Non-ribosomal halogenated protease inhibitors from cyanobacterial isolates as attractive drug targets.

Cyanobacteria possess the ability to produce compounds with remarkable biological activity, and have thus attracted the attention of the pharmaceutical industry. Cyanopeptides acting as protease inhibitors have shown potential in the field of pharmacotherapy through regulation of abnormal physiological processes in the human body. Despite the already described cyanopeptide protease inhibitors, the search for new congeners is of considerable interest which may pave the way for more efficient molecules. In this study, the presence of the protease inhibitors aeruginosin and cyanopeptolin with non-, mono- and dichlorination and also genes coding for their synthetases was investigated in 90 cyanobacterial strains. Mass spectrometry analyses highlighted production of 91, 19 and 3 non-, mono- and dichlorinated congeners, respectively. The purified extract of Microcystis botrys SPC759 inhibited 61% of pepsin protease. PCR amplifications of aeruginosin and cyanopeptolin synthetase gene regions were observed in 41 and 28% of evaluated strains, respectively. The sequences obtained for the aerA-aerB (aeruginosin) and mcnC-mcnE (cyanopeptolin) gene regions grouped together with their homologues found in other cyanobacterial strains in the phylogenetic analyses with high bootstrap support. Antimicrobial activity assays performed using all intracellular extracts inhibited 31 and 26% of Gram-negative and Gram-positive pathogenic bacterial growth, respectively. The results of this study showed the production of aeruginosin and cyanopeptolin and the presence of their genes in several cyanobacterial genera for the first time besides the discovery of novel congeners.

[Percutaneous transluminal coronary angioplasty. Analysis of 305 dilatations]. / Angioplastia coronária transluminal percutânea. Análise de 305 dilatações.

PURPOSE: To show the initial experience of this service with the technique of percutaneous transluminal coronary angioplasty. PATIENTS AND METHODS: Between january 1988 and december 1989, 305 coronary angioplasties were performed in 280 patients with age range of 33 to 82 years (being 49% above 60 years old) and 71% male. Among those, 212 (75%) experienced clinical picture of stable angina and 68 (25%) of unstable angina or myocardial infarction. Patients were divided in three groups: group A--those with lesions of 70% or worse in more than one vessel or in the same vessel with or without any other vessel total occlusion (multiple lesions or multiple vessels: 36 patients; group B--those with lesions of 70% or worse in one vessel with at least one occluded vessel: 64 patients; group C--those with lesions of 70% or worse isolated in a single vessel: 180 patients. RESULTS: Of the 280 treated patients, 229 were considered successful (75%). There has been 22 complications (7%) and 9 deaths (3%). The late follow-up (from 1 to 24 months), displayed 28 new procedures based on clinical suspicion of restenosis. Obstruction or occlusion were present in 16 of the later, with 10 being selected to undergo new procedure, one of those twice. The remaining 12 patients received clinical or surgical treatment. CONCLUSION: Aside from the fact that early and midterm results indeed are promising, the procedure is not safe from immediate risks, and limiting late restenosis. Nevertheless, the lesions might be redilated by the same technique, with success rates comparable to the initial one.