• Biomolecules & Therapeutics
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• v.31 no.4
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• pp.466-472
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• 2023

Exon skipping is an efficient technique to inhibit specific gene expression induced by a short-sequence peptide nucleic acid (PNA). To date, there has been no study on the effects of PNA on skin pigmentation. In melanocytes, the tripartite complex is responsible for the transport of mature melanosomes from the nucleus to the dendrites. The tripartite complex is composed of Rab27a, Mlph (Melanophilin), and Myosin Va. Defects in the protein Mlph, a melanosome transport-related protein, are known to cause hypopigmentation. Our study shows that Olipass peptide nucleic acid (OPNA), a cell membrane-permeable PNA, targets exon skipping in the Mlph SHD domain, which is involved in Rab27a binding. Our findings demonstrate that OPNA induced exon skipping in melan-a cells, resulting in shortened Mlph mRNA, reduced Mlph protein levels, and melanosome aggregation, as observed by microscopy. Therefore, OPNA inhibits the expression of Mlph by inducing exon skipping within the gene. These results suggest that OPNA, which targets Mlph, may be a potential new whitening agent to inhibit melanosome movement.

• Journal of Applied Biological Chemistry
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• v.61 no.3
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• pp.267-273
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• 2018

Matricaria chamomilla L. has been used as a bath agent in Europe because of its sterilization effect on the skin. Flowers contain terpenes, flavonoids are effective in relieving inflammation. Matricaria chamomilla L. has been reported to have various drug efficacies such as sedation, anti-diabetic effect and anti-arthritic effect, but there is little research on the scientific efficacy of whitening effect. The purpose of this study was to examine the whitening effect of Matricaria chamomilla L. extract and to investigate the mechanism of inhibition of melanogenesis. The extracts were used to determine tyrosinase inhibitory activity. The tyrosinase inhibitory activity of extracts was ineffective for water extract but in 60% ethanol extract was shown in a concentration-dependent manner. B16F10 melanoma cell was measured using a powder obtained by lyophilization of 60% ethanol extract. The toxicity was observed at a concentration of $75{\mu}g/mL$. And concentration range was selected to be at most $50{\mu}g/mL$. The effect of tyrosinase, MITF, TRP-1 and TRP-2 on the expression of melanin protein was investigated in melanoma cells of B16F10 melanoma cells. As a result, it was confirmed that as the concentration of the extract increased, the melanogenesis level decreased and the protein expression level also decreased in a concentration dependent manner. Therefore, it was concluded that Matricaria chamomilla L. extract inhibited melanogenesis in cells. Based on the above results, it is expected that it will be used as a useful basic data for industrialization of whitening functional food of Matricaria chamomilla L.

• Journal of Life Science
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• v.31 no.11
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• pp.1004-1009
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• 2021

Angelica gigas Nakai (AGN) has been used in Korean herbal medicine for various pharmacological activities, such as to create antioxidant and skin whitening effects. Decursin and decursinol angelate of AGN extracts can be used as potential active drugs and cosmetic ingredients. This study investigated the possibility of topical delivery of AGN extracts using a manufactured emulsion system. Lotion was formulated by using Tefose^® and paraffin for the oil phase, Kolliphor RH 40 for the surfactant and solubilizing agent-which showed high solubility in water (0.82 mg/ml)-and a water phase with a carbomer. In vitro skin permeation of decursin and decursinol angelate was determined using a Strat-M^® membrane in Franz diffusion cells. Lotion samples as the experimental group (248.08±19.72 ug/cm²) significantly increased the permeation of decursin and decursinol angelate for up to 24 hr compared to the control group (119.18±19.23 ug/cm²). The permeability was also characterized by the flux (penetration rates) and Kp (permeability coefficient) values. The experimental group (17.20±1.23 ug/h/cm² and 5.73±1.39 cm/h^*10^-3) had higher flux and Kp than the control group (8.22±1.24 ug/h/cm² and 2.74±0.51 cm/h^*10^-3). Lotion with decursin and decursinol angelate of AGN extracts could be used for the topical application of drug and cosmetic products.

• Journal of Embryo Transfer
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• v.28 no.3
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• pp.243-250
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• 2013

Pyracantha is a genus of thorny evergreen large shrubs in the family of Rosaceae, with common names Firethorn or Pyracantha. It's extract has also been used in cosmetics as a skin-whitening agent and functioning through tyrosinase inhibition. Recent studies have shown that pyracantha extract possesses antioxidant activities and may significantly improve lipoprotein metabolism in rats. Although the mode of action of Pyracantha extract is not fully understood, a strong relationship was observed between antioxidant and apoptosis in some types of cells. Thus, the aim of this study was to evaluated the effect of pyracantha extract on blastocysts formation and their quality of the porcine parthenogenetic embryos. After parthenogenetic activation by chemicals, presumptive porcine parthenogenetic embryos were cultured in PZM-3 medium supplemented with extracts of pyracantha leaf, stalk and root for 6 day (1, 5 and $10{\mu}g/ml$, respectively). In our results, the frequency of blastocyst formation in pyracantha root extract ($5{\mu}g/ml$) treated group had increased that of other groups. Furthermore, blastocysts derived from pyracantha root extract ($5{\mu}g/ml$) treated group had increased the total cell numbers and reduced apoptotic index. Blastocyst development was significantly improved in the pyracantha root extract ($5{\mu}g/ml$) treated group when compared with the $H_2O_2$ treated group (p<0.05). Subsequent evaluation of the intracellular levels of ROS in pyracantha root extract ($5{\mu}g/ml$) treated groups under $H_2O_2$ induced oxidative stress were decreased (p<0.05). In conclusion, our results indicate that treatment of pyracantha root extract may improve in vitro development of porcine parthenogenetic embryos through its antioxidative and antiapoptotic effects.

• Journal of the Korean Society of Food Science and Nutrition
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• v.43 no.5
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• pp.705-711
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• 2014

In order to develop a skin-whitening agent, melanin contents and intracellular tyrosinase activity were determined by western blotting. Ethyl acetate fractions of 80% ethanol extracts from lily (Lilium Oriental Hybrid 'Siberia') bulbs (R-EA) inhibited melanin synthesis in a dose-dependent manner in ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH)-treated B16/F10 murine melanoma cells. Intracellular tyrosinase activity and melanin contents were suppressed by 45% and 74%, respectively, in response to treatment with $100{\mu}g/mL$ of R-EA. Examination of protein expression associated with ${\alpha}$-MSH-induced melanogenesis showed that tyrosinase related protein (TRP)-1 was inhibited more strongly than tyrosinase, and these results were correlated with stronger inhibition of melanin synthesis than intracellular tyrosinase activity. Taken together, R-EA containing p-coumaric acid and resveratrol could be used as a hypopigmentation agent through suppression of sustained extracellular signal-regulated kinase (ERK) activation via melanogenic induction.

• Microbiology and Biotechnology Letters
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• v.40 no.3
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• pp.250-260
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• 2012

In the present study, the antioxidative and antibacterial activities of Artemisia princeps Pampanini (A. princeps Pamp.) extract were investigated. The ethyl acetate fraction of A. princeps Pamp. showed the most prominent free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity ($FSC_{50}=12.27{\mu}g/mL$). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of A. princeps Pamp. extract on $Fe^{3+}-EDTA/H_2O_2$ systems were investigated using a luminol-dependent chemiluminescence assay. The ethyl acetate fraction of the extract ($OSC_{50}=0.33{\mu}g/mL$) had a 5 times greater ROS scavenging activity than L-ascorbic acid ($1.50{\mu}g/mL$), known as a water soluble antioxidant. The cellular protective effects of fractions of A. princeps Pamp. on the rose-bengal sensitized photohemolysis of human erythrocytes were examined. The aglycone fraction of extracts suppressed photohemolysis in a concentration dependent manner. The inhibitory effects of A. princeps Pamp. extract on tyrosinase were investigated to assess their whitening efficiency. The ethyl acetate fraction demonstrated a 7 times higher tyrosinase inhibitory effect ($IC_{50}=29.20{\mu}g/mL$) than albutin, known as a whitening agent. The antibacterial activity of ethyl acetate fractions against various normal skin flora were measured. The results showed that the antibacterial activity of the fraction was the highest on Staphylococcus aureus, Bacillus subtilis, and Propionibacterium acnes. Antioxidant substances were isolated and purified from the ethyl acetate fractions. Eupatilin and jaceosidin were identified. These results indicate that the extract/fractions of A. princeps Pamp. can function as antioxidant and/or antibacterial agents for the skin.

• Journal of Life Science
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• v.31 no.8
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• pp.719-728
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• 2021

Melanin pigments are abundantly distributed in mammalian skin, hair, eyes, and nervous system. Under normal physiological conditions, melanin protects the skin against various environmental stresses and acts as a physiological redox buffer to maintain homeostasis. However, abnormal melanin accumulation results in various hyperpigmentation conditions, such as chloasma, freckles, senile lentigo, and inflammatory pigmentation. Tyrosinase, a copper-containing enzyme, plays an important role in the regulation of the melanin pigment biosynthetic pathway. Although several whitening agents based on tyrosinase inhibition have been developed, their side effects, such as allergies, DNA damage, mutagenesis, and cytotoxicity of melanocytes, limit their applications. In this study, we synthesized 4-chromanone derivatives (MHY compounds) and investigated their ability to inhibit tyrosinase activity. Of these compounds, (E)-3-(4-hydroxybenzylidene)chroman-4-one (MHY1294) more potently inhibited the enzymatic activity of tyrosinase (IC₅₀ = 5.1±0.86 μM) than kojic acid (14.3±1.43 μM), a representative tyrosinase inhibitor. In addition, MHY1294 showed competitive inhibitory action at the catalytic site of tyrosinase and had greater binding affinity at this site than kojic acid. Furthermore, MHY1294 effectively inhibited α-melanocyte stimulating hormone (α-MSH)-induced melanin synthesis and intracellular tyrosinase activity in B16F10 melanoma cells. The results of the present study indicate that MHY1294 may be considered as a candidate pharmacological agent and cosmetic whitening ingredient.

• Journal of the Korean Society of Food Science and Nutrition
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• v.40 no.8
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• pp.1086-1091
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• 2011

Anti-oxidative activity and tyrosinase inhibitory activity of various ethanol extracts of Polygoni multiflori radix (PMR) and Cynanchi wilfordii radix (CWR) were compared to identify an anti-oxidant and whitening agent source from nature. We conducted an investigation into the anti-oxidant activities of PMR and CWR ethanol extracts by measuring total polyphenol content, total flavonoid content, and ABTS radical capacity. The total polyphenol contents of PMR and CWR were 17.31${\pm}$0.54 mg GA/eq g, and 2.75${\pm}$0.22 mg GA/eq g, respectively. The total flavonoid contents of PMR and CWR were 6.38${\pm}$0.39 mg naringine/eq g, and 1.34${\pm}$0.09 mg naringine/eq g, respectively. The 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) radical decolorization of PMR and CWR were 96.89${\pm}$0.21% at 1 mg/mL and 93.49${\pm}$0.76% at 50 mg/mL. Melanoma cells were cultured with the PMR and CWR ethanol extracts for 48 hr, and total melanin content as a final product and the activity of tyrosinase, a key enzyme, in melanogenesis, were estimated. The PMR and CWR ethanol extracts increased melanin content and tyrosinase activity in a dose-dependent manner. These results suggest that PMR and CWR ethanol extracts could be useful as a skin whitening agent.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.38 no.1
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• pp.57-65
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• 2012

In the present study, the antioxidative properties, inhibitory activity on tyrosinase, and active components of Eriobotrya japonica (E. japonica) leaf extract were investigated. The free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity ($FSC_{50}$) of extract/fraction of E. japonica leaf was in the order 50 % ethanol extract ($22.625{\mu}g/mL$) < ethyl acetate fraction (6.75) < deglycosylated aglycone fraction (5.06). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of fraction/extracton ROS generated in $Fe^{3+}-EDTA/H_2O_2$ system using the luminol-dependent chemiluminescenceassay were investigated. $OSC_{50}$ of the ethyl acetate fraction, deglycosylated aglycone fraction, and ethanol extract were 0.75, 0.79, and $1.61{\mu}g/mL$, respectively. The cellular protective effects of E. japonica leaf extract on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The protective effects of extract/fraction of E. japonica leaf were increased in a in a concentration dependent manner ($5{\sim}50{\mu}g/mL$). Especially, ${\tau}50$ of ethyl acetate fraction at concentrations of $10{\mu}g/mL$ and $50{\mu}g/mL$ showed the most protective effects at 390.8 min and 1471.5 min. The inhibitory effect ($IC_50$) on tyrosinase of E. japonica leaf extracts was higher than arbutin, known as a skin-whitening agent. The order of inhibitory effects was acetate fraction ($75.25{\mu}g/mL$) < 50 % extract (74.1) < deglycosylated aglycone fraction (43.35). TLC of the ethyl acetate fraction showed 7 bands (EJL 1 - EJL 7). HPLC of the aglycone fraction exhibited 2 peaks, kaempferol and quercetin. The amounts of kaempferol and quercetin were 53.7 and 46.3 %. respectively. Therefore, The amounts of kaempferol and its glucoside were a little bit higher than quercetin and its glucoside in E. japonica leaf extract. Accordingly, these findings suggest that extracts/fractions of E. japonica leaf can function as antioxidants in biological systems, especially skin exposed to UV radiation, and protect cellular membranes against ROS. Thus, the extract/fraction of E. japonica leaf may be used in novel functional cosmetics as antioxidants against skin photoaging.

• KSBB Journal
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• v.23 no.4
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• pp.311-316
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• 2008

We investigated several biological activities using the ethanol extract and its fractions from Dictyota coriacea to evaluate the usefulness of its extract as a functional biomaterial. The ethanol extract and n-hexane and ethyl acetate fractions showed dependently inhibitory effect on tyrosinase activity and melanin content in B16F10 cells. The ethanol extract and its fractions showed inhibitory effect on Tyrosinase and TRP-1 gene transcription but didn't showed inhibitory effect on TRP-2 gene transcription. Also, the n-hexane and ethyl acetate fractions dose-dependently inhibited the NO production in a RAW 264.7 cells. These results suggest that extract of Dictyota coriacea could be used as functional biomaterial in developing a skin whitening agent having the anti-inflammatory activity.