Various extracts of aerial parts of Varthemia (
Varthemia iphionoides Boiss) were investigated for radical-scavenging activity, antioxidative activity, and porcine pancreas α-amylase inhibitory activity. The ethanol and water extracts showed a pronounced 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activity, with inhibition of about 90% at a concentration of 100 μg/ml, and α-amylase inhibitory activity of about 70% at a concentration of 200 μg/ml by the 2-chloro-4-nitrophenyl α-maltotrioside (CNP-G
3) degradation method. The ethanol extract was purified by column chromatography to give seven 3-methoxyflavones (
1–
7) and eudesmane sesquiterpene, selina-4,11(13)-dien-3-on-12-oic acid (
8). The structures of these compounds were established by NMR, MS, and UV spectroscopy. Of 3-methoxyflavones, 5,7,4′-trihydroxy-3,6-dimethoxyflavone (
1), 5,7,4′-trihydroxy-3,3′-dimethoxyflavone (
2), and 5,4′-dihydroxy-3,7,3′-trimethoxyflavone (3,7,3′-tri-
O-methyl-quercetin) (
7) exhibited pronounced radical-scavenging activity. The antioxidative activity in the linoleic acid system was considerable in compounds
1,
2, and 5,4′-dihydroxy-3,6,7-trimethoxyflavone (
4). Compounds
1,
2,
4,
5 (5,7,4′-trihydroxy-3-methoxyflavone), and
6 (5,4′-dihydroxy-3,7-dimethoxyflavone) showed markedly high inhibitory activity against porcine pancreas α-amylase. Eudesmane sesquiterpene did not show any activity.
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