AI Article Synopsis
- A new compound, ethyl 2,4,6-trihydroxybenzoate (ETB), derived from Celtis biondii, acts as a liver X receptor (LXR) activator, enhancing the activity of both LXR-α and LXR-β.
- ETB was shown to effectively reduce cholesterol accumulation in various cell types, including macrophages and hepatocytes, while promoting the expression of beneficial LXR-responsive genes in a dose-dependent manner.
- Importantly, ETB does not trigger lipogenic gene expression or increase triglyceride levels in liver cells, indicating its potential as a dual-LXR modulator for maintaining cholesterol balance without the risk of lipid buildup.
Article Abstract
The present study reports a novel liver X receptor (LXR) activator, ethyl 2,4,6-trihydroxybenzoate (ETB), isolated from Celtis biondii. Using a reporter gene assay, time-resolved fluorescence resonance energy transfer (TR-FRET), and surface plasmon resonance (SPR) analysis, we showed that ETB directly bound to and stimulated the transcriptional activity of LXR-α and LXR-β. In macrophages, hepatocytes, and intestinal cells, ETB suppressed cellular cholesterol accumulation in a dose-dependent manner and induced the transcriptional activation of LXR-α/-β-responsive genes. Notably, ETB did not induce lipogenic gene expression or cellular triglyceride accumulation in hepatocytes. These results suggest that ETB is a dual-LXR modulator that regulates the expression of key genes in cholesterol homeostasis in multiple cells without inducing lipid accumulation in HepG2 cells.
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| http://dx.doi.org/10.1016/j.bmcl.2012.04.071 | DOI Listing |
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