Search results for " activity"

Isolation, identification and toxicological characterization of TSS 1, a new mycotoxin of the rosenane class.

1990

11-β-hydroxy-7-deoxy-rosenonolactone (TSS1), a product of the pathogenic fungusTrichothecium roseum (Moniliaceae) was isolated from culture medium extracts and completely described in its structure by spectroscopical methods.TSS 1 was classified as a representative of the lactone series of the rosenane class and as a structural isomer to Rosenololactone (1) and Rosololactone (2, 3).TSS1 showed toxic effects in the growth inhibition test toE coli (EC 50: lOμg/mL) andB subtil is (EC 50: 17μg/mL), inhibited fermentation of yeast (EC 50: 2.8μg/mL) and suppressed motility ofAnemia satina larvae (EC 50: 45/μg/mL).Rosenonolactone, the best known representative of that mycotoxin class, showed only …

2-Aryl-substituted 4H-3,1-benzoxazin-4-ones as novel active substances for the cardiovascular system

1991

4H-3,1-Benzoxazin-4-ones of the structural types 3 and 4 are accessible by cyclization reactions. The introduction of the phosphonate group was achieved by way of Wohl-Ziegler bromination and subsequent Michaelis-Arbuzow reaction with a trialkyl phosphite. Pharmacological investigations on isolated left atria, ileum specimens, and Langendorff hearts as well as in vivo circulatory studies on anesthetized rats revealed that the phosphonates 4 exert calcium antagonistic effects. Whereas 2-(arylvinyl)benzoxazinones gave rise to pronounced negative inotropic effects, compound 3e exhibited relaxing effects on smooth musculature in particular and markedly increased the coronary flow through Langen…

Thioredoxin-related protein of 14 kDa may directly reduce protein cysteinylation motifs

2018

Disulfide stress has been associated with inflammation and characterized by an increase in cystine levels and protein cysteinylation. Furthermore, it was recently discovered that thioredoxin-related protein of 14 kDa (TRP14, encoded by TXNDC17) exhibits efficient cystine reductase activity. The aim of our research was to elucidate if TRP14 is also able to reduce cysteinylated proteins in mammalian cells. Thus, protein cysteinylation was assessed in control and TRP14 knockdown cells in vitro through their pre-treatment with 25 µg/ml cycloheximide for 30 min and incubation with 250 µM biotinylated cysteine for 1 h. Moreover, such TRP14 knockdown cell lysates were tested as cysteinylated subst…

Convenient Synthesis of Biologically Important Retinoids

1995

The toxic and teratogenic effects caused by the highly biologically active (all-E)-retinoic acid and its derivatives prompted us to synthesize a number of retinoids. We developed synthetic approaches to (all-E)-retinyl β-D-glucuronide 3, methyl (retinoyl β-D-glucopyranoside)uronate 5, (all-E)-retinoic acid β-D-glucopyranosyl ester 8 and (all-E)-retinoyl β-D-glucuronide 6 in high purity and yield. Compound 3 was synthesized under Koenigs-Knorr conditions from (all-E)-retinol and an α-halogenose. Compounds 5 and 8 were prepared by esterification of a silver salt of (all-E)-retinoic acid with an α-glycosyl halide in pyridine. (all-E)-Retinoyl β-D-glucuronide 6 was prepared by reaction of (all-…

Oligosaccharide recognition by selectins: Synthesis and biological activity of multivalent sialyl lewis-X ligands

1995

Abstract Trivalent sialyl Lewis-X ligands 6–8 anchored onto flexible templates have been synthesized and evaluated as inhibitors of E-selectin and P-selectin mediated cell adhesion in cell culture assays and in vivo. Biological activities in vitro correlated with spacer length and lead to ligands with 3-fold (E-selectin) and 5-fold (P-selectin) improved receptor binding avidity per single tetrasaccharide moiety.

Synthesis, structural aspects and bioactivity of the marine cyclopeptide hymenamide C

2001

Abstract Head-to-tail proline containing cyclopeptide hymenamide C [cyclo(Leu-Trp-Pro 3 -Phe-Gly-Pro 6 -Glu); 1 ], isolated from a marine sponge and for which a preliminary immunomodulating activity was reported, was efficiently synthesized by a three-dimensional orthogonal solid-phase strategy (Fmoc/tBu/Allyl) via anchoring the ω -carboxyl function of the glutamic acid to the solid support (PAC–PEG–PS). The linear precursor was entirely assembled and subsequently cyclized on resin, yielding a major product identical to the natural hymenamide C and a minor one, a geometric isomer of hymenamide C ( 2 ), differing for the geometry of peptide linkages at Pro residues. Both the ‘proline-rich’ c…

Chromatographic quantitation of the hydrophobicity of ionic compounds by the use of micellar mobile phases

1998

Abstract Many biologically active compounds of interest in structure–activity relationships are ionic at physiological pH. However, ionic organic compounds are only weakly or not retained in conventional RPLC which impedes the chromatographic estimation of their hydrophobicity and the development of quantitative retention–activity relationship studies. The use of micellar mobile phases allows the retention of ionic compounds. Hydrophobic and electrostatic forces govern the retention of ionic compounds in micellar liquid chromatography. In this paper three different retention models log k–log P for ionic compounds are tested (P=partition coefficient). The retention model (log k=a log P+bα+c)…

Influence of the physical state of water on the barrier properties of hydrophilic and hydrophobic films.

2000

Water transfer through different films, as a function of the physical state of water in contact with the film, the relative humidity difference, and the water vapor pressure difference, was investigated. The films were two synthetic packagings (hydrophobic polyethylene and hydrophilic cellophane) and an edible film. The physical state of water affects water sensitive films, such as cellophane, inducing a higher liquid water transfer due to interactions with the polymer. For hydrophobic polymers, such as polyethylene, neither the physical state of water nor the relative humidity has an influence on the water permeability. In complex system, such as an edible film composed of hydrophilic part…

Analysis of kynurenine transaminase activity in Drosophila by high performance liquid chromatography

1991

Abstract A sensitive assay for kynurenine transaminase activity (E.C. 2.6.1.7) based on rapid separation of the reaction product by high performance liquid chromatography (HPLC) has been developed. Drosophila sordidula extracts have been assayed by this new method and this is the first time that kynurenine transaminase activity has been demonstrated in Drosophila . The method of assay developed can be extended to any other organism. Kynurenine and 3-hydroxykynurenine were both used as substrates, and they were transaminated to kynurenic acid and xanthruenic acid, respectively. HPLC is used to separate and quantitate these reaction products from all other components in the reaction mixture. …

2003

Jerboa (Jaculus orientalis) is a deep hibernating rodent native to subdesert highlands. During hibernation, a high level of ketone bodies i.e. acetoacetate (AcAc) and D-3-hydroxybutyrate (BOH) are produced in liver, which are used in brain as energetic fuel. These compounds are bioconverted by mitochondrial D-3-hydroxybutyrate dehydrogenase (BDH) E.C. 1.1.1.30. Here we report, the function and the expression of BDH in terms of catalytic activities, kinetic parameters, levels of protein and mRNA in both tissues i.e brain and liver, in relation to the hibernating process. We found that: 1/ In euthemic jerboa the specific activity in liver is 2.4- and 6.4- fold higher than in brain, respective…