Inhibitors of 5α -Reductase Type I in LNCaP Cells from the Roots of Angelica koreana

Eun-Kyoung Seo; Kyeong Ho Kim; Min Ki Kim; Myung-Haing Cho; Eun Wook Choi; Ki Nam Kim; Woongchon Mar

doi:10.1055/s-2002-20258

Planta Medica, Table of Contents

Planta Med 2002; 68(2): 162-163
DOI: 10.1055/s-2002-20258

Letter

Inhibitors of 5α -Reductase Type I in LNCaP Cells from the Roots of Angelica koreana

Eun-Kyoung Seo¹ , Kyeong Ho Kim² , Min Ki Kim² , Myung-Haing Cho³ , EunWook Choi⁴ , KiNam Kim⁴ , Woongchon Mar⁴

¹Natural Products Chemistry Laboratory, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea
²College of Pharmacy, Kangwon National University, Chunchon, Korea
³NIAST, RDA and College of Veterinary Medicine, Seoul National University, Suwon, Korea
⁴Natural Products Research Institute, Seoul National University, Seoul, Korea

Abstract

A prenylated coumarin, osthenol (1) and a sesquiterpene, bisabolangelone (2) have been isolated as active principles with 5α-reductase type I inhibitory effects in LNCaP cells from the roots of Angelica koreana Max. by bioassay-guided chromatographic fractionation. Osthenol exhibited a highly potent inhibitory activity on 5α-reductase type I in LNCaP cells with an IC₅₀ value of 0.1 μg/ml, which is about 200 times more potent than the positive control, finasteride (IC₅₀ = 19.8 μg/ml). Bisabolangelone also inhibited the activity of 5α-reductase type I in LNCaP cells (IC₅₀ = 11.6 μg/ml), indicating that these compounds are possible candidates for the development of new drugs to treat human endocrine disorders associated with overproduction of DHT by 5 α-reductase type I. In addition, four compounds isooxypeucedanin, oxypeucedanin hydrate, oxypeucedanin and isoimperatorin were also isolated and found to be inactive in the 5α-reductase assay systems used in the present study.

Full Text

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Prof. Ph. D. Woongchon Mar

Natural Products Research Institute

Seoul National University

Seoul 110-460

Korea

Phone: +82-2-740-8911

Fax: +82-2-3672-5488

Email: mars@snu.ac.kr