Inhibitors of 5α-reductase type I in LNCaP cells from the roots of Angelica koreana

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

doi:10.1055/s-2002-20258

Inhibitors of 5α-reductase type I in LNCaP cells from the roots of Angelica koreana

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

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

34 Scopus citations

Abstract

A prenylated coumarin, osthenol (1) and a sesquiterpene, bisabolangelone (2) have been isolated as active principles with 5α-reductase type 1 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 5α-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.

Original language	English
Pages (from-to)	162-163
Number of pages	2
Journal	Planta Medica
Volume	68
Issue number	2
DOIs	https://doi.org/10.1055/s-2002-20258
State	Published - 2002

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title = "Inhibitors of 5α-reductase type I in LNCaP cells from the roots of Angelica koreana",

abstract = "A prenylated coumarin, osthenol (1) and a sesquiterpene, bisabolangelone (2) have been isolated as active principles with 5α-reductase type 1 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 5α-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.",

author = "Seo, {Eun Kyoung} and Kyeong, {Ho Kim} and Min, {Ki Kim} and Cho, {Myung Haing} and Choi, {Eun Wook} and Kim, {Ki Nam} and Woongchon Mar",

year = "2002",

doi = "10.1055/s-2002-20258",

language = "English",

volume = "68",

pages = "162--163",

journal = "Planta Medica",

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T1 - Inhibitors of 5α-reductase type I in LNCaP cells from the roots of Angelica koreana

AU - Seo, Eun Kyoung

AU - Kyeong, Ho Kim

AU - Min, Ki Kim

AU - Cho, Myung Haing

AU - Choi, Eun Wook

AU - Kim, Ki Nam

AU - Mar, Woongchon

PY - 2002

Y1 - 2002

N2 - A prenylated coumarin, osthenol (1) and a sesquiterpene, bisabolangelone (2) have been isolated as active principles with 5α-reductase type 1 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 5α-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.

AB - A prenylated coumarin, osthenol (1) and a sesquiterpene, bisabolangelone (2) have been isolated as active principles with 5α-reductase type 1 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 5α-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.

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JO - Planta Medica

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ER -

Inhibitors of 5α-reductase type I in LNCaP cells from the roots of Angelica koreana

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