Downregulation of aryl hydrocarbon receptor-mediated gene expression by Fraglide-1, a PPARγ agonist isolated from aromatic vinegar
Year: 2024
Type: preprint
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.
Source: Research Square
Language: English
Subfield: Dermatology
Field: Medicine
Domain: Health Sciences
Open Access status: green
Awards: A bisindole-containing compound affects the proper function of Rab6, resulting in Golgi disruption and secretion inhibition, G3939487023, G4170939786, G5246182142, Identification and characterization of phytochemical-targeted genes using a genome wide yeast screening system, New Synthetic Methods for Glycoproteins and the Integrated Approaches to Elucidate the Functions of Post-translational Modifications, G7075460940, Influence of genetic background unique to the Japanese on metabolism and physiological activities of functional food components
OpenAlex ID: W4391133918
