• Journal of the Society of Cosmetic Scientists of Korea
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• v.46 no.2
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• pp.159-166
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• 2020

Propolis is a sticky resinous substance that is formed by the combination of honeybee secretions and resin of plants, which serves to protect from bacteria and viruses. This study aims to evaluate the efficacy of propolis extract from Korea (KPE), China (CPE), and Brazil (BPE) through antioxidant, antibacterial, whitening, and anti-inflammatory tests, and to examine their potential as cosmetic materials. KPE, CPE, and BPE showed significant antioxidant activities on flavonoid/polyphenol content and free radical scavenging activity. The antibacterial effect of propolis on skin flora was determined by measuring the minimal inhibitory concentration (MIC). KPE showed better antibacterial efficacy than CPE and BPE in C. acnes (KPE, CPE, and BPE: (62.5, 250, and 500) ㎍/mL, respectively). Furthermore, KPE inhibited the melanin synthesis in human epidermal melanocytes and production of nitric oxide and PGE₂ induced by lipopolysaccharide (LPS) in mouse macrophages, which showed better than did CPE or BPE. Taken together, the propolis extracts can be applied to antioxidant, antibacterial, and anti-inflammatory ingredient for cosmetics, while KPE showed superior potential in antibacterial, anti-inflammatory, and whitening efficacies.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2007.11a
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• pp.79-92
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• 2007

Oxidative stress have known to be a risk factor for the degenerative processes and closely related to a lot of diseases. It is well established that antioxidants are good in protection and therapeutic means against oxidative damage. There is increasing interest in natural antioxidants and many natural antioxidants have been found and utilized as the possible protection for various diseases and skin aging. We have screened natural antioxidant agents for cosmeceuticals, nutraceuticals, and drugs as therapeutic and preventive means against oxidative stress, and have developed a number of novel antioxidants from various natural sources. A novel melanin synthesis inhibitor, Melanocin A, isolated from the metabolite of a fungal strain Eupenicillium shearii F80695 inhibited mushroom tyrosinase and melanin biosynthesis of B16 melanoma cells with $IC_{50}$ value of 9.0 nM and MIC value of $0.9\;{\mu}M$, respectively. Melanocin A also exhibited potent antioxidant activity by scavenging of DPPH and superoxide anion radicals. UV was found to increase the level of hydrogen peroxides and other reactive oxygen species (ROS) in skin tissues. This increase in ROS may not only alter the structure and function of many genes and proteins directly but may also modulate their expressions through signal transduction pathways and, ultimately, lead to skin damage. We investigated the effect of Melanocin A on UV-induced premature skin aging. Firstly, the effect of Melanocin A on UV-induced matrix metalloproteinase (MMP)-9 expression in an immortalized human keratinocyte cell line, HaCaT in vitro was investigated. Acute UV irradiation induced MMP-9 expression at both the mRNA and protein levels and Melanocin A suppressed this expression in a dose-dependent manner. We then investigated UV-induced skin changes in hairless mice in vivo by Melanocin A. Chronic exposure of hairless mouse dorsal skin to UV increased skin thickness and induced wrinkle formation and the gelatinase activities of MMP-2 and MMP-9. Moreover, Melanocin A significantly suppressed UV-induced morphologic skin changes and MMP-2 and MMP-9 expression. These results show that Melanocin A can prevent the harmful effects of UV that lead to skin aging. Therefore, we suggest that Melanocin A should be viewed as a potential therapeutic agent for preventing and/or treating premature skin aging. Terrein is a bioactive fungal metabolite isolated from Penicillium species. Terrein has a relatively simple structure and can be easily synthesized. However, the biologic effects of terrein are comparatively unknown. We found for the first time that terrein potently inhibit melanin production in melanocytes and has a strong hypopigmentary effect in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab. Treatment of Mel-Ab cells with terrein (10-100 mM) for 4 days significantly reduced melanin levels in a dose-dependent manner. In addition, terrein at the same concentration also reduced tyrosinase activity. We then investigated whether terrein influences the extracellular signal-regulated protein kinase (ERK) pathway and the expression of microphthalmia-associated transcription factor (MITF), which is required for tyrosinase expression. Terrein was found to induce sustained ERK activation and MITF down-regulation, and luciferase assays showed that terrein inhibits MITF promoter activity in a dose-dependent manner. To elucidate the correlation between ERK pathway activation and a decreased MITF transcriptional level, PD98059, a specific inhibitor of the ERK pathway, was applied before terrain treatment and found to abrogate the terrein-induced MITF attenuation. Terrein also reduced the tyrosinase protein level for at least 72 h. These results suggest that terrain reduces melanin synthesis by reducing tyrosinase production via ERK activation, and that this is followed by MITF down-regulation.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.48 no.4
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• pp.365-372
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• 2022

Cellobiose is a dissacharide constituted by two glucose units joined by a β-('1,4') glycosidic bond that is produced by the decomposition of cellulose. This product exists naturally in plants and has been utilized in different industries as a food sweetener, and as a cosmetic and pharmaceutical material. In this study, the potential of cellobiose as a whitening cosmetic product was evaluated by analyzing autophagy induction and the inhibition of melanin production. A cytotoxicity test conducted in the human melanin-producing cell line MNT-1 with increasing concentrations of cellobiose revealed that this compound did not cause cytotoxicity at 20 mg/mL or less. Based on this, autophagy was firstly evaluated by immunostaining with the autophagy marker microtubule-associated protein 1 light chain 3 (LC3) after treatment with 20 mg/mL of cellobiose. The subsequent confocal microscopy analysis revealed an increase in LC3 puncta, indicating induction of autophagy. In addition, autophagy was further confirmed by western blot analysis, which demonstrated that cellobiose converted LC3-I to LC3- ∏ in a concentration- and time-dependent manners. An analysis of melanin contents after cellobiose treatment at a concentration of 20 mg/mL during 7 days revealed that melanin production was reduced by more than 50%. Additionally, the expression levels of melanogenesis-related proteins TYR and TYRP1 were markedly decreased after cellobiose treatment. Based on these studies, a cosmetic cream formulation containing cellobiose was prepared and the change in formulation was tested for 4 weeks, and it was confirmed that the appearance changed to liquid form at high temperature, but the pH did not change. In conclusion, the present research demonstrated that cellobiose activates autophagy and inhibits melanin production, and showed the potential of this product as a material for whitening cosmetics.