A cytochemical section bioassay for plasma trilostane: an orally active inhibitor of 3β-hydroxysteroid dehydrogenase activity
作者： R. J. EARNSHAW , R. MITCHELL , W. R. ROBERTSON
DOI: 10.1111/J.1365-2265.1984.TB00131.X
关键词: Internal medicine 、 In vivo 、 Endocrinology 、 Enzyme inhibitor 、 Serial dilution 、 Trilostane 、 Corpus luteum 、 Chemistry 、 Androstenedione 、 Dehydrogenase 、 Bioassay
摘要: SUMMARY Trilostane is a competitive inhibitor of 3β-hydroxysteroid dehydrogenase activity in vitro and an orally active steroidogenesis vivo. A cytochemical section bioassay for this drug (4α, 5-epoxy-17β-hydroxy-3-oxo-5α-androstane-2α-carbonitrile) human plasma has been developed. The assay based upon the inhibition (3β-HSD) corpus luteum unfixed tissue sections (6 μm) mature dioestrous rat ovary. Trilostane extracted from by simple chloroform procedure. stanuard curve (0·15–2·5 μmol/I pure trilostane) exhibits four-fold change 3β-HSD constructed presence extract control pools. detection limit 2μmol/I trilostane after allowing dilution effects recovery losses. This level gives significantly different response zero quality (P 2 μmol/1. Intra- inter-assay coefficients variation using both controls unknown samples are 4% (n= 15) 13·9% 27) respectively. Recovery 80·9% 13) 79·10% 10) containing 12 4·8 μmol/1 Dilutions (up to 1:5) extracts parallel standard throughput approximately 16 samples/week technician. Testosterone, oestradiol, oestriol, dehydroepiandros-terone (DHEA), DHEA-sulphate, progesterone, cortisol, androstenedione dexamethasone (all at 1 μmol/1) were without effect on assay. It concluded that suitable assaying plasma.
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