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J.Health Sci., 56(4), 451-455, 2010

-Research Letter-

Abietic Acid from Resina Pini of Pinus Species as a Testosterone 5α-Reductase Inhibitor

Seong-Soo Roh,a Moon-Ki Park,b and Yong-ung Kim*, b

aDepartment of Preparatory Oriental Medicine, College of Oriental Medicine, Daegu Haany University, 165 Sangdong, Suseong-gu, Daegu 706-060, Republic of Korea and bDepartment of Herbal Pharmaceutical Engineering, College of Herbal Bio-industry, Daegu Haany University, 290 Yugokdong, Gyeongsan-si, Gyeongsangbuk-do 712-715, Republic of Korea

The 50% ethanol extracts from Resina Pini of Pinus sp. (Pinaceae) showed more potent inhibitory activity against testosterone 5α-reductase prepared from rat prostate than those from several medicinal plants used for the treatment of androgen-dependent diseases such as benign prostatic hyperplasia. The fraction responsible for this activity was purified, and the active constituent was isolated and identified as abietic acid, a diterpene resin acid, which exhibited potent testosterone 5α-reductase inhibitory activity. Methyl abietate was substantially inactive against testosterone 5α-reductase, whereas other diterpene resin acids, pimaric acid and neoabietic acid, were as active as abietic acid against testosterone 5α-reductase, indicating that the negatively charged anionic carboxyl group on the molecule is an important structural moiety for the inhibitory activity. These findings suggest that a nonsteroidal anionic diterpene compound of natural origin may have the potential to act as a transition state analogue inhibitor of testosterone 5α-reductase in the treatment of androgen-dependent diseases.