• Korean Journal of Medicinal Crop Science
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• v.17 no.2
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• pp.83-89
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• 2009

This study was performed to improve antioxidant activities and skin-whitening effects of Rubus coreanus Miquel extracts by nano-encapsulation. R. coreanus was extracted at $60^{\circ}C$ and encapsulated by lecithin and gelagine. Nano-encapsulated extracts showed highest free radical scavengering effect as 97.62% in adding sample ($500\;{\mu}g/m{\ell}$), compared to the extracts from conventional processes. It was showed strong inhibition effect on melanin production test by Clone M-3 cells as 55.23%. High inhibitory potency on tyrosinase was also measured as 155.8% by adding nano-sample of 1 $mg/m{\ell}$. The improvement of biological activity was demonstrated by real time confocal microscope. We could consider that the water soluble extracts of R. coreanus could be definitely enhanced by nano-encapsulated as a potent natural resources for antioxidant and skin-whitening agent.

• The Korean Journal of Physiology and Pharmacology
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• v.18 no.3
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• pp.249-254
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• 2014

The purpose of this study is to characterize the effects of KHG26792 (3-(naphthalen-2-yl(propoxy)methyl)azetidine hydrochloride), a potential skin whitening agent, on melanin synthesis and identify the underlying mechanism of action. Our data showed that KHG26792 significantly reduced melanin synthesis in a dose-dependent manner. Additionally, KHG26792 downregulated microphthalmia-associated transcription factor (MITF) and tyrosinase, the rate-limiting enzyme in melanogenesis, although tyrosinase was not inhibited directly. KHG26792 activated extracellular signal-regulated kinase (ERK), whereas an ERK pathway inhibitor, PD98059, rescued KHG26792-induced hypopigmentation. These results suggest that KHG26792 decreases melanin production via ERK activation. Moreover, the hypopigmentary effects of KHG26792 were confirmed in a pigmented skin equivalent model using Cervi cornus Colla (deer antler glue), in which the color of the pigmented artificial skin became lighter after treatment with KHG26792. In summary, our findings suggest that KHG26792 is a novel skin whitening agent.

• Bulletin of the Korean Chemical Society
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• v.34 no.10
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• pp.3017-3021
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• 2013

Coumaroyl dipeptide amide, Coumaric acid-LG-$NH_2$, was prepared successfully using the solid-phase method, and its efficacy as a skin whitening agent was studied. Coumaric acid-LG-$NH_2$ was prepared with Rink-amide resin, and 96.354% of purity was obtained. Using MTT assay and LDH release assay, we found that it exhibited very low cytotoxicity. And, we found that Coumaric acid-LG-$NH_2$ inhibited tyrosinase activity dose-dependently and showed superior tyrosinase inhibitory activity to well-known whitening agent, arbutin. $IC_{50}$ value of Coumaric acid-LG-$NH_2$ was 182.4 ${\mu}M$, and $IC_{50}$ value of arbutin was 384.6 ${\mu}M$. Also, in measurement of melanin contents using B16F1 melanoma cell lines, Coumaric acid-LG-$NH_2$ reduced melanin production induced by ${\alpha}$-MSH statistically significant, and showed superior melanin inhibitory activity to p-coumaric acid or arbutin. In addition, Coumaric acid-LG-$NH_2$ reduced MC1R mRNA expression level. Thus, we concluded that MC1R pathway is the significant pathway of Coumaric acid-LG-$NH_2$, and Coumaric acid-LG-$NH_2$ has great potential to be used as novel whitening agents.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.24 no.3
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• pp.45-50
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• 1998

13 develop an active agent for skin whitening, we examined the inhibitory effects of 285 plant extracts on tyrosinase activity and found some plant extracts have an ability to inhibit tyrosinase activity. Of these plant extracts, ramulus mori extracts showed the highest inhibiting activity on enzyme activity. From these results, we selected ramulus mori as a new active agent for skin whitening. $IC_{50}$/ of this extracts on tyrosinase activity is 12.48$\mu\textrm{g}$/m1. Also, ramulus mori extracts showed inhibitory activity on melanin synthesis in B-16 melanoma cells. We isolated active compound from ramulus mori extracts using various column chromatography and recrystalization and identified its chemical structure using Mass spectroscopy, IR and NMR analysis. So, it is identified as Mulberrin, a maior compound of ramutus mori and turned out that it has potent ability on tyrosinase inhibition. $IC_{50}$/ of this compound for tyrosinase activity is 0.5$\mu\textrm{g}$/ml. Also, this compound showed potent inhibitory activity on melanin synthesis in B-16 melanoma cells. This extracts was turned out to be safe in many safety tests.

• Biomedical Science Letters
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• v.13 no.4
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• pp.313-317
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• 2007

Melanogenesis refers to the biosynthesis of melanin pigment in melanocytes. Melanogenesis is controlled by the intra- and extracellular environments. In the present study, to develop a new whitening agent, it was investigated the antioxidant activity and the inhibitory effect of Ailanthi Radicis Cortex extract on tyrosinase activity and on melanogenesis in the B16/F1 melanoma cells. The inhibition ratio of tyrosinase activity of ethylacetate fraction from Ailanthi Radicis Cortex was higher than that of arbutin. The ethylacetate fraction showed scavenging activities of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and superoxide anion radicals in a dose dependent manner. The highest inhibitory activity of melanogenesis was also in ethylacetate fraction ($40.0{\pm}5%$ at the concentration of $400{\mu}g/ml$). This study demonstrates that the Ailanthi Radicis Cortex extract might be used to be a potential agent for skin whitening.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.22 no.2
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• pp.82-91
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• 2009

Objectives : The purpose of this study is to investigate whitening effects and anti-wrinkle effects of a few 80% ethanol extracted herbal medicines. Methods : In the first study, a few 80% ethanol extracted herbal medicines were screened for their inhibitory activities against the tyrosinase. In the second study, a few 80% ethanol extracted herbal medicines were screened for their inhibitory activities against elastase. Results : 1. We showed 28%, 27% and 19% inhibitions of mushroom tyrosinase at 500 $\mu$g/ml concentration of ASR, AIF and ABR extracts and they were showed higher anti-tyrosinase activity than arbutin's. We also could observe that the decreased mushroom tyrosinase activities in RR, CML, LR, AGR and TH extracts. 2. RR, AF and ABR (final concentrstion 1 mg/ml) were appeared 60%, 98%, 83% of inhibitions of elastase activity, and they were showed higher anti-elastase activity than that of ursolic acid. We also could observe that the decreased elastase activities in AIF, AR, LR and CML extracts. Conclusions : These results suggest that ASR, AIF and ABR extracts contribute to the anti-melanin activities and represent potential sources of whitening agent, and RR, AF and ABR extracts contribute to the anti-elastase activities and represent potential sources of anti-wrinkle agent. These results suggest that some herbal medicines could be strong potential sources of inhibition about anti-aging and whitening effects for the skin.

• Journal of the Korean Applied Science and Technology
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• v.28 no.2
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• pp.161-169
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• 2011

To develope new natural substances for whitening agent, Baeckji(Angelica dahuria;BK), Seasin(Asarum sieboldii;SS). Baecjgangjam(Bombycis corpus;BGJ) and Mynkanbang(MKB) were selected and extracted by hot water and 70% EtOH, respectively. Hydrothermal and ethanolic extracts of BK, SS, BGJ and MKB were evaluated for anti-oxidative effect, tyrosinase activity, melanogenesis of B16 melanoma cells and changes in level of tyrosinase expression by using Western blotting. All hydrothermal and ethanolic extracts showed scavenging activities of free radicals against 1,1-diphenyl-2-picrylhydrazyl(DPPH) but no inhibitory effect on tyrosinase activity. Ethanolic extracts of BK, SS, and BGJ and especially highly, those of MKB inhibited production of melanin in B16 melanoma cells and were able to reduce the level of tyrosinase expression in B16 melanoma cells. These results suggest that ethanolic extracts of BK, SS, BGJ and MKB can be an effective whitening agent from natural plant.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.42 no.1
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• pp.29-35
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• 2016

RS White (resorcinol bis-ethylhexanoate) is used in cosmetics as a skin whitening agent. In this study, we studied the possibility of nano-emulsion formation containing whitening agent, RS White, with different types of emulsifying agents. With Tween 80, 60, HCO 60 and 40 as a hydrophilic surfactants and Span 80 as ahydrophilic surfactant, nano-emulsions were formed at appropriate concentrations, but they were not formed in the system using the Myrj 52, Montanov L, and Tegocare 450 with Span 80. The diameter of nano-emulsion sphere was smaller than 100 nm. The emulsion showed a translucent appearance and maintained stability in stability evaluation with time. In vitro skin permeation experiments showed that amounts of skin permeated nano-emulsion for 24 h were $70.84{\mu}g/cm^2$ and those of O/W emulsion were $28.97{\mu}g/cm^2$. In conclusion, a stable nano-emulsion containing the resorcinol bis-ethylhexanoate is effective for potential efficacy system as an efficient delivery system of the functional materials into skin.

• Journal of the Korean Applied Science and Technology
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• v.38 no.3
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• pp.651-661
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• 2021

Eruca sativa, called arugula, is a perennial plant in the Brassicaceae family, an edible plant commonly used in Italian cuisine. To study as a cosmetic material application E. sativa was extracted with 70% ethanol (ES). Then ES was fractionated using n-hexane, chloroform, ethyl acetate, n-butyl alcohol and water (EHex, EEA, ECHCl₃, EBuOH and EDW). EEA showed mushroom tyrosinase inhibitory activity. ES, EEA and EBuOH showed inhibition of tyrosinase activity. As a result, ES is expected to have skin whitening efficacy. ES was applied to 0.05, 0.1% the toner and emulsion formulation to test the stability. The anti-microbial activity of eight bacteria and fungi including Staphylococcus aureus and Propionibacterium acnes which cause dermatitis and acne was evaluated. EEA showed effects in all of microorganisms. The toner and emulsion containing ES with 0.05, 0.1% were passed in the challenge test. At -20, 4, 25, 55 ℃ and daylight, there was no significant change on pH, viscosity for 4 months. However, emulsions had phase separation phenomenon at 55 ℃, so the base formulation needs improvement. In addition, through the skin penetration test, EEA penetrated 0.058% in 6 hr, predicting the clinical efficacy. This means that E. sativa can contribute whitening agent and the synergistic effect of preservatives.

• 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.