Inhibitors of 5alpha -reductase type I in LNCaP cells from the roots of Angelica koreana.
A prenylated coumarin, osthenol (1) and a sesquiterpene, bisabolangelone (2) have been isolated as active principles with 5alpha-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 5alpha-reductase type I in LNCaP cells with an IC50 value of 0.1 microg/ml, which is about 200 times more potent than the positive control, finasteride (IC50 = 19.8 microg/ml). Bisabolangelone also inhibited the activity of 5alpha-reductase type I in LNCaP cells (IC50 = 11.6 microg/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 alpha-reductase type I. In addition, four compounds isooxypeucedanin, oxypeucedanin hydrate, oxypeucedanin and isoimperatorin were also isolated and found to be inactive in the 5alpha-reductase assay systems used in the present study.
Seo
Eun-Kyoung
EK
Kim
Kyeong Ho
KH
Kim
Min Ki
MK
Cho
Myung-Haing
MH
Choi
EunWook
E
Kim
KiNam
K
Mar
Woongchon
W
D013741:3-Oxo-5-alpha-Steroid 4-Dehydrogenase / Q000187:drug effects*; D058891:5-alpha Reductase Inhibitors; D029969:Angelica; D003374:Coumarins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018120:Finasteride / Q000494:pharmacology; D011564:Furocoumarins / Q000494:pharmacology; D006801:Humans; D008297:Male; D008518:Medicine, East Asian Traditional; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013739:Testosterone / Q000031:analogs & derivatives / Q000378:metabolism; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000378:metabolism
D058891:5-alpha Reductase Inhibitors; D003374:Coumarins; D011564:Furocoumarins; D010936:Plant Extracts; D012717:Sesquiterpenes; C455067:bisabolangelone; C055542:isoimperatorin; D013739:Testosterone; C114745:osthenol; D018120:Finasteride; C013915:boldenone; D013741:3-Oxo-5-alpha-Steroid 4-Dehydrogenase; C031535:oxypeucadanin