Characterization of the binding sites of the anticancer ruthenium(III) complexes KP1019 and KP1339 on human serum albumin via competition studies

Indazolium trans-[tetrachloridobis(1H-indazole)ruthenate(III)] (KP1019) and its Na+ analogue (KP1339) are two of the most prominent non-platinum antitumor metal complexes currently undergoing clinical trials. After intravenous administration, they are known to bind to human serum albumin (HSA) in a noncovalent manner. To elucidate their HSA binding sites, displacement reactions with the established site markers warfarin and dansylglycine as well as bilirubin were monitored by spectrofluorimetry, ultrafiltration-UV-vis spectrophotometry, and/or capillary zone electrophoresis. Conditional stability constants for the binding of KP1019 and KP1339 to sites I and II of HSA were determined, indicating that both Ru(III) compounds bind to both sites with moderately strong affinity (log K (1)' = 5.3-5.8). No preference for either binding site was found, and similar results were obtained for both metal complexes, demonstrating low influence of the counter ion on the binding event

New perspectives to control Colorado potato beetle (Leptinotarsa decemlineata Say) – a short review devoted to the recent identification of the aggregation pheromone of Colorado potato beetle

The short review of investigations done in the field of identification, application and synthesis of the aggregation pheromone of Colorado potato beetle, (S)-3,7-dimethyl-2-oxooct-6-en-1,3-diol, is presented

Contemporary trends in development of active substances possessing the pesticidal properties: neonicotinoid insecticides

A new group of insecticides, widely introduced to the agriculture practice since the 90-ies of XX century - neonicotinoides, is discussed. The history of its arise, and insecticidal properties, mode of action, and short characteristics of some of its representatives is presented

Hybrid Scheme with Triangulations for Transform Coding

Our approach to image region approximation offers a complete schemeconsisting of several steps. We separate the encoding of regionboundaries from the texture description. The original image is firstsegmented using an unsupervised segmentation method for color-textureregions. Following polygonal approximation of created regions causesthe degradation of region boundaries. The triangulation is then appliedto polygons and either all short edges, or all small triangles arefiltered out from the triangular mesh. This results in new smallerregions. The encoding and decoding of polygons and triangles is veryefficient, because we need to store only the vertices. For textureapproximation we use 2D shape independent orthogonal transforms (e.g.DCT II). The texture is encoded with a code similar to JPEG arithmeticcode. The encoding scheme proposed in this paper is much faster thanlatest approaches with polygonal approximation. We present the twotriangulation algorithms - constrained greedy (CGT) and constrainedDelaunay triangulation (CDT). Both CGT and CDT provide similar results

Contemporary trends in development of active substances possessing the pesticidal properties: spinosyn insecticides

A new group of insecticides belonging to the category of bio-pesticides, namely – spinosyns, is discussed. The spinosyns are the products of bacterial fermentation by microorganisms Saccharopolyspora spinosa (Actinomycetes group) in a nutrient media. The chemical structures of spinosyns, also those developed by the semi-synthetic and biochemical modifications, as well as their insecticidal properties and mechanism of biological activity, the range of their application in crop protection and the commercially available products based on them, are reviewed

Contemporary trends in development of active substances possessing the pesticidal properties: ryanodine-receptor targeting insecticides

The latest developed classes of synthetic insecticides – phthalic acid diamides and antranilic diamides, acting as ryanodine receptor modulators, are discussed. The mode of their activity, the insecticidal properties and characteristics of their representatives is reviewed

Ethyl N,N-dimethyl- and N,N-dimethylamidophosphoric acids sodium salts. Preparation and hydrolysis

Sodium salts of ethyl N,N-dimethyl- and N,N-dimethylamidophosphoric acids I and II were obtained and their hydrolysis to respective acids was investigated. The salts and acids were characterized by spectral methods (MS, FT/IR, 1H, 13C, 31P NMR)

Ethyl [1S, 2RS]-and [1S,2S]-2-[2-chloro-propanoyloxy]propanoate. Preparation and hydrolysis

Ethyl (1S,2RS)-2-(2-chloropropanoyloxy)propanoate ((1S,2RS)-(I)) was obtained from rac-2-chloropropionyl chloride and ethyl L-lactate. (1S,2S)- (I) was also synthesized from (S)-2-chloropropionyl chloride and ethyl L-lactate with 93% d.e. (I) was undertaken hydrolysis by different media: NaOH/THF-H2O, Na2CO3/THF-H2O, LiOHxH2O/THF-H2O, 25% NaOH/H2O, and weakly acidic ion-exchange resin Amberlite IRC748 dispersion in MeOH. (1S,2RS)-2-(2-Chloropropanoyloxy) propanoic acid (II) diastereomers were identified as products of acidic hydrolysis with the ionic resin. GC/MS, HPLC and HPLC/MS analyses of resulted products are presented