The inhibitory effects of 17 samples prepared from Thailand plants on 5α-reductase activity were examined. The acetone extract of leaves of Artocarpus altilis showed potent 5α-reductase inhibitory activity. Fractionation guided by 5α-reductase inhibition led to the isolation of 2-geranyl-2′,3,4,4′-tetrahydroxydihydrochalcone from the acetone extract of leaves of A. altilis. This compound showed more potent inhibitory effect (IC50 = 38 μM) than α-linolenic acid known as a naturally occurring potent inhibitor.
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