Glaucic acid isolated from the root of Lindera glauca, was investigated by the biotransformation methods via the endophytic fungi, resulting in the production of five new glausesquiterpenes A‒E (1‒5), along with a known analogue 6. Their structures were elucidated based on spectroscopic methods and electronic circular dichroism (ECD) calculations. In the bioassays, glausesquiterpene A (1) showed good inhibitory activity of NO production in LPS-activated RAW 264.7 macrophages with an IC50 value of 20.1 µM than positive control (Indomethacin, IC50 24.1 µM). Further in vitro studies demonstrated that glausesquiterpene A significantly suppressed the protein expression of iNOS and COX-2 at the concentration of 25.0 µM.