• Journal of the Society of Cosmetic Scientists of Korea
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• v.45 no.1
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• pp.49-56
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• 2019

Pueraria thomsonii Benth. as a medicinal ingredient, has been traditionally used in Chinese medicine to treat fever, acute dysentery, diarrhea, diabetes, and cardiovascular disease. The effects of P. thomsonii flower on skin have not been reported yet. In this study, the whitening effect of P. thomsonii flower was verified using B16F1 melanoma cells and HS68 fibroblasts. P. thomsonii flower extract reduced melanin contents of B16F1 cells in a dose-dependent manner. To identify its active components, we analyzed P. thomsonii flower extract using high performance liquid chromatography (HPLC). As a result, we identified three major isoflavones of tectorigenin, tectoridin, and tectorigenin 7-O-xylosylglucoside. At a non-cytotoxic concentration, the three components also reduced melanin contents of B16F1 cells in a dose-dependent manner. The depigmentation effects were attributed to the reduced gene expression of tyrosinase and microphthalmia-associated transcription factor (MITF). In order to elucidate another depigmentation mechanism, their effects on DKK-1, a fibroblast-derived depigmentation factor, was determined in HS68 cells. As a result, P. thomsonii flower extracts, tectoridin and tectorigenin 7-O-xylosylglucoside, reduced DKK-1 gene expression, while tectorigenin increased DKK-1 gene expression in a dose-dependent manner. These results suggest that tectorigenin can be used as an effective whitening agent that inhibit melanin synthesis in melanocytes and promote the secretion of depigmentation factor from fibroblasts.

• Molecules and Cells
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• v.42 no.6
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• pp.480-494
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• 2019

Aggregates of disease-causing proteins dysregulate cellular functions, thereby causing neuronal cell loss in diverse neurodegenerative diseases. Although many in vitro or in vivo studies of protein aggregate inhibitors have been performed, a therapeutic strategy to control aggregate toxicity has not been earnestly pursued, partly due to the limitations of available aggregate models. In this study, we established a tetracycline (Tet)-inducible nuclear aggregate (${\beta}23$) expression model to screen potential lead compounds inhibiting ${\beta}23$-induced toxicity. High-throughput screening identified several natural compounds as nuclear ${\beta}23$ inhibitors, including peucedanocoumarin III (PCIII). Interestingly, PCIII accelerates disaggregation and proteasomal clearance of both nuclear and cytosolic ${\beta}23$ aggregates and protects SH-SY5Y cells from toxicity induced by ${\beta}23$ expression. Of translational relevance, PCIII disassembled fibrils and enhanced clearance of cytosolic and nuclear protein aggregates in cellular models of huntingtin and ${\alpha}$-synuclein aggregation. Moreover, cellular toxicity was diminished with PCIII treatment for polyglutamine (PolyQ)-huntingtin expression and ${\alpha}$-synuclein expression in conjunction with 6-hydroxydopamine (6-OHDA) treatment. Importantly, PCIII not only inhibited ${\alpha}$-synuclein aggregation but also disaggregated preformed ${\alpha}$-synuclein fibrils in vitro. Taken together, our results suggest that a Tet-Off ${\beta}23$ cell model could serve as a robust platform for screening effective lead compounds inhibiting nuclear or cytosolic protein aggregates. Brain-permeable PCIII or its derivatives could be beneficial for eliminating established protein aggregates.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.19 no.12
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• pp.62-70
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• 2018

In this study, we synthesized Oligo Peptide (Lys-Val-Ala-Arg-Pro: KVARP) and peptide derivatives using Solid Phase Peptide Synthesis(SPPS). KVARP was commonly known to improve whitening of skin. We measured bio-activity of the synthesized compounds. The whitening effect was measured in tyrosinase inhibition and the result showed to be highly effective with 93% inhibition rate at $5000{\mu}g/m{\ell}$ of Geranic-KVARP, on the other hand the IC50 value was $68{\mu}g/m{\ell}$. The wrinkle-reducing effect was measured by elastase inhibition at a concentration of 63% at $400{\mu}g/m{\ell}$ of Salicylic-KVARP, and the IC50 value was $253{\mu}g/m{\ell}$. In the DPPH assay, Caffeic-KVARP showed more than 95% antioxidant activity at $400{\mu}g/m{\ell}$ with high concentration and IC50 value was $31{\mu}g/m{\ell}$. The anti-inflammatory effect of Nitric Oxide inhibition was 67% at $400{\mu}g/m{\ell}$ of Lipoic-KVARP. Therefore, the four types of KVARP derivative that were synthesized from various experiments has shown that it could have potential to be used to develop new medicines, cosmetics as well as in various industries.

• Applied Chemistry for Engineering
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• v.22 no.4
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• pp.358-366
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• 2011

A homologous series of linear liquid crystal dimers, the ${\alpha},{\omega}$-bis(4-cyano-azobenzene-4'-oxy)alkanes (CATWETn, where n, the number of methylene units in the spacer, is 2~10) were synthesized, and their thermotropic liquid crystalline phase behavior were investigated. The CATWETn with n of 3 and 6 exhibited monotropic nematic phases, whereas other derivatives showed enantiotropic nematic phases. The nematic-isotropic transition temperatures of the dimers and their entropy variation at the phase transition showed a large odd-even effect as a function of n. This phase transition behavior was rationalized in terms of the change in the average shape of the spacer on varying the parity of the spacer. The thermal stability and degree of order in the nematic phase and the magnitude of the odd-even effect of CATWETn were similar to those for the methoxy-, nitro-, and pentyl-substituted dimers, while they were significantly different from those for the monomesogenic compounds, 1-{4-(4'-cyanophenylazo)phenoxy}alkylbromides and the side-chain liquid-crystalline polymers, the poly[1-{4-(4'-cyanophenylazo)phenoxyalkyloxy}ethylene]s. The results were discussed in terms of 'virtual trimer model' by Imrie.

• Food Science and Industry
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• v.53 no.1
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• pp.69-83
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• 2020

For the development of the chitosan industry in Korea, the catch of red snow crabs caught on the east coast is rapidly decreasing. Therefore, it is urgent to develop raw materials that can replace the red snow crab as the top priority to solve the supply and demand problems, as well as wastewater treatment costs account for a large proportion of the cost of chitosan. In order to solve the problems, continuous research on biological extraction methods such as enzymatic extraction and microbial fermentation will increase production efficiency and lower unit cost as well as chemical extraction methods. Further efficient manufacturing method can be established. Establishing of novel techniques is indispensable for production of high-purity chitosan and the ability to regulate and separate the molecular weight, as well as joint research with industry, academia and research institute for the research and development of high-functional chitosan derivatives.

• Journal of Ginseng Research
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• v.45 no.1
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• pp.126-133
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• 2021

Background: 20(S)-protopanaxadiol (20(S)-PPD), one of the aglycone derivatives of major ginsenosides, has been shown to have an anticancer activity toward a variety of cancers. This study was initiated with an attempt to evaluate its anti-cancer activity toward human endometrial cancer by cell and xenograft mouse models. Methods: Human endometrial cancer (HEC)-1A cells were incubated with different 20(S)-PPD concentrations. 20(S)-PPD cytotoxicity was evaluated using MTT assay. Apoptosis was detected using the annexin V binding assay and cell cycle analysis. Cleaved poly (ADP-ribose) polymerase (PARP) and activated caspase-9 were assessed using western blotting. HEC-1A cell tumor xenografts in athymic mice were generated by inoculating HEC-1A cells into the flank of BALB/c female mice and explored to validate 20(S)-PPD anti-endometrial cancer toxicity. Results: 20(S)-PPD inhibited HEC-1A cell proliferation in a dose-dependent manner with an IC50 value of 3.5 μM at 24 h. HEC-1A cells morphologically changed after 20(S)-PPD treatment, bearing resemblance to Taxol-treated cells. Annexin V-positive cell percentages were 0%, 10.8%, and 58.1% in HEC-1A cells when treated with 0, 2.5, and 5 μM of 20(S)-PPD, respectively, for 24 h. 20(S)-PPD subcutaneously injected into the HEC-1A cell xenograft-bearing mice three times a week for 17 days manifested tumor growth inhibition by as much as 18% at a dose of 80 mg/kg, which sharply contrasted to controls that showed an approximately 2.4-fold tumor volume increase. These events paralleled caspase-9 activation and PARP cleavage. Conclusion: 20(S)-PPD inhibits endometrial cancer cell proliferation by inducing cell death via a caspase-mediated apoptosis pathway. Therefore, the 20(S)-PPD-like ginsenosides are endowed with ample structural information that could be utilized to develop other ginsenoside-based anticancer agents.

• The Korean Journal of Food And Nutrition
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• v.33 no.6
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• pp.655-665
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• 2020

In this study, chemical information on a total of 20 individual compounds was constructed to identify isoflavones from the previous reports related with used parts(seeds, leaves, stems, pods) and products of soybean(Glycine max L.). Through constructed library and UPLC-DAD-QToF/MS analysis, a total of 19 individual isoflavones including aglycones, glucosides, acetylglucosides and malonylglucosides as major compounds was identified and quantified from 14 selected soybean seeds. Among them, genistein 7-O-(2"-O-apiosyl)glucoside and genistein 7-O-(6"-O-apiosyl)glucoside(ambocin) were identified tentatively as novel compounds in soybean seeds. Besides, among malonylglucosides, glycitein 4'-O-(6"-O-malonyl)glucoside was estimated for the first time. Total isoflavone contents were distributed from 240.21 to 445.21(mg/100 g, dry matter) and 7-O-6"-O-malonylglucosides were composed of 77.8% on total isoflavone as well as genistein derivatives were confirmed as major class. It was considered importantly that the development of isoflavone-rich varieties was necessary to strengthen their effects such as anti-inflammation, anti-cancer and menopause mitigation. The qualitative and quantitative data presented precisely in this study could be help to select and breed isoflavone-rich varieties. Furthermore, their basic isoflavone profile is expected to be applied to estimate the change of isoflavone conjugates on bioavailability after soy food supplements.

• Journal of Ginseng Research
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• v.45 no.1
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• pp.48-57
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• 2021

Background: Ginsenoside Rh2 is well known for many pharmacological activities, such as anticancer, antidiabetes, antiinflammatory, and antiobesity properties. Glycosyltransferases (GTs) are ubiquitous enzymes present in nature and are widely used for the synthesis of oligosaccharides, polysaccharides, glycoconjugates, and novel derivatives. We aimed to synthesize new ginsenosides from Rh2 using the recombinant GT enzyme and investigate its cytotoxicity with diverse cell lines. Methods: We have used a GT gene with 1,224-bp gene sequence cloned from Lactobacillus rhamnosus (LRGT) and then expressed in Escherichia coli BL21 (DE3). The recombinant GT protein was purified and demonstrated to transform Rh2 into two novel ginsenosides, and they were characterized by nuclear magnetic resonance (NMR) techniques and evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide assay. Results: Two novel ginsenosides with an additional glucopyranosyl (6→1) and two additional glucopyranosyl (6→1) linked with the C-3 position of the substrate Rh2 were synthesized, respectively. Cell viability assay in the lung cancer (A549) cell line showed that glucosyl ginsenoside Rh2 inhibited cell viability more potently than ginsenoside Rg3 and Rh2 at a concentration of 10 μM. Furthermore, glucosyl ginsenoside Rh2 did not exhibit any cytotoxic effect in murine macrophage cells (RAW264.7), mouse embryo fibroblasts cells (3T3-L1), and skin cells (B16BL6) at a concentration of 10 μM compared with ginsenoside Rh2 and Rg3. Conclusion: This is the first report on the synthesis of two novel ginsenosides, namely, glucosyl ginsenoside Rh2 and diglucosyl ginsenoside Rh2 from Rh2 by using recombinant GT isolated from L. rhamnosus. Moreover, diglucosyl ginsenoside Rh2 might be a new candidate for treatment of inflammation, obesity, and skin whiting, and especially for anticancer.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.47 no.1
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• pp.65-73
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• 2021

It is very important to control the inflammation of the skin because it can develop into diseases such as atopy as well as scarring and aging. In this work, we recently identified the in vitro synthesis of specialized pro-resolving mediators (SPMs) known to control inflammation in the human body and the applicability of cosmetics. Using recombinant protein of lipoxygenase from Glycine max, we succeeded to prepare mixtures of mono- or di-hydroxy DHA named as S-SPMs and used them for in vitro efficacy test. To investigate anti-inflammatory effect of S-SPMs, mRNA level of TNF-α and IL-6 were analyzed. Under UVB exposed condition, expression of both were decreased by S-SPMs treatment. And we observed reduced production of nitric oxide (NO) by S-SPMs application under the condition with diesel particulate matter (DPM). At the same experimental condition, malondialdehyde (MDA) production was decreased by S-SPMs, indicating the inhibitory effect of S-SPMs in lipid peroxidation. In addition, S-SPMs treatment resulted in reduction of matrix metalloproteinases-1 (MMP-1) expression and elevation of procollagen type I synthesis. Together with this, mRNA level of filaggrin and loricrin were increased by S-SPMs, indicating enhancement of skin barrier function. These results demonstrate that S-SPMs is a good candidate to develop as a cosmetic ingredient for anti-inflammation, anti-wrinkle, and improvement of skin barrier function.

• Applied Chemistry for Engineering
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• v.31 no.6
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• pp.653-659
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• 2020

This study was focused on the synthesis of methoxy polyethylene glycol-oleanolic acid ester (mPEG-OA derivative) and investigation of its water solubility and anti-melanogenic effects. mPEG-OA derivative was identified by 1H and 13C NMR and FT-IR spectroscopic measurements. The water solubilities of mPEG-OA derivative and OA were found to be 13 and 0.013 mg/mL and that of mPEG-OA was found to be 1000-fold higher than that of OA. The effects of mPEG-OA derivative and OA on cell viability were measured using B16F10 melanoma cells. The viability of cells treated with mPEG-OA derivative (250 μM) increased 4-fold compared to that of cells treated with OA (62.5 μM). At mPEG-OA derivative and OA concentrations where the cell viability was unaffected, the inhibitory effect of mPEG-OA derivative and OA on the melanogenesis in B16F10 melanoma cells were 36 and 35% at 50 and 10 μM, respectively. The expression level of microphthalmia-associated transcription (MITF) was also reduced in B16F10 melanoma cells treated with mPEG-OA and OA. Overall, mPEG-OA derivative showed excellent water solubility and inhibitory effects of the melanogenesis, which could be used as a potential formulation for use in whitening functional cosmetic material.