Synthesis of cationic beta-vinyl substituted meso-tetraphenylporphyrins and their in vitro activity against herpes simplex virus type 1

An easy route to cationic beta-vinyl substituted meso-tetraphenylporphyrin derivatives is described. Two novel compounds were tested in vitro for their antiviral photoactivity against herpes simplex virus type 1. One of these compounds exhibited a significant activity, reaching 99% of virus inactivation after 15 min of photoactivation.     

Modelling and Operation of a Turbidity-Meter for On-Line Monitoring of Microbial Growth in Fermenters

The PROIMI-2 prototype turbidity-meter for measuring cell concentrations in stirred tanks, has been designed and constructed using theories based on kinetic laws and the general principles of cell growth. Laboratory assays were carried out with batch cultures of Bacillus amyloliquefaciens, Zymomonas mobilis and Saccharomyces cerevisae. The signals showed a good correlation with optical density and biomass. In the latter case up to 4·0 g per dm³ expressed as dry weight could be monitored successfully.     

Cell types and evidences for traumatic cell death in a pressure-bearing tendon of Rana catesbeiana

Tendon fibrocartilages appear in areas subjected to compressive forces. The bullfrog plantaris longus tendon was shown to be subjected to compression and to develop a modified region which differs from fibrocartilage in many respects. Ultrastructural analyses of the compression region of the bullfrog tendon demonstrated the existence of typical fibroblasts in the fibrous areas and large cells with abundant cytoplasm filled with intermediate type filaments. This large cell type has organelles restricted to a small perinuclear area or dispersed in the network of intermediate type filaments. Other cells were also found and exhibited less abundant deposition of intermediate filaments, showing an organization intermediate between fibroblasts and typical cells from the compression region. These intermediate type cells are closely associated with collagen bundles while the large cells seemed to have no connection with the fibrous components, but are immersed in a glycosaminoglycan-rich extracellular matrix. Aspects of cell death in association with extracellular matrix disruption were observed in some instances and it is likely that these are associated with traumatic stimulation of the tendon, especially when it is submitted to the sudden and strong mechanical loading expected to occur during jumping. Since the damage occurred mainly in cells of the intermediate type, it is assumed that accumulating intermediate type filaments is a protective mechanism against compressive forces to which this tendon is subjected.     

Lamotrigine and phenytoin, but not amiodarone, impair peripheral chemoreceptor responses to hypoxia.

Amiodarone, lamotrigine, and phenytoin, common antiarrhythmic and antiepileptic drugs, inhibit a persistent sodium current in neurons (I(NaP)). Previous results from our laboratory suggested that I(NaP) is critical for functionality of peripheral chemoreceptors. In this study, we determined the effects of therapeutic levels of amiodarone, lamotrigine, and phenytoin on peripheral chemoreceptor and ventilatory responses to hypoxia. Action potentials (APs) of single chemoreceptor afferents were recorded using suction electrodes advanced into the petrosal ganglion of an in vitro rat peripheral chemoreceptor complex. AP frequency (at Po(2) approximately 150 Torr and Po(2) approximately 90 Torr), conduction time, duration, and amplitude were measured before and during perfusion with therapeutic dosages of the drug or vehicle. Hypoxia-induced catecholamine secretion within the carotid body was measured using amperometry. With the use of whole body plethysmography, respiration was measured in unanesthesized rats while breathing room air, 12% O(2), and 5% CO(2), before and after intraperitoneal administration of amiodarone, lamotrigine, phenytoin, or vehicle. Lamotrigine (10 microM) and phenytoin (5 microM), but not amiodarone (5 microM), decreased chemoreceptor AP frequency without affecting other AP parameters or magnitude of catecholamine secretion. Similarly, lamotrigine (5 mg/kg) and phenytoin (10 mg/kg) blunted the hypoxic but not the hypercapnic ventilatory response. In contrast, amiodarone (2.5 mg/kg) did not alter the ventilatory response to hypoxia or hypercapnia. We conclude that lamotrigine and phenytoin at therapeutic levels impair peripheral chemoreceptor function and ventilatory response to acute hypoxia. These are consistent with I(NaP) serving an important function in AP generation and may be clinically important in the care of patients using these drugs.     

Purification of a thermostable antinociceptive lectin isolated from Andira anthelmia

Andira anthelmia (tribe Dalbergieae), a plant from Brazilian Amazon, possesses a seed lectin that was purified by affinity chromatography in sepharose–mannose. This novel Dalbergieae lectin, named AAL, agglutinated rabbit erythrocytes treated with trypsin. The hemagglutinating activity of AAL was maintained after incubation at a wide range of temperature (40 to 70 °C) and pH, was shown to be dependent on divalent cations, and was inhibited by d ‐mannose and d ‐sucrose. AAL showed an electrophoretic profile in sodium dodecyl sulfate–polyacrylamide gel electrophoresis similar to other lectins of the tribe Dalbergieae, presenting a double band of molecular weight with approximately 20 kDa and other minor bands of 17, 15, and 13 kDa, being the smaller fragment glycosylated. AAL injected by intravenous route in mice showed antinociceptive activity in two behavioral tests (writhing and formalin). In the writhing test induced by acetic acid, AAL showed inhibitory effect at 0.01 mg/kg (68%), 0.1 mg/kg (46%) and 1 mg/kg (74%). In the formalin test, AAL (0.1 mg/kg) inhibited by 48% the licking time in the inflammatory phase, an effect that was recovered by the lectin association with mannose. In conclusion, AAL presents analgesic effect involving the lectin domain via peripheral mechanisms of inflammatory nociception. This activity highlights the importance of lectins as tools to be used for understanding the interaction of protein–carbohydrate in processes associated to inflammatory pain. Copyright © 2015 John Wiley & Sons, Ltd.     

Selection of an extracellular esterase-producing microorganism

Summary The conventional esterase plate-screening technique has been modified in order to obtain a better differentiation of high producing strains. A short exposure to Lugol's iodine solution after colony growth enhanced the contrast between the precipitation halo and the background. Batch cultures of a selected strain characterized as belonging to theBacillus subtilis group showed a high level of extracellular activity at pH 6.6 to 8.0 and 35°C. In crude extracts the optimum enzymatic activity was obtained at 35°C and pH 7.0.     

Evaluation of Parasiticide Treatment with Benznidazol in the Electrocardiographic,Clinical, and Serological Evolution of Chagas Disease

IntroductionChagas disease is one of the most important endemic parasitic diseases in Latin America. In its chronic phase, progression to cardiomyopathy has high morbidity and mortality. The persistence of a normal electrocardiogram (ECG) provides a similar prognosis to that of a non-diseased population. Benznidazole (BNZ) is the only drug with trypanocidal action available in Brazil.Materials/Methods/ResultsA group of 310 patients with chronic Chagas disease who had normal ECGs at the first medical visit performed before 2002 were included. There were 263 patients treated with BNZ and 47 untreated. The follow-up period was 19.59 years. Univariate analyses showed that those treated were younger and predominantly male. As many as 79.08% of those treated and 46.81% of those untreated continued with normal electrocardiograms (p <0.0001). The occurrence of electrocardiographic abnormalities and relevant clinical events (heart failure, stroke, total mortality, and cardiovascular death) was less prevalent in treated patients (p <0.001, p: 0.022, p: 0.047 respectively). In multivariate analyses, the parasiticide treatment was an independent variable for persistence of a normal ECG pattern, which was an independent variable in the prevention of significant clinical events. The immunofluorescence titers decreased with the parasitological treatment. However, the small number of tests in untreated patients did not allow the correlation of the decrease of these titers with electrocardiographic alterations.ConclusionThese data suggest that treatment with benznidazole prevents the occurrence of electrocardiographic alterations. On the other hand, patients who develop ECG abnormalities present with more significant clinical events.