[Beclobrate (Turec) in the treatment of primary hyperlipoproteinemia. I. Effect on cholesterol, lipid and apoprotein levels]. / Beklobrat (Turec) w leczeniu pierwotnej hiperlipoproteinemii. Czesc I: Wplyw na stezenie cholesterolu, lipidy i apoproteiny.

The effects of a new fibric acid derivative--beclobrate (Turec, Zyma) on serum lipid and apoprotein concentrations in 63 patients with primary hyperlipoproteinemia were examined. Beclobrate was given in the evening, 100 mg, once daily. After 3 months of beclobrate treatment mean total cholesterol concentration in serum decreased from 9.35 to 7.73 mmol/l (17.3%), mean LDL-cholesterol concentration from 6.32 to 5.38 mmol/l (14.9%), mean HDL-cholesterol concentration increased by 0.21 mmol/l (15.3% of initial value). The greatest decrease was observed in triglyceride concentration--by 50% of the initial value. Apoprotein B concentration decreased by 19.7%, apoprotein A1 and A2 concentration increased by 20.3% and 26.8% respectively. Higher initial values of total cholesterol and triglyceride concentration in serum were associated with greater concentration decrease after beclobrate treatment.

[Beclobrate (Turec) in the treatment of primary hyperlipoproteinemia. II. Results of the treatment in relation to the type of hyperlipoproteinemia]. / Beklobrat (Turec) w leczeniu pierwotnej hiperlipoproteinemii. Czesc II: Zaleznosc wyników leczenia od postaci hiperlipoproteinemii.

After three months of beclobrate treatment (100 mg once daily) of 63 patients with primary hyperlipoproteinemia (HLP) significant decrease of total cholesterol concentration was found in type IIa by 12.9%, IIb by 23.7%, IV by 20.8%. LDL cholesterol concentration decreased in type IIa by 15.4%, IIb by 8.3%, in type IV non significant increase of LDL cholesterol by 21.6% was observed. Decrease of initial triglyceride level in type IIa by 36.1%, IIb by 41.2%, in type IV by 56.6% was found. HDL-cholesterol concentration increased in all examined HLP types in IIa by 19.5%, IIb by 19.3%, IV by 14.5%. Also initial apolipoprotein A1 and A2 levels increased in all HLP types examined, namely in type IIa respectively by 21.2% and 12.4%, IIb by 25.1% and 11.0%, in type IV by 23.6% and 34.9%. Serum apolipoprotein B concentration decreased significantly in type IIa by 20.5%, IIb by 28.4%, however in type IV a slight increase of apoprotein B level was observed. Comparison of HLP types response to beclobrate treatment revealed that the HLP types examined are significantly different in change size of LDL cholesterol concentration, triglyceride concentration and apoprotein B concentration after treatment.

Degradation of elastin by a cysteine proteinase from Staphylococcus aureus.

Staphylococcus aureus is known to produce three very active extracellular proteinases. One of these enzymes, a cysteine proteinase, after purification to homogeneity was found to degrade insoluble bovine lung elastin at a rate comparable to human neutrophil elastase. This enzyme had no detectable activity against a range of synthetic substrates normally utilized by elastase, chymotrypsin, or trypsin-like proteinases. However, it did hydrolyze the synthetic substrate carbobenzoxy-phenylalanyl-leucyl-glutamyl-p-nitroanilide (Km = 0.5 mM, kcat = 0.16 s-1). The proteolytic activity of the cysteine proteinase was rapidly and efficiently inhibited by alpha 2-macroglobulin and also by the cysteine-specific inhibitor rat T-kininogen (Ki = 5.2 X 10(-7) M). Human kininogens, however, did not inhibit. Human plasma apparently contains other inhibitors of this enzyme, since plasma depleted of alpha 2-macroglobulin retained significant inhibitory capacity. The elastolytic activity of this S. aureus proteinase and its lack of control by human kininogens or cystatin C may explain some of the connective tissue destruction seen in bacterial infections due to this and related organisms such as may occur in septicemia, septic arthritis, and otitis.