• Journal of the Society of Cosmetic Scientists of Korea
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• v.31 no.4 s.54
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• pp.349-357
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• 2005

New antioxidative substances for cosmeceuticals were screened from natural resources such as microbial metabolites, mushrooms, and medicinal plants. Four antioxidants were isolated from the fungal metabolite of Eupenicillium shearii and their structures were determined to be new phenolic compounds. The compounds were designated as melanocins A, B, C, and D. Melanocins $A{\sim}D$ exhibited free radical scavenging activity on DPPH and superoxide with $EC_{50}$ values of $21{\sim}94\;and\;7{\sim}84{\mu}M$, respectively, which were stronger activity than those of ${\alpha}-tocopherol$ and BHA. Melanocin A showed anti-wrinkle effects on the UV-irrated hairless mouse skin. A novel hispidin antioxidative compound designated as inoscavin A was isolated from the fruiting body of the mushroom, Inonotus xeranticus. Inoscavin A scavenged superoxide radical with $EC_{50}$ values of $0.03{\mu}g/mL$, and inhibited rat liver microsomal lipid peroxidation with $EC_{50}$ values of $0.3{\mu}g/mL$. Benzastatins $A{\sim}G$, the novel antioxidants isolated from the culture of Streptomyces nitrosporeus showed potent lipid peroxidation inhibitory activity with $EC_{50}$ values of $3{\sim}30{\mu}M$. A cyclopentene compound with strong hypopigmentary effect was isolated from the fungal metabolite of Penicillium sp. and identifed as terrein. Terrein significantly reduced melanin levels in a melanomacyte cell line, Mel-Ab. It showed 10 times stronger activity than kojic acid, but exhibited no cytotoxic effect even in $100{\mu}M$. It was suggested that terrein reduced melanin synthesis by reducing tyrosinase production by MITF down-regulation.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.26 no.1
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• pp.149-162
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• 2000

Coenzyme Q10 is found in all tissues including skin and it is the well-known coenzyme for mitochondrial enzymes. The electron and proton transfer functions of the quinone ring are of fundamental importance for the oxidative phosphorylation pathway to generate energy in the cells. Coenzyme Q10 has been studied as a potent antioxidant molecule in the skin. It is involved in the skin's response to UVR irradiation. The concentration of this antioxidant in UVR exposed skin is higher than in non-exposed skin. However, recent studies have also shown that coenzyme Q10 is one of the first antioxidants to be depleted when skin is UVR-irradiated. This indicates that coenzyme Q10 is primarily involved in defense mechanisms of the skin. Therefore, we questioned whether coenzyme Q10 shows reulatory effect of melanogenesis. Here we report that coenzyme Q10 inhibits melanin neosynthesis of normal human melanocytes grown in culture, and lightens UVB-induced hyperpigmentation of the guinea pig skin in vivo. We treated human melanocytes with 0.05mM to 0.5mM of coenzyme Q10 for a total of two days. This inhibited melanin neosynthesis of cultured human melanocytes dose-dependently. The inhibitory effect of coenzyme Q10 was as effective as kojic acid or vitamin C on cultured human melanocytes. CoQ10 didn't have direct inhibitory effect on tyrosinase activity in in vitro tyrosine hydroxylase activity To further clarify the effect of coenzyme Q10 on the melanogenesis, we established UVB-induced hyperpigmentation on the shaved backs of brownish guinea pigs. The UVB intensity was 500mJ/$\textrm{cm}^2$ and the total energy dose was 1,500 mJ/$\textrm{cm}^2$. The animals were exposed to UVB radiation one times a week for three consecutive weeks. Coenzyme Q10, kojic acid, Arbutin, vitamin C(1% in vehicle) or vehicle alone as a control were then topically applied daily to the hyperpigmented areas twelve times per week far four successive weeks. The lightening effect was evaluated by visual scoring, chromameter and immunohistochemistry. Coenzyme Q10 had lightening effect on the UVB-induced hyperpigmentation without any other side effects, whereas another compounds showed weak lightening efficacies. Therefore, these results suggest that coenzyme Q10 may be useful for solving physiological hyperpigmenting problems for cosmetic purposes.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.41 no.4
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• pp.391-400
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• 2015

In the present study, 50% ethanol extract, the ethyl acetate and aglycone fraction were prepared from mate (Ilex paraguariensis) and their antioxidative ability was evaluated. The yields of extract and fractions were 32.0, 4.48 and 0.82% per dried powder, respectively. Free radical scavenging activities were performed by 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and total antioxidant capacity was estimated using luminol-dependent chemiluminescence assay. Free radical scavenging activities ($FSC_{50}$) of 50 % ethanol extract, ethyl acetate fraction and aglycone fraction were 8.83, 5.84 and $6.05{\mu}g/mL$, respectively. Their total antioxidant capacities ($OSC_{50}$) were similar to that of L-ascorbic acid ($1.72{\mu}g/mL$), known as a prominent water soluble antioxidant, in all extracts and 50% ethanol extract ($1.03{\mu}g/mL$) was the most effective. The cellular protective effects on the $^1O_2$-induced cellular damage of erythrocytes were evaluated and the results showed that all extracts were significantly higher than (+)-${\alpha}$-tocopherol at $10{\mu}g/mL$. Especially, the ${\tau}_{50}$ value of aglycone fraction was 5 times higher than (+)-${\alpha}$-tocopherol at $10{\mu}g/mL$ and $50{\mu}g/mL$. The inhibitory effects of the ethyl acetate and aglycone fractions on tyrosinase were similar to arbutin, known as the whitening agent in cosmetics. These results suggest that the extracts of mate have the applicability as antioxidant and anti-aging cosmeceutical ingredients.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.45 no.2
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• pp.161-173
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• 2019

In this study, the antioxidative and inhibitory activity of tyrosinase and collagenase for the solvent extract and silica column fractions of Artocarpus nitidus were evaluated. The activities were quantified using the 4 parameter logistic. LC/MS analysis showed that the major component of the fractions was polyphenol and the total polyphenol content of the extract was $48.1{\pm}2.6mg\;GAE/g$. The radical scavenging activities ($SC_{50}$) for 1,1-diphenyl-2-picrylhydrazyl of the extract, fraction-1 and fraction-2 were 16.7, 42.0 and $10.1{\mu}g/mL$, respectively. The value for fraction-2 was the closest to ascorbic acid ($1.5{\mu}g/mL$). The tyrosinase inhibitory activity of the extracts and the fractions showed $IC_{50}$ of 64.9, 0.9 and $1.2{\mu}g/mL$, respectively, and overall activity was higher than that of kojic acid ($7.4{\mu}g/mL$) and arbutin ($119.0{\mu}g/mL$). In the experiment by zebrafish embryo, the whitening activity of fraction-2 (27.5%) was higher than that of kojic acid (18.6%), and there was no adverse effect up to $500{\mu}g/mL$ of fraction-2. For the collagenase inhibitory activity, the samples showed $IC_{50}$ of 139.8, 20.6, and $16.8{\mu}g/mL$, respectively, which were competitive to 1, 10-Phenanthroline ($55.4{\mu}g/mL$). The extract and fraction-2 showed $IC_{50}$ of 61.8 and $67.1{\mu}g/mL$ for elastase. These results suggest that A. nitidus extract can be used as a cosmetic material useful for antioxidant, whitening, and prevention of skin aging without adverse effects.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2019.04a
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• pp.21-22
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• 2019

Melanin is a mixture of pigmented biopolymers synthesized by epidermal melanocytes that determine the skin, eye, and hair colors. Melanocytes produce two different kinds of melanin, eumelanin (dark brown/black insoluble pigments found in dark skin and dark hair and pheomelanin (lighter red/yellow). The biological role of melanin is to prevent skin damage by ultraviolet (UV) radiation. However, the overproduction or deficiency of melanin synthesis could lead to serious dermatological problems, which include melasma, melanoderma, lentigo, and vitiligo. Therefore, regulating melanin production is important to prevent the pigmentation disorders. Myanmar has a rich in natural resources. However, the chemical constituents of these natural resources in Myanmar have not been fully investigated. In the effort to search for compounds with anti-melanin deposition activity from Myanmar natural resources, five plants were collected in Myanmar. Extracts of these collected five plants were tested for anti-melanin deposition activity against a mouse melanoma cell line (B16-F10) induced with ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH) and 3-isobutyl-1-methylxanthine (IBMX), and their anti-melanin deposition activities were compared with the positive control, arbutin. Among the tested extracts, the CHCl3 extracts of the Premna serratifolia (syn: P. integrifolia) wood showed anti-melanin deposition activities with IC50 values of $81.3{\mu}g/mL$. Hence, this study aims to identify secondary metabolites with anti-melanin deposition activity from P. serratifolia wood of Myanmar. P. serratifolia belongs to the Verbenaceae family and is widely distributed in near western sea coast from South Asia to South East Asia, which include India, Malaysia, Vietnam, Cambodia, and Sri Lanka. People in Tanintharyi region located in the southern part of Myanmar utilize the P. serratifolia, Sperethusa crenulata, Naringi crenulata, and Limonia acidissima as Thanaka, traditional cosmetics in Myanmar. Thanaka is applied in the form of paste onto skins to make it smooth and clear, as well as to prevent wrinkles, skin aging, excessive facial oil, pimples, blackheads, and whiteheads. However, the chemical constituents responsible for their cosmetic properties are yet to be identified. Moreover, the chemical constituents of P. serratifolia was almost uncharacterized. Investigation of the P. serratifolia chemical constituents is thus an attractive endeavor to discover new anti-melanin deposition active compounds. The investigation of the chemical constituents of the active CHCl3 extract of P. serratifolia led to isolation of four new lignoids, premnan A (1), premnan B (2), taungtangyiol C (3), and 7,9-dihydroxydolichanthin B (4), together with premnan C (5) (assumed to be an artifact), one natural newlignoid,(3R,4S)-4-(1,3-benzodioxol-5-ylcarbonyl)-3-[(R)-1-(1,3-benzo dioxol-5-yl)-1-hydroxy methyl]tetrahydro-2-furanone (6), and five known compounds (7-11)1,2). The structures of all isolated compounds were determined on the basis of their spectroscopic data and by comparison with the reported literatures. The absolute configurations of 1-3 and 5 were also determined by optical rotation and circular dichroism (CD) data analyses1). The anti-melanin deposition activities of all the isolated compounds were evaluated against B16-F10 cell line. 7,9-Dihydroxydolichanthin B (4) and ($2{\alpha},3{\alpha}$)-olean-12-en-28-oic acid (11) showed strong anti-melanin deposition activities with IC50 values of 18.4 and $11.2{\mu}M$, respectively, without cytotoxicity2). On the other hand, compounds 1-3, 5, and 7 showed melanogenesis enhancing activities1). To better understand their anti-melanin deposition mechanism, the effects of 4 and 11 on tyrosinase activities were investigated. The assay indicated that compounds 4 and 11 did not inhibit tyrosinase. Furthermore, we also examined the mRNA expression of microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), tyrosinase-related protein-1 (TRP-1), and tyrosinase-related protein-2 (TRP-2). Compounds 4 and 11 down-regulated the expression of Tyr and Mitf mRNAs, respectively. Although the P. serratifolia wood has been used as traditional cosmetics in Myanmar for centuries, there are no scientific evidences to support its effectiveness as cosmetics. Investigation of the anti-melanin deposition activity of the chemical constituents of P. serratifolia thus provided insight into the effectiveness of the P. serratifolia wood as a cosmetic agent.