One new compound, styrene dimer-type listeanol-4-O-α-ʟ-rhamnopyranosyl-(1→4)-β-ᴅglucopyranoside (1), and four known compounds namely listeanol (2), isorhapotigenin (3), genetifolin E (4), gnetifolin K (5) were isolated from the methanolic extract from the aerial part of the Gnetum montanum Markgr. in Vietnam. Their chemical structures were determined by modern spectroscopic methods (NMR and HR-ESI-MS) and comparison with those of published data. These compounds were evaluated for their anti-inflammatory and cytotoxic activities. Among them, compound 3 exhibited the NO inhibitory production on RAW264.7 cell line, and inhibited the HepG2 cell line with respective IC50 values of 79.88 ± 5.51 (µg/mL) (L-NMMA 7.90 ± 0.63 µg/mL), and 63.48 ± 3.63 (µg/mL) (Ellipticine 0.40 ± 0.01 µg/mL).