Two new phenolic glycosides (<b>1-2</b>), along with six existing compounds (<b>3-8</b>), were isolated from the ethanolic extract of <i>Ilex pubescens</i> roots, a traditional folk medicine. These structures were determined using HR-ESI-MS, IR, UV, and NMR (including 1 D, 2 D-NMR). The anti-inflammatory activities of three phenolic glycosides (<b>1-3</b>) were evaluated in the human HepG2 cell lines. The results showed that compound <b>3</b> could induce P-gp and BCRP expression through the Nrf2-mediated pathway.