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        Diallyl Biphenyl-Type Neolignans Have a Pharmacophore of PPARα/γ Dual Modulators

        ( Yujia Han ),( Jingjing Liu ),( Sungjin Ahn ),( Seungchan An ),( Hyejin Ko ),( Jeayoung C. Shin ),( Sun Hee Jin ),( Min Won Ki ),( So Hun Lee ),( Kang Hyuk Lee ),( Song Seok Shin ),( Won Jun Choi ),( 한국응용약물학회 2020 Biomolecules & Therapeutics(구 응용약물학회지) Vol.28 No.5

        Adiponectin secretion-promoting compounds have therapeutic potentials in human metabolic diseases. Diallyl biphenyl-type neolignan compounds, magnolol, honokiol, and 4-O-methylhonokiol, from a Magnolia officinalis extract were screened as adiponectin- secretion promoting compounds in the adipogenic differentiation model of human bone marrow mesenchymal stem cells (hBM-MSCs). In a target identification study, magnolol, honokiol, and 4-O-methylhonokiol were elucidated as PPARα and PPARγ dual modulators. Diallyl biphenyl-type neolignans affected the transcription of lipid metabolism-associated genes in a different way compared to those of specific PPAR ligands. The diallyl biphenyl-type neolignan structure provides a novel pharmacophore of PPARα/γ dual modulators, which may have unique therapeutic potentials in diverse metabolic diseases.

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        Recyclable One-Step Extraction and Characterization of Intact Melanin from Alpaca Fibers

        Yujia Liang,Qi Han,Nolene Byrne,Lu Sun,Xungai Wang 한국섬유공학회 2018 Fibers and polymers Vol.19 No.8

        Melanin, a ubiquitous natural pigment, has attracted much attention in energy and nanotechnology areas in recent years. With the increasing demand for high-quality melanin materials and sustainable experimental environment, this study was conducted to achieve melanin with intact structure through recyclable extraction method using ionic liquid (IL). Melanin extracted from base dissolution and acid isolation (BA) method and acid hydrolysis (AH) method were also used for comparison. SEM and 13C-NMR characterizations indicated that IL treatment has retained the original structure of melanin while other methods caused particle damage to various degrees. In addition, the recycled IL (up to five times) showed good reproducibility, and the performance of extracted melanin at the 5th cycle was well-maintained.

      • Functional Insights of Ceramides in Epidermis

        ( Eunyoung Lee ),( Yujia Han ),( Jeayoung Shin ),( Yeon Kyung Kim ),( Jeongjoo Pyo ),( Sungjin Ahn ),( Jaehyoun Ha ),( Minsoo Noh ) 한국피부장벽학회 2018 한국피부장벽학회지 Vol.20 No.1

        Intercellular lipids of stratum corneum mainly consist of ceramides, free fatty acids, and cholesterol. Ceramides are synthesized in endoplasmic reticulum and transported to the lamellar bodies which provide intercellular lipids in stratum corneum during epidermal differentiation. The lipid mass of ceramides is approximately 50% of the intercellular lipid contents in stratum corneum. The decrease in ceramide levels significantly impairs the integrity of skin permeability barrier and results in the increase in transepidermal water loss. The content and quantity of ceramides can directly affect the lamellar layer rigidity of stratum corneum lipid matrix and genetic mutations or polymorphisms of ceramide metabolic enzymes are associated with the disrupted skin barrier functions. In addition to the structural role in skin permeability barrier, ceramides are important in the regulation of cell biology functions such as ultraviolet B irradiation-induced cellular apoptosis, inflammation-related autophagy, and the proliferation and differentiation of epidermal keratinocytes. Besides skin, ceramides and their metabolites are also interested in other tissues because ceramides are associated with various human diseases like diabetes and cancers. Notably, skin microbiota can affect the ceramide metabolism and change the content of ceramides and their metabolites in stratum corneum lipid matrix. Sphingosine choline phosphotransferase and sphingomyelin deacylase may increase sphingosylphosphorylcholine (SPC), a ceramide metabolite increased in the stratum corneum of some atopic patient population. The genes of these metabolic enzymes responsible for the increase in SPC have not been discovered in human cell studies. It is possible that the abnormal SPC production in atopic skin may be associated with microorganism-derived ceramide metabolic enzymes. Therefore, research on skin microbiota should be directed toward the elucidation of microbiota-associated ceramide metabolic enzymes to understand the ceramide homeostasis in human epidermis.

      • Kojyl cinnamate esters are peroxisome proliferator-activated receptor α/γ dual agonists

        Kim, Sae On,Han, Yujia,Ahn, Sungjin,An, Seungchan,Shin, Jeayoung C.,Choi, Hyunjung,Kim, Hyoung-June,Park, Nok Hyun,Kim, Yong-Jin,Jin, Sun Hee,Rho, Ho Sik,Noh, Minsoo Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.21

        <P><B>Abstract</B></P> <P>Adiponectin is an adipocytokine with insulin-sensitizing, anti-inflammatory, anti-atherosclerotic, and anti-aging properties. Compounds with the ability to promote adiponectin secretion are of interest for the development of anti-aging drugs to improve skin-aging phenotypes. In the phenotypic assay to measure adiponectin secretion during adipogenesis in human adipose tissue-derived mesenchymal stem cells (hAT-MSCs), kojyl cinnamate ester derivatives increased adiponectin secretion. A target identification study showed that the kojyl cinnamate ester derivatives competitively bound to peroxisome proliferator-activated receptor α/γ (PPARα/γ). The upregulation of adiponectin production induced by kojyl cinnamate ester derivatives was significantly correlated with PPARα and PPARγ binding activities. Kojyl cinnamate ester derivatives significantly increased the transcription of genes encoding cholesterol and fatty acid synthesizing enzymes in hAT-MSCs. Notably, the kojyl cinnamate esters upregulated the gene transcription of lipid metabolic enzymes in human epidermal keratinocytes, which are important in the integrity of skin permeability barrier. In addition, the kojyl cinnamate esters that function as PPARα/γ dual modulators inhibited ultraviolet B irradiation-induced inflammation in human epidermal keratinocytes. Therefore, kojyl cinnamate ester derivatives are a novel class of PPARα/γ dual agonists with the potential to improve skin-aging phenotypes.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

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