Abstract:
:Porcine sulfotransferase 2A1 (pSULT2A1) is a key enzyme involved in the testicular and hepatic sulfoconjugation of steroids such as dehydroepiandrosterone (DHEA) and potentially androstenone. This latter steroid is a major cause of boar taint, which is an unpleasant off-odour and off-flavour in pork from male pigs. Sulfotransferase 2B1 (pSULT2B1) may also be important, although no direct evidence exists for its involvement in sulfoconjugation of steroids. The purpose of this study was to investigate the sulfoconjugation activity of human and porcine sulfotransferases towards DHEA and androstenone. pcDNA 3.1 vectors expressing porcine (p) SULT2A1, pSULT2B1, human (h) SULT2A1, hSULT2B1a, and hSULT2B1b enzymes were transfected into human embryonic kidney cells. Transfected cells were then incubated with either androstenone or dehydroepiandrosterone (DHEA) in both time-course and enzyme kinetics studies. The production of sulfonates of androstenone metabolites and DHEA sulfonate increased over time for all enzymes with the exception of pSULT2B1. Enzyme kinetics analysis showed that androstenone and DHEA were poor substrates for the human orthologs, hSULT2B1a and hSULT2B1b. Human and porcine SULT2A1 showed substantially different substrate affinities for androstenone (Km 5.8 ± 0.6 µM and 74.1 ± 15.9 µM, respectively) and DHEA (Km 9.4 ± 2.5 µM and 3.3 ± 1.9 µM, respectively). However, these enzymes did show relatively similar sulfonation efficiencies for DHEA (Vmax/Km 50.5 and 72.9 for hSULT2A1 and pSULT2A1, respectively). These results highlight the species differences in sulfonation activity and provide direct evidence, for the first time, suggesting that pSULT2B1 is not involved in sulfonation of either androstenone metabolites or DHEA.
journal_name
Steroidsjournal_title
Steroidsauthors
Laderoute H,Bone C,Squires EJdoi
10.1016/j.steroids.2018.05.010subject
Has Abstractpub_date
2018-08-01 00:00:00pages
8-16eissn
0039-128Xissn
1878-5867pii
S0039-128X(18)30098-9journal_volume
136pub_type
杂志文章相关文献
STEROIDS文献大全abstract::The efficiencies for estrogen conjugate hydrolysis were compared between enzyme hydrolysis, acid solvolysis and a new method, ammonolysis. Samples included: 1) crystalline 1,3,5(10)-estratriene-3, 17 beta-diol disulfate (estradiol 3,17-disulfate), 2) squirrel monkey urine collected following an intravenous injection o...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(84)90023-0
更新日期:1984-06-01 00:00:00
abstract::Agave plants are popular for their myriad applications in traditional medicine attributed to their reported anti-inflammatory, immunomodulatory, cytotoxic and antifungal activities. The aim of this study was to examine the anti-inflammatory, immunomodulatory and ulceroprotective activity of Agave species in relation t...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2020.108648
更新日期:2020-08-01 00:00:00
abstract::In an attempt to justify use of trypsin to achieve more thorough dispersion of luteal cell clumps in vitro, progesterone (P) production by collagenase dispersed monkey luteal cells from the mid-luteal phase corpus luteum (CL) was examined in vitro either after 10 min, or continuous (3h) exposure to trypsin (TR). In th...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(80)90110-5
更新日期:1980-01-01 00:00:00
abstract:BACKGROUND:Once a septic condition is progressing, administration of steroids in the pro-inflammatory phase of septic shock ought to yield maximal effect on the subsequent, devastating inflammatory response. Recently, a retrospective study showed that early initiation of corticosteroid therapy improved survival in sept...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2012.06.001
更新日期:2012-09-01 00:00:00
abstract::A short and efficient synthesis of steroid synthons, di(tert-butyldimethylsilyl) ethers of 3,21-dihydroxy-24-nor-chol-5-en-23-al (8 and 10) and of ethyl 3,21-dihydroxy-25-homo-chola-5,23-dien-25-oate (9 and 11), having natural (20R) and unnatural (20S) configuration from 3β-(tert-butyldimethylsilyloxy)-14α,20ξ-card-5-...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2011.01.010
更新日期:2011-04-01 00:00:00
abstract::The abilities of a variety of estrogens and antiestrogens to stimulate DNA synthesis in the prepuberal rat uterus were compared. One microgram of each compound was administered in vivo via a single intraperitoneal injection. DNA synthesis was assayed in vitro in isolated nuclei 24 h later. The relative mitogenicities ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(89)90096-2
更新日期:1989-08-01 00:00:00
abstract::The synthesis of 16 alpha-3H androgens and estrogens is described. 1-(3H)-Acetic acid in the presence of zinc dust reacts with 16 alpha-bromo-17-ketosteroids to produce 16 alpha-3H-17-ketosteroids. This chemical reaction was used to prepare 16 alpha-3H-dehydroepiandrosterone (I) and 16 alpha-3H-estrone acetate (XI) fr...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(81)80016-5
更新日期:1981-02-01 00:00:00
abstract::15alpha-Hydroxydehydroisoandrosterone and 15alpha-hydroxypregnenolone were isolated from hydrolyzed extracts of human late pregnancy urine and identified by means of the isotope dilution technique. In two separate determinations the excretion rate of 15alpha-hydroxydehydroisoandrosterone was found to be 1.7 and 3.2 mi...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(78)80002-6
更新日期:1978-05-01 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
pub_type: 杂志文章
doi:10.1016/j.steroids.2007.03.014
更新日期:2007-10-01 00:00:00
abstract::A phytochemical study of Physalis pubescens L. afforded twelve compounds, including six new withanolides (1, 4, and 6i-9), four new withanolide glucosides (2, 3, 5, and 6), and two known withanolides (10 and 11). Their structures were established via extensive spectroscopic analysis. The absolute configuration of 3 wa...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2016.09.002
更新日期:2016-11-01 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
pub_type: 杂志文章
doi:10.1016/j.steroids.2016.03.001
更新日期:2016-05-01 00:00:00
abstract::We synthesized various analogues of 1alpha,25-(OH)(2)D(3)-26,23-lactone and examined the effects of them on HL-60 cell differentiation using the evaluation system of the genomic action of 1alpha,25-(OH)(2)D(3). We found that (23S)- and (23R)-25-dehydro-1alpha-OH-D(3)-26,23-lactone (TEI-9647 and TEI-9648) strongly boun...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(00)00146-x
更新日期:2001-03-01 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
pub_type: 杂志文章
doi:10.1016/j.steroids.2010.01.007
更新日期:2010-03-01 00:00:00
abstract::This article describes the origins and evolution of "antiestrogenic" medicines for the treatment and prevention of breast cancer. Developing drugs that target the estrogen receptor (ER) either directly (tamoxifen) or indirectly (aromatase inhibitors) has improved the prognosis of breast cancer and significantly advanc...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2006.10.009
更新日期:2007-01-01 00:00:00
abstract::The hormone 1alpha,25(OH)2vitamin D3 (1,25-D) produces biological responses via both genomic and rapid mechanisms. The genomic responses are linked to a nuclear receptor, while the rapid responses are believed to utilize other signal transduction pathways that are likely linked to a putative cell membrane receptor for...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/s0039-128x(98)00091-9
更新日期:1999-01-01 00:00:00
abstract::Over the past 30 years, numerous studies in invertebrates and vertebrates have established a role of calcium in oocyte maturation as well as in the resumption and progression of follicular development. Polycystic ovarian syndrome (PCO) is characterized by hyperandrogenic chronic anovulation, theca cell hyperplasia, an...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(99)00012-4
更新日期:1999-06-01 00:00:00
abstract::To investigate the effects of conjugated bile acid on bacterial growth and cholylglycine hydrolase activity, Clostridium perfringens from human feces was exposed to varying concentrations of taurine- or glycine-conjugated chenodeoxycholic acid. Extracellular enzyme activity was determined by deconjugation of radiolabe...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(94)90062-0
更新日期:1994-08-01 00:00:00
abstract::Previous studies have demonstrated a persistent rise in serum cortisol concentrations after cardiac surgery. To further investigate this finding and to evaluate the effect of hemodilution that occurs with the onset of cardiopulmonary bypass (CPB), concentrations of cortisol-binding globulin (CBG), total and unbound co...
journal_title:Steroids
pub_type: 临床试验,杂志文章
doi:10.1016/s0039-128x(00)00133-1
更新日期:2000-09-01 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
pub_type: 杂志文章
doi:10.1016/0039-128x(85)90019-4
更新日期:1985-06-01 00:00:00
abstract::Corticosteroids were used normally as anti-inflammatory drugs. However, in some area certain corticosteroids might be illegally used as growth promoting agent in feed, and as prohibited doping substances in game and sport for human or/and animal performance-enhancing. Synthesized structural similar corticosteroids wer...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2020.108739
更新日期:2021-01-01 00:00:00
abstract::Oleoyl-estrone (OE) induces a marked loss of body fat in rats by maintaining energy expenditure, body protein and blood glucose despite decreasing food intake. OE increases glucocorticoids, but they arrest OE lipid-mobilization. We studied here whether OE induces a direct effect on adrenal glands function as part of t...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2009.09.009
更新日期:2010-01-01 00:00:00
abstract::Antiandrogens are widely used agents for the treatment of androgen dependent diseases as inhibitors of androgen receptors (AR) action. Although the precise mechanism of antiandrogen action is not yet elucidated, recent studies indicate the involvement of the structure of the ligand in relation with the nuclear co-repr...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2008.03.006
更新日期:2008-09-01 00:00:00
abstract::In addition to using radioimmunoassays for the determination of estrogens and other steroids, the possibility of using mass fragmentography for analysis was investigated. t-Butyldimethylsilyl chloride was selected as a reagent for derivatisation because it forms rather stable silylethers. In all the mass-spectra obrai...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(79)90013-8
更新日期:1979-04-01 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
pub_type: 杂志文章
doi:10.1016/0039-128x(83)90068-5
更新日期:1987-07-01 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
pub_type: 杂志文章
doi:10.1016/0039-128x(80)90077-x
更新日期:1980-11-01 00:00:00
abstract::The apolar ecdysteroid present in the developing embryo of the blue crab, Callinectes sapidus Rathbun, is tentatively identified as ponasterone A (2 beta, 14 alpha, 20,22-pentahydroxy-5, beta-cholest-7-en-6-one) on the basis of chromatographic, immunological, and mass spectral evidence. The apolar ecdysteroid present ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(79)90092-8
更新日期:1979-12-01 00:00:00
abstract::Sex steroid-binding protein receptor was detected on membranes prepared from human premenopausal endometrium. The binding of sex steroid-binding protein to membranes was specific, saturable, and high affinity. Scatchard analysis showed the presence of two binding sites at different affinities. The addition of estradio...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(91)90058-4
更新日期:1991-06-01 00:00:00
abstract::From the aerial parts of Euphorbia sogdiana Popov, obtusifoliol (1) and two related steroids (2-3) have been isolated and characterized along with a known cycloartane derivative (4). The chemical structure of the obtusifoliol-related compounds, obtained by 1D and 2D NMR, and MS measurements, have been determined as: 3...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2016.07.008
更新日期:2016-11-01 00:00:00
abstract::Estrogen is an important atheroprotective molecule that causes the rapid dilation of blood vessels by stimulating endothelial nitric oxide synthase (eNOS). There is also evidence that estrogen modulates airway epithelial NO production, thereby potentially affecting bronchial hyperresponsiveness. Studies in cultured en...
journal_title:Steroids
pub_type:
doi:10.1016/s0039-128x(98)00105-6
更新日期:1999-01-01 00:00:00
abstract::A series of final twelve propanoyloxy derivatives of 5β-cholan-24-oic acid (O-propanoyl derivatives of cholic acid) as potential drug absorption modifiers (skin penetration enhancers, intestinal absorption promoters) was generated by multistep synthesis. Structure confirmation of all generated compounds was accomplish...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2013.02.001
更新日期:2013-05-01 00:00:00