In vitro study of rat prostate 5 alpha-reductase activity and its inhibition
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 sy...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
1992
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| Sorozat: | INTERNATIONAL UROLOGY AND NEPHROLOGY
24 No. 2 |
| Tárgyszavak: | |
| doi: | 10.1007/BF02549642 |
| mtmt: | 1942097 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/32220 |
| Tartalmi kivonat: | 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. |
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| Terjedelem/Fizikai jellemzők: | 145-154 |
| ISSN: | 0301-1623 |