Design, synthesis and biological evaluation of novel 5α, 8α-endoperoxide steroidal derivatives with hybrid side chain as anticancer agents.

abstract：:Guinea pig adrenal estrogen sulfotransferase from either sex was eluted as a single peak, irrespective of buffer salt concentration, when subjected to fast protein liquid chromatography on gel filtration columns. The same enzyme was consistently eluted in two distinct peaks during chromatofocusing. Adrenal pregnenolon...

journal_title：Steroids

authors： Glasier MA,Glutek SM,Hobkirk R

更新日期：1992-06-01 00:00:00

abstract：:20S-hydroxyvitamin D3 (20S-(OH)D3), an in vitro product of vitamin D3 metabolism by the cytochrome P450scc, was recently isolated, identified and shown to possess antiproliferative activity without inducing hypercalcemia. The enzymatic production of 20S-(OH)D3 is tedious, expensive, and cannot meet the requirements fo...

journal_title：Steroids

authors： Li W,Chen J,Janjetovic Z,Kim TK,Sweatman T,Lu Y,Zjawiony J,Tuckey RC,Miller D,Slominski A

更新日期：2010-12-01 00:00:00

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

authors： Stalvey JR

更新日期：2002-07-01 00:00:00

abstract：:The free sterol mixture of the sponge Psammaplysilla purpurea was shown to contain aplysterol as the major constituent. In addition to other sterols such as 5,7-cholestadien-3beta-ol, cholesterol, 5alpha-cholestan-3beta-ol, 24epsilon-methylcholesta-5,22-dien-3beta-ol, 24epsilon--methylcholesterol, 24epsilon-ethylchole...

journal_title：Steroids

authors： Ayanoglu E,Djerassi C,Erdman TR,Scheuer PJ

更新日期：1978-06-01 00:00:00

abstract：:The biosynthesis of progesterone from [3H]pregnenolone was curvilinear over a 6 h time course in human placenta cytotrophoblasts and in human placenta choriocarcinoma cells (JEG-3 cells). Mass measurements determined independently by radioimmunoassay indicate that the progesterone synthesized by cytotrophoblasts (21.0...

journal_title：Steroids

authors： Sharp RB,Penning TM

更新日期：1988-05-01 00:00:00

abstract：:Metandienone is one of the most frequently detected anabolic androgenic steroids in sports drug testing. Metandienone misuse is commonly detected by monitoring different metabolites excreted free or conjugated with glucuronic acid using gas chromatography mass spectrometry (GC-MS) and liquid chromatography tandem mass...

journal_title：Steroids

authors： Gómez C,Pozo OJ,Garrostas L,Segura J,Ventura R

更新日期：2013-12-11 00:00:00

abstract：:A series of clickable bile acid-nucleosides conjugates linked directly or via amino acid linker were synthesized, and characterized by spectroscopic techniques such as 1H NMR, 13C NMR, FT-IR, HRMS and HPLC. The synthesized compounds 6a-p were screened for their in vitro anticancer property against a panel of three can...

journal_title：Steroids

authors： Agarwal DS,Siva Krishna V,Sriram D,Yogeeswari P,Sakhuja R

更新日期：2018-11-01 00:00:00

abstract：:Using cultured Y-1 mouse adrenal tumor cells which produce 20 alpha-hydroxy-4-pregnen-3-one (20-DHP), it was found that 0.01 mM corticosterone and deoxycorticosterone increased basal and inhibited ACTH-induced 20-DHP production during consecutive 30 and 120 min incubations. Steroid effects were concentration-dependent...

journal_title：Steroids

authors： Mattson MP,Mrotek JJ

更新日期：1985-07-01 00:00:00

abstract：:Immature hypophysectomized rats were injected with PMS; some groups received hCG 48h later. The C17,20-lyase activity in the granulosa cells removed from the large preovulatory follicles was estimated by the amount of labelled acetic acid produced from 21 (14C) progesterone or 17-hydroxyprogesterone. 17 alpha-hydroxyl...

journal_title：Steroids

authors： Johnson DC,Griswold T

更新日期：1983-11-01 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：:Some properties of immunoreactive estradiol secreted by adrenals and ovaries of immature female rats were studied. It was shown that adrenals and ovaries of 15-day-old animals secrete approximately equal amounts of immunoreactive estradiol, with thin-layer chromatogram of immunoreactive material being identical for bo...

journal_title：Steroids

authors： Tinnikov AA,Bazhan NM,Yakovleva TV

更新日期：1992-04-01 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：:Mouse models of cystic fibrosis (CF) display increased sulfotransferase 1E1 (SULT1E1) activity in hepatocytes of cystic fibrosis transmembrane receptor (CFTR)-deficient animals. SULT1E1 is responsible for the sulfation and inactivation of beta-estradiol (E2) at physiological concentrations. IGF-1 message levels in CFT...

journal_title：Steroids

authors： Li L,He D,Wilborn TW,Falany JL,Falany CN

更新日期：2009-01-01 00:00:00

abstract：:Boldenone is an anabolic-androgenic steroid that is prohibited in equine sports. Urine from the uncastrated male horse contains boldenone that is thought to be of endogenous origin and thus a threshold ('cut-off') concentration has been adopted internationally for free and conjugated boldenone to help distinguish case...

journal_title：Steroids

authors： Viljanto MJ,Kicman AT,Walker CJ,Parkin MC,Wolff K,Pearce CM,Scarth J

更新日期：2019-06-01 00:00:00

abstract：:Carbon-11-labeled casimiroin analogues were first designed and synthesized as new potential PET agents for imaging of quinone reductase (QR) 2 and aromatase expression in breast cancer. [(11)C]casimiroin (6-[(11)C]methoxy-9-methyl-[1,3]dioxolo[4,5-h]quinolin-8(9H)-one, [(11)C]11) and its carbon-11-labeled analogues 5,...

journal_title：Steroids

authors： Wang M,Gao M,Miller KD,Sledge GW,Hutchins GD,Zheng QH

更新日期：2010-12-01 00:00:00

abstract：:Structural modifications of natural products with complex structures like steroids require great synthetic effort. A review of literature is presented on the chemistry of the steroidal hormone 17α-methyltestosterone that is approved by Food and Drug Administration (FDA) in the United States as an androgen for estrogen...

journal_title：Steroids

authors： El-Desoky el-SI,Reyad M,Afsah EM,Dawidar AA

更新日期：2016-01-01 00:00:00

abstract：OBJECTIVE:To evaluate the role of physiologic levels of androgens and their precursors in the regulation of body composition, energy and substrate metabolism and aerobic capacity in healthy, cycling, premenopausal women. EXPERIMENTAL:We evaluated 30 young (27±1 year) premenopausal, non-obese (23±0.5 kg/m(2)), normally...

journal_title：Steroids

authors： Keller JL,Casson PR,Toth MJ

更新日期：2011-11-01 00:00:00

abstract：:Smith-Lemli-Opitz syndrome (SLOS) is caused by deficiency in the terminal step of cholesterol biosynthesis, which is catalyzed by 7-dehydrocholesterol reductase (DHCR7). The disorder exhibits several phenotypic traits including dysmorphia and mental retardation with a broad range of severity. Pathogenesis of SLOS is c...

journal_title：Steroids

authors： Marcos J,Shackleton CH,Buddhikot MM,Porter FD,Watson GL

更新日期：2007-10-01 00:00:00

abstract：:Steroids possessing an ethynyl group at position 17α (tertiary alcohols) are well known to be more stable than their non-ethynyl analogs (secondary alcohols). To facilitate the development of new drugs with better metabolic stability, we developed a new diethylsilyl acetylenic linker allowing us to rapidly synthesize ...

journal_title：Steroids

authors： Talbot A,Maltais R,Kenmogne LC,Roy J,Poirier D

更新日期：2016-03-01 00:00:00

abstract：:Removal of free calcium ions from the incubation medium of isolated bovine adrenocortical cells with EGTA reduced basal cortisol synthesis and blocked the effects of ACTH; additional calcium restored normal steroid synthesis. Calcium channel blockers, verapamil and nitrendipine and the calmodulin antagonist, trifluope...

journal_title：Steroids

authors： Davies E,Kenyon CJ,Fraser R

更新日期：1985-06-01 00:00:00

abstract：:Biologic sex and sex steroids are important factors in clinical and experimental stroke. This review evaluates key evidence that biological sex strongly alters mechanisms and outcomes from cerebral ischemia. The role of androgens in male stroke is understudied and important to pursue given that male sex is a well know...

journal_title：Steroids

authors： Cheng J,Hurn PD

更新日期：2010-11-01 00:00:00

abstract：:The non-genomic action of steroid hormones regulates a wide variety of cellular responses including regulation of ion transport, cell proliferation, migration, death and differentiation. In order to achieve such plethora of effects steroid hormones utilize nearly all known signal transduction pathways. One of the key ...

journal_title：Steroids

authors： Alzamora R,Harvey BJ

更新日期：2008-10-01 00:00:00

abstract：:Circadian rhythms in physiology and behavior are known to be influenced by the estrous cycle in female rodents. The clock genes responsible for the generation of circadian oscillations are widely expressed both within the central nervous system and peripheral tissues, including those that comprise the reproductive sys...

journal_title：Steroids

authors： Nakamura TJ,Sellix MT,Kudo T,Nakao N,Yoshimura T,Ebihara S,Colwell CS,Block GD

更新日期：2010-03-01 00:00:00

abstract：:For the purpose of describing the pathway by which estrones are synthesized in the rhesus monkey (Macaca mulatta) corpus luteum (CL), CL were obtained during the midluteal phase of the menstrual cycle and fragments incubated with equimolar amounts of [7-3H]pregnenolone plus [4-14C]progesterone. Metabolites including 3...

journal_title：Steroids

authors： Sholl SA,Wolf RC

更新日期：1980-08-01 00:00:00

abstract：:Mass spectra and fragmentation patterns of the epimeric 17-, 16-, 15- and 14-hydroxy derivatives of 3-methoxy-1,3,5(10)-estratriene are compared. The main fragmentation pathways are differently influenced, depending on the position of the hydroxy group. The different configuration of the hydroxy groups is reflected on...

journal_title：Steroids

authors： Schade W,Ihn W,Vokoun J,Schönecker B,Schubert G

更新日期：1980-11-01 00:00:00

abstract：:Glucocorticoids (GCs) and progesterone have been employed as immunosuppressive agents during pregnancy for many years. Intracellular acidification by GCs is due to a rapid non-genomic inhibition of membrane Na(+)/H(+)-exchange 1 (NHE1) activity and is followed by immunosuppression of PHA-stimulated proliferation. NHE1...

journal_title：Steroids

authors： Chien EJ,Hsu CH,Chang VH,Lin EP,Kuo TP,Chien CH,Lin HY

更新日期：2016-07-01 00:00:00

abstract：:By analyzing the steroidal content of fresh whole plants of Tacca subflabellata (Taccaceae), we isolated one sapogenin and eight glycosides with four kinds of steroidal skeletons including four new glycosides, named taccasubosides A-D (1-4), together with five known compounds. Among them, compound 1 is the first penta...

journal_title：Steroids

authors： Li L,Ni W,Li XR,Hua Y,Fang PL,Kong LM,Pan LL,Li Y,Chen CX,Liu HY

更新日期：2011-09-01 00:00:00

abstract：:Plasma concentrations of dehydroepiandrosterone (DHEA), 5-androstene-3beta,17beta-diol (AED), and 17beta-estradiol (E2) in dairy cows and heifers and AED binding to uterine cytosolic estrogen receptor (ER) were studied. Plasma samples were collected from the subcutaneous abdominal (SA) and jugular (J) veins of heifers...

journal_title：Steroids

authors： Gabai G,Marinelli L,Simontacchi C,Bono GG

更新日期：2004-02-01 00:00:00

abstract：:The applications of sterically crowed trialkyksilyl ether derivatives to the analysis and characterization by thin-layer chromatography, gas chromatography and mass spectrometry, of metabolites of 2alpha, 3alpha-cyclopropano-5alpha-androstan-17beta-ol in the rabbit are described. These derivatives are complementary to...

journal_title：Steroids

authors： Quilliam MA,Templeton JF,Westmore JB

更新日期：1977-05-01 00:00:00

abstract：:This study aimed to develop a quantitative and in vivo magnetic resonance imaging (MRI) approach to investigate the muscle growth effects of anabolic steroids. A protocol of MRI acquisition on a standard clinical 1.5 T scanner and quantitative image analysis was established and employed to measure the individual muscl...

journal_title：Steroids

authors： Wu EX,Tang H,Tong C,Heymsfield SB,Vasselli JR

更新日期：2008-04-01 00:00:00