The Journal of Steroid Biochemistry and Molecular Biology
PaperFK143, a novel nonsteroidal inhibitor of steroid 5α-reductase: (1) In vitro effects on human and animal prostatic enzymes
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2020, European Journal of Medicinal ChemistryRepurposing steroidogenesis inhibitors for the therapy of neuropsychiatric disorders: Promises and caveats
2019, NeuropharmacologyCitation Excerpt :MK-386 selectively reduces DHT levels in sebum without affecting its concentrations in semen (Schwartz et al., 1997). Unlike the competitive inhibition of finasteride, FK-143 showed robust inhibition of both human and rat 5αR1 in a noncompetitive fashion (Hirosumi et al., 1995). Bexlosteride was developed as a treatment for prostate cancer (Hirsch et al., 1993; Neubauer et al., 1996); in Phase I and II clinical trials, the substance was found to be safe and well-tolerated.
Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3
2014, Bioorganic and Medicinal ChemistryCitation Excerpt :This experiment was carried out twice under the same conditions. The activity of the 5α-reductase type 1 and 2 were determined by following the conversion of T to DHT, as previously described.21,22 The reagent mixture (final volume, 1 mL) contained 1 mM of DTT in 40 mM sodium phosphate buffer (pH 8.0 for type 1; pH 6.5 for type 2), 2 nM [1,2,6,73H] T, 6.31 μM T (for type 1), and 2 mM NADPH.
Bioactive withanolides from Withania obtusifolia
2014, Phytochemistry LettersCitation Excerpt :MIC of each compound was measured in triplicate and was defined as the lowest concentration of drug resulting in a complete absence of turbidity compared with the drug-free control. The in vitro 17β-HSD and 5α-R activity assays were carried out using the membrane fraction obtained from human prostate homogenates, as described previously (Cabeza et al., 2009, 2011; Hirosumi et al., 1995). Phytochemical investigation of the ethanolic extract of the leaves of W. obtusifolia resulted in the isolation of seven withanolides (1–7), namely obtusifonolide (1), sitoindoside IX (2), 6α-chloro-5β-hydroxy withaferin A (3), isowithanone (4), 2,3-dihydro-3-ethoxywithaferin A (5), daturataturin A (6), and withaferin A (7).
New steroidal lactones as 5α-reductase inhibitors and antagonists for the androgen receptor
2011, Journal of Steroid Biochemistry and Molecular BiologyCitation Excerpt :The suspension, 5 mg of protein/mL for human prostates, determined by the Bradford's method [14] was used as source of 5α-reductase. The enzyme 5α-reductase was assayed as previously described [16,17]. The reaction mixture for human prostate contained: 1 mM dithiothreitol, sodium phosphate buffer 40 mM, at pH 6.5, 2 mM, NADPH, 2 nM [1,2,6,7-3H]T [16] in a final volume of 1 mL.