A bioassay-guided fractionation and chemical investigation of the MeOH extract from the twigs of
Lindera glauca (SIEB. et ZUCC.) BLUME resulted in the isolation and identification of six lignans (
1–
6) including three new lignan derivatives, named linderuca A (
1), B (
2), and C (
3). The structures of the new compounds (
1–
3) were determined on the basis of spectroscopic analyses, including two dimensional NMR and circular dichroism (CD) spectroscopy studies. The cytotoxic activities of the isolates (
1–
6) were evaluated by determining their inhibitory effects on human tumor cell lines. Compounds
1–
5 showed antiproliferative activities against A549, SK-OV-3, SK-MEL-2, and HCT-15 cell lines with IC
50 values of 7.79–29.42 µM. Based on the understanding that inflammation is a crucial cause of tumor progression, we also investigated the anti-inflammatory activities of the isolates (
1–
6) in the lipopolysaccharide-stimulated murine microglia BV-2 cell line by measuring nitric oxide (NO) levels. The new lignans (
1–
3) significantly inhibited NO production with IC
50 values of 12.10, 9.48, and 9.87 µM, respectively, without cytotoxicity.
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