Ethyl 2,4,6-trihydroxybenzoate, a natural product isolated and purified from the herbs of Celtis biondii, suppresses cellular cholesterol accumulation in a dose-dependent manner and induces the transcriptional activation of LXR-α/-β-responsive genes, and 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.