• 한국미생물·생명공학회지
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• 제51권3호
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• pp.250-256
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• 2023

Cannabis sativa (CS) has been in the spotlight not only for its medical uses but also as a raw material for cosmetics. As fermented cosmetics are known to have various health benefits, they have been extensively researched. Here, we investigated the characteristics of CS stems fermented using various gut microbes. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide assay and melanin content analysis revealed that melan-a cells containing CS stems fermented with Weissella paramesenteroides (CSWP) showed considerably reduced melanin content. Additionally, CSWP downregulated the expression of several melanogenesis factors, tyrosinase-related protein-1, and tyrosinase-related protein-2. This study suggests that the anti-melanogenic effect of CSWP could provide a new basis for the development of skin-lightening agents.

• 대한본초학회지
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• 제32권3호
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• pp.71-78
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• 2017

Objectives : The various grape extracts derived from grape pulp, seed and skin, containing various types of polyphenols and flavonoids, have been known to have anti-inflammatory, antioxidant and improve cardiovascular condition as well as sun's damaging effects. However, there have been rare reports of various beneficial effects of grape fruit stem extract (GFSE), one of the waste products of grapes. We investigated anti-inflammatory and melanogenesis inhibitory effects of GFSE. Methods : One-hundred gram of grape fruit stem was extracted with 80% ethanol at room temperature for 3 days. After filtration, the ethanol was removed using vacuum evaporator, then lyophilized to obtain the dry extract which was stored at $-20^{\circ}C$ until used. NO levels were measured by using Greiss reagent. Prostaglandin $E_2$ ($PGE_2$) production was measured by ELISA assay. The expression levels of iNOS, COX-2, TRP-1 and TRP-2 were evaluated by western blot analysis. Results : GFSE reduced the level of nitric oxide and prostaglandin $E_2$ ($PGE_2$) production in a dose-dependent manner, compared to control. Expressions of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) protein were also effectively inhibited by the GFSE. In a tyrosinase inhibitory activity, GFSE significantly reduced the tyrosinase activity and melanin content in a dose dependent manner, compared to control. GFSE also decreased the expression of tyrosinase related protein-1 (TRP-1) and tyrosinase related protein-2 (TRP-2), known as a melanocyte-specific gene product involved in melanin synthesis. Conclusions : Therefore, these results indicated that GFSE had powerful anti-inflammatory and anti-melanogenic effects.

• 한국작물학회:학술대회논문집
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• 한국작물학회 2017년도 추계학술대회
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• pp.235-235
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• 2017

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2007년도 Proceedings of The Convention
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• pp.129-139
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• 2007

Many modalities of treatment for acquired skin hyperpigmentation are available including chemical agents or physical therapies, but none are completely satisfactory. The ideal depigmenting compound should have a potent. rapid and selective bleaching effect on hyperactivated melanocytes, carry no short- or long-term side-effects and lead to a permanent removal of undesired pigment. acting at one or more steps of the pigmentation process. Depigmentation can be achieved by regulating (i) the transcription and activity of tyrosinase, tyrosinase related protein-1 (TRP-1), tyrosinase related protein-2 (TRP-2), and/or peroxidase; (ii) the uptake and distribution of melanosomes in recipient keratinocytes and (iii) melanin and melanosome degradation and turnover of pigmented keratinocytes. One of the interesting point for development of skin whitening agent is Mitf(Microphthalmia-associated transcription factor). Mitf belongs to the basic helix-loop-helix-zip family of trabscription factors and it is crucial as it regulates both melanocyte proliferation as well as melanogenesis and is the major regulator of tyrosinase and the related enzymes (TRPs), as well as many melanosome structural proteins such as pMel17. Recently, we developed MITF-down-regulating agents from natural and synthetic sources, which have anti-melanogenic effect on in vitro and in vivo. We suggested that potent MITF-down regulating agents might be used for skin whitening cosmeceuticals.

• Journal of Microbiology and Biotechnology
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• 제32권8호
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• pp.982-988
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• 2022

Licorice (Glycyrrhiza) has been used as preventive and therapeutic material for hyperpigmentation disorders. Previously, we isolated noble compounds including dehydroglyasperin C (DGC), dehydroglyasperin D (DGD) and isoangustone A (IAA) from licorice hexane/ethanol extracts. However, their anti-melanogenic effects and underlying molecular mechanisms are unknown. The present study compared effects of DGC, DGD and IAA on pigmentation in melan-a melanocytes and human epidermal melanocytes (HEMn). DGD exerted the most excellent anti-melanogenic effect, followed by DGC and IAA at non-cytotoxic concentrations. In addition, DGD significantly inhibited tyrosinase activity in vitro cell-free system and cell system. Western blot result showed that DGD decreased expression of microphthalmia-associated transcription factor (MITF), tyrosinase and tyrosinase-related protein-1 (TRP-1) in melan-a cells and HEMn cells. DGD induced phosphorylation of MITF, ERK and Akt signal pathway promoting MITF degradation system. However, DGD did not influence p38 and cAMP-dependent protein kinase (PKA)/CREB signal pathway in melan-a cells. These result indicated that DGD inhibited melanogenesis not only direct regulation of tyrosinase but also modulating intracellular signaling related with MITF level. Collectively, these results suggested a protective role for DGD against melanogenesis.

• The Korean Journal of Physiology and Pharmacology
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• 제26권2호
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• pp.113-123
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• 2022

Diarylpropionitrile (DPN), a selective agonist for estrogen receptor β (ERβ), has been reported to regulate various hormonal responses through activation of ERβ in tissues including the mammary gland and brain. However, the effect of DPN on melanogenesis independent of ERβ has not been studied. The aim of this study is to examine the possibility of anti-melanogenic effect of DPN and its underlying mechanism. Melanin contents and cellular tyrosinase activity assay indicated that DPN inhibited melanin biosynthesis in alpha-melanocyte stimulating hormone-stimulated B16F10 melanoma cell line. However, DPN had no direct influence on in vitro tyrosinase catalytic activity. On the other hand, 17β-estradiol had no effect on inhibition of melanogenesis, suggesting that the DPN-mediated suppression of melanin production was not related with estrogen signaling pathway. Immunoblotting analysis showed that DPN down-regulated the expression of microphthalmia-associated transcription factor (MITF), a central transcription factor of melanogenesis and its down-stream genes including tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2. Also, DPN attenuated the phosphorylation of protein kinase A (PKA) and cAMP-response element-binding protein (CREB). Additionally, DPN suppressed the melanin synthesis in UVB-irradiated HaCaT conditioned media culture system suggesting that DPN has potential as an anti-melanogenic activity in physiological conditions. Collectively, our data show that DPN inhibits melanogenesis via downregulation of PKA/CREB/MITF signaling pathway.

• Biomolecules & Therapeutics
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• 제31권1호
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• pp.89-96
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• 2023

Uric acid produced by guanine deaminase (GDA) is involved in photoaging and hyperpigmentation. Reactive oxygen species (ROS) generated by uric acid plays a role in photoaging. However, the mechanism by which uric acid stimulates melanogenesis in GDA-overexpressing keratinocytes is unclear. Keratinocyte-derived paracrine factors have been identified as important mechanisms of ultraviolet-induced melanogenesis. Therefore, the role of paracrine melanogenic growth factors in GDA-induced hypermelanosis mediated by uric acid was examined. The relationships between ROS and these growth factors were examined. Primary cultured normal keratinocytes overexpressed with wild type or mutant GDA and those treated with xanthine or uric acid in the presence or absence of allopurinol, H₂O₂, or N-acetylcysteine (NAC) were used in this study. Intracellular and extracellular bFGF and SCF levels were increased in keratinocytes by wild type, but not by loss-of-function mutants of GDA overexpression. Culture supernatants from GDA-overexpressing keratinocytes stimulated melanogenesis, which was restored by anti-bFGF and anti-SCF antibodies. Allopurinol treatment reduced the expression levels of bFGF and SCF in both GDA-overexpressing and normal keratinocytes exposed to exogenous xanthine; the exogenous uric acid increased their expression levels. H₂O₂-stimulated tyrosinase expression and melanogenesis were restored by NAC pretreatment. However, H₂O₂ or NAC did not upregulate or downregulate bFGF or SCF, respectively. Overall, uric acid could be involved in melanogenesis induced by GDA overexpression in keratinocytes via bFGF and SCF upregulation not via ROS generation.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2022년도 추계학술대회
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• pp.104-104
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• 2022

Dendropanax morbiferus H. Lev has been reported to have some pharmacologic activities and also interested in functional cosmetics. We found that the water extract of D. morbiferus leaves significantly inhibited tyrosinase activity and melanin formation in α-melanocyte stimulating hormone (MSH)-induced B16-F10 cells. D. morbiferus reduced melanogenesis-related protein levels, such as microphthalmia? associated transcription factor (MITF), TRP-1, and TRP-2, without any cytotoxicity. Two active ingredients of D. morbiferus, (10E)-9,16-dihydroxyoctadeca-10,17-dien-12,14-diynoate (DMW-1) and (10E)-(?)-10,17-octadecadiene-12,14-diyne-1,9,16-triol (DMW-2) were identified by testing the anti-melanogenic effects and then by liquid chromatography-tandem mass spectrometry (LC/MS/MS) analysis. DMW-1 and DMW-2 significantly inhibited melanogenesis by the suppression of protein kinase A (PKA)/cyclic AMP (cAMP)-responsive binding protein (CREB) and p38 MAPK phosphorylation. DMW-1 showed a better inhibitory effect than DMW-2 in α-MSH-induced B16-F10 cells. D. morbiferus and its active component DMW-1 inhibited melanogenesis through the downregulation of cAMP, p-PKA/CREB, p-p38, MITF, TRP-1, TRP-2, and tyrosinase. These results indicate that D. morbiferus and DMW-1 may be useful ingredients for cosmetics and therapeutic agents for skin hyperpigmentation disorders.

• Preventive Nutrition and Food Science
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• 제15권2호
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• pp.98-104
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• 2010

The seeds from two mulberry fruits [Morus alba (MA) and Cudrania tricuspidata (CT)] were examined for their oil content, and fatty acid, phytosterol and tocopherol compositions and contents. Moreover, polyphenolic compounds and biological activity of the two defatted seed residue extracts were also evaluated. Oil contents of MA and CT seeds were 29.36% and 16.69%, respectively, while MeOH extracts of the defatted MA and CT seed residues were 5.10% and 6.22%, respectively. The two seed oils were composed of 81.4 and 74.37% linoleic, 5.75 and 11.39% oleic, 8.40 and 10.18% palmitic acid, and 3.52 and 3.0% stearic acids, and two other minor fatty acids, such as linolenic and arachidic acids. MA seed had higher contents of phytosterols (507.59 mg/100 g of oil), tocopherols (99.64 mg/100 g of oil), and total flavonoid (106.50 mg/100 g of seed) than CT seed, whereas CT seed had higher levels of total polyphenol than MA seed. The MeOH extract of MA seed residue showed higher antioxidant, anti-diabetic, and anti-melanogenic activity than that of CT seed residue. trans-Resveratrol (9.62 mg/100 g), quercetin (54.83 mg/100 g), and 4-prenylmoracin (48.70 mg/100 g), were found to be the main polyphenolic components in the MeOH extract of MA seed residue. These results indicate that MA seeds are good sources of essential dietary phytochemicals with antioxidant, anti-diabetic and anti-melanogenic activity.

• 대한화장품학회지
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• 제42권2호
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• pp.195-201
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• 2016

히솝(Hyssopus officinalis)은 통화식물목 꿀풀과의 여러해살이풀로 방부제, 기침, 거담제 등 일반적으로 방향족 허브와 약용식물로 사용되어왔다. 본 연구에서는 항산화 및 미백소재의 개발을 위해 히솝을 열수와 주정으로 추출하여 각 추출물의 in vitro 상에서의 항산화 효과 및 B16F10 melanoma 세포에서 멜라닌 생성 저해효과를 평가하였다. DPPH와 ABTS assay 시험법을 이용하여 항산화 효과를 측정한 결과, 히솝 추출물의 항산화 활성이 모두 농도 의존적으로 증가하였다. 또한 히솝 추출물은 tyrosianse 활성을 저해시켰으며, B16F10 세포에서 UVB로 증가된 활성산소와 ${\alpha}$-MSH로 유도된 멜라닌 또한 감소시키는 효과를 보였다. 멜라닌 생합성에 관여하는 유전자의 발현에 미치는 영향을 알아보기 위해 RT-PCR을 실시한 결과 히솝 추출물에 의해 MITF, tyrosinase, TRP-2의 발현이 감소되는 것을 확인할 수 있었다. 이러한 결과에 따라 히솝 추출물은 미백개선을 위한 화장품 소재로서 이용 가능성이 높을 것으로 사료된다.