• Journal of Digital Convergence
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• v.13 no.4
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• pp.417-423
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• 2015

Oil-in-water(o/w) nanoemulsions were prepared in the system of water/Span 80-Tween 80/long-chain paraffin oil via PIC method. With the increase of preparation temperature from 30 oC to 80 oC, the diameter of emulsion droplets decreased from 150 nm to 40 nm. By varying the HLB of mixed surfactants, we found that there was an optimum HLB around 13.0~14.0 corresponding to the minimum droplet size. The size of emulsion droplets increased upon increasing the ratio of oil/emulsifying agent. At $f{\leq}0.15$, the size of nanoemulsions could be kept constant more than 2 months. The increase in preparation temperature makes it possible for producing monodisperse nanoemulsions. Once the nanoemulsion is produced, the stability against Ostwald ripening is outstanding due to the extremely low solubility of the liquid paraffin oil in the continuous phase.

• The Korean Journal of Physiology and Pharmacology
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• v.24 no.2
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• pp.149-156
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• 2020

Sodium 2-mercaptoethanesulfonate (mesna) is a protective agent that is widely used in medicine because of its antioxidant effects. Recently, reactive oxygen species (ROS) were shown to increase pigmentation. Thus, ROS scavengers and inhibitors of ROS production may suppress melanogenesis. Forkhead box-O3a (FoxO3a) is an antimelanogenic factor that mediates ROS-induced skin pigmentation. In this study, we aimed to investigate the whitening effect of mesna and the signaling mechanism mediating this effect. Human melanoma (MNT-1) cells were used in this study. mRNA and protein expression were measured by real-time quantitative PCR and Western blotting analysis to track changes in FoxO3a-related signals induced by mesna. An immunofluorescence assay was performed to determine the nuclear translocation of FoxO3a. When MNT-1 melanoma cells were treated with mesna, melanin production and secretion decreased. These effects were accompanied by increases in FoxO3a activation and nuclear translocation, resulting in downregulation of four master genes of melanogenesis: MITF, TYR, TRP1, and TRP2. We found that mesna, an antioxidant and radical scavenger, suppresses melanin production and may therefore be a useful agent for the clinical treatment of hyperpigmentation disorders.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.27 no.1
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• pp.119-131
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• 2001

Exposure of the human skin to UV-light can cause sun-tanning, photoaging and even photo-carcinogenesis. Melanin is important in protecting the skin against UV damage, but excessive or uneven melanin production can lead to the formation of freckles and aged spot. Control of hyperpigmentation is becoming even more important as aged population continues to grow. These needs led us to develop effective and safe depigmenting-agent, kojyl 3-aminopropyl phosphate (kojyl-APPA), called Whitegen. The development of whitegen was based on the fact that phosphate group of 3-aminopropyl phosphate can make kojic acid more compatible to the skin membrane and more stable. Instability of kojic acid has been a problem in cosmetic use. The insertion of phosphoester group has been recognized as a powerful tool to improve such physical properties as solubility and stability, because the phosphodiester residue is well characterized as a non-toxic moiety, having a high affinity for cell membranes. Kojyl-APPA showed no tyrosinase inhibition effect compared to kojic acid in vitro, but showed tyrosinase inhibition effect in situ. It means that kojyl-APPA is converted to kojic acid enzymatically in cells. Kojyl-APPA showed the inhibitory activity on melanin synthesis in mouse melanoma and normal humal melnaocytes and also showed long-lasting stability in comparison with its original form (kojic acid). Kojyl-APPA showed depigmenting effects when applied to UVB-induced hyperpigmentated region of guinea pig skin. Based on these results, kojyl 3-aminopropyl phosphate can be used as a safe and effective ingredient for the brightness and cleanness of skin.

• Natural Product Sciences
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• v.22 no.3
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• pp.193-200
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• 2016

This study describes the anti-inflammatory, anti-oxidant, and melanogenesis inhibition activities of methanol extract and various organic solvent fractions of Arecae Pericarpium. We examined the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging activity, mushroom tyrosinase inhibition activity and melanin contents. The study showed that, among all tested fractions, methylene chloride fraction showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells ($IC_{50}$ value $8.89{\mu}g/mL$) and DPPH radical scavenging activity ($EC_{50}$ value $21.39{\mu}g/mL$). Methylene chloride and ethyl acetate fractions similarly inhibited mushroom tyrosinase activity. Methanol extract exhibited strongest reduction of melanin content in B16F10 melanoma cells. Based on the bioactivity assay results, methylene chloride and ethyl acetate fractions were further separated. Eight phenolic compounds were isolated, which are dimeric syringol (1), catechol (2), 4-hydroxybenzaldehyde (3), vanillin (4), 4-hydroxyacetophenone (5), apocynin (6), protocatechuic acid (7) and 4-hydroxybenzoic acid (8). Among the isolated compounds tested, catechol showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells. Catechol also showed the concentration-dependent NF-${\kappa}B$ inhibition activity. Arecae Pericarpium might have potentials to be developed as anti-inflammatory agent or dermatological product for skin-whitening agent.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.28 no.1
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• pp.135-149
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• 2002

To date, research on the regulation of melanogenesis has focused on factors which affect tyrosinase, the rate-limiting enzyme in the melanogenic pathway, by searching for chemicals which competitively inhibit tyrosinase function. Many types of tyrosinase inhibitors have been developed, but no satisfactory results have been made clinically until now, To find a new whitening agent, which effectively inhibits melanogenesis, we synthesized several compounds and selected compounds by cell-based assay system. Finally, 3, 4, 5-trimethoxy cinnamaie thymol ester(TCTE, Melasolv) was selected and the effects of TCTE on melanogenesis were investigated. Treatment of mouse-derived melanocyte melan-a cells with TCTE results in a marked down-regulation of tyrosinase activity. 80% decrease of tyrosinase activity occurs with 30uM TCTE treatment for 72 hours without affecting cell growth. The inhibition of tyrosinase activity is dose-dependent and melanin content was also decreased to 40%. From the in vitro tyrosinase assay using cell extract, TCTE does not act as a direct inhibitor of the enzyme. Treatment of melan-a cultures with TCTE blocks the increase in tyrosinase activity by either forskolin, 3-isobutyl-1-methtyl-xanthine. TCTE decreased the expression of tyrosinase, TRP-1 without effects on TRP-2 protein expression through the down regulation of tyrosinase and TRP-1 mRNA. From the results of cAMP immunoassays, intracellular levels of the cyclin nucleotide are unaffected in cells treated with TCTE. The inhibitory effects of melanin synthesis were also shown in reconstitute human epidermis model by topical application. These findings suggest that TCTE can be used for studying the regulation of melanogenesis and depigmenting agent.

• Korean Chemical Engineering Research
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• v.56 no.3
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• pp.309-314
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• 2018

In this study, methanol extracts of the Oxalidaceae were tested with a potential functional cosmetic agent. As cosmetic agent tests, cell toxicity, polyphenol content, antioxidation, anti-wrinkle, and whitening effects were measured. Cell toxicity of the extracts was weak up to $1,000{\mu}g/mL$. Polyphenol contents of Oxalis corniculata L., Oxalis obtriangulata Maximowicz and Oxalis articulata Savigny were $116.036{\pm}0.37mg/g$, $54.72{\pm}0.52mg/g$ and $88.18{\pm}1.15mg/g$, respectively. Oxalis corniculata L., Oxalis obtriangulata Maximowicz and Oxalis articulata Savigny extracts showed 89%, 80% and 88% of antioxidation effects at $1,000{\mu}g/mL$ concentration using DPPH free radical scavenging assay. Oxalis corniculata L., Oxalis obtriangulata Maximowicz and Oxalis articulata Savigny extracts indicated 81%, 51% and 57% of antiwrinkle effects at $1,000{\mu}g/mL$ concentration using elastase inhibition assay. Oxalis corniculata L. extract was particularly excellent in elastase inhibition effect. Whitening effect using tyrosinase inhibition assay was relatively weak. Lotion formulation including 1% Oxalis obtriangulata Maximowicz extract was stable based on the temperature stability test for 28 days in terms of pH, viscosity and appearance. However, Lotion formulation including 1% Oxalis corniculata L. extract and Oxalis articulata Savigny extract need formulation improvement. From the research, methanol extract of Oxalis corniculata L. seems to be good candidate for antiwrinkle functional cosmetic agent.

• The Journal of the Korea Contents Association
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• v.12 no.1
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• pp.353-360
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• 2012

The purpose of this study was to evaluate tooth color and microhardness after 15% carbamide peroxide(CP) bleaching treatments with/without potassium nitrate and fluoride(PF), which were used home bleaching. Thirty tooth specimens were obtained from thirty premolar and were randomly divided into three groups: 1, untreated controls(Distilled water): 2, treatment with 15% CP bleaching agent; 3, treatment with 15% CP bleaching agent (contained 3% potassium nitrate and 0.11% fluoride). All groups were treated 6h per day for 14 days then immersed in distilled water. Changes in enamel color were evaluated on Baseline and Day 14. Microhardness were evaluated on Baseline, Days 7 and 14. All the bleached enamel specimens revealed increased whiteness without control group. Groups 2 and 3 showed significantly decreased enamel microhardness compared to control group. On Day 7, Groups 2-3 showed significantly decreased enamel microhardness compared to control group and respective baseline data. The percentage microhardness loss(PML) look at Day 7 and 14 for Group 1, respectively, there was little difference between 1.7 and 0.8. However, Group 2 was 21.9 and 3.5, Group 3 was 16.7 and 1.4 as a baseline and Day 7 were significantly different (p<0.05). The PML of group 2 was significantly highest than that of group 3 on Day 7. As a result, the data indicate that the addition of PF did not influence the whitening efficacy of the bleaching agent negatively. PF-containing bleaching agent reduce the percentage microhardness loss. PF-containing tooth bleaching your teeth with a whitening effect can be reduced by decreasing the hardness of enamel.

• The Journal of Korean Academy of Prosthodontics
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• v.40 no.5
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• pp.451-469
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• 2002

The purpose of this study was to estimate the effect of a bleaching agent on tooth surfaces and to evaluate the resin bond strength according to different surface treatments on bleached teeth. To prepare for the experimental samples, first, extracted human third molars were used and the body portions of the crowns were cut into four equal-sized specimens. Next, each specimen was mounted in an plastic bottle with self-cured resin and highly polished to have them reveal the enamel or dentin surfaces. Then, the enamel(E) and dentin(D) specimens were divided into four ; 1) non-bleached, laser-treated(NBLA) group 2) bleached, laser-treated(BLLA) group 3) non-bleached, acid-treated(NBAC) group and 4) bleached, acid-treated(BLAC) group. Here, $opalescence^{(R)}$ (10% carbamide peroxide) was used for bleaching agent. The treated specimens were observed by confocal laser scanning microscopy and bonded with composite resin for shear bond test. The following results were obtained from this experiment : 1. Compared with the ENB group, the EBL group was shown be dyed about $20{\mu}m$ deeper with rhodamine B. The DBL group appeared to be caved in at the entry part of the dentinal tubules, was dyed about $20{\mu}m$ deeper and $5{\mu}m$ wider in diameter, compared with the DNB group. 2. In comparison with the EBLAC group, the ENBAC group looked evenly bonded with the resin, while the DNBAC group, compared to DBLAC group, was observed to have its resin tags penetrated about $50{\mu}m$ deeper. Other than those, however, no observable differences between ENBLA and EBLLA group or between DNBLA and DBLLA group were found. 3, At the shear bond test, the ENBAC group was shown to have statistically significant higher shear bond strength than the EBLAC group(p<0.05). No statistically significant differences between the ENBLA and the EBLLA groups were observed(p>0.05). 4. At the shear bond test, the DNBAC group was shown to have statistically significant higher shear bond strength than the DBLAC group(p<0.05). No statistically significant differences between the DNBLA and the DBLLA groups were observed(p>0.05). The in vitro observations above suggest that tooth-bleaching procedure brings a certain change on enamel and dentin surfaces and it weakens the shear bond strength with composite resin when the bleached tooth was acid-treated.

• Journal of Technologic Dentistry
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• v.23 no.1
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• pp.85-93
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• 2001

The purpose of this study was to evaluate the effects of commercial home-tooth bleaching agents on the color of tooth. Twenty five sound extracted teeth were randomly divided into five groups. The color differences between before and after treatment with five types of tooth bleaching agents (7.5% hydrogen peroxide Nite White $Excel^{(R)}$, 10% carbamide peroxide Nite White $Excel^{(R)}$, 16% carbamide peroxide Nite White $Excel^{(R)}$, 10% carbamide peroxide Insta-BriteTM, 20% carbamide peroxide Insta-$Brite^{TM}$) were evaluated. The results were as follows: 1. By 2 week home tooth bleaching agent applications, the values ($L^*$) of bovine teeth increased as high as 4.38 $\sim$ 8.80 when comparing to those of the samples before treatment, and the color difference (${\Delta}E^*$) showed as high as 10.16 $\sim$ 15.04. 2. 16% carbamide peroxide Nite White Excel induced significantly greater ${\Delta}L^*$ than other test edgroups except for 7.5% hydrogen peroxide Day White Excel, and significantly greater ${\Delta}E^*$ than other tested groups by 2 week bleaching agent treatments (p<0.01). 3. 16% carbamide peroxide Nite White Excel(${\Delta}L^*$=8.80, ${\Delta}E^*$=15.04) induced significantly greater ${\Delta}L^*$ and ${\Delta}E^*$ than 10% carbamide peroxide Nite White Excel(${\Delta}L^*$=5.01, ${\Delta}E^*$=10.16)(p<0.01), but significant difference between 10% carbamide peroxide Insta-Brite(${\Delta}L^*$=4.38, ${\Delta}E^*$=10.51) and 20% carbamide peroxide Insta-Brite(${\Delta}L^*$=5.63, ${\Delta}E^*$=11.23) was not shown in ${\Delta}L^*$ and ${\Delta}E^*$(p>0.01). 4. 16% carbamide peroxide Nite White Excel(${\Delta}L^*$=8.80, ${\Delta}E^*$=15.04) which were applied in night time induced significantly greater ${\Delta}L^*$ and ${\Delta}E^*$ than 7.5% hydrogen peroxide Day White Excel(${\Delta}L^*$=8.47, ${\Delta}E^*$=12.75) which were applied in day time. Conclusions: These results demonstrate that all the commercial home-tooth bleaching agents have appreciable bleaching effect on teeth, and the effects of home-tooth bleaching agents which are used during night time are affected by content of carbamide peroxide. Especially the whitening effect of home tooth bleaching agents that are used through night time is greater than that of short time-applying tooth bleaching agent.

• 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.