Formation of aminosuccinyl derivative from β-phenacyl aspartyl peptides catalyzed by sodium thiophenoxide

In the solid-phase synthesis of cholecystokinin 30–33, Trp-Met-Asp-Phe- amide, the β-phenacyl ester was used to protect the β-carboxyl of aspartyl residue. The ester was cleaved, on the solid support, with a 1 M solution of sodium thiophenoxide in DMF, prior to ammonolysis. The product, after purification by countercurrent distribution, was identified as a mixture of isoasparaginyl and aspartyl peptides. A study of the deprotection step, with sodium thiophenoxide, on a model peptide (t-butyloxycarbonyl-β-phenacyl-aspartyl-phenylalanineamide) showed the rapid formation of the aminosuccinyl derivative, catalyzed by this reagent.     

Management of Pseudomonas Aeruginosa Lung Infection in Danish Cystic Fibrosis Patients

ABSTRACT. The annual mortality rate of cystic fibrosis patients with chronic Pseudomonas aeruginosa lung infection at the Danish CF-centre ranged from 10 to 20% in the years 1970–1975. In this period the patients received antipseudomonal chemotherapy only during acute exacerbations of infection. From 1976 99 patients acquired chronic P. aeruginosa infection and were given regular and intensive antipseudomonal treatment 3–4 times per year. The patients were followed for 612 patient-years; 7 died and the 10-year survival rate after onset of P. aeruginosa infection was 90%±4%. The annual mortality rate is now 1–2%. Although precipitating antibodies against P. aeruginosa increased significantly, pulmonary function did not deteriorate with duration of infection. Cross-infection between patients caused an increased incidence of chronic P. aeruginosa infection which was reduced by hygienic measures.     

Complications related to thoracic epidural analgesia: a prospective study in 1071 surgical patients

In a prospective study, the complications of 1071 patients scheduled for thoracic epidural catheterization for postoperative analgesia (TEA) were studied. All catheters were inserted preoperatively between segment Th 2/3 and Th 11/12 under local anesthesia. Balanced anesthesia with endotracheal intubation and TEA were combined. Postoperatively 389 patients (36.9%) were monitored on a normal surgical ward. Buprenorphine, 0.15 to 0.3 mg, and if needed bupivacaine 0.375% 3–5 ml h^-1 were given epidurally. Primary perforation of the dura occurred in 13 patients (1.23%). Radicular pain syndromes were observed in six patients (0.56%). In one patient (0.09%) respiratory depression was seen in close connection with the epidural administration of 0.3 mg buprenorphine. Although 116 patients (10.83%) showed one abnormal clotting parameter but no clinical signs of hemorrhage, there was no complication related to this group. No persisting neurological sequelae caused by the thoracic epidural catheters were found. In conclusion, continuous TEA with buprenorphine for postoperative pain relief after major abdominal surgery is a safe method without too high a risk of catheter-related or drug-induced complications, even on a normal surgical ward and when one clotting parameter is abnormal.     

The pathogenesis of miliaria rubra

Anhidrosis was induced in volunteers by covering the skin with an impermeable plastic film. The degree of sweat suppression and miliaria after a thermal stimulus was directly proportional to the increase in the density of resident aerobic bacteria, notably cocci. No anhidrosis resulted when antibacterial substances were used to prevent the expansion of the microflora. Histological study showed a PAS-positive diastase resistant amorphous mass deep within the acrosyringium after 2 days of occlusion, accompanied by a periductal dermal infiltration of leukocytes. After another 2 days the duct became clogged by an amalgam of degenerating leukocytes. This impaction sloughed after about 3 weeks as a result of epidermal renewal. Colonies of bacteria were never found within the ducts. It is postulated that cocci secrete a toxin which injures luminal cells and precipitates a cast within the lumen. Infiltration by leukocytes creates an impaction which completely obstructs the passage of sweat for several weeks.     

Cleavage of aspartyl β-phenacyl esters by selenophenol under neutral conditions

Neutral selenophenol in DMF accomplished the removal of the β-phenacyl protecting group of aspartic acid in solution, on the peptide Boc-Asp(β-OPac)-Phe amide and on the resin peptide Boc-Trp(Nⁱⁿ-For)-Met-Asp(β-OPac)-Phe- (CCK 30–33) without α, β-rearrangement.     

Circadian Characteristics of Urinary Melatonin from Clinically Healthy Young Women at Different Civilization Disease Risks

ABSTRACT Rhythm characteristics in the about-daily (circadian) and about-yearly (circannual) frequency ranges were assessed for urinary melatonin. Clinically healthy women in Minnesota, USA, and Kyushu, Japan, were sampled around the clock once in 1-4 seasons. Possible differences that could reflect the large difference in breast cancer incidence in these two geographic locations were investigated. Each subject's risk of developing breast cancer, cardiovascular diseases resulting from an elevated blood pressure, and emotional conditions was numerically evaluated according to epidemiologic questionnaires. A prominent circadian rhythm characterizes urinary melatonin in both populations, peaking in the middle of the night. The American women exhibit a larger circadian rhythm-adjusted mean (mesor) than do the Japanese women. A circannual rhythm is also apparent in the North American women, but not in the Japanese women. The circadian mesor of urinary melatonin correlates negatively with the risk score of emotional depression and positively with that of developing cardiovascular diseases.