Trilostane, an orally active inhibitor of steroid biosynthesis.

Abstract:

:Trilostane is a competitive inhibitor of 3beta-hydroxysteroid dehydrogenase. In vitro, the drug inhibits conversion of pregnenolone to progesterone but does not alter conversion of cholesterol to pregnenolone nor progesterone to corticoid hormones. When given orally to rats, trilostane inhibits corticosterone and aldosterone production and elevates circulating levels of pregnenolone at doses lower than those that produce adrenal hypertrophy or inhibit gonadal steroidogenesis.

journal_name

Steroids

journal_title

Steroids

authors

Potts GO,Creange JE,Hardomg HR,Schane HP

doi

10.1016/0039-128x(78)90010-7

subject

Has Abstract

pub_date

1978-09-01 00:00:00

pages

257-67

issue

2

eissn

0039-128X

issn

1878-5867

pii

0039-128X(78)90010-7

journal_volume

32

pub_type

杂志文章

相关文献

STEROIDS文献大全
  • Antidepressant effects of magnolol in a mouse model of depression induced by chronic corticosterone injection.

    abstract::Evidence showed that the stress hormone corticosterone (CORT) injection resulted in dysregulation of the hypothalamic-pituitary-adrenal (HPA) axis implicated in major depressive disorder. Magnolol, main constituent identified in the barks of Magnolia officinalis, exerted antidepressant effects in a rat model of depres...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2018.03.005

    authors: Bai Y,Song L,Dai G,Xu M,Zhu L,Zhang W,Jing W,Ju W

    更新日期:2018-07-01 00:00:00

  • Quantification of steroid conjugates using fast atom bombardment mass spectrometry.

    abstract::Fast atom bombardment/mass spectrometry or liquid secondary ion mass spectrometry provides the capability for direct analysis of steroid conjugates (sulfates, glucuronides) without prior hydrolysis or derivatization. During the analysis of biologic extracts, limitations on the sensitivity of detection arise from the p...

    journal_title:Steroids

    pub_type: 杂志文章,评审

    doi:10.1016/0039-128x(90)90014-3

    authors: Gaskell SJ

    更新日期:1990-10-01 00:00:00

  • Inhibition of 3beta-hydroxysteroid dehydrogenase-isomerase in mouse adrenal cells: a direct effect of testosterone.

    abstract::Gonadal steroids modulate adrenal gland size and function in a variety of species, and our previous studies demonstrate that circulating androgens suppress 3beta-hydroxysteroid dehydrogenase-isomerase (3betaHSD) activity in the adrenal cortex of male mice. The present study tests the hypothesis that androgens have a d...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(02)00023-5

    authors: Stalvey JR

    更新日期:2002-07-01 00:00:00

  • In vitro effects of RU486 on proliferation and differentiation capabilities of human bone marrow mesenchymal stromal cells.

    abstract::Although exogenous glucocorticoids (GC) play a role in the regulation of bone marrow mesenchymal stem/stromal cells (MSCs) proliferation and differentiation, the function of endogenous GC is not well understood. The purpose of this study was to investigate the effect of the blockage of endogenous GC using RU486, an an...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2011.10.017

    authors: Yu Y,Wei N,Stanford C,Schmidt T,Hong L

    更新日期:2012-01-01 00:00:00

  • Regulation of steroid production and its function within the corpus luteum.

    abstract::During the second half of the luteal phase, the human corpus luteum becomes responsive to regular luteinizing hormone (LH) pulses. These LH pulses stimulate progesterone secretion tonically, and during this tonic stimulation, additional LH-independent progesterone pulses occur, which are particularly pronounced in wom...

    journal_title:Steroids

    pub_type: 杂志文章,评审

    doi:10.1016/s0039-128x(98)00037-3

    authors: Wuttke W,Theiling K,Hinney B,Pitzel L

    更新日期:1998-05-01 00:00:00

  • Estrogen receptor signaling pathways in human non-small cell lung cancer.

    abstract::Lung cancer is the most common cause of cancer mortality in male and female patients in the US. The etiology of non-small cell lung cancer (NSCLC) is not fully defined, but new data suggest that estrogens and growth factors promote tumor progression. In this work, we confirm that estrogen receptors (ER), both ERalpha ...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2006.11.019

    authors: Márquez-Garbán DC,Chen HW,Fishbein MC,Goodglick L,Pietras RJ

    更新日期:2007-02-01 00:00:00

  • Invalidation of a commercially available human 5α-dihydrotestosterone immunoassay.

    abstract::Enzyme immunoassays (EIA) are commonly utilized for the evaluation of androgens in biological fluids; however, careful consideration must be given to cross-reactivity with other endogenous sex-steroid hormones. Our purpose was to determine the validity of a commonly-utilized commercially-available dihydrotestosterone ...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2013.08.013

    authors: Yarrow JF,Beck DT,Conover CF,Beggs LA,Goldberger BA,Borst SE

    更新日期:2013-12-11 00:00:00

  • A paradox: elevated 21-hydroxypregnenolone production in newborns with 21-hydroxylase deficiency.

    abstract::21-Hydroxypregnenolone and its metabolite 5-pregnene-3 beta, 20 alpha 21-triol have been measured in the sulfate fraction of neonatal urine. These two steroids are the major two 21-hydroxylated 5-pregnenes produced by neonates and are almost exclusively excreted as disulfates. The excretions of these steroids by norma...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(87)90006-7

    authors: Shackleton CH,Homoki J,Taylor NF

    更新日期:1987-04-01 00:00:00

  • Structural classification of steroid-binding sites on proteins by coarse-grained atomic environment and its correlation with their biological function.

    abstract::Steroid hormone is extensively used for transmitting variety of biological signals in organisms. Natural steroid hormone is synthesized from cholesterol in adrenal cortex and in sexual gland in vertebrates. Appropriately dosed synthetic steroid hormones can be used for medication. Despite their positive effects as med...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2015.01.015

    authors: Hori-Tanaka Y,Yura K,Takai-Igarashi T,Tanaka H

    更新日期:2015-04-01 00:00:00

  • Synthetic approaches toward total synthesis of 12 beta-methyl- and 12-methylene-19-norpregnanes.

    abstract::The effect of a substituent in the 12-position of progestagens was studied. To this end, various approaches toward the preparation of 12 beta-alkyl- and 12-alkylidenenorpregnanes were investigated. Eventually, the desired compounds 17 beta-hydroxy-12 beta-methyl-18a-homo-19-nor-17 alpha-pregn-4-en-20-yn-3-one (37) and...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(92)90020-a

    authors: Broess AI,van Vliet NP,Groen MB,Hamersma H

    更新日期:1992-11-01 00:00:00

  • Characterization of desoxymethyltestosterone main urinary metabolite produced from cultures of human fresh hepatocytes.

    abstract::Desoxymethyltestosterone (DMT; 17β-hydroxy-17α-methyl-5α-androst-2-ene) is a designer steroid present in hormonal supplements distributed illegally as such or in combination with other steroids, for self-administration. It figures on the list of substances prohibited in sports and its detection in athlete's urine samp...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2012.02.008

    authors: Gauthier J,Poirier D,Ayotte C

    更新日期:2012-05-01 00:00:00

  • Interleukins 1α and 1β as regulators of steroidogenesis in human NCI-H295R adrenocortical cells.

    abstract::Inflammatory cytokines interleukin-1 (IL-1) and tumor necrosis factor-α (TNF-α) regulate the activity of the hypothalamo-pituitary-adrenal (HPA) axis at several levels. Although hypothalamic CRH secretion may be the primary mechanism by which these cytokines activate the HPA axis, IL-1 expression is increased within t...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2011.04.018

    authors: Tkachenko IV,Jääskeläinen T,Jääskeläinen J,Palvimo JJ,Voutilainen R

    更新日期:2011-09-01 00:00:00

  • A novel sterol from Chinese truffles Tuber indicum.

    abstract::From the fruiting bodies of Ascomycetes Tuber indicum, a new steroidal glucoside with polyhydroxy ergosterol nucleus, tuberoside (2), has been isolated along with additional four known ergosterol derivatives, (22E, 24R)-ergosta-7, 22-dien-3beta, 5alpha, 6beta-triol (1), 5alpha, 8alpha-epidioxy-(22E, 24R)-ergosta-6, 22...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(01)00105-2

    authors: Jinming G,Lin H,Jikai L

    更新日期:2001-10-01 00:00:00

  • Isolation and structure of a cytotoxic epoxy sterol from the marine mollusc Planaxis sulcatus.

    abstract::A novel epoxy sterol isolated from the marine mollusc Planaxis sulcatus has been identified as 9 alpha,11 alpha-epoxycholest-7-ene-3 beta,5 alpha,6 beta-triol by spectrometric methods. ...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(88)90216-4

    authors: Alam M,Sanduja R,Weinheimer AJ

    更新日期:1988-07-01 00:00:00

  • Steroidal alkenylphosphonates via palladium-catalyzed coupling reactions.

    abstract::The palladium-catalyzed coupling of various 17-iodo-delta 16 steroids (17-iodo-androst-16-ene, 17-iodo-4-methyl-4-aza-androst-16-en-3-one, and 17-iodo-4-aza-androst-16-en-3-one) with dialkyl phosphites (dimethyl phosphite, diethyl phosphite, and diisopropyl phosphite) was examined in detail. The only successful condit...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(95)00121-6

    authors: Skoda-Földes R,Kollár L,Horváth J,Tuba Z

    更新日期:1995-12-01 00:00:00

  • Biotransformation of progestonic hormone dydrogesterone with Macrophomina phaseolina, and study of the effect of biotransformed products on phagocytes oxidative burst.

    abstract::Biotransformation of a synthetic progestonic hormone dydrogesterone (1), C21H28O2, with a plant pathogenic fungus Macrophomina phaseolina yielded two new 2 and 3, and a known 4 metabolites. These analogues were identified as, 3β,11α-dihydroxy-5β,9β,10α-pregna-7-ene-6,20-dione (2), 15β-hydroxy-9β,10α-pregna-4,6-diene-3...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2018.12.009

    authors: Wajid A,Ahmad MS,Yousuf S,Atia-Tul-Wahab,Jabeen A,Atta-Ur-Rahman,Choudhary MI

    更新日期:2019-03-01 00:00:00

  • Steroid delta 4-5 beta-reductase in human mammary tumors.

    abstract::Steroid delta 4-5 alpha- and delta 4-5 beta-reductase activity was determined in 16 human mammary tumors and 8 DMBA-induced rat mammary tumors using a spectrophotometric assay. Steroid delta 4-5 alpha-reductase was present in all tumors investigated while delta 4-5 beta-reductase was detected in only 6 estrogen recept...

    journal_title:Steroids

    pub_type: 历史文章,杂志文章

    doi:10.1016/s0039-128x(79)80010-0

    authors: Abul-Hajj YJ

    更新日期:1979-01-01 00:00:00

  • Presence of 11 beta-hydroxysteroid dehydrogenase in human semen: evidence of correlation with semen characteristics.

    abstract::11 beta-hydroxysteroid dehydrogenase (11 beta-HSD), the enzyme that catalyzes the conversion of biologically active glucocorticoids to their inactive metabolites, was shown to be located exclusively in Leydig cells of the rat testis, and its appearance was associated with the developmental rise in testosterone. Thus, ...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(96)00225-5

    authors: Nacharaju VL,Muneyyirci-Delale O,Khan N

    更新日期:1997-03-01 00:00:00

  • A facile synthesis of 5 beta-cholestane-3 alpha,7 alpha,12 alpha,25-tetrol.

    abstract::A convenient procedure for the synthesis of 5 beta-cholestane-3 alpha,7 alpha,12 alpha,25-tetrol via a modified homologation sequence of the intermediate 3 alpha,7 alpha,12 alpha-triformyloxy-24-oxo-25-diazo-25-homo-5 beta-cholane involving a homogeneous medium is described. This involves treating the intermediate alp...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(80)90144-0

    authors: Dayal B,Bagan E,Speck J,Salen G

    更新日期:1980-04-01 00:00:00

  • Androstenedione and testosterone biosynthesis by the adrenal cortex of the horse.

    abstract::An homogenate from cortical tissue of mare adrenals was incubated in the presence of tritiated pregnenolone. The (3H) androstenedione and the (3H) testosterone synthesized during the incubation were extracted, purified, and co-crystallized to constant specific activity in the presence of unlabeled carriers. The rate o...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(84)90033-3

    authors: Silberzahn P,Rashed F,Zwain I,Leymarie P

    更新日期:1984-02-01 00:00:00

  • Evidence for a new biologic pathway of androstenedione synthesis from 11-deoxycortisol.

    abstract::17-Hydroxyprogesterone is a well-known precursor of androstenedione in adrenal biosynthesis. This study using sheep adrenal incubations demonstrates that 11-deoxycortisol, the precursor of cortisol synthesis, also can be a precursor of androstenedione. Indeed, our data show that androstenedione synthesis is negatively...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(91)90112-9

    authors: Auzéby A,Bogdan A,Touitou Y

    更新日期:1991-01-01 00:00:00

  • Serum 11-deoxycorticosterone levels in adrenal-regeneration hypertension under conditions of quiescence and stress.

    abstract::A time course study to measure adrenal cortical function was undertaken for the period prior to the development of hypertension until the onset of hypertension in the adrenal-regeneration hypertension (ARH) model. Quiescent rat kills were used so that all adrenal cortical parameters investigated would reflect basal or...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(75)90090-2

    authors: Bergon L,Gallant S,Brownie AC

    更新日期:1975-03-01 00:00:00

  • Anabolic hormone profiles in elite military men.

    abstract::We recently characterized the awakening responses and daily profiles of the catabolic stress hormone cortisol in elite military men. Anabolic hormones follow a similar daily pattern and may counteract the catabolic effects of cortisol. This companion report is the first to characterize daily profiles of anabolic hormo...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2016.04.001

    authors: Taylor MK,Kviatkovsky SA,Hernández LM,Sargent P,Segal S,Granger DA

    更新日期:2016-06-01 00:00:00

  • Predictive algorithms for adjuvant therapy: TransATAC.

    abstract::Estrogen receptor (ER) positive primary breast cancers have a wide range of clinical outcomes. Prediction of the likely course of the disease aids treatment decision-making. In the translational arm of the ATAC (anastrozole or tamoxifen alone or combined) trial (TransATAC) we have assessed individual and multiparamete...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2011.02.032

    authors: Dowsett M,Salter J,Zabaglo L,Mallon E,Howell A,Buzdar AU,Forbes J,Pineda S,Cuzick J

    更新日期:2011-07-01 00:00:00

  • Differential binding of dexamethasone to ammonium sulfate precipitates of human adipose tissue cytosols.

    abstract::Saturation analysis of the binding of [3H]dexamethasone [( 3H]DEX) to ammonium sulfate precipitates (ASPs) confirmed the presence of a limited-capacity, high-affinity binder in human adipose tissue cytosols. Various non-radioactive steroids competed with [3H]DEX for binding to the ASPs in the following sequence: dexam...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(87)90091-2

    authors: Miller LK,Kral JG,Strain GW,Zumoff B

    更新日期:1987-06-01 00:00:00

  • Ovulation: a multi-gene, multi-step process.

    abstract::The luteinizing hormone (LH) surge initiates a cascade of proteolytic events that control ovulation. One of the genes induced by LH is the progesterone receptor (PR). Because mice with a mutant PR gene (PRKO) fail to ovulate and are infertile, we have used them as a model in which to determine PR target genes that mig...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(00)00114-8

    authors: Robker RL,Russell DL,Yoshioka S,Sharma SC,Lydon JP,O'Malley BW,Espey LL,Richards JS

    更新日期:2000-10-01 00:00:00

  • Glucocorticoid receptor signaling in the eye.

    abstract::Glucocorticoids (GCs) are essential steroid hormones that regulate numerous metabolic and homeostatic functions in almost all physiological systems. Synthetic glucocorticoids are among the most commonly prescribed drugs for the treatment of various conditions including autoimmune, allergic and inflammatory diseases. G...

    journal_title:Steroids

    pub_type: 杂志文章,评审

    doi:10.1016/j.steroids.2017.11.002

    authors: Sulaiman RS,Kadmiel M,Cidlowski JA

    更新日期:2018-05-01 00:00:00

  • NFκB pathway is down-regulated by 1α,25(OH)(2)-vitamin D(3) in endothelial cells transformed by Kaposi sarcoma-associated herpes virus G protein coupled receptor.

    abstract::We have previously demonstrated that 1α,25 dihydroxy-vitamin D(3) (1α,25(OH)(2)D(3)) has antiproliferative effects on the growth of endothelial cells transformed by the viral G protein-coupled receptor associated to Kaposi sarcoma (vGPCR). In this work, we have investigated whether 1α,25(OH)(2)D(3) exerts its growth i...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2012.05.006

    authors: Gonzalez-Pardo V,D'Elia N,Verstuyf A,Boland R,Russo de Boland A

    更新日期:2012-09-01 00:00:00

  • Steroidal saponins from Raphia vinifera and their cytotoxic activity.

    abstract::Phytochemical analysis of the fruits of Raphia vinifera led to the isolation of four new steroidal saponins (1-4), along with six known secondary metabolites (6-10). The structures of the isolated compounds were determined based on the analyses of NMR and mass spectrometric data, and chemical degradation reactions. Am...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2020.108724

    authors: Chi GF,Sop RVT,Mbaveng AT,Omollo Ombito J,Fotso GW,Nguenang GS,Kuete V,Efferth T,Ngadjui BT

    更新日期:2020-11-01 00:00:00

  • Quantification of endogenous testosterone and dihydrotestosterone in fetal tissues from male guinea-pig.

    abstract::Testosterone (17 beta -hydroxy-4-androsten-3-one ; T) and dihydrotestosterone (17 beta -hydroxy-5 alpha -androstan-3-one ; DHT) concentrations were determined by radioimmunoassay in different fetal tissues taken from male guinea-pigs. Androgen concentrations were maximal in the components of the Wolffian duct (vas def...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(81)90032-5

    authors: Rigaudière N

    更新日期:1981-08-01 00:00:00