• Journal of Pharmaceutical Investigation
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• 제39권2호
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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.

• 대한화장품학회지
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• 제29권1호
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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.

• 대한방사성의약품학회지
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• 제3권2호
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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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• 제20권2호
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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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• 제22권3호
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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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• 제36권5호
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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.

• 대한화장품학회지
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• 제30권3호
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• pp.415-418
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• 2004

알부틴은 glycosylated hydroquinone으로 여러 식물들에서, 고농도로 발견되며 비교적 안정한 물질이다. 이는 멜라닌화를 억제하는 작용이 있는 것으로 보고되어 있고, 베타-글루코시다제에 의해 포도당과 hydroquinone으로 쉽게 가수분해된다. Hydroquinone 역시 우수한 항멜라닌화 작용을 가지나, 여러 가지 부작용들로 인해 그 사용이 제한적이거나 주의를 요한다. 이 연구는 알부틴과 베타-글루코시다제를 포함하는 미백 화장품이 자외선 조사로 유도된 색소 침착을 억제하는 효과를 알아보고자 하였다. 대상은 10명의 건강한 성인으로 등 부위에 자외선 B를 조사하여 색소 침착 병변을 만들었고 이 병변들은 세 그룹: 알부틴과 베타-글루코시다제를 함유하는 미백 화장품 도포군, vehicle 대조군, no-application 대조군으로 나누었다. 알부틴과 베타-글주코시다제를 함유하는 미백 화장품 도포군은 no-application 대조군에 비교하여 색소 침착을 $50.17\%$ 억제하였다(N = 10:P<0.05). 따라서 알부틴과 베타-글루코시다제를 함유하는 미백 화장품이 기미 등 자외선 조사로 유도되거나 악화되는 과색소성 질환에 효과적으로 사용될 수 있겠다.

• Natural Product Sciences
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• 제5권1호
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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.

• 대한화장품학회:학술대회논문집
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• 대한화장품학회 2003년도 IFSCC Conference Proceeding Book II
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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.

• 한국응용곤충학회지
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• 제7권
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• pp.61-64
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• 1969

배나무 적성병균의 병자각세대에 분필하는 병자적 성분중 free sugar를 중심으로 기생엽중의 free sugar와의 상관관계를 생화학적으로 연구 고찰하여 아래와 같은 결과를 얻었다. 1. 병자각세대에 분필하는 병자적 성분중 free sugar를 paper chrmarography로 분석한 결과 fructose만이 확인되었다. 2. 기주 향나무 엽중의 free sugar는 galactose와 glucose 및 미지물질 2종임을 확인하였다. 3. 기주 배나무엽중의 free sugar로는 glucose, fructose 및 galactose를 확인하였다. 4. 배나무엽중의 arbutin-을 결정화하고 그 구조를 일반적인 방법과 paper chromatography로 분석하여 glucose와 hydroquinone의 결합체임을 확인하였다. 5. 0.05M arbutin 용액에 Emulsin을 조제하여 배양한 결과 분해 생성물로서 glucose를 확인하였고 이들 Emulsin은 모두 $\beta-glycosidase$를 함유하고 있음이 확정되었다. 이상 결과에서 보는 바와같이 병자적중의 fructose는 배나무 엽중에 있는 free sugar 및 glycoside인 arbutin이 Emulsin에 의하여 분해되어 glucose로 변화된 다음 균체내의 isomerase에 의하여 isomerization된 것이라 추측된다.