Free amino acids (AA) and biogenic amines (BA) were quantified for the first time in Cannonau and Vermentino wines, the two most popular “Controlled Designation of Origin” wines from Sardinia (Italy). An analytical method for the simultaneous determination of AA and BA was developed, using sel...

2-selena-A-nor-5α-androstan-17β-ol was studied in vitro and in vivo in the rat prostate gland. The data demonstrates the ability of this compound to selectively complex with the specific receptors of 5α-dihydrotestosfcerone (5α-DHT) in the cytosol and to be retained in the nuclei in an unalt...

Methenolone acetate (17β-acetoxy-1-methyl-5α-androst-1-en-3-one), a synthetic anabolic steroid, is frequently abused in human sports. It is preferred for its therapeutic efficiency and lower hepatic toxicity compared with its 17α-alkylated analogs. As with other anabolic steroids, methenolone...

4,17α-Dimethyl-4-aza-5-androsten-17β-ol-3-one, 4,17α-dimethyl-4-aza-5α-androstan-17β-ol-3-one, 4,17α-dimethyl-4-aza-5α-androstan-17β-ol, and their corresponding acetate esters were synthesized and compared for antimicrobial activity. 4,17α-Dimethyl-4-aza-5α-androstan-17β-ol acetate ex...

The crystal and molecular structure of 1,2-seco-A-bisnor-5α-androstan-17β-ol acetate has been determined to evaluate the conformational importance of the intact steroid nucleus. The resulting tricyclic compound retains nearly the same steric profile for the remainder of the molecule when compa...

Many 17-substituted androstan-3α-ol analogs act as positive allosteric modulators of GABAA receptors and exert anticonvulsant and anxiolytic-like activity actions in animal models. The endogenous neurosteroid allopregnanolone (17β-acetyl; 1) is among the most potent of these. Here we demonstra...

Two distinct Δ5-3-ketosteroid isomerases, one acting on the androst-5-ene-3,17-dione and the other on pregn-5-ene-3,20-dione, were demonstrated in beef adrenal cortex homogenates and were partly separated by ammonium sulfate fractionation from a solubilized preparation of the glands. In one enz...

To develop androgen and progesterone receptor-based radioligands for SPECT imaging we synthesized several radioiodinated 17α-iodovinyl testosterone and 19-nortestosterone analogs and evaluated their biological properties. The synthesis of these compounds proceeds via the (17α,20E/Z)stannyl int...

A method for the measurement of 7α-methyl-19-nortestosterone (7MENT) in serum/plasma by radioimmunoassay (RIA) is described. The antiserum, raised against 7α-methyl-19-nortestosterone-3-O-oxime-bovine serum albumin, had a low titer (final dilution = 1:4500) and low affinity (Ka = 1.17 × 109 1...

The binding of estradiol (E2) to estrogen receptors (ER) is followed by conformational changes resulting in coactivator or corepressor recruitment that influences gene transcription. A series of synthetic A-ring reduced 19-nortestosterone-derived progestins has the capacity to selectively bind a...

We report the preparation of the 7α-cyano derivative of the isomeric (17α,20E/Z)-[125I]iodovinyl-19-nortestosterones (IVNT) together with their binding affinity for the androgen receptor (AR) and their biodistribution in two different animal models. The cyano group was introduced at the 7α-po...

We examined ten strains of cultured whole-cell yeasts for the asymmetric reduction of commercially available ethyl 2-oxocyclohexanecarboxylate, and found that the (1S,2S)-stereoisomer of ethyl 2-hydroxycyclohexanecarboxylate was the major stereoisomer produced by Williopsis californica JCM 3600....

Tyrosyl-tRNA synthetase (TyrRS) is an aminoacyl-tRNA synthetase family protein that possesses an essential role in bacterial protein synthesis. The synthesis, structure-activity relationship, and evolution of a novel series of adenosine-containing 3-arylfuran-2(5H)-ones as TyrRS inhibitors are d...

The aim of this study was to investigate the therapeutic effects of methyl dehydroabietate (mDA) on adipocyte differentiation in 3T3-L1 preadipocytes and obesity characteristics induced by high-fat diet (HFD) in mice. Adipocyte differentiation in 3T3-L1 cells was evaluated after 14 days of incub...

The current study focuses on the analysis of in vitro biological activity of extract from bark of Norway spruce (Picea Abies), which can find potential application in food and cosmetic industry and pharmacology. Milled bark was subjected to Soxhlet extraction and supercritical fluid extraction t...

Acetonyltriphenylphosphonium bromide (ATPB) is a useful catalyst for the cyclotrimerization of the aliphatic aldehydes under solvent-free condition. The aldehydes tethered with a variety of functionality such as olefin, ether, ester, bromide, azide and diester could also be cyclotrimerized under...

A practical synthetic method for the direct synthesis of unsymmetrically substituted ureas from N-Alloc-, N-Cbz-, and N-Boc-protected amines is described. In this study, efficient direct conversion of the Alloc-, Cbz-, and Boc-carbamate compounds to ureas was achieved in the presence of DABAL-Me...

The B3LYP/6-311+G(d,p) optimized structures of 1,3-bis(4-nitrophenyl)urea receptor (1) and its complexes with halide ions F−, Cl−, Br−, oxygen-containing anions NO2-, NO3-, HCO3-, HSO4-, H2PO4-, CH3COO− and C6H5COO− ions were obtained. Binding energies and thermodynamic properties of binding bet...

An understanding of how cosolutes affect the viscosity and storage stability of highly concentrated mAbs as a function of protein-protein interactions (PPIs) would be desirable for improving processing and administration of protein therapeutics. The effects of inorganic and organic cosolutes on ...

Site-directed mutagenesis was used to produce a Synechocystis mutant containing a histidine tag at the C terminus of the CP 47 protein of Photosystem II. This mutant cell line, designated HT-3, exhibited slightly above normal rates of oxygen evolution and appeared to accumulate somewhat more Pho...