract might be used to be a potential agent for skin whitening.

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Melanogenesis Inhibitory Effects of Methanolic Extracts of Umbilicaria esculenta and Usnea longissima

  • Kim, Moo-Sung;Cho, Hong-Bum
    • Journal of Microbiology
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    • v.45 no.6
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    • pp.578-582
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    • 2007
  • The primary objective of this study was to assess the in vitro melanogenesis inhibitory effects of methanolic extracts of the edible and medicinal lichens, Umbilicaria (Gyrophora) esculenta and Usnea longissima. The quantities of the total phenolic compounds of methanolic extract of the two lichen extracts were determined to be 1.46% and 2.62%, respectively. In order to evaluate the antioxidative effects of the extracts, we also measured electron donating abilities (EDA) and lipid peroxidation rates. The EDA values measured by the reduction of 1.1'-diphenyl-2-picrylhydrazyl (DPPH) were 72.8% and 80.7% for the extracts, with $SC_{50}$ (median scavenging concentration) values of $1.29{\pm}0.05\;mg/ml$ and $1.03{\pm}0.06\;mg/ml$, respectively. The rates of inhibition of lipid peroxidation using linoleic acid were 92.1% and 97.3% for the extracts, with $IC_{50}$ (median inhibitory concentration) values of $0.57{\pm}0.05\;mg/ml$ and $0.53{\pm}0.06\;mg/ml$, respectively. The inhibitory rates of the extracts against tyrosinase were 67.4% and 84.8%, respectively. The extracts were shown to reduce melanin formation in human melanoma cells. Melanin contents in the samples treated with 0.01% and 0.1% U. esculenta were 47.1% and 31.2%, respectively, and those treated with 0.01% and 0.1% Usnea longissima were 51.1% and 34.9%, respectively, whereas a value of 54.0% was registered when ascorbic acid was utilized as a positive control. In addition to direct tyrosinase inhibition, it was determined that the lichen extracts affected the activity of tyrosinase via the inhibition of tyrosinase glycosylation. As a result, the methanolic extracts of U. esculenta and Usnea longissima evidenced melanogenesis inhibitory effects, which occurred via multiple routes.