• Journal of the Korean Applied Science and Technology
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• v.36 no.2
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• pp.635-644
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• 2019

The aim of this study was to investigate whitening effect of combination between arbutine and oil soluble licorice extract. Inhibitory effects of arbutin and oil soluble licorice extract against tyrosinase activity and melanogenesis in B16 melanoma cells were assessed in vitro to determine whitening effect. MTT assay with B16 melanoma cells showed that mixture (arbutin and oil soluble) was not each concentration. Both oil soluble licorice extract and arbutin induced dose-dependent inhibition of mushroom tyrosinase activity. Various concentrations (oil soluble extract : arbutin = 1:1. 1:1.5, 1:2, 1:2.5, 1:5) of mixtures also significantly inhibited tyrosinase activity in B16 melanoma cells by 40-51%. In addition, the mixtures reduced the melanin contents of B16 melanoma cells by more than 50% at each concentration. These results suggest that mixtures of arbutin and oil soluble licorice extract are very effective whitening ingredients.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.1
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• pp.33-38
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• 2004

Melanin pigmentation in human skin is a major defense mechanism against ultraviolet light of the sun, but abnormal pigmentation such as freckles, liver spot could be a serious aesthetic problem. Nearly all studies are mainly concentrated on searching for the materials that have inhibitory activities on tyrosinase. In this work, to isolate phenolic compounds from Gastrodia elata, we purified the extract through solvent fractionation, column chromatography, and recrystallization. They were identified as 4-hydroxybenzyl alcohol 1, bis(4-hydroxyphenyl)methane 2, gastrodin (4-${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 on the base of spectroscopic evidences. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cells were evaluated in vitro. We have found that 4-hydroxybenzyl alcohol 1 and gastrodin (4- ${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 have no tyrosinase inhibitory activity, but inhibit the melanin synthesis in B16 melanoma cells. Tyrosinase inhibitory activities of bis(4-hydroxyphenyl)methane 2 (IC$\_$50/ = 400 $\mu\textrm{g}$/mL) and butanol fraction (IC$\_$50/ = 46 $\mu\textrm{g}$/mL) were lower/higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL), but inhibitory activities of melanin synthesis in B16 melanoma cells were much higher than that of arbutin. Especially, tyrosinase inhibitory activities of isolated phenolic fraction (IC$\_$50/ = 2.37 $\mu\textrm{g}$/mL) from butanol fraction was very higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL). Therefore, these results suggest that isolated phenolic compounds from Gastrodia elata have inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in 816 melanoma cells in vitro.

• Journal of Life Science
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• v.30 no.7
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• pp.598-605
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• 2020

Padina gymnospora is a brown algae of the class Phaeophyceae. It has been established that P. gymnospora ameliorates amyloid-β-induced neuropathology and has an anticoagulation effect, but this study was designed to estimate its skin-whitening effect and identify its active component. The ingredients of P. gymnospora were extracted with ethanol and its activity was compared with arbutin. First, the P. gymnospora extract was observed to inhibit tyrosinase activity in a dose-dependent manner, tyrosinase being the rate-limiting enzyme of melanin synthesis. Notably, where 200 μM of arbutin inhibited tyrosinase activity by 58.1%, P. gymnospora extract (0.5%) achieved 76.7%. The P. gymnospora extract also significantly reduced α-melanocyte-stimulating hormone-induced TRP-1 and TRP-2 mRNA expression. In addition, it significantly inhibited melanin synthesis in B16F10 melanoma cells. We identified the 0.66% fucosterol content that inhibited melanin synthesis as comparable to that of arbutin. Additionally, we tested the potential cytotoxicity of P. gymnospora by MTT and LDH release assay and found that the extract significantly reduced LDH release in CCD-986sk cells. These results indicate that P. gymnospora extract could be a potential active ingredient of cosmetics with a skin-whitening effect.

• Journal of the Korean Applied Science and Technology
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• v.24 no.4
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• pp.410-415
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• 2007

Functional cosmetics are intensively investigated for the effectiveness of skin whitening, anti-aging and slimming. For enhancing the effectiveness, active ingredients should be delivered into the cell in the dermis. The amounts of penetration of caffeine and $Arbutin^{(R)}$ were tested, in vitro, using Franz diffusion cell. Oil-in-water emulsions were used for the vehicles of the transport. For the measuring the amounts of active ingredients delivered into the dermal skin, tape stripping was done after finishing the penetration experiments. The amounts of delivered caffeine were $8.45{\pm}$ 1.26ug/ml before tape stripping and $3.45{\pm}$ 1.80ug/ml after tape stripping, however, the amounts of delivered $Arbutin^{(R)}$ was quite small to detect. From now on, proper vehicles are considered for enhancing the delivery of $Arbutin^{(R)}$ Hairless mouse skin was compared with pig skin as a transdermal delivery membrane. The aspects of delivery were similar, but the amount of delivered ingredients using pig skin was larger than that of using hairless mouse skin. Therefore, the pig skin would be considered as a membrane for drug delivery experiments.

• Toxicological Research
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• v.33 no.1
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• pp.55-62
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• 2017

We evaluated the antioxidant activity and anti-melanogenic effects of Oenothera laciniata methanol extract (OLME) in vitro by using melan-a cells. The total polyphenol and flavonoid content of OLME was 66.3 and 19.0 mg/g, respectively. The electron-donating ability, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical-scavenging activity, and superoxide dismutase (SOD)-like activity of OLME ($500{\mu}g/mL$) were 94.5%, 95.6%, and 63.6%, respectively. OLME and arbutin treatment at $50{\mu}g/mL$ significantly decreased melanin content by 35.5% and 14.2%, respectively, compared to control (p < 0.05). OLME and arbutin treatment at $50{\mu}g/mL$ significantly inhibited intra-cellular tyrosinase activity by 22.6% and 12.6%, respectively, compared to control (p < 0.05). OLME ($50{\mu}g/mL$) significantly decreased tyrosinase, tyrosinase-related protein-1 (TRP-1), TRP-2, and microphthalmia-associated transcription factor-M (MITF-M) mRNA expression by 57.1%, 67.3%, 99.0%, and 77.0%, respectively, compared to control (p < 0.05). Arbutin ($50{\mu}g/mL$) significantly decreased tyrosinase, TRP-1, and TRP-2 mRNA expression by 24.2%, 42.9%, and 48.5%, respectively, compared to control (p < 0.05). However, arbutin ($50{\mu}g/mL$) did not affect MITF-M mRNA expression. Taken together, OLME showed a good antioxidant activity and anti-melanogenic effect in melan-a cells that was superior to that of arbutin, a well-known skin-whitening agent. The potential mechanism underlying the anti-melanogenic effect of OLME was inhibition of tyrosinase activity and down-regulation of tyrosinase, TRP-1, TRP-2, and MITF-M mRNA expression.

• Journal of the Korean Applied Science and Technology
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• v.33 no.4
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• pp.667-675
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• 2016

Nanoemulsions are actively used in several applications for pharmaceutical, cosmetic and chemical industries. In this study, we propose the use of microfluidizer known as high pressure homogenizer to prepare lipid nanoemulsion as a potent cosmetic delivery carrier. The lipid nanoemulsions were prepared by O/W emulsion with hydrogenated lecithin and different type of oils. Effects of oil type on the stability of the lipid nanoemulsion were investigated with Dynamic Light Scattering (DLS) and Zeta-potential. Arbutin was used as model drug for transdermal administration through hairless mouse skin. Transdermal arbutin delivery using the lipid nanoemulsions was studied with HPLC method.

• Bulletin of the Korean Chemical Society
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• v.31 no.7
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• pp.1825-1826
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• 2010

• Proceedings of the SCSK Conference
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• 2003.09a
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• pp.719-732
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• 2003

A kojic acid derivative, kojic acid 7-O-$\beta$-D-tetraacetylglucopyranoside(KTG) was synthesized. Regio-and stereo-selective glycosylation at 7-postion in kojic acid with $\beta$-D-pentaacetylglucose was achieved with high yield(80％) by the use of Lewis acid and organic base in nonpolar solvent. KTG was hydrolyzed in methanol by the aid of sodium methoxide to give kojic acid 7-O-$\beta$-D-glucopyranoside(KGP). KGP is freely soluble in water and soluble in methanol and ethanol. Its structure was comfirmed by $^1$H-NMR and $^{13}$ C-NMR. Tyrosinase activity inhibition of KGP was measured with mushroom tyrosinase compared with ascorbic acid, kojic acid and arbutin. KGP showed higher tyrosinase inhibition activity($IC_{50}$/=33.3 $\mu\textrm{g}$/ml) than ascorbic acid(63.2 $\mu\textrm{g}$/ml) and arbutin(91.8 $\mu\textrm{g}$/ml) but lower inhibition activity than kojic acid(8.3 $\mu\textrm{g}$/ml). To test free-radical scavenging activity, we used 1, 1-diphenyl-2-picrylhydrazyl(DPPH) as a free-radical source. Free-radical scavenging activity of KGP was very low($SC_{50}$/>1000 $\mu\textrm{g}$/ml) compared with ascorbic acid($SC_{50}$/=2.68 $\mu\textrm{g}$/ml) and arbutin($SC_{50}$/=180$\mu\textrm{g}$/ml). Melanin formation inhibition of KGP was measured in B16 melanoma, compared with kojic acid, arbutin and Vitamin C. Inhibition activity of KGP for melanin formation was not found within test concentrations.

• Journal of Mushroom
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• v.11 no.2
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• pp.99-106
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• 2013

This study was initiated to investigate the skin whitening activities of methanol extracts from fruiting bodies of I. obliquus. The total polyphenols and flavonoids contents of I. obliquus methanol extracts were 31.85 mg/g and 28.33 mg/g, respectively. The methanol extract of the mushroom treated on B16/F10 melanoma and NIH3T3 cell lines did not show cytotoxic activity. 2,2-diphenyl-1-picrylhydrazyl(DPPH) free radical scavenging activity and chelating activity on ferrous ions of I. obliquus methanol extract were lower than those of positive control, tocopherol and BHT. The tyrosinase and L-DOPA inhibitory activities of the extract were lower than those of positive control, kojic acid and ascorbic acid. The tyrosinase and melanin synthesis inhibitory activities of the melanoma cells treated with the extract were comparable with positive control, arbutin. The experimental results suggested that methanol extract of I. obliquus contained inhibitory activities of tyrosinase and melanin synthesis in the B16/F10 melanoma cells by dose dependent manner. High ultra-violet absorption spectra in the range of 280-350 nm showed that I. obliquus extract could protect skin from UV radiation damage. Therefore, fruiting bodies of I. obliquus can be used for developing skin whitening, anti-UV and skin care agents.

• Archives of Pharmacal Research
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• v.29 no.12
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• pp.1187-1192
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• 2006

The aims of this study were to encapsulate arbutin (AR) in liposome to enhance the skin-whitening activity, and to investigate the effect of liposome formulation on the entrapment efficiency (EE%), skin permeation rate and skin deposition. The liposomes were prepared by a film dispersion method with several different formulations and were separated from the solution by using the gel-filtration method. The physical (size distribution, morphology) and chemical (drug entrapment efficiency, hairless mouse skin permeation and deposition) properties of liposomes were characterized. The entrapment efficiency in all liposome formulations varied between 4.35% and 17.63%, and was dependent on the lipid content. The particle sizes of liposomes were in the range of $179.9{\sim}212.8\;nm$ in all liposome formulations. Although the permeation rate of AR in the liposome formulations decreased compared with AR solution, the deposition amount of AR in the epidermis/dermis layers increased in AR liposomal formulation. These results suggest that liposomal formulation could enhance the skin deposition of hydrophilic skin-whitening agents, thereby enhancing their activities.