• Bulletin of the Korean Chemical Society
• /
• v.33 no.1
• /
• pp.149-152
• /
• 2012

The (S)-(+)-decursin and its analogues are reported as potent inhibitors of melanin production in B16 murine melanoma cells. In order to understand the factors responsible for potency as well as inhibition of potency of (S)-(+)-decursin and its analogues, three-dimensional quantitative structure-activity relationship (3D-QSAR) studies were performed. Since receptor structures are not available, a pharmacophore model was constructed. Using PHASE, we generated 3 different models and selected the seven-site model, which returned excellent statistical values ($r^2$ = 0.9127, $Q^2$ = 0.6878, Pearson-R = 0.9014). Using the generated pharmacophore model, we screened a natural products library and obtained 4'-epi-decursin as the most related compound. 4'-epidecursin is similar to (S)-(+)-decursin, but shows additional interaction possibilities with tyrosinase. The study thus sheds some light on possibility of developing more potent tyrosinase inhibitors.

• Korean Journal of Pharmacognosy
• /
• v.45 no.3
• /
• pp.262-267
• /
• 2014

Royal jelly composes of many components, especially protein. Protein is a major factor which cause allergy. We focused on water soluble royal jelly (WSRJ) that was removed allergy - inducing protein. 10-hyroxy-2-decenoic acid content of WSRJ is 2.42 g/100 g, which is double compared to that of lypophilized RJ. To further access WSRJ as a cosmetic ingredient and potential external treatment for topical use, we investigated its ability to inhibit tyrosinase activity and melanin biosynthesis on melanogenesis in B16F1 melanoma cells. We found that WSRJ increased the cell viability in B16F1 melanoma cell and WSRJ (1~10 mg/ml) inhibited melanin synthesis in with 10 nM ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH) for 48 h. WSRJ inhibited direct tyrosinase activity, which decreased melanin synthesis in ${\alpha}$-MSH stimulated B16F1 melanoma cells. Thease findings suggest that WSRJ induces the down regulation of melanogenesis by inhibiting tyrosinase activation.

• Proceedings of the Plant Resources Society of Korea Conference
• /
• 2023.04a
• /
• pp.56-56
• /
• 2023

The cone of Pinus rigida × Pinus taeda (PRT), a plant in the Pinaceae family, has long been used in traditional medicine to treat hemostasis, bruises, and burns. Previous research has shown that regulating oxidation-reduction reactions in reactive oxygen species can help inhibit melanogenesis, the process of melanin synthesis, which is a common target for addressing hyperpigmentation. Inhibiting tyrosinase is also known to be effective in this regard. Based on these findings, we conducted an investigation into the inhibitory effect of the ethyl acetate fraction of PRT (ERT) on melanogenesis in B16 F10 cells. We know that the expression levels of melanin biosynthesis-related proteins, including tyrosinase, TRP-1, and TRP-2, are regulated by MITF (microphthalmia-associated transcription factor) and cAMP, with cAMP affecting the activity of protein kinase A (PKA). PKA can reduce melanogenesis, and CREB reduces the phosphorylation of melanin-producing enzymes. In addition, the MAPK signaling pathway, composed of ERK, JNK, p38, and other factors, is also known to play a role in the inhibition of melanogenesis in melanocytes. Our immunoblotting results showed that ERT inhibited the expression of melanin production-related proteins (tyrosinase, TRP-1, TRP-2, and MITF) that were significantly increased by a-MSH treatment to promote melanin production. Furthermore, the phosphorylation levels of factors related to cAMP/PKA/CREB and MAPK signaling pathways were significantly reduced without affecting the total form. In conclusion, we believe that treatment with ERT can inhibit melanin synthesis by modulating the phosphorylation of cAMP/PKA/CREB and MAPK signaling pathways at the cellular level. These findings suggest the potential of ERT as a raw material for functional cosmetics and pharmaceuticals, thanks to its antioxidant activity and ability to inhibit melanogenesis. We thought that these findings of ERT as a natural plant resource will inspire further research and development in this area.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.33 no.2
• /
• pp.87-92
• /
• 2007

To develop the skin whitening agent, we investigated the effects of Acanthopeltis japonica, a rhodophyta on the coast of Jeju island, on melanogenesis. Dried A. japonica was refluxed with 70 % aqueous ethanol and the extract was evaporated to dryness. To validate the activity as a depigmenting agent, various in vitro tests, polyphenol contents, and free radical scavenging activity were performed. In addition, cellular tyrosinase activity and protein expression of p-ERT, tyrosinase, TRP-1, and TRP-2 were measured in B16/F10 murine melanoma cells. A. japonica had low polyphenol contents and low free radicals scavenging activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. A. japonica suppressed cellular tyrosinase activity up to 86.9 % at $100{\mu}g/mL$ with inhibition or tyrosinase and TRP-1 expression in ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH)-treated B16/F10 melanoma cells. Our results suggest that inhibitory effects of A. japonica on melanogenesis are due to inhibiting the pathways involving ${\alpha}$-MSH-induced ERK activation. Therefore, A. japonica nay be useful as a skin whitening agent associated with the suppressive effect of melanotrophin-induced signaling pathway to inhibit melanin synthesis.

• Journal of the Korean Applied Science and Technology
• /
• v.41 no.3
• /
• pp.756-770
• /
• 2024

This study confirmed emulsion stability after performing antioxidant, whitening, antibacterial, and anti-inflammatory efficacy evaluation to find out the availability of Sicyos angulatus L. (SA) which is designated as an ecological disturbance species as a functional cosmetic material. SA was extracted with Deionized Water (SAW) and 70% EtOH (SAE). Compared to SAW, SAE has excellent antioxidant efficacy by showing scavenging activity and SOD-like activity against DPPH radical and ABTS⁺ radical, and inhibits melanin production by inhibiting the activity of tyrosinase. SAW had no antibacterial effect on Escherichia coli (E.c), Staphylococcus epidermidis (S.e), Staphylococcus aureus (S.a), Pseudomonas aeruginosa (P.a), and Cutibacterium acnes (C.a) strains, while SAE showed antibacterial activity by producing clear zones in E.c, S.e, P.a, and C.a strains except S.a. In LPS-treated RAW 264.7 cells, SAE showed efficacy against anti-inflammatory by inhibiting the production of NO by inhibiting the expression of iNOS and COX-2 than SAW. It was confirmed that the SAE-added emulsion was not separated at temperatures of 4℃, 25℃, and 50℃, the pH and viscosity did not change significantly in numerical terms, and the particle size was similar to that of the control emulsion, so it did not affect the formulation. Based on these results, we suggest its potential as a new material for functional cosmetics research.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
• /
• v.31 no.3
• /
• pp.39-49
• /
• 2018

Objectives : This study is designed to clarify whitening, anti-inflammatory effect of fractions extracted from the mixture of Phaseolus radiatus L. and ethanol. Methods : In this experiment, we were intended to reveal whitening, anti-inflammatory effect of fractions extracted from the mixture of Phaseolus radiatus L. and ethanol. The whitening activity was confirmed by UV blocking activity, tyrosinase inhibiting activity, and melanin formation inhibiting activity. Anti-inflammatory activity is confirmed by measurement of cytotoxicity level by MTT assay and measurement of Cytokine expression, which is the main mediator of inflammation reaction. Results : As a results, overall activity was high in the ethyl acetate fraction. Tyrosinase inhibitory activity was less than 20% at all concentrations, but the activity to inhibit melanin self-production was higher than that of ethyl acetate fraction at $32.19{\pm}2.79%$ at $100{\mu}g/m{\ell}$. And ethyl acetate fraction had a relatively high UV blocking activity. In the anti-inflammatory test, the concentration-dependent activity was shown, and the chloroform and ethyl acetate fractions showed significant NO production inhibitory activity. Cytokine expression was superior to that of the final stage of B cell differentiation, and cell viability was over 80% except for the chloroform fraction at the concentration of $200{\mu}g/m{\ell}$. Conclusions : The results of this experiment confirmed the whitening effect and anti-inflammatory effect of Phaseolus radiatus L.'s extracts and fractions and report the possibility of application as external medicine.

• Applied Chemistry for Engineering
• /
• v.25 no.5
• /
• pp.468-473
• /
• 2014

Dendropanax morbifera (D. morbifera) grows in the southern coastal areas and on Jeju Island in Korea. In this study, D. morbifera leaf extract was investigated to determine the mechanism of its whitening effect. The inhibitory activities of the extract on melanogenesis were tested in B16 melanoma cells treated with the ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH). D. morbifera leaf extracts remarkably decreased the melanin content at 25 and $50{\mu}g/mL$. The extracts significantly inhibited the intracellular tyrosinase activity and protein expression of tyrosinase and tyrosinase related protein-2 (TRP-2). In conclusion, D. morbifera leaf extracts would show a whitening effect by inhibiting intracellular tyrosinase activities and the expression of enzymes directly involved in the melanin biosynthesis. The results indicate that fractions of D. morbifera leaf extracts show potential for application as a whitening agent in the new whitening cosmetics.

• Journal of Acupuncture Research
• /
• v.35 no.4
• /
• pp.182-186
• /
• 2018

Background: The purpose of this study was to investigate the effects of wild ginseng pharmacopuncture on melanin production in B16/F10 murine melanoma cells. Methods: To determine the effect of wild ginseng pharmacopuncture solution on B16/F10 cells, cytotoxicity was evaluated using the 3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyl-tetrazolium bromide (MTT) method. To observe B16/F10 cell growth, death, and morphological changes, Trypan blue solution was used. The Hosoi method was used to investigate the effect of wild ginseng pharmacopuncture solution on melanin production. The Martinez-Esparza method was used to investigate the effect of wild ginseng pharmacopuncture solution on tyrosinase activity. To determine the pathway involved in the melanogenesis in cells exposed to wild ginseng pharmacopuncture solution, a cell-free tyrosinase was used. Results: Following treatment with $200{\mu}L$ of wild ginseng solution, the cell survival rate was $76.32{\pm}2.45%$ which significantly decreased with higher concentrations (${\mu}L$) of wild ginseng (up to $200{\mu}L$). When $100{\mu}L$ of wild ginseng was used, the cell survival rate was $89.95{\pm}2.07%$. No morphological changes or abnormalities were observed in the B16/F10 murine melanoma cells as observed in the Trypan blue test. Melanin production was significantly reduced to $72.17{\pm}3.74%$ at $100{\mu}L$. Using $100{\mu}L$ of wild ginseng solution, tyrosinase activity was significantly decreased to $80.15{\pm}1.05%$. Wild ginseng pharmacopuncture solution reduced melanin production both directly and indirectly. Conclusion: This study suggests that wild ginseng pharmacopuncture solution may be effective in inhibiting melanin production. Further studies are needed to determine safe and effective clinical applications.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.20 no.5
• /
• pp.1271-1274
• /
• 2006

We investigated the effects of aqueous extracts from twelve medical herbs on ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH)-induced melanogenesis in B16F10 mouse melanoma cell. The cells were incubated with ${\alpha}$-MSH and aqueous extracts 5 days and 2 days and then analysed melanin amount and tyrosinase activities, respectively. Nine aqueous extract of herbs examined at 1 mg/m${\ell}$ level decreased melanin synthesis in B16F10 cell, especially in Agastache rugosa, Leonurus siviricus and Murus bombycis. The significant decrease of released extracellular melanin were also observed in treated cells with aqueous extract from Leonurus siviricus, Murus bombycis and Ledebouriella seseioides. The ${\alpha}$-MSH-induced activation of tyrosinase was inhibited in cells treated with aqueous extract from Cuscutae semen, Angelica tenuissima and Agastache rugosa. These results suggest that herbs inhibiting melanogenesis through tyrosinase activity may apply to develop whitening drugs and cosmetics.

• Food Science and Preservation
• /
• v.19 no.6
• /
• pp.946-950
• /
• 2012

The antioxidant activity and whitening effect of the distilled water (DW) and ethanol extracts of the Prunus persica flower and calyx were studied. In the oxygen radical absorption capacity (ORAC) assay for antioxidant activity measurement, it was confirmed that the flower extract was stronger than the calyx extract, and that the ethanol extract was relatively stronger than the DW extract. To define the whitening effect, an experiment was conducted involving tyrosinase inhibitory assay and measurement of the melanin content of B16F10. As a result of the use of tyrosinase, the DW extract of calyx showed 53% inhibition as the highest activity. The melanin content inhibitory rates were defined as 57% for the ethanol flower extract and 63% of the ethanol calyx extract, based on a $10{\mu}g/mL$ concentration. Based on these results, mixture with the whitening effect in the extract of P. persica and another compounds should be researched for development as a cosmetic ingredient.