Affiliation:
1. Okayama University
2. Japan Advanced Institute of Science and Technology
3. Kyoto University
4. Kobe University
Abstract
Abstract
Fraglide-1 (FG1), a lactone isolated from the traditional Chinese Zhenjiang aromatic vinegar Kozu, has previously demonstrated antiobesity, antifungal, and antioxidant properties. Given the role of the aryl hydrocarbon receptor (AhR) in the pathogenesis of atopic dermatitis and its association with the neurotrophic factor artemin, we investigated the potential of FG1 as an AhR ligand in this study. Docking simulations revealed promising interactions between FG1 and AhR. Subsequent cell-based reporter assays using a human skin keratinocyte cell line showed that FG1 effectively suppressed the AhR-mediated induction of genes with a xenobiotic response element (AhR/XRE), which in turn downregulated the expression of artemin, a biomarker of atopic dermatitis. FG1 demonstrated not only comparable efficacy but also superior safety compared with the known AhR inhibitor StemRegenin 1. These results not only underscore the therapeutic promise of FG1 in atopic dermatitis but also reinforce its previously known bioactivities, such as antiobesity, antifungal, and antioxidant effects, which indicate that it is a versatile compound with multiple health benefits.
Publisher
Research Square Platform LLC
Reference49 articles.
1. Quantification of fraglide-1, a new functional ingredient, in vinegars;Yatmaz AH;J. Oleo Sci.,2017
2. Matsutani, F. et al. PARγ Activating Agent. WO2016006548A1. World Intellectual Property Organization. https://patentimages.storage.googleapis.com/bc/f2/b3/64086d93eea975/WO2016006548A1.pdf, (2016).
3. A new agonist for peroxisome proliferation-activated receptor γ (PPARγ), fraglide-1 from zhenjiang fragrant vinegar: screening and characterization based on cell culture experiments;Tsujino Y;J. Oleo Sci.,2017
4. Stienstra, R., Duval, C., Müller, M. & Kersten, S. PPARs, obesity, and inflammation. PPAR Res. 2007, 95974, (2007).
5. Gamahonolides A, B, and gamahorin, novel antifungal compounds from stromata of epichloe typhina on phleum pratense;Koshino H;Biosci. Biotechnol. Biochem.,1992