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A series of new steroidal peroxides – 3′-trifluoromethylated 1,2,4-trioxolanes and 1,2,4,5-tetraoxanes based on deoxycholic acid were prepared via the reactions of the Griesbaum coozonolysis and peroxycondensation, respectively. 1,2,4-Trioxolanes were synthesized by the interaction of methyl O-methyl-3-oximino-12α-acetoxy-deoxycholate with CF3C(O)CH3 or CF3C(O)Ph and O3 as the mixtures of four possible...
Late night salivary cortisol measurement is a clinically important and convenient screening test for Cushing’s syndrome. Tandem mass spectrometry (LC-MS/MS) assays have superior sensitivity and specificity compared to immunoassays. Our goal was to improve a LC-MS/MS method to measure salivary cortisol in both adult and pediatric patients and to characterize its analytical performance by method validation...
As active components of ginseng, 25-methoxylprotopanaxadiol and 25-hydroxyprotopanaxadiol exhibited an ability to inhibit the growth and proliferation or to induce the differentiation and apoptosis of tumour cells. We modified 25-OCH3-PPD and 25-OH-PPD with non-protein amino acids and a series of derivatives was obtained by chromatographic separation, purification and spectroscopy analysis. Thirteen...
Four new 4,5-dihydro-1,3-oxazole, and four new benzo-[d]-oxazole derivatives of [17(20)E]-21-norpregnene, differing in the structure of steroid moiety, were synthesized and evaluated for their potency to inhibit 17α-hydroxylase/17,20-lyase (CYP17A1) activity. Among new compounds, the only oxazolinyl derivative comprising 5-oxo-4,5-seco-3-yn- moiety potently inhibited CYP17A1. Binding modes of the...
1, 25-dihydroxyvitamin D3 (1, 25 (OH)2 D3) and mechanical stimuli in physiological environment contributes greatly to osteoporosis pathogenesis. Wide investigations have been conducted on how 1, 25-dihydroxyvitamin D3 and mechanical stimuli separately impact osteoblasts. This study reports the collective influences of 1, 25-dihydroxyvitamin D3 and flow shear stress (FSS) on biological functions of...
Three new highly oxygenated sterols (1–3) and a new dihydroisocoumarin (7) together with six known compounds were isolated from the extracts of the culture of a sponge-derived fungus Cladosporium sp. SCSIO41007. The structures of all new compounds (1–3, 7) were determined by the extensive spectroscopic analysis including NMR, MS, IR, and UV. Their absolute configurations were determined by X-ray single-crystal...
Polycystic ovary syndrome (PCOS) is an androgen excess disorder associated with obesity and adipose tissue disturbances. Our aim was to evaluate gene expression of adipocytokines and adipocyte characteristics in abdominal subcutaneous adipose tissue (SAT) of PCOS women.Twelve PCOS (PCOSw) and 12 control (Cw) premenopausal women (BMI 20–35 kg/m2) were included, with measurements of whole-body composition...
The aim of this study was to investigate the relationship between estrogen and leptin, thyroid (T3), Uncoupling Protein2 (UCP2), sex hormone binding globulin (SHBG), and resting energy expenditure(REE) in obese subjects with normal and low REE, and to investigate the relationship of estrogen with body composition and energy intake.A total 49 subjects (25–50 years old) were selected. Anthropometric...
Synthesis and biological evaluation of steroidal derivatives with anticancer properties is an active area of drug discovery. Here we measured the relative affinities of d-seco modified steroidal derivatives for estrogen receptor α, estrogen receptor β or androgen receptor ligand binding domains using an optimized non-transcriptional fluorescent cell assay in yeast. Ligand binding domains of steroid...
Although only a small proportion of cholesterol in the body is esterified, in several diseases marked expansion of the esterified cholesterol (EC) pool occurs. These include Wolman disease (WD) and Cholesteryl Ester Storage Disease (CESD) which both result from mutations in LIPA, the gene that encodes lysosomal acid lipase (LAL). The respective contributions that our three cholesterol esterifying...
In this study a new high sensitive method of spironolactone (SP) determination is proposed using voltammetric technique. As the working electrode amalgam film silver based electrode (Hg(Ag)FE) was applied, that resulted in obtaining low limit of spironolactone detection, ex. for the preconcentration time 45 s obtained detection limit was 4.7·10−9 mol L−1 (1.96·10−6 g L−1). The linear response of spironolactone...
An effort with the goal of discovering single-dose, long-lasting (>6 months) injectable contraceptives began using levonorgestrel (LNG)-17-β esters linked to a sulfonamide function purposed as human carbonic anhydrase II (hCA 2) ligands. One single analog from this first series showed noticeably superior anti-ovulatory activity in murine models, and a subsequent structure-activity relationship...
During our search for bioactive secondary metabolites in the jellyfish-derived fungus Penicillium chrysogenum J08NF-4, several bile acid derivatives (2–6) were isolated along with a new steroidal artifact (1). An in vitro anti-inflammatory assay showed that pretreatment with 1 suppressed NO production and the gene expressions of the pro-inflammatory mediators iNOS and TNF-α in LPS-induced RAW 264...
There is a growing concern about the impacts of hypovitaminosis D on the health of pregnant woman, fetal development, childhood, and adult life. Variations in maternal nutrition during gestation and/or lactation play a critical role in the physiological and metabolic development of the fetus and neonate, which can induce phenotypic changes and trigger important consequences throughout life, such as...
A short and efficient synthesis, based on a one-step double elimination, of a key intermediate in the synthesis of various glucocorticosteroids has been developed. This method can be carried out on large scale for further industrial applications. The synthesis allowed us to identify a novel prednisolone derivative 10 and its anti-inflammatory activity was determined in an in vivo model of inflammation...
Androgen insensitivity syndrome (AIS) is the most common cause of 46,XY disorders of sex development (46,XY DSD). This syndrome is an X-linked recessive genetic disease characterized by resistance to the actions of androgens in an individual with a male karyotype and it is caused by mutations in the androgen receptor (AR) gene. We evaluated two siblings with primary amenorrhea, normal secondary sex...
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