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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>
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.