Inhibition of 17 alpha-hydroxylase/C17-C20 lyase by bifluranol and its analogues.
A simple assay for the measurement of the activities of both 17 alpha-hydroxylase and C17-C20 lyase is described. No extraction procedures are required. The separation of substrate and products is achieved using HPLC which allows the collection of the components of interest and the monitoring of the recovery of various steroids. Using this assay, bifluranol (known to show anti-prostatic activity in vivo) and some analogues were tested for inhibitory activity towards these enzyme activities. Each compound was active, although less potent than ketoconazole, and this activity may contribute towards the in vivo action.
Barrie
S E
SE
Institute of Cancer Research, Sutton, Surrey, U.K.
Rowlands
M G
MG
Foster
A B
AB
Jarman
M
M
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D005464:Fluorobenzenes; D006589:Hexestrol / Q000031:analogs & derivatives* / Q000494:pharmacology; D008190:Lyases / Q000037:antagonists & inhibitors*; D008297:Male; D008861:Microsomes / Q000201:enzymology; D011374:Progesterone / Q000302:isolation & purification; D051381:Rats; D011919:Rats, Inbred Strains; D013254:Steroid 17-alpha-Hydroxylase / Q000037:antagonists & inhibitors*; D013250:Steroid Hydroxylases / Q000037:antagonists & inhibitors*; D013737:Testis / Q000201:enzymology
D005464:Fluorobenzenes; D006589:Hexestrol; C017070:bifluranol; D011374:Progesterone; D013250:Steroid Hydroxylases; D013254:Steroid 17-alpha-Hydroxylase; D008190:Lyases