Epoxyalkanoyls as novel ACE inhibitors

The epoxyalkanoyl derivatives were designed and synthesized as ACE inhibitors. Coupling of unsaturated carboxylic acids with amino acids and following epoxidation with dimethyldioxirane gave the epoxyalkanoyls with high yield. The inhibitory activity of synthesized compounds on angiotensin converting enzyme was IC₅₀ values of 0.06≈5.5 μM.     

A preliminary study of the changes in the direct-acting mutagenicities of several nitropolycyclic aromatic hydrocarbons after exposure under sunlight

Five commercially available nitropolyclyclic aromatic hydrocarbons (nitro-PAH), namely, 4-nitrobiphenyl, 2-nitrofluorene, 9-nitroanthracene, 1-nitropyrene, and 2,7-dinitrofluorene, were exposed under restricted sunlight in the open air. The direct-acting mutagenicities of the samples after an exposure of 45 days were measured in order to compare them with those of the original samples in the Ames Salmonella typhimurium bioassay. It was found that the mutagenicities of some nitro-PAH do not change significantly while the mutagenicities of others increase or decrease after exposure. A preliminary study of nitro-PAH reaction products after exposure using GC, GC/MS, and FT-IR is also reported.     

Root avulsion of brachial plexus in infants and children.

Twenty-one patients, under 6 years of age, with root avulsion of the brachial plexus were treated from 1975 to 1987. Among them, 9 had root avulsion of the upper trunk, 2 root avulsion of the lower trunk with middle trunk broken, and 10 root avulsion of the whole brachial plexus. Follow-up of 16 patients showed excellent results in 2 patients, good in 11, fair in 1 and poor in 2. It is suggested that good results can be obtained if multi-paired nerve transfer is adopted in treatment. We conclude that owing to anatomical and physiological characteristics of the respiratory system in children, it is harmful to perform phrenic nerve transfer concomitantly with intercostal nerve transfer. Advisably, two-stage operation is required, otherwise dyspnea and pneumonia are liable to occur. In addition, the time of the operation could be extended to 4-5 years after injury in children, but best results are obtained if the operation is performed within 1 year.

     

Obstructive urinary tract diseases and prenatal diagnosis. Timing of surgical correction]

The Authors are reviewing their experience of Obstructive Uropathies diagnosed and treated surgically in neonates, the last 8 years in their Institution. 67 cases were reviewed, in which 37 presented with ureteropelvic junction obstruction (UPJ). 13 with posterior urethral valves, 11 with primary megaureter and 6 with ureterocele. Prenatal ultrasonography allowed the diagnosis to be made in two third of the patients. UPJ is the most common obstructive uropathy observed. Posterior urethral valves the most severe because of high pulmonary and renal (dysplasia) complication rate. Surgery, when indicated, has no more complications to be expected than in general population, if oriented prophylactic measures are taken in the early peri- and postoperative period.     

Monitoring of serum markers for fibrosis during CCl4-induced liver damage. Effects of anti-fibrotic agents.

Liver fibrosis was induced in rats by repeated peritoneal injections of carbon tetrachloride (CCl4) over a period of 2-11 weeks. Serum procollagen III peptide (SPIIINP), prolidase (SP) and alanine aminotransferase (SALT) levels were monitored during the period of induction. The extent of fibrosis was semi-quantitatively estimated after collagen staining, and the anti-fibrotic effects of 16,16-dimethyl prostaglandin E2 (DMPGE2), colchicine, and zinc sulphate were studied. SPIIINP and SP were increased the first 2 weeks after CCl4 administration and peaked at 6 weeks. Alterations in SPIIINP and SP correlated well to the semi-quantitative histological score of liver sections during the first 6 weeks, and SP was positively related to SPIIINP throughout the whole induction period. DMPGE2 decreased SPIIINP, SP and SALT significantly in addition to a markedly decreased formation of liver collagens. Colchicine had a similar but less dramatic effect, whereas zinc sulphate only reduced SPIIINP without influencing liver damage. In conclusion SPIIINP seems to be a valuable indicator of liver fibrogenesis, and SP may play a limited role in indicating accelerated collagen metabolism in the liver. DMPGE2 obviously inhibited the production of collagens induced by CCl4. Colchicine also had an apparent effect on liver fibrosis, whereas zinc sulphate merely seemed to postpone it.     

The echocardiographic evolution of left ventricular hypertrophy in treated hypertensive patients. A long-term follow-up]

In order to study the possible regressive changes of left ventricular hypertrophy in treated hypertensive patients and to correlate them either with the drugs they received and/or the blood pressure reduction obtained, a long-term (6 years) echocardiographic follow-up study was performed in 61 patients. B and M mode echocardiographic septum and posterior wall thickness and left ventricular mass index were measured yearly and the type of ventricular hypertrophy, asymmetric septal or concentric (symmetric), were compared before and after the follow-up. Sixteen patients received only diuretics; 14, only propranolol, and associated therapy was used in the remaining 31 patients. Average blood pressure was significantly reduced in the whole group of patients, but, individually, 30 of them achieved normal levels for the diastolic (90 mmHg), remaining it over this value in the other, although all of them experienced an average reduction 10 mmHg with therapy. Those patients with concentric hypertrophy at entry showed a significant septal, posterior wall thickness and total ventricular mass reduction during the follow-up, those with initial asymmetric septal hypertrophy, a significant septal thickness and ventricular mass reduction, and those without hypertrophy on admission, showed an average paradoxical increase in septal thickness. We conclude that left ventricular hypertrophy disappeared or decreased in 48% of the patients and that treatment seems to prevent its progression or development in the 43% of all patients. The regressive or favorable changes were significantly more frequent among patients with normal blood pressure after treatment as well as among patients treated only with propranolol in comparison to those treated only with diuretics.