The 5α-Reductase Inhibitory Components from Heartwood of Artocarpus incisus: Structure-Activity Investigations

Abstract

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.

Key words

Artocarpus incisus L. f. - Moraceae - heartwood - 5α-reductase inhibitor - structure-activity relationship

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