To analyse the coronary effects of endothelin-1 after ischemia–reperfusion, the left anterior descending coronary artery of anesthetized pigs was subjected to 30-min occlusion followed by 60-min reperfusion. Then, rings distal (ischemic arteries) and proximal (control arteries) to the occlusion...

We used in vitro autoradiography to identify the endothelin-1 receptor subtype(s) in the superficial gray layer of the superior colliculus of rats. These studies showed dense binding of (3-[125I]iodotyrosyl13)-[Ala11,15]Ac-endothelin-1-(6-21) (BQ3020) (for endothelin ETB receptors), while tissue...

Endothelin-1 is known to be a potent vasoconstrictor. Administration of endothelin-1 to the central nervous system (CNS) induces antinociceptive effects. Nociceptive stimuli affect dorsal root ganglion (DRG) neurons and neurons/astrocytes/microglia in the dorsal horn of the spinal cord. Surgical...

We sought to examine the effects of endothelin-1 on the intracellular free Ca2+ concentration ([Ca2+]i) and mitogenic response in the neuroblastoma cell line, B103 (B103 cells). The results obtained from an [125I] endothelin-1 binding assay demonstrated that B103 cells express the endothelin rec...

The influence of diabetes on regulatory mechanisms and specific receptors implicated in the contractile response of isolated rabbit carotid arteries to endothelin-1 was examined. Endothelin-1 induced a concentration-dependent contraction that was greater in arteries from diabetic rabbits than in...

Air re-oxidation of fully reduced human endothelin-1 under optimized conditions yields the natural isomer with parallel disulfide bridges and the non-natural isomer with crossed disulfide bridges at a ratio of 3:1. In view of the recently determined highly reducing redox potential of selenocyste...

The influence of diabetes on regulatory mechanisms and specific receptors implicated in the response of isolated rabbit renal artery to endothelin-1 was examined. Endothelin-1 induced a concentration-dependent contraction that was less potent in arteries from diabetic rabbits than in arteries fr...

Six new (+)-muricatacin mimics bearing a furano-furanone core have been synthesized and their in vitro antiproliferative activity was evaluated against a panel of human tumour cell lines. A straightforward total synthesis of (+)-muricatacin (1) from d-xylose is disclosed providing a sample of 1 ...

With the aim to discover a gastric antisecretory agent more potent than the existing proton pump inhibitors, novel 3,4-dihydro-1H-spiro(naphthalene-2,2′-piperidin)-1-one derivatives, which could occupy two important lipophilic pockets (described as LP-1 and LP-2) of H+,K+-ATPase and can strongl...

The enantioselective synthesis of (3S, 4S)-4-hydroxy-2, 3, 4, 5-tetrahydropyridazine-3-carboxylic acid 1 is described. The two stereogenic centers in anti relationship are obtained by sequential enantio and chemoselective hydrogenation of β-ketoester in presence of chiral ruthenium catalyst and...

We describe a protocol for the multigram preparation of a tripeptide found in peptin antibiotics. The N-terminus is an azido group, while the C-terminus is an allyl ester. The molecule may be cleanly and selectively deblocked under neutral conditions, facilitating strategic planning for the crea...

A modified Rapoport procedure was used to synthesize a tripeptide containing N-methyl-3-hydroxyvaline, an unusual aminoacid found in Luzopeptins.

The effect of luzopeptin on the mobility of DNA in polyacrylamide gels has been determined. Experiments on a mixture of DNA fragments of various lengths have shown that the drug does not form intermolecular cross-links. Gel analysis of complexes of the drug with short DNA fragments (15–35 base ...

The luzopeptins are DNA bisintercalating antibiotics that contain a decadepsipeptide to which are attached two quinoline chromophores. We have used atomic force microscopy (AFM) to investigate the interaction between luzopeptin B and DNA in an attempt to shed light on the binding mode of this an...

Publisher SummarySince their isolation, luzopeptins have attracted interest in the biomedical arena, but their rarity and chemical sensitivity have precluded any sort of chemical modification that may be required for a thorough medicinal chemistry study. A viable synthesis was needed to address ...

The synthesis of luzopeptin C has been accomplished by self-assembly of the macrocycle via activation of a pentapeptide monomer. The present work underscores the generality of the spontaneous macrocyclization approach to the peptins, a strategy introduced by us in connection with the synthesis o...

The chemical constitution of C.I. Disperse Yellow 232 [Intrasil Brilliant Yellow 10GF] was elucidated as 3-(5'-chloro-2'-benzoxazolyl)-7-diethyl-ammo-2H-1-benzopyran-2-one (1). The structure of the dye was confirmed by synthesis from commercially available starting materials. The relat...

The effect of ultraviolet irradiation on generation of radicals and formation of intermediates was investigated in electrochemical oxidation of the azo-dye Orange II using a TiO2-modified β-PbO2 electrode. It was found that a characteristic absorbance of quinonic compounds at 255 nm, which is r...

Bimetallic Fe-Co/GAC (granular activated carbon) was prepared and used as heterogeneous catalyst in the ultrasound enhanced heterogeneous activation of peroxydisulfate (PS, S2O2−8) process. The effect of initial pH, PS concentration, catalyst addition and stirring rate on the decolorization of A...

Micrococcus glutamicus NCIM-2168 exhibited complete decolorization and degradation of C.I. Reactive Green 19A (an initial concentration of 50 mg l−1) within 42 h at temperature 37 °C and pH 8, under static condition. Extent of mineralization was determined with total organic carbon (TOC) and ch...