• Journal of Ginseng Research
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• 제39권1호
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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.

• Journal of Microbiology and Biotechnology
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• 제30권5호
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• pp.749-752
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• 2020

In the search for novel, natural melanogenesis inhibitors, a new sesquiterpene, inularin, was isolated from the flowers of Inula britannica, and the structure was determined using spectroscopic and chemical methods. The antimelanogenic effects of inularin on B16F10 melanoma cells and zebrafish embryos were evaluated. Inularin dose-dependently reduced melanocyte-stimulating hormone-induced melanin production and L-DOPA oxidation in B16F10 cells. Zebrafish embryos were used to confirm the antimelanogenic activity. Inularin significantly decreased the pigmentation of embryos compared with untreated controls.

• 약학회지
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• 제42권1호
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• pp.39-45
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• 1998

Kojic acid, antimelanogenic agent, has been widely used in cosmetics to lighten the skin color. However, it has skin irritancy and instability against pH, temperature and light. To overcome these problems and optimize the molecular structure of kojic acid (KA), a prodrug, kojic acid monostearate(KMS), has been synthesized to modify the topical drug delivery in the point of sustained release of the parent drug via enzymatic hydrolysis during skin absorption. The prodrug was tested for enzymatic hydrolysis with cytosolic fraction of hairless mouse, skin. From the in vitro skin permeation study through hairless mouse skin, we found that KMS was retained in the skin and generated KA continuously by the skin esterase cleavage. In addition, topical formulations of o/w type creams and polyolprepolymer-containing cream were further tested for whitening effects using in vivo yellow skin guinea pig model.

• Journal of Ginseng Research
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• 제39권3호
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• pp.238-242
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• 2015

Background: Panax ginseng has been used to prolong longevity and is believed to be useful for improving skin complexion. Ginsenosides are the most active components isolated from ginseng, and ginsenoside Rg3 (G-Rg3) in particular has been demonstrated to possess antioxidative, antitumorigenic, and anti-inflammatory properties. The aim of this study was to examine the ability of G-Rg3 to inhibit melanogenesis. Methods: The effects of G-Rg3 on melanin contents and the protein levels of tyrosinase, microphthalmia-associated transcription factor (MITF), and tyrosinase-related protein 1 (TRP1) were evaluated. Melanogenesis-regulating signaling molecules such as Akt and extracellular signal-regulated kinase (ERK) were also examined to explore G-Rg3-induced antimelanogenic mechanisms. Results: G-Rg3 was found to significantly inhibit the synthesis of melanin in normal human epidermal melanocytes and B16F10 cells in a dose-dependent manner. The activity of cellular tyrosinase and the expression of MITF, tyrosinase, and TRP1 were all reduced, whereas ERK was strongly activated. PD98059 (a specific inhibitor of ERK) attenuated the G-Rg3-induced inhibition of melanin synthesis and tyrosinase activity. Conclusion: Taken together, these results showed that G-Rg3 induces the activation of ERK, which accounts for its antimelanogenic effects. G-Rg3 may be a promising safe skin-whitening agent, adding to the long list of uses of P. ginseng for the enhancement of skin beauty.

• 대한화장품학회:학술대회논문집
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• 대한화장품학회 2003년도 IFSCC Conference Proceeding Book II
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• pp.73-86
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• 2003

Endothelins secreted from keratinocytes are intrinsic madiators for human melanocytes in UVB-induced pigmentation. Antimelanogenic ingredient, 1,2-Ο-diferulylglycerol(SM709) isolated from bamboo extract inhibited the melanin synthesis of Bl6F10 melanoma cells by 62%. To understand the cellular mechanism of antimelanogenic activity of SM709 in human melanocytes, the effects of SM709 on the ET-l-induced $Ca^{2+}$ mobilization were investigated. ET-l receptors in human melanocytes were characterized by using specific antagonist and found that ET-l increased intracellular $Ca^{2+}$ by activating ET-B receptor. SM709 completely blocked the ET-l-induced intracellular $Ca^{2+}$ increase and its inhibitory effect showed dose- and time- dependent manners. To investigate the role of SM709 on intracellular $Ca^{2+}$ store, when the $Ca^{2+}$ store was partially depleted by thapsigargin; a specific inhibitor of ER-type $Ca^{2+}$-ATPase, caffeine-induced $Ca^{2+}$ mobilization did not changed in the presence or absence of SM709, suggesting that SM709 has no effect on the $Ca^{2+}$ store. It is known that LPA receptor and P$_2$ receptor are linked to InsP$_3$ second messenger system. When these receptors in melanocytes were activated by LPA and ATP, the intracellular $Ca^{2+}$ signaling was observed even in the presence of SM709. From the above results, it can be suggested that SM709 has an antimelanogenic activity by antagonizing the ET-B receptor, resulting in subsequent intracellular $Ca^{2+}$ signaling, in UV induced pigmentation.nduced pigmentation.

• 한국약용작물학회지
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• 제21권5호
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• pp.361-371
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• 2013

This study was performed to determine the antimelanogenic effect and tyrosinase inhibitory activities of anthocyanin rich fraction (AN-SLP) from Liriope platyphylla Wang et Tang seeds. Anthocyanins isolated from L. platyphylla seeds revealed the presence of four major anthocyanin components, which were tentatively identified as delphinidin-3-Oglucoside, delphinidin-3-O-rutinoside, petunidin-3-O-rutinoside, and malvidin-3-O-rutinoside using semipreparative HPLC, $^1H$-NMR, $^{13}C$ NMR, FAB-MS and LC/ES-MS. The inhibitory effect of AN-SLP on tyrosinase activity was studied using in vitro (against mushroom tyrosinase) and ex vivo (against B16 melanoma cell tyrosinase) models. Cellular tyrosinase activity was decreased by AN-SLP treatment in B 16 melanoma cells through dose dependent manner, but AN-SLP did not inhibit mushroom tyrosinase and L-DOPA oxidation directly. AN-SLP showed melanin inhibition by 53.2% at 50 ${\mu}g/m{\ell}$ which was 0.7 times more efficient than the antimelanogenic effect of commercial arbutin and kojic acid (36.5%) also did not show cell toxicity. Additionally, AN-SLP inhibited the activity of ${\alpha}$-glucosidase and the glycosylation of tyrosinase in melanoma cell. The resulting unsaturated glycosylation of tyrosinase makes it unstable and disturb correct transportation. From theses results, we conclude that AN-SLP could be used as anti-melanogenic agent for skin whitening.

• The Korean Journal of Physiology and Pharmacology
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• 제7권6호
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• pp.311-316
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• 2003

Endothelins secreted from keratinocytes are intrinsic mitogens and melanogens of human melanocytes in UVB-induced hyperpigmentation. To elucidate the cellular mechanism of antimelanogenic activity of bamboo extract, the effects of three ingredients of bamboo extract on endothelin 1 (ET-1)-induced $Ca^{2+}$ mobilization were investigated in cultured human melanocytes. ET-1 receptors in human melanocytes were characterized by using specific antagonist, and ET-1 was found to increase intracellular $Ca^{2+}$ concentration ($[Ca^{2+}]_i$) by activating ET-B receptor. SM709 (1,2-O-diferulyl-glycerol), an ingredient of bamboo extract, inhibited ET-1-induced $[Ca^{2+}]_i$ increase in a concentration- and time-dependent manner, although another ingredients SM707 and SM708 had no effect on ET-1-induced $[Ca^{2+}]_i$ increase in human melanocytes. SM709 ($100{\mu}M$), however, did not affect $[Ca^{2+}]_i$ increase induced by thapsigargin and caffeine, suggesting that SM709 has no effect on the $Ca^{2+}$ store in melanocytes. Furthermore, SM709 did not affect $[Ca^{2+}]_i$ increase induced by LPA or ATP, known as G protein-mediated PLC activators like ET-1. Taken together, it is suggested that SM709 antagonizes ET-1-induced transmembrane signaling through ET-B receptor, which maybe a possible underlying mechanism of antimelanogenic activity of bamboo extract in human melanocytes.

• 약학회지
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• 제51권5호
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• pp.350-354
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• 2007

Taurine has been shown to be tissue-protective against oxidant-induced injury and is a powerful regulator of the immune system. However, there is no study on the antimelanogenic effect of taurine. In this study, we investigated the whitening effect of taurine in B16F10 mouse melanoma cells. Cell viability was measured by MTT assay. We examined melanin contents and tyrosinase activity according to time and concentration. Extracellular signal regulated kinase (ERK) is an important regulator of melanogenesis. It has been reported that activated ERK induced microphthalmia associated transcription factor (MITF) phosphorylation and its subsequent degradation and thus reduced melanin synthesis. In our B16F10 cell culture system, taurine led to decrease melanin contents by 21% at 48 hr. We then observed taurine effects on ERK-P, MITF and tyrosinase by Western blot. ERK was activated at 18 hr and 24 hr, whereas MITF reduced. We could not observe any differences in the levels of tyrosinase. These results suggested that taurine inhibited melanogenesis by ERK signal pathway via MITF degradation. We expect that taurine has potential skin whitening agents in cosmetics.

• 대한화장품학회지
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• 제34권4호
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• pp.287-301
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• 2008

천연물로부터 미백활성 성분의 개발을 위하여 국내 자생식물 60종으로부터 추출물을 얻어, 이들의 멜라닌 생성과정의 주된 효소인 tyrosinase 활성 억제력을 평가하였다. 평가결과 노랑하늘타리(열매), 죽황, 누리장나무(잎), 우산고로쇠(잎) 추출물이 비교적 높은 tyrosinase 활성억제효과를 보였고, 이들의 $IC_{50}$ 값은 $50{\sim}100{\mu}g/mL$ 이었다. 이들의 멜라닌생성 억제효과를 B16F10 흑색종세포주를 이용하여 실험한 결과, 죽황추출물이 가장 높은 52%의 멜라닌생성 저해활성을 보였으며, 이는 기존 미백제인 arbutin (42%)에 비해 10% 높은 것이다. 죽황추출물로부터 용매추출 및 크로마토그래피 등의 분리과정을 거쳐 10가지 미백활성 성분을 분리하였다. 이들은 모두 페놀유도체 화합물로서, SM701과 SM702, SM703, BPR211은 hydroquinone계 화합물이며, SM707은 gallic acid계, SM704와 SM705, SM706, SM708, SM709는 ferulic acid계로 확인되었다. 이들의 유리기 소거효과를 hydorquinone과 비타민 C와 비교하여 측정하였을 때. $SC_{50}$ 값이 SM702와 SM709의 경우 $60{\sim}70{\mu}M$로 hydroquinone과 유사하였고, SM701과 SM708은 $30{\sim}40{\mu}M$로 비타민 C ($45{\mu}M$)보다 낮은 값을 보여 죽황추출물은 항산화활성이 높은 성분들을 함유하고 있음을 확인하였다. 이들 중 1,2-O-diferulylglycerol로 확인된 SM709 성분은 tyrosine hydroxylase 및 DOPA oxidase 활성을 각각 18, 60% 억제하였고, B16F10 흑색종세포주를 이용한 멜라닌생성량 억제시험에서 62%의 저해효과를 나타내 가장 높은 미백활성을 보였다. 따라서 죽황추출물의 미백활성은 주로 멜라닌 생성과정의 DOPA oxidsae 저해효과와 항산화효과에 의해 나타나는 것으로 생각된다.

• Journal of Microbiology and Biotechnology
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• 제31권7호
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• pp.990-998
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• 2021

Melanin is a natural skin pigment produced by specialized cells called melanocytes via a multistage biochemical pathway known as melanogenesis, involving the oxidation and polymerization of tyrosine. Melanogenesis is initiated upon exposure to ultraviolet (UV) radiation, causing the skin to darken, which protects skin cells from UVB radiation damage. However, the abnormal accumulation of melanin may lead to the development of certain skin diseases, including skin cancer. In this study, the antioxidant and antimelanogenic activities of the cell-free supernatant (CFS) of twenty strains were evaluated. Based on the results of 60% 2,2-diphenyl-1-picrylhydrazyl scavenging activity, 21% 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) scavenging capacity, and a 50% ascorbic acid equivalent ferric reducing antioxidant power value, Limosilactobacillus fermentum JNU532 was selected as the strain with the highest antioxidant potential. No cytotoxicity was observed in cells treated with the CFS of L. fermentum JNU532. Tyrosinase activity was reduced by 16.7% in CFS-treated B16F10 cells (but not in the cell-free system), with >23.2% reduction in melanin content upon treatment with the L. fermentum JNU532-derived CFS. The inhibitory effect of the L. fermentum JNU532-derived CFS on B16F10 cell melanogenesis pathways was investigated using quantitative reverse transcription polymerase chain reaction and western blotting. The inhibitory effects of the L. fermentum JNU532-derived CFS were mediated by inhibiting the transcription of TYR, TRP-1, TRP-2, and MITF and the protein expression of TYR, TRP-1, TRP-2, and MITF. Therefore, L. fermentum JNU532 may be considered a potentially useful, natural depigmentation agent.