In vitro study of rat prostate 5 alpha-reductase activity and its inhibition
| Autor: | I. Tóth, S. Scultéty, I. Faredin, J. Oszlánczy |
|---|---|
| Rok vydání: | 1992 |
| Předmět: |
Male
medicine.medical_specialty Antiandrogens Urology In Vitro Techniques Flutamide chemistry.chemical_compound 5-alpha Reductase Inhibitors 3-Oxo-5-alpha-Steroid 4-Dehydrogenase Prostate Internal medicine medicine Animals IC50 chemistry.chemical_classification business.industry Cyproterone acetate Androgen Antagonists Rats Inbred Strains Mifepristone Hormones Rats Endocrinology Enzyme medicine.anatomical_structure chemistry Nephrology Ketoconazole business medicine.drug |
| Zdroj: | International urology and nephrology. 24(2) |
| ISSN: | 0301-1623 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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