The GALA peptide (WEAALAEALAEALAEHLAEALAEALEALAA) was originally designed to induce the destabilization of endosomal membranes based on its ability to undergo a pH-dependent conformational change from a random coil to an α-helix. We recently found that liposomes modified with GALA peptide (GALA...

In this work, we attempted to synthesize homoeriodictyol by transferring one methyl group of S-adenosyl-l-methionine (SAM) to eriodictyol using flavone 3′-O-methyltransferase ROMT-9, which was produced by recombinant Yarrowia lipolytica. Specifically, the ROMT-9 gene from rice was synthesized a...

Excess intracellular reactive oxygen species (ROS) production is a significant causative factor of many diseases, exemplified by vascular diseases. Mitochondria are a major source of endogenous ROS, which simultaneously induce mitochondrial dysfunction. Nuclear factor-erythroid 2-related factor ...

Background Major depression has a significant impact on years lived with disability (YLD) globally. In resource-limited countries, depression may accompany daily challenges of economic security that people face, hence there is a critical need to develop depression screening tools at primary leve...

The present study describes the use of metabolic engineering to achieve the production of R,R-2,3-butanediol (R,R-2,3-BD) of ultra-high optical purity (>99.99%). To this end, the diacetyl reductase (DAR) gene (dud A) of Paenibacillus polymyxa ZJ-9 was knocked out via homologous recombination bet...

Two highly sensitive fluorescent dye-labelled peptide indicators for metalloproteinase 9 (MMP-9) activity were designed and tested in vitro. Excellent sensitivity of these indicators is achieved by careful selection of the amino acid sequence corresponding to the substrate recognition preference...

Oxysterols exhibit a wide variety of biological activities, including potent immunosuppressive effects. 7ß,25-Dihydroxycholesterol (7,25-OHC), a synthetic oxysterol, has been shown to strongly inhibit the lymphocyte respo0nse to different stimuli. This compound has been chosen as a model compoun...

Several oxysterols are powerful immunosuppressors. Among them 7,25-dihydroxycholesterol (7,25-OHC) seems to be particularly interesting. The effect of this synthetic sterol on murine lymphocytes, stimulated by Con A, or by allogeneic or TNP-modified syngeneic lymphocytes, was investigated. The r...

The effects of an oxysterol, 7,25-dihydroxycholesterol (7,25-OHC), cyclosporin A (CsA) and dexamethasone (Dex) on the blastogenic response of murine lymphocytes to various stimuli were investigated. 7,25-OHC markedly depressed the rresponse to Con A, anti-T3 monoclonal antibodies and to the comb...

Acanthothamine, a new sesquiterpene alkaloid, with an iso-evoninic acid residue, was isolated from Acanthothamnus aphyllus and characterized by chemical and spectroscopic data as 8-epieuonyminol tetraacetate iso-evoninate.

Cytosolic phospholipase A2α (cPLA2α) and fatty acid amide hydrolase (FAAH) are enzymes, which have emerged as attractive targets for the development of analgetic and anti-inflammatory drugs. We recently reported that 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid (10) and related c...

The ion pair concept was applied for the assessment of lipophilicity of cefepime and cefpirome. Octanol–water distribution coefficients were determined in presence of different concentrations [X−] of sodium octanesulphonate. The log Dx values within the linear part of the log Dx/[X−] relationsh...

Activation of the title acid 1 as acyl derivatives of 1-methyl-5-mercaptotetrazole (13) and 2-methyl-5-mercapto-1,3,4-thiadiazole (9, 14) and subsequent acylation of penultimate 4 (X = Cl, I) gave good yields of cefepime sulfate 5.

The aim of the current study was to develop and validate a robust multi-analyte high performance liquid chromatography tandem mass spectrometry (HPLC–MS/MS) method for simultaneous quantification of cefepime, meropenem, ciprofloxacin, moxifloxacin, linezolid and piperacillin, which are the most...

Asymmetric synthesis of the novel highly sterically constrained (2S,3S)-3-methyl-3-trifluoromethyl- and (2S,3S,4R)-3-trifluoromethyl-4-methylpyroglutamic acids has been developed via diastereoselective Michael addition reactions between a Ni(II) complex of the chiral non-racemic Schiff base of g...

The stereochemical outcome of the Michael reaction between ethyl 4,4,4-trifluorocrotonate and a Ni(II) complex of the Schiff base of glycine with (S)-o-[N-(N-benzylprolyl)amino]benzophenone was found to be subjected to kinetic and thermodynamic control. Thus, under kinetically controlled conditi...

An efficient asymmetric synthesis of biologically important (2S,3S)-3-methyl- and (2S,3S)-3-trifluoromethylpyroglutamic acid has been developed. The method consists of diastereoselective Michael addition reaction between ethyl crotonate or ethyl 4,4,4-trifluorocrotonate and a Ni(II) complex of t...

Rats engrafted with transplantable N-[4-(5-nitro-2-furyl)-2-thiazolyl] formamide (FANFT) induced urothelial tumors were treated with purpurin derivatives and red light (>590 nm., 360 joules/cm.2). Treated and control tumors were harvested 12 days after treatment and dry weights compared. At dose...

F420-dependent glucose-6-phosphate dehydrogenase (FGD) is involved in the committed step of the pentose phosphate pathway within mycobacteria, where it catalyzes the reaction between glucose-6-phosphate (G6P) and the F420 cofactor to yield 6-phosphogluconolactone and the reduced cofactor, F420H2...

SummaryNecroptosis is an inflammatory form of programmed cell death executed through plasma membrane rupture by the pseudokinase mixed lineage kinase domain-like (MLKL). We previously showed that MLKL activation requires metabolites of the inositol phosphate (IP) pathway. Here we reveal that I(1...