The methanol extract of heartwood of Artocarpus incisus showed potent 5α-reductase inhibitory activity. We investigated the 5α-reductase inhibitory effects of nine compounds isolated from A. incisus. Chlorophorin (IC50 = 37 μM) and artocarpin (IC50 = 85 μM) showed more potent inhibitory effects than did α-linolenic acid, which is known as a naturally occurring potent inhibitor. Structure-activity investigations suggested that the presence of an isoprene substituent (prenyl and geranyl) would enhance 5α-reductase inhibitory effects.
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