Two stability indicating spectrofluorimetric methods were developed and validated for the determination of sertindole (SER) in the presence of its acid and oxidative degradates at λex 257 nm and λem 335 nm. Method A was based on measuring the native fluorescence of SER using isopropanol as sol...

The total synthesis of renierone, mimocin, renierol, renierol acetate, renierol propionate, and 7-methoxy-1,6-dimethylisoquinoline-5,8-dione was successfully achieved by the regioselective oxidation of 5-oxygenated isoquinoline. The synthetic method of the 5-oxygenated isoquinoline is based on t...

The C1–C9 northern fragment of aurisides 12a was prepared in eight steps and 41% overall yield starting from Grieco's bicyclic lactone (+)-4. The synthesis features a key stereoselective Meinwald reaction of the lithium enolate of alkyl propionate with the functionalized δ-lactone 3.

Production of chromogranin (Cg)A and B derived peptides [pancreastatin (PST), GAWK, CCB] was studied using human lung carcinoma derived cell lines. PST-like immunoreactivity (LI) was detected in the culture medium in 3 of 6 small cell lung carcinoma (SCLC) cell lines, while GAWK- and CCB-LIs wer...

Sensitive and specific in situ hybridization detection of CGA mRNA, and immunohistochemistry with an antibody recognizing the CGA(316–329) epitope within CGA and its proteolytic fragments were employed to determine whether or not CGA mRNA or protein expression are restricted to specific neurona...

The abuse of esters of natural androgenic steroids in cattle fattening and sports is hard to control via routine urine testing. The esters are rapidly hydrolysed in vivo into substances which are also endogenously present in urine. In veterinary control strange findings of 17β-testosterone and ...

Boldenone (BOLD), an anabolic steroid, is likely to be abused in livestock breeding and in sports. Although some of BOLD metabolites in human urine, such as 5β-adrost-1-en-17β-ol-3-one (BM1), have been detected, investigations on their excretion patterns for both genders are insufficient. More...

We applied antiserum to PEP-19, a presumptive calcium-binding polypeptide, to the auditory brainstem of cats to determine whether this antiserum would selectively reveal cochlear nucleus neurons and their projections. We report that the entire populations of ventral cochlear nucleus bushy and mu...

SummaryPeptide 19 (PEP 19) is a 7.6 kDa polypeptide which can bind to calmodulin and inhibit calcium–calmodulin signaling. In this study, PEP 19-immunoreactivity (ir) was examined in the rat trigeminal sensory nuclei. Numerous PEP 19-immunoreactive (ir) neurons were detected in the medullary do...

We have investigated the distribution of PEP-19, a neuron-specific protein, in the adult human brain. Immunohistochemistry for PEP-19 appears to define the basal ganglia and related structures. The strongest immunoreactivity is seen in the caudate nucleus and putamen, each of which showed both c...

PEP-19 is a 61 amino acid polypeptide that is localized to neurons. PEP-19 is translated from a 0.6 kb poly(A)+ RNA; however, the gene from which it is transcribed spans more than 30 kbp and comprises three exons and two large introns. Exon 1 contains the 5′-untranslated region of PEP-19 and th...

PEP-19 is a 7.6 kDa neuronally expressed polypeptide that contains a single calmodulin-binding IQ motif. The calmodulin-binding activity of several neuronal IQ motif proteins is regulated by phosphorylation of a conserved serine. We propose that the serine residue within the IQ motif of PEP-19 i...

Excessive elevation of intracellular Ca2+ levels and, subsequently, hyperactivation of Ca2+/calmodulin-dependent processes might play an important role in the pathologic events following cerebral ischemia. PEP-19 is a neuronally expressed polypeptide that acts as an endogenous negative regulator...

In this paper, polypeptide membranes composed by surfactant-like peptides were studied by using molecular dynamics simulations. The studied membranes are composed by 15 amino acids, being a hydrophobic part consisting of 3 isoleucine (ILE - I), 3 valine (VAL - V), 3 alanine (ALA - A), 3 glycine ...

.The precise molecular mechanisms leading to disturbance of Ca2+/calmodulin-dependent intracellular signalling in cardiac hypertrophy remains unclear. As an endogenous calmodulin regulator protein, the pathophysiology role of PEP-19 during cardiac hypertrophy was investigated in the present stud...

A practical and efficient α-selective aromatic glycosylation with simple per-O-acetyl glycopyranosyl trichloroacetimidates is reported. The method is particularly effective for L-fucosyl and 2-azido-2-deoxy-d-galatosaminyl imidates, with which exclusive α-selectivity was achieved. The syntheti...

Azinomycin B is an environmental DNA crosslinking agent produced by the soil microorganism Streptomyces sahachiroi. While the agent displays potent cytotoxic activities against leukemic cell lines and animal mouse models, the lack of a consistent supply of the natural product has hampered detail...

SummaryAzinomycin B is a complex natural product containing densely assembled functionalities with potent antitumor activity. Cloning and sequence analysis of the azi gene cluster revealed an iterative type I polyketide synthase (PKS) gene, five nonribosomal peptide synthetases (NRPSs) genes and...

SummaryStudies on the mechanism of action of the antitumor agent azinomycin B in vitro suggest that the drug elicits its lethal effects by the formation of interstrand crosslinks within the major groove of DNA. Here, we demonstrate the biological effects of the drug in vivo. Fluorescence imaging...

The electrode sensitive to dibenzyl dimethyl ammonium (DDA+), which is considered to be an indicator of the membrane potential, was constructed by using tetraphenyl borone (TPB−) embedded in dichloroethane. Rapid and Nernstian responses were exhibited against DDA+ solutions ranging between 10−2 ...