Preparation of N-2-Nitrophenylsulfenyl Imino Peptides and Their Catalyst-Controlled Diastereoselective Indolylation

N-2-Nitrophenylsulfenyl (Nps) imino dipeptides bearing various functional groups were successfully prepared via MnO2-mediated oxidation and then subjected to diastereoselective indolylation. Each diastereomer of the adduct was selectively obtained from the same substrates using the appropriate chiral phosphoric acid catalysts. These transformations would be useful for synthesizing non-canonical amino acid-containing peptides as novel drug candidates

Transabdominal Approach for Spontaneous Oesophageal Perforation: A Review of Four Cases

Spontaneous oesophageal perforation is an uncommon and life-threatening disease. Although several methods of treatment have been proposed, surgical treatment is considered the standard procedure. Primary repair using the transthoracic approach is the most common. However, few studies have evaluated the characteristics of the transabdominal approach. This study aimed to investigate the clinical outcomes of spontaneous oesophageal perforation that was surgically treated using the transabdominal approach. We retrospectively reviewed all patients with spontaneous oesophageal perforation who were admitted to the surgical department of our institution between November 2010 and April 2017, and identified a total of four patients. Data including demographic factors (age and sex), location of perforation, time to operation, operative method, complications, length of hospital stay, and postoperative recovery were reviewed. In all four cases, we treated the defect using the transabdominal approach, which provides a good surgical field of view. The aims of operative intervention, namely primary repair and access for enteral feeding, can be achieved using this approach. The most commonly observed complication was pyothorax, and we suggest the addition of intrapleural drainage for its prevention. Dysgraphia was observed in two patients, which improved with conservative treatment. The overall mortality rate was 0%. Our results demonstrate that primary repair using the transabdominal approach is safe and effective for the management of spontaneous oesophageal perforation. Addition of intrapleural drainage can improve the outcome associated with this approach

Acute diffuse peritonitis due to spontaneous rupture of a primary gastrointestinal stromal tumor of the jejunum: A case report

Introduction: Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal tumors of the gastrointestinal tract. Overt peritonitis caused by GIST rupture is very uncommon. Three types of GIST rupture have been described: closed perforation due to abscess (abscess type), hemoperitoneum leading to rupture of the hematoma capsule in the tumor (hemoperitoneum type), and perforation of the digestive tract via a fistula leading to central necrosis of the tumor (bowel perforation type). This report describes a patient with spontaneous tumor rupture and diffuse peritonitis, a variant of the bowel perforation type of GIST rupture. Presentation of case: A 74-year-old man presented with symptoms of vomiting and abdominal pain. Computed tomography (CT) scan revealed an approximately 10 × 7-cm mass in the pelvis with free air and fluid collection. Emergency laparotomy revealed a tumor in the jejunum, which was ruptured with a hole measuring 5 mm in diameter. The tumor and part of the jejunum were resected. Immunohistochemically, the mass was diagnosed as a GIST originating from the gastrointestinal tract. Despite chemotherapy with imatinib mesylate, the patient died 22 months after surgery. Conclusions: This report describes a patient with acute diffuse peritonitis due to spontaneous rupture of a primary GIST of the jejunum

ガスクロマトグラフィー法による肝胆道疾患の血清胆汁酸測定について : 空腹時血清胆汁酸および内因性胆汁酸負荷テスト

The methods and results of a gas-liquid chromatographic analysis of bile acids in serum are presented. The analysis of bile acids in serum involves enzymatic hydrolysis (cholylglycine hydrolase), preparation of propionated methyl ester derivatives of bile acid and gas chromatographic procedure with 2.5 % OV-1. Adequate separation of the individual bile acids, (cholic, chenodeoxycholic and deoxycholic acid) was achieved with vitamine E caprylate as an internal standard. A detector response was linear and recovery of radioactive taurocholic acid and non-radioactive vitamine E caprylate added to the serum was 82.10±6.86 and 80.96±1.62% respectively. The serum fasting bile acid concentrations of normal controls were 3.17±2.34 for total bile acids, 1.17±1.25 for cholic acid, 1.34±2.11 for chenodeoxycholic acid and 1.29±0.95 μg/ml for deoxycholic acid. The differences in the serum total bile acid levels, magnitude of the increase in the serum concentration between cholic and chenodeoxycholic acid and serum concentration level of deoxycholic acid which were all characterized in various hepatobiliary diseases seemed to be useful for the diagnosis and differential diagnosis of hepatobiliary diseases. However, these serum bile acid concentrations were frequently observed overlapped in some of the individuals among hepatobiliary diseases. An endogenous bile add tolerance test with 2 μg/kg caerulein injection demonstrated more distinction in serum bile acid levels between normal and chronic active hepatitis and between chronic active hepatitis and liver cirrhosis than indicated by a fasting total bile acid level alone. Percent chenodeoxycholic acid increased more than any other individual bile acids during the endogenous bile acid tolerance test suggesting the most important role of chenodeoxycholic acid

Noradrenergic activation in the paraventricular nucleus during acute and chronic immobilization stress in rats: an in vivo microdialysis study

In vivo microdialysis was used to study the effects of single (2 h) or repeated (2 h for 7 consecutive days) immobilization (IMMO) stress on extracellular fluid concentrations of norepinephrine (NE) and the deaminated metabolites of NE and dopamine, dihydroxyphenylglycol (DHPG) and dihydroxyphhenylacetic acid (DOPAC) in the paraventricular nucleus of conscious rats. During IMMO, NE, DHPG, and DOPAC levels increased markedly, with similar peak values and time courses in the repeatedly stressed and previously unstressed groups. NE levels during a 2-h baseline period were lower in the repeatedly stressed group than in the unstressed group (99 ± 9 pg/ml vs. 167 ± 13 pg/ml, P\u3c 0.05), whereas DHPG (1,697 ± 263 pg/ml vs. 1,424 ± 194 pg/ml) and DOPAC (5,989 ± 863 pg/ml vs. 4,428 ± 1150 pg/ml) levels tended to be higher, so that the NE/DHPG ratio at baseline was significantly lower in the repeatedly stressed group (P \u3c 0.05). The results indicate that IMMO stress enhances NE release, reuptake, metabolism, and synthesis in the PVN. Repeated exposure to IMMO may decrease the microdialysate NE/DHPG ratio by inhibiting exocytotic release or enhancing neuronal reuptake of NE. In either case, the results suggest that repeated exposure to stress alters the release and disposition of NE in the PVN of conscious animals. © 1992

Biophysical characterization and single-chain Fv construction of a neutralizing antibody to measles virus

The measles virus (MV) is a major cause of childhood morbidity and mortality worldwide. We previously established a mouse monoclonal antibody, 2F4, which shows high neutralizing titers against eight different genotypes of MV. However, the molecular basis for the neutralizing activity of the 2F4 antibody remains incompletely understood. Here, we have evaluated the binding characteristics of a Fab fragment of the 2F4 antibody. Using the MV infectious assay, we demonstrated that 2F4 Fab inhibits viral entry via either of two cellular receptors, SLAM and Nectin4. Surface plasmon resonance (SPR) analysis of recombinant proteins indicated that 2F4 Fab interacts with MV hemagglutinin (MV-H) with a K-D value at the nm level. Furthermore, we designed a single-chain Fv fragment of 2F4 antibody as another potential biopharmaceutical to target measles. The stable 2F4 scFv was successfully prepared by the refolding method and shown to interact with MV-H at the mu m level. Like 2F4 Fab, scFv inhibited receptor binding and viral entry. This indicates that 2F4 mAb uses the receptor-binding site and/or a neighboring region as an epitope with high affinity. These results provide insight into the neutralizing activity and potential therapeutic use of antibody fragments for MV infection