Sterically crowded trialkylsilyl ether derivatives for the analysis of steroid metabolites.

abstract：:A series of amphiphilic derivatives of (3β,17β)-3-hydroxyandrost-5-ene-17-carboxylic acid (1) with the polyamine spermine and three other diamines, 1,2-diaminoethane, piperazine and cadaverine, were synthesized and their antimicrobial activity and cytotoxicity were investigated. Among the target compounds, several one...

journal_title：Steroids

authors： Özdemir Z,Bildziukevich U,Šaman D,Havlíček L,Rárová L,Navrátilová L,Wimmer Z

更新日期：2017-12-01 00:00:00

abstract：:We describe a novel steroid, which we have named "Ionotropin". Its unique features are: [1] it has 23 carbon atoms and [2] it is a phosphocholine ester. There are no other known mammalian steroids with either structural feature. Ionotropin cross reacts with digoxin-specific antibodies and may be the long-sought, endog...

journal_title：Steroids

authors： Chasalow F,Pierce-Cohen L

更新日期：2018-08-01 00:00:00

abstract：:Contrary to the long-held postulate of steroid-hormone binding globulin action, these protein carriers of steroids are major players in steroid actions in the body. This manuscript will focus on our work with sex hormone binding globulin (SHBG) and corticosteroid binding globulin (CBG) and demonstrate how they are act...

journal_title：Steroids

authors： Caldwell JD,Jirikowski GF

更新日期：2014-03-01 00:00:00

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

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

更新日期：1984-02-01 00:00:00

abstract：:Bioconversion of the aromatase inhibitor formestane (4-hydroxyandrost-4-ene-3,17-dione) (1) by the fungus Rhizopus oryzae ATCC 11145 resulted in a new minor metabolite 3,5α-dihydroxyandrost-2-ene-4,17-dione (2) and the known 4β,5α-dihydroxyandrostane-4,17-dione (3) as the major product. The structural elucidation and ...

journal_title：Steroids

authors： Martin GD,Narvaez J,Bulmer R,Durrant MC

更新日期：2016-09-01 00:00:00

abstract：:Glucocorticoids are important regulators of metabolism and immune function. Synthetic glucocorticoids are extensively used for immunosuppression/anti-inflammatory therapy. Since the glucocorticoid receptor (GR) is central to most hormone effects; its in vivo regulation will influence hormone/drug action. An alternativ...

journal_title：Steroids

authors： DuBois DC,Sukumaran S,Jusko WJ,Almon RR

更新日期：2013-02-01 00:00:00

abstract：:Initial excretion studies with orally administered [monoethyl-1-3H] DES demonstrated the feces to be the principal mode of elimination of DES in the C3H mouse. Metabolic studies with tritiated DES and/or [UL-14C] DES were performed with orally dosed C3H high (MTV+) and low (MTV-) titer MMTV female mice. Extraction and...

journal_title：Steroids

authors： Helton ED,Gough BJ,King JW Jr,Thenot JP,Horning EC

更新日期：1978-04-01 00:00:00

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 aldo...

journal_title：Steroids

authors： Potts GO,Creange JE,Hardomg HR,Schane HP

更新日期：1978-09-01 00:00:00

abstract：:Cell cycle regulator p21(CIP1) has controversial biological effects in breast cancer since in spite of its role as cell cycle inhibitor and promoter of cellular senescence, it also induces cell proliferation and chemoteraphy resistance. We here explored the molecular mechanisms involved in progestin regulation of p21(...

journal_title：Steroids

authors： Diaz Flaqué MC,Vicario R,Proietti CJ,Izzo F,Schillaci R,Elizalde PV

更新日期：2013-06-01 00:00:00

abstract：:In this study, we assessed the rate of estradiol degradation via the 17 beta-hydroxysteroid dehydrogenase (HSD) enzyme in breast tumors from postmenopausal women. We initially studied the effects of time, level of enzyme activity, amount of tissue assayed, and substrate concentration on the linearity of conversion of ...

journal_title：Steroids

authors： Leszczynski D,Santner SJ,Feil PD,Santen RJ

更新日期：1988-03-01 00:00:00

abstract：:Two unnatural steroid sapogenins bearing a furospirostane side chain were prepared starting from the readily available spirostane sapogenins, tigogenin and diosgenin following a synthetic protocol that included: (i) introduction of a carbonyl group at position C-23, (ii) diacetoxyiodobenzene-induced F-ring contraction...

journal_title：Steroids

authors： Sánchez-Flores J,Romero-Ávila M,Rosado-Abón A,Flores-Álamo M,Iglesias-Arteaga MA

更新日期：2013-09-01 00:00:00

abstract：:Androstane brassinosteroid analogues with alpha-azido acid ester groups in position 17beta were synthesized from 2alpha,3alpha,17beta-trihydroxy-5alpha-androstan-6-one after the protection of the 2alpha,3alpha-diols upon treatment with the corresponding alpha-azido acid and the subsequent deprotection of the diol grou...

journal_title：Steroids

authors： Hnilickova J,Kohout L,Capdevila E,Esteve A,Vilaplana M,Molist M,Brosa C,Swaczynova-Oklestkova J,Slavikova B

更新日期：2010-12-01 00:00:00

abstract：:MDL 18,962 was shown to be a highly specific, potent (Ki = 3-4 nM), enzyme-activated inhibitor of aromatase with minimal intrinsic endocrine properties. The affinity of MDL 18,962 was higher for human and baboon placental aromatase than for rhesus placental or rodent ovarian aromatase. These species differences necess...

journal_title：Steroids

authors： Johnston JO

更新日期：1987-07-01 00:00:00

abstract：:The isolated perfused rat kidney allows a simultaneous kinetic study of both the renal metabolism and the urinary excretion of cortisol and its metabolites in the rat. In this system, cortisol was completely metabolized within 120 minutes. The main renal metabolites of cortisol (cortisone, 20 reduced cortisol and 20 r...

journal_title：Steroids

authors： Reach G,Nakane H,Nakane Y,Auzan C,Corvol P

更新日期：1977-11-01 00:00:00

abstract：:Adult female mice were adrenalectomized and ovariectomized and the concentration of Type I and Type II receptors in whole brain, kidney, and liver cytosol determined at various time thereafter by incubation with [3H]aldosterone (+ RU 26988 to prevent binding to Type II receptors) or [3H]dexamethasone, respectively. Ty...

journal_title：Steroids

authors： Luttge WG,Rupp ME

更新日期：1989-01-01 00:00:00

abstract：:The adverse effects of hypercortisolism on the human brain have been highlighted in previous studies of Cushing's disease (CD). However, the reversibility of brain damage after the resolution of hypercortisolism remains unclear. Thus, we studied the potential volumetric reversibility in biochemically remitted CD patie...

journal_title：Steroids

authors： Jiang H,Liu C,Pan SJ,Ren J,He NY,Sun YH,Bian LG,Yan FH,Yang WJ,Sun QF

更新日期：2019-11-01 00:00:00

abstract：:Two dimeric steroidal terephthalates derived from epimeric 4,5-seco-cholest-3-yn-5-ols were prepared starting from cholesterol in a five-step synthetic sequence. X-ray crystallography shows that the obtained compounds display novel supramolecular networks in the solid state in which the facial hydrophobicity of the st...

journal_title：Steroids

authors： Alarcón-Manjarrez C,Arcos-Ramos R,Álamo MF,Iglesias-Arteaga MA

更新日期：2016-05-01 00:00:00

abstract：:We assayed Type 1 (high K+) and Type 2 (high Na+) human breast cyst fluids for DHEA-S. When an antibody specific for the 3-sulfoconjugate end of DHEA-S was used, Type 1 cyst fluids (n = 18) showed a content of 114 +/- 68 micrograms/mL (mean +/- sigma) and Type 2 cyst fluids (n = 14) of 35 +/- 17 micrograms/mL (P less ...

journal_title：Steroids

authors： Chasalow FI,Blethen SL,Bradlow HL

更新日期：1988-09-01 00:00:00

abstract：:An enzyme immunoassay for estrone in swine serum was established. For this, beta-galactosidase from E. coli was conjugated through estrone-17 (O-carboxymethyl)oxime using a mixed anhydride reaction. The percentage of immunoreactive estrone-17 (O-carboxymethyl)oxime-beta-galactosidase conjugate was estimated to be abou...

journal_title：Steroids

authors： Tamamura F,Nakao T,Tsunoda N,Kawata K

更新日期：1982-06-01 00:00:00

abstract：:Two new sterols, (24E)-24-n-propylidenecholesterol and 24 epsilon-n-propylcholesterol, were isolated from a cultured marine Chrysophyte. Since most of the steroids found in marine invertebrates are unchanged or modified sterols of algal or symbiotic origin, the discovery of these two unusual sterols in a unicellular a...

journal_title：Steroids

authors： Rohmer M,Kokke WC,Fenical W,Djerassi C

更新日期：1980-02-01 00:00:00

abstract：:Ventral prostate was used as a system to study the nature and properties of microsomal androgen receptor. The endoplasmic reticulum from rat ventral prostate contains high-affinity, low-capacity binding sites for androgen that are intrinsic to this intracellular compartment. Microsomal androgen receptors are not due t...

journal_title：Steroids

authors： Steinsapir J,Muldoon TG

更新日期：1991-02-01 00:00:00

abstract：:In an endeavour to develop potent anti-tumor agents from diosgenin, a series of C-6 derived 1,2,3-triazolyl derivatives were designed and synthesized by employing Cu(I) catalyzed Huisgen 1,3-dipolar cycloaddition reaction of novel azides - (22R,25R)-6β-azidospirostan-3β,5α-diol and 6β-azido-7α-hydroxyspirosta-1,4-dien...

journal_title：Steroids

authors： Mironov ME,Oleshko OS,Pokrovskii MA,Rybalova TV,Pechurov VK,Pokrovskii AG,Cheresis SV,Mishinov SV,Stupak VV,Shults EE

更新日期：2019-11-01 00:00:00

abstract：:It has been shown that stress or disease-induced increases in plasma corticosterone result in diminished testosterone secretion from the testes. This article reviews investigations from our laboratories that explore the role of 11 beta-hydroxysteroid dehydrogenase (11 beta-OHSD) in this process. It is proposed that th...

journal_title：Steroids

authors： Monder C,Hardy MP,Blanchard RJ,Blanchard DC

更新日期：1994-02-01 00:00:00

abstract：:The hepatic metabolism of 3-oxoandrost-4-ene-17 beta-carboxylic acid (etienic acid), a probable acidic catabolite of deoxycorticosterone, was investigated using rats prepared with an external biliary fistula. Metabolic products were identified by GC-MS after hydrolysis with beta-glucuronidase and by proton nuclear mag...

journal_title：Steroids

authors： Radominska A,Little JM,Lester R,St Pyrek J

更新日期：1992-07-01 00:00:00

abstract：:Circulating levels (mean +/- SD) of estrone sulfate (E1S), estrone (E1) and estradiol-17 beta (E2) were measured in normal and cirrhotic postmenopausal women matched for body weight and age. In cirrhotic postmenopausal women, the E1S concentrations (201 +/- 46 pg/ml), while both E1 and E2 levels showed an increase (46...

journal_title：Steroids

authors： Jasonni VM,Bulletti C,Bolelli GF,Franceschetti F,Bonavia M,Ciotti P,Flamigni C

更新日期：1983-05-01 00:00:00

abstract：:Periodontitis is a complication of diabetes mellitus, and the two diseases are highly associated with the dysfunction of inflammatory mediators. 25-hydroxyvitamin D(3) (25(OH)D(3)) plays a pivotal role in inflammatory modulation, but little is known about its effects on the progression of diabetic periodontitis and th...

journal_title：Steroids

authors： Li H,Xie H,Fu M,Li W,Guo B,Ding Y,Wang Q

更新日期：2013-02-01 00:00:00

abstract：:In our effort to develop imaging agents for brain glucocorticoid receptors, we have prepared several novel glucocorticoids possessing a 2-methylsulfanyl-acetyl side chain. The synthesis was accomplished via a Mitsunobu reaction with thiobenzoic acid starting from cortisol, prednisolone, dexamethasone and triamcinolone...

journal_title：Steroids

authors： Wuest F,Carlson KE,Katzenellenbogen JA

更新日期：2008-01-01 00:00:00

abstract：:Estrogen levels in breast tumors of post-menopausal women are as much as 10 times higher than estrogen levels in plasma, presumably due to in situ formation of estrogen. The major source of estrogen in breast cancer cells may be conversion of estrone sulfate to estrone by the enzyme estrone sulfatase. Thus, inhibitors...

journal_title：Steroids

authors： Li PK,Chu GH,Guo JP,Peters A,Selcer KW

更新日期：1998-07-01 00:00:00

abstract：:The LNCaP-Fast Growing Colony (FGC) human prostate cancer cell line proliferates in response to the addition of dihydrotestosterone (DHT) 10(-10)-10(-8) M in charcoal-stripped serum-supplemented media. LNCaP-FGC cells will not attach or proliferate in serum-free conditions. LNCaP-FGC stock cultures were maintained in ...

journal_title：Steroids

authors： Kirschenbaum A,Ren M,Levine AC

更新日期：1993-09-01 00:00:00

abstract：:Corticosterone-and progesterone-binding activity were measured by saturation analysis, with dextran-charcoal separation, in plasma obtained from male and female rats, and a normal male and female human. In plasma from normal male and female rats, progesterone was much less effective than corticosterone in displacing 3...

journal_title：Steroids

authors： Calvano SE,Reynolds RW,Keith LD

更新日期：1980-09-01 00:00:00