Abstract
A simple and rapid method of measuring 5 alpha-reductase (5 alpha-R) activity and of determining the kinetic parameters (KM and Vmax) of the enzyme is described. The 5 alpha-R activity in the homogenate of the prostate of Wistar rats aged 8-12 weeks was established, and the effects of natural and synthetic steroids and of non-steroidal antiandrogens (IC50) upon the 5 alpha-R activity were studied. Of the natural steroids, 17-OH-progesterone was found to have the highest inhibitory effect (IC50 = 1.35 microM), followed in decreasing order by progesterone (IC50 = 5.0 microM) and 4-androstene-3,17-dione (IC50 = 21.6 microM). Oestradiol-17 beta had practically no inhibitory effect. Of the synthetic steroids, 4-MA had the highest inhibitory effect (IC50 = 0.068 microM), followed by nortestosterone (IC50 = 7.4 microM) and RU-486 (Mifepristone) (IC50 = 115 microM). Even at 1000 microM, cyproterone acetate exerted no inhibitory effect. Of the nonsteroidal compounds, ketoconazole proved a weak inhibitor (IC50 = 115 microM), while flutamide was practically ineffective.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
