• Journal of Pharmaceutical Investigation
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• v.39 no.2
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• pp.121-125
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• 2009

The objective of this study was to investigate the feasibility of applying the Intense Pulsed Light (IPL) as a tool to enhance the skin absorption of arbutin, a well-known skin-whitening agent. Arbutin solution or skin formulation was applied on the back of hairless mouse skin in vivo after IPL treatment, and then the skin deposition of arbutin was determined by HPLC. IPL treatment significantly increased the amount of arbutin in the skin after 6 hours when arbutin solution was applied 20 times. IPL also enhanced the skin deposition of arbutin when arbutin formulation was applied, although it was not significantly different. Significant increase of surface skin temperature was observed by IPL treatment, which might be a mechanism of the enhanced skin absorption of arbutin. These results suggest the feasibility of using IPL as a tool to increase the skin absorption of whitening agents, although further research needs to be conducted to understand its exact mechanism.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.29 no.1
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• pp.151-167
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• 2003

Melanin biosynthesis is a human defense mechanism to protect skin from UV irradiation and also determines colors of hair and skin. However, as a interest on skin-whitening increases, researches to prevent pigmentation and hypersynthesis of melanin in skin are being actively in progress. Active components used as a whitening agent in cosmeceuticals are kojic acid, arbutin, vitamin C and hydroquinone. However, until now, because comparison researches among them in the aspect of both melanin formation and cellular toxicity have not been performed, we can't exactly estimate merits and defects of them as a whitening agent. To this end, we performed experiments to compare their effects on cell viability and melanin formation. As a first step, in vitro tyrosinase inhibition assay was done. While kojic acid and hydroquinone showed strong inhibition activities(their IC$\_$50/s are all < 100uM), arbutin and vitamin C showed weak activities. IC$\_$50/s of arbutin and vitamin C are 100uM and 400∼500uM, respectively. In B16BL6 melanoma cells, like in vitro tyrosinase inhibition assay, arbutin and kojic acid showed more strong inhibition effect on melanin synthesis than vitamin C. And unlike arbutin, vitamin C and kojic acid induced cell death at high concentration. Although arbutin showed no cytotoxicity, it has side effect to induce morphological change at high concentration.. In this paper, we suggest both kojic acid and arbutin have stronger ability to inhibit melanogenesis than vitamin C. And they also have side effect, that is, kojic acid induces cell death like vitamin C and arbutin changes cell morphology respectively.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.72-79
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• 2017

Arbutin is a hydroquinone derivative with a glucose moiety. As a tyrosinase inhibitor, it is widely used as a skin-whitening cosmetic agent for the treatment of cutaneous hyperpigmentary disorders, such as melasma and freckles. In the medical field, many studies have addressed the use of arbutin in various tumors, but the mechanism for tumor uptake of arbutin is still unclear. In this paper, we radiolabeled arbutin using radioiodine and studied its pharmacokinetics and tumor uptake via biodistribution experiments and single-photon emission computed tomography (SPECT) imaging. Radiolabeled $^{131}I-arbutin$ was stable for up to 24 h in PBS and serum. Biodistribution studies and SPECT imaging indicated high uptake of the compound in the bladder and kidneys shortly after injection. Twenty-four hours post-injection, significant deiodination was observed. Apart from high thyroid uptake, selective tumor uptake was clearly observed. The tumor-to-muscle and tumor-to-blood ratios were 26 and 9, respectively.

• Biomolecules & Therapeutics
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• v.20 no.2
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• pp.196-200
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• 2012

Role of metabolism by intestinal bacteria in arbutin-induced immunotoxicity was investigated in splenocyte cultures. Following an incubation of arbutin with 5 different intestinal bacteria for 24 hr, its aglycone hydroquinone could be produced and detected in the bacterial culture media with different amounts. Toxic effects of activated arbutin by intestinal bacteria on lymphoproliferative response were tested in splenocyte cultures from normal mice. Lipopolysaccharide and concanavalin A were used as mitogens for B- and T-cells, respectively. When bacteria cultured medium with arbutin was treated into the splenocytes for 3 days, the medium cultured with bacteria producing large amounts of hydroquinone induced suppression of lymphoproliferative responses, indicating that metabolic activation by intestinal bacteria might be required in arbutin-induced toxicity. The results indicated that the present testing system might be applied for determining the possible role of metabolism by intestinal bacteria in certain chemical-induced immunotoxicity in animal cell cultures.

• Archives of Pharmacal Research
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• v.22 no.3
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• pp.232-236
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• 1999

In this study, we present evidence that cotreatment of aloesin and arbutin inhibits tyrosinase activity in a synergistic manner by acting through a different action mechanism. Aloesin or arbutin similarly inhibited enzyme activity of human- and mushroom-tyrosinases with an IC50 value of 0.1 or 0.04 mM, respectively. Lineweaver-Burk plots of the enzyme kinetics data showed that aloesin inhibited tyrosinase activity noncompetitively with a Ki value of 5.3 mM, whereas arbutin did it competitively (Maeda, 1996). We then examined whether cotreatment of these agents inhibits the tyrosinase activity in a synergistic manner. The results showed that 0.01 mM aloesin in the presence of 0.03 mM arbutin inhibited activity of mushroom by 80% of the control value and the reverse was also true. The inhibitory effects were calculated to be synergistic according to the B rgi method. Taken together, we suggest that aloesin along with arbutin inhibits in synergy melanin production by combined mechanisms of noncompetitive and competitive inhibitions of tyrosinase activity.

• Journal of Pharmaceutical Investigation
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• v.36 no.5
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• pp.299-304
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• 2006

The aim of this study was to investigate the effect of deformable liposomes with sodium cholate on the skin permeation and skin deposition of arbutin, a hydrophilic skin-whitening agent. Various compositions of liposomes were prepared by the extrusion method. Particle size distribution and entrapment efficiency were determined by the laser light scattering and the gel permeation chromatography, respectively. The in vitro rat skin permeation and deposition of arbutin in various skin layers were investigated using the Keshary-Chien diffusion cells at $37^{\circ}C$. The average particle size of the deformable liposomes ranged from 217.4 to 117.4 nm, depending on the composition. The entrapment efficiency was dependent on surfactant concentration and loading dose of arbutin. The permeation rate of 5% arbutin in deformable liposomes was $8.91({\pm}1.33){\mu}g/cm^2/h$, and was not significantly different from 5% arbutin aqueous solution $[9.82({\m}0.86){\mu}g/cm^2/h]$. The deposition of arbutin was $43.34({\pm}12.13)$ and $16.99({\pm}7.83){\mu}g/cm^2$ in stratum corneum layer and epidermis/dermis layer, respectively, after 12 h of permeation study. These results are consistent with several earlier studies for the localization effect of liposomal formulations in stratum corneum, and demonstrated the feasibility of the deformable liposomes as a promising carrier for the skin deposition of hydrophilic skin-whitening compounds.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.3 s.47
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• pp.415-418
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• 2004

Arbutin is a glycosylated hydroquinone found at high concentration in certain plants capable of surviving extreme and sustained dehydration. It has been reported to have an inhibitory effect of melanogenesis and to be hydrolyzed easily to yield glucose and hydroquinone by ${\beta}-glucosidase.$ While hydroquinone also has an anti-melanogenic effect, however, is carefully used as a topical whitening agent because of side effects. The present study was undertaken to examine the inhibitory effect of an whitening agent containing arbutin and ${\beta}-glucosidase$ on UV radiation induced pigmentation in human skin. Experimental subjects were UVB-irradiated on the back. UVB-irradiated areas were assigned to three groups: arbutin and ${\beta}-glucosidase$ treated group, vehicle control, and no-application control. Arbutin and ${\beta}-glucosidase$ treatment inhibited pigmentation by 50.17 percent, compared with the controls (N : 10: P<0.05). These results suggest that the whitening agent containing arbutin and ${\beta}-glucosidase$may be used as an agent to inhibit melanin formation induced by UV radiation.

• Natural Product Sciences
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• v.5 no.1
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• pp.60-63
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• 1999

From the leaves of Vaccinium koreanum, isoquercitrin, quercetin, avicularin, 2'-O-caffeoyl-arbutin and arbutin were isolated and their structures were elucidated by spectral data.

• Proceedings of the SCSK Conference
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• 2003.09b
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• pp.163-173
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• 2003

Research objective:To exactly evaluate their functions of kojic acid, arbutin and vitamin C as a whitening agent, we performed experiments to compare their abilities to inhibit melanin synthesis. Experimental methods and techniques: The effects of kojic acid, arbutin and vitamin C on cell viability and melanin synthesis were evaluated by the level of melanin content and the number of viable cells upon treatment of them.

• Korean journal of applied entomology
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• v.7
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• pp.61-64
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• 1969

By way of paper chromatography, free sugars in pycnial drops of Gymnosporangium haraeanum Sydow were investigated in regard of their biochemical interrelation with free sugars of Chinese juniper and pear leaf. The free sugar in pycnial drops of Gynnosporangium haraeanum Sydow were identified to only Fructose spot. Free sugars in Chinese juniper leaf were identified to Glucose. Galactose and two unknown spots. Free sugars of another sample in pear leaf were identified to spots of Glucose, Furctose and Galactose. The Arbutin from pear leaf was crystalized and its structure was identified to Glucose and Hydroquinone. The acetone powder of Emulsin was incubated for 1 hour at $40^{\circ}C$ with 0.05 M Arbutin substrate in test tube and purified by general method with the purpose of analysis of its. metabolic products. And the paper chromatographic analysis showed it to be Glucose spot. From the above results, this Fructose in pycinal drops of Gymnosporangium haraeanum Sydow is presumed to be the exchangeable from free sugars in pear leaf or to be the hydrolyzed of $\beta-glycoside$ (Arbutin)-the metabolic isomerization of Glucose into Fructose by pycnia isomerase.