Investigation of pH and substituent effects on the distribution ratio of novel steroidal ring D- and A-fused arylpyrazole regioisomers and evaluation of their cell-growth inhibitory effects in vitro.

abstract：:Traditional interpretation of GC-MS output involved the semi-quantitative estimation of outstanding low or high specific metabolites and the ratio between metabolites. Here, we utilize a systems biology approach to steroid metabolomics of a complex steroid-related disorder, using an all-inclusive analysis of the stero...

journal_title：Steroids

authors： Vitkin E,Ben-Dor A,Shmoish M,Hartmann MF,Yakhini Z,Wudy SA,Hochberg Z

更新日期：2014-10-01 00:00:00

abstract：:We have previously shown that the photoactive 4-azasteroid, [1,2 3H]N-4(benzylbenzoyl)-3-oxo-4-aza-4-methyl-5alpha-androst an-17beta-carboxamide is an effective probe of rat steroid 5alpha-reductase (isozyme-1) (5alphaR-1). In the current investigation, PEG-fractionated (6.5%) detergent-solubilized preparations contai...

journal_title：Steroids

authors： Bhattacharyya AK,Wang M,Rajagopalan K,Taylor MF,Hiipakka R,Liao S,Collins DC

更新日期：1999-03-01 00:00:00

abstract：:A rapid and efficient synthesis of 6E-hydroximinosteroid homodimers is described. The two new compounds were linked at position 3 of the steroid nucleus via a ruthenium catalyzed cross-metathesis reaction. The cytotoxic activity of these compounds was evaluated in vitro on human lung carcinoma A549 (ATCC CCL-185), col...

journal_title：Steroids

authors： Rega M,Jiménez C,Rodríguez J

更新日期：2007-10-01 00:00:00

abstract：:The preparation of 9alpha, 11xi-tritiated 17alpha-ethinyl estradiol, mestranol, estradiol-17beta, and norethindrone are described. Estrone-3-methyl ether was employed as starting material, and ethinylation with lithium acetylide-ethylene diamine resulted in 95% mestranol. Demethylation of mestranol with boron tribro...

journal_title：Steroids

authors： Rao PN

更新日期：1971-08-01 00:00:00

abstract：:CGS 16949A inhibited the conversion of [4-14C]androstenedione (A) to [4-14C]estrone by human placental microsomes in a competitive manner (Ki = 1.6 nM). Aminoglutethimide, also a competitive inhibitor, had a Ki = 0.7 microM in this assay system. The Km for the aromatization of A was 0.11 microM. Using ovarian microsom...

journal_title：Steroids

authors： Steele RE,Mellor LB,Sawyer WK,Wasvary JM,Browne LJ

更新日期：1987-07-01 00:00:00

abstract：:In demyelinating or non-demyelinating neurodegenerative diseases, increased levels of 7-ketocholesterol (7KC), 7β-hydroxycholesterol (7β-OHC) and 24(S)-hydroxycholesterol (24S-OHC) can be observed in brain lesions. In 158N murine oligodendrocytes, 7KC triggers a complex mode of cell death defined as oxiapoptophagy, in...

journal_title：Steroids

authors： Nury T,Zarrouk A,Mackrill JJ,Samadi M,Durand P,Riedinger JM,Doria M,Vejux A,Limagne E,Delmas D,Prost M,Moreau T,Hammami M,Delage-Mourroux R,O'Brien NM,Lizard G

更新日期：2015-07-01 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：:Six naturally occurring C27 ecdysteroids were isolated and identified from the tobacco hornworm during pupal-adult development five days after peak titer of molting hormone activity. In order of decreasing quantities the hormones were: 20,26-dihydroxyecdysone, 3-epi-20-hydroxyecdysone, 20hydroxyecdysone, 3-epi-20,26-d...

journal_title：Steroids

authors： Kaplanis JN,Thompson MJ,Dutky SR,Robbins WE

更新日期：1979-09-01 00:00:00

abstract：:Although aldosterone production declines with age, so does the aldosterone metabolic clearance rate (MCR), and the net effect of age on the circulating level of aldosterone may be less than can be predicted from production rates alone. The effect of age on aldosterone production and plasma levels was studied in a grou...

journal_title：Steroids

authors： Pratt JH,Hawthorne JJ,Debono DJ

更新日期：1988-01-01 00:00:00

abstract：:(25S)-3-Oxocholesta-1,4-dien-26-oic acid (1) and a new (25S)-18-acetoxy-3-oxocholesta-1,4-dien-26-oic acid (2) were isolated from a soft coral Minabea sp. (cf. aldersladei) collected in North Sulawesi, Indonesia, together with two known cholic-acid-type compounds, 3-oxochol-1,4-dien-24-oic acid (3) and 3-oxochol-4-en-...

journal_title：Steroids

authors： Wang W,Lee JS,Nakazawa T,Ukai K,Mangindaan RE,Wewengkang DS,Rotinsulu H,Kobayashi H,Tsukamoto S,Namikoshi M

更新日期：2009-09-01 00:00:00

abstract：:A radioimmunoassay technique has been developed for the measurement of cortisol in a single methylene chloride extract of human plasma without chromatography. The antiserum, obtained by immunizing rabbits with cortisol-3-carboxymethyl-oxime conjugated to bovine serum albumin, had a high affinity (KA = 1.8 X 10(9) 1/mo...

journal_title：Steroids

authors： Dash RJ,England BG,Midgley AR Jr,Niswender GD

更新日期：1975-11-01 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：:The properties of 5-ene-3 beta hydroxysteroid oxidoreductase (3 beta-HSD) from human placental homogenates were studied in vitro. The apparent Michaelis constants for 3 beta-HSD with the substrates pregnenolone (delta 5P) and dehydroepiandrosterone (DHA) were 170 nM and nM respectively. The optimal pH for both these s...

journal_title：Steroids

authors： Yoshida N

更新日期：1979-01-01 00:00:00

abstract：:Data are presented on the urinary corticosteroid metabolic profile of the mouse strain 129/svJ. Through the use of GC/MS we have characterized, or tentatively identified corticosterone (Kendall's compound B) metabolites of both the 11beta-hydroxy and 11-carbonyl (compound A) series in urine. Full mass spectra of the m...

journal_title：Steroids

authors： Shackleton CH,Hughes BA,Lavery GG,Walker EA,Stewart PM

更新日期：2008-10-01 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：:1 alpha, 25-Dihydroxyvitamin D3 (1 alpha, 25-(OH)2D3) has been shown to rapidly increase cytosolic calcium in freshly isolated and cultured rat hepatocytes. The rise in cytosolic calcium is dependent on phospholipase A2 (PLA2) activation and cell alkalinization through the Na+/H+ antiport system. To further characteri...

journal_title：Steroids

authors： Rockwell JC,Sorensen AM,Baran DT

更新日期：1993-10-01 00:00:00

abstract：:Explants prepared from the neocortex and the fetal zone of the human fetal adrenal (gestational age 13 to 18weeks) were maintained under conditions of organ culture for 7 to 9 days during which time they were exposed to hACTH and various related peptides. Corticotrophic activity was monitored by the daily release of d...

journal_title：Steroids

authors： Branchaud CT,Goodyer CG,Hall CS,Arato JS,Silman RE,Giroud CJ

更新日期：1978-04-01 00:00:00

abstract：:The abundant expression of progesterone receptors (PR) in human meningiomas is well established. It is unknown, however, how PR expression is regulated, especially since estrogen receptors (ER) are virtually absent in these tumors. At the mRNA level, ER splice variants occur in meningioma but these appear not to be in...

journal_title：Steroids

authors： Blankenstein MA,Verheijen FM,Jacobs JM,Donker TH,van Duijnhoven MW,Thijssen JH

更新日期：2000-10-01 00:00:00

abstract：:18,20-Epoxy-11 beta,17 alpha,20 beta,21-tetrahydroxypregn-4-en-3-one was synthesized by the application of hypoiodite reaction to the cortisol acetonide. The intermediary 18-iodo derivative was converted to the 11-oxo steroid by chromic acid prior to silver ion-assisted solvolysis. Removal of the protective group with...

journal_title：Steroids

authors： Kurosawa T,Ikegawa S,Chiba H,Ito Y,Nakagawa S,Kobayashi K,Tohma M

更新日期：1992-09-01 00:00:00

abstract：:13beta-Ethyl-3-methoxy-17beta-ol-8,14-seco-1,3,5(10),8-gonatetraen-14-one (IIIa) was isolated and its participation in the well-known acidic cyclization process was established. ...

journal_title：Steroids

authors： Makk N,Tóth G,Tömörkény E

更新日期：1975-05-01 00:00:00

abstract：:The metabolism of testosterone (T) was studied in normal adult male rats using a constant infusion of trace amounts of the 3H-steroid into a tail vein for 3 h in order to attain a state of equilibrium. Samples of plasma, liver, kidney, prostate, seminal vesicles and muscle were analysed for 3H-testosterone, 3H-5alpha-...

journal_title：Steroids

authors： Lee DK,Bird CE,Clark AF

更新日期：1975-07-01 00:00:00

abstract：:The steroid nucleus is an interesting scaffold for the development of new therapeutic agents. Within the goal of identifying anticancer agents, new pregnane derivatives were prepared by using a sequence of liquid and solid-phase reactions. After we dehydrated epi-allopregnanolone in one step with diethylaminosulfur tr...

journal_title：Steroids

authors： Jegham H,Maltais R,Dufour P,Roy J,Poirier D

更新日期：2012-11-01 00:00:00

abstract：:We report the synthesis of 3 beta,15 beta,17 alpha-trihydroxy-5-pregnen-20- one (1) from 3 beta,15 beta-dihydroxy-5,16-pregnadien-20-one (11) in 7 steps using boronate derivatives as a means of protecting the 17,20-glycol side-chain of steroid intermediates. 16 alpha,17 alpha-Epoxy-3 beta,15 beta-dihydroxy-5- pregnen-...

journal_title：Steroids

authors： Joannou GE,Reeder AY

更新日期：1996-01-01 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：:Many flavonoids and isoflavonoids have anti-diabetic effects in animal models. However, the mechanisms that are involved are generally unclear. Since 11β-hydroxysteroid dehydrogenases (HSD11Bs) play important roles in diabetes, we hypothesize that flavonoids and isoflavonoids may affect diabetes by targeting two isofo...

journal_title：Steroids

authors： Zhu Q,Ge F,Dong Y,Sun W,Wang Z,Shan Y,Chen R,Sun J,Ge RS

更新日期：2018-04-01 00:00:00

abstract：:The synthesis of a radioiodinated diethylstilbestrol (DES) derivative is described. This derivative was prepared by coupling the previously synthesized active ester of 6-(4-O-diethylstilbestryl)hexanoic acid with mono-[125I]iodotyramine in dry tetrahydrofuran (20 to 22 C, 16 hours). The mono-[125I]iodotyramine was pre...

journal_title：Steroids

authors： Economou EV,Livaniou E,Evangelatos GP,Ithakissios DS

更新日期：1992-01-01 00:00:00

abstract：:Bile acid derivatives, with and without C-3 sulfate groups, and having either the diazo- or halomethylketone moieties, have been synthesized in good yield and purity. The synthetic sequence, COOH leads to COC1 leads to COCHN2 leads to COCH2X, was used with deoxycholic and cholic acids, which requires carefully control...

journal_title：Steroids

authors： Fried AA,Petrow V,Lack L

更新日期：1979-08-01 00:00:00

abstract：:Nuclear membrane bound testosterone 5 alpha-reductase solubilized in active form from human prostatic tissue by 0.5% n-octyl beta-D-glucopyranoside was purified by a four-step chromatographic procedure including DEAE-Trisacryl ion exchange, hydroxylapatite adsorption, testosterone-Sepharose affinity and Sepharose 4B g...

journal_title：Steroids

authors： Quemener E,Amet Y,di Stefano S,Fournier G,Floch HH,Abalain JH

更新日期：1994-12-01 00:00:00

abstract：:For the study of hepatic bile acid transport in vivo, a series of modified bile salts were synthesized. The N-cholyl derivatives of L-leucine, L-alanine, D-alanine, beta-alanine, L-proline, and gamma-amino-butyric acid were prepared from cholic acid, ethyl chloroformate and the corresponding amino acid. Structural ana...

journal_title：Steroids

authors： Ballatore AM,Beckner CF,Caprioli RM,Hoffman NE,Liehr JG

更新日期：1983-02-01 00:00:00

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

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

更新日期：2012-01-01 00:00:00