Synthesis and in vitro evaluation of potential antichagasic dipeptide prodrugs of primaquine

American trypanosomiasis (Chagas' disease) is an endemic parasitic disease afflicting more than 20 million people in Latin America. Currently, therapy is unsatisfactory and only two drugs are available. Primaquine, an antimalarial drug, has trypanocidal activity. Dipeptide derivatives of primaquine, Phe-Arg-PQ, Lys-Arg-PQ, and Phe-Ala-PQ, were synthesized. The choice of the peptides was based on the primary specificity of cruzipain, the major cysteine proteinase from T. cruzi. The prodrugs obtained were tested on the LLC-MK2 cell culture infected with trypomastigotes forms of T. cruzi Phe-Arg-PQ, Lys-Arg-PQ, and Phe-Ala-PQ were active in all stages.

In vitro susceptibility testing of Microsporum gypseum isolated from healthy cattle and soil samples against itraconazole, terbinafine, fluconazole and topical veterinarian drugs

The present study evaluated in vitro susceptibility testing of dermatophytes isolates from healthy cattle and soil samples against three antifungal agents and three topical veterinarian drugs. Itraconazole and terbinafine showed a higher in vitro fungicidal activity than fluconazole. The veterinarian drugs LEPECID (R) and iodine 5% were more active in vitro than the UNGUENTO (R) spray. All drugs showed fungicidal activity against Microsporum gypseum, and they may be considered as efficient agents for the topical treatment of dermatophytoses in cattle.

Evaluation of the performance of pharmacists in terms of providing health assistance at a university hospital

OBJETIVE: This study aimed to assess the practices of pharmacists in Hospital Care. Method - we interviewed 20 pharmacists from the Pharmacy Division by applying a structured instrument, in September 2005. This instrument addressed aspects related to the main activities at the Hospital Pharmacy, which were assessed according to indicators organized into five areas: sector management, hospital pharmacotechniques, committee activities, information and pharmacotherapeutic follow-up, as well as teaching and research activities.RESULTS: the Pharmacy Division considered all structural aspects under analysis as essential for the good development and application of its services. We found that some essential services, such as the Medication Information Service and Pharmacotherapeutic Follow-up, were absent. Pharmacist professionals were dissatisfied about human resource and physical structure dimensioning, and they presented as not very active in terms of Pharmaceutical Care.CONCLUSION: Results indicate that care is still centered on the drug, with few clinical activities. We suggest reformulations in service management, particularly in the management of pharmacists.

Evaluation of transformation growth factor beta(1), interleukin-10, and interferon-gamma in male symptomatic and asymptomatic dogs naturally infected by Leishmania (Leishmania) chagasi

The aims of this study were to evaluate the immunomodulatory role of TGF-beta(1), 1L-10, and INF-gamma in spleen and liver extracts and supernatant cultures of white spleen cells from male symptomatic and asymptomatic dogs, naturally infected by Leishmania (Leishmania) chagasi. Thirty dogs from Aracatuba, São Paulo, Brazil, an endemic leishmaniosis area, were selected by positive ELISA serological reaction for Leishmania sp. and divided into two groups: asymptomatic (n=15) and symptomatic (n=15) consisting of animals with at least three characteristic signs (fever, dermatitis, lymphoadenopathy, onychogryphosis, weight loss, cachex a, locomotion problems, conjunctivitis, epistaxis, hepatosplenomegaly, edema, and apathy). After euthanasia, spleen and liver fragments were collected for ex vivo quantification of TGF-beta(1), IL-10, and INF-gamma. Naturally active in vitro produced TGF-beta(1) was also evaluated in spleen cell culture supernatant. Spleen and liver extract of asymptomatic dogs had higher mean TGF-beta(1) levels than symptomatic dogs. High concentrations of IL-10 were found in spleen, and mainly in liver extract of both groups. Higher INF-gamma concentrations were found in spleen extracts of symptomatic dogs, and in liver extracts of asymptomatic dogs. Extract of this cytokire was lower in spleen extract. Although INF-gamma is being produced in canine infection, mean levels of TGF-beta(1) and IL-10 from spleen and liver extracts were quantitatively much higher; suggesting that immune response in both asymptomatic and symptomatic dogs A as predominantly type Th2. (c) 2006 Elsevier B.V. All rights reserved.

Nymphs in foraging populations of Coptotermes gestroi (Isoptera: Rhinotermitidae)

Food searching activity by subterranean termites involves workers, soldiers and nymphs. The present study was carried out for elucidating aspects of nymph foraging behavior in Brazil where the species Coptotermes gestroi (Wasmann, 1896) is exotic. Monitoring was conducted through making regular collections from seven different colonies for a period of 22 months, which exhibited the production of forager nymphs all year round. A biometric study was conducted to determine the instars of the forager nymphs collected. The identification of male and female nymphs was also conducted for establishing the sex proportion, which was slightly male-biased. From the 533 forager nymphs collected, 34 were from the 3rd instar, 280 from the 4th instar and 219 from 5th instar. The results suggest that 3rd instar nymphs were not too active in the foraging activities because they were collected only in one colony and in an insignificant quantity. (C) Koninklijke Brill NV, Leiden, 2011.

The protist Trichomonas vaginalis harbors multiple lineages of transcriptionally active Mutator-like elements

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

msechBari, a new MITE-like element in Drosophila sechellia related to the Bari transposon

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Electromyographic study of levator scapulae and rhomboideus major muscles in movements of the shoulder and arm

In 21 normal adult male subjects, the muscular activity of the levator scapulae and rhomboideus major muscles was studied electromyographically during the movements of the shoulder and arm. Two single coaxial needle electrodes were used for registering the action potentials. Concerning shoulder movement, it was shown that the levator scapulae was active in elevation and rhomboideus major was active in retraction. Both muscles were inactive during protrusion, in most events. Concerning free movements of the arm, both muscles were active in abduction, elevation, adduction, flexion and circumduction, but inactive in extension. During the same movements, performed with a load, we observed greater intensity in the activity of these muscles in comparison to their activity during free movements.

Electromyographic analysis of superior belly of the omohyoid muscle and anterior belly of the digastric muscle in mandibular movements

The superior belly of the omohyoid muscle and the anterior belly of the digastric muscle, were studied electromyographically in 20 young volunteers. For each muscle, 1 pair of monopolar electrodes was employed. One was a surface electrode and the other a needle electrode, which was inserted in the belly of the muscle. The surface electrode was placed 1 cm apart from the needle electrode. The most marked action of both muscles was on the movement of lowering the mandible. They also act in those movements for the performance of which they have associated a component of lowering the jaw, propulsion, laterality to the right and the left and retrusion. They are not active in the resting position and during jaw movements of elevation, extrusion and protrusion. Both muscles are active most of the time, simultaneously, but it is not possible to demonstrate that there is a synchronism between their actions.

Variation of genetic expression during development, revealed by esterase patterns in Aedes aegypti (Diptera, Culicidae)

Polyacrylamide gel electrophoresis was used to analyze esterase patterns during development of Aedes aegypti from the cities of Marília and São José do Rio Preto (SJRP), Brazil. The zymograms showed a total of 23 esterase bands, 22 of which were in the specimens from Marília and 19 in those from SJRP. These esterase bands were considered to be the product of 23 alleles distributed tentatively in eight genetic loci. Most of the alleles were developmentally regulated. The larval stage expressed the greatest number of them (19 alleles, from the eight loci, in Marília; and 17 alleles, from seven loci, in SJRP). The pupal stage expressed 10 alleles from seven loci, in both populations, and the adult stage expressed 8 alleles from five and six loci in SJRP and Marília, respectively. Some alleles that were active in every stage were developmentally controlled at the level of expression (amount of product). A single allele was constitutively and highly expressed, in larvae, pupae, and adults, in both populations. Differences in esterase synthesis among stages are probably due to regulatory mechanisms acting in agreement with the requirements of a variable number of processes in which esterases are involved. The larval stage is the most active in developmental processes and shows very intense intake of food and very high mobility. These features may demand increased esterase production at that stage. Comparison of the two populations examined showed (besides the existence of alleles that they do not share) that they exhibit differences in the control of expression of other alleles. Such findings may reflect genetic differences between founders in each population, but the possibility of involvement of the intensive use of insecticides in SJRP is also discussed.

Lipids in oocytes of ants Neoponera villosa (Hymenoptera: Ponerinae)

Elements of oocyte of Neoponera villosa ants (workers and queen) were analyzed histochemically and ultrastructurally. It was observed that lipids are the first element to be deposited. They appear in oocytes of all stages. Lipids probably arose in the younger oocytes (stages I and II) from mitochondria of their own cytoplasm and from the nurse cells as well. In mature oocytes (stage III) the cells of the follicular epithelium appears with droplets of lipids in their cytoplasm showing that besides the other sites, this epithelium can also be active in lipid synthesis.

Role of annexin 1 gene expression in mouse craniofacial bone development

BACKGROUND: Annexin 1 is a 37-kDa protein that has complex intra- and extracellular effects. To discover whether the absence of this protein alters bone development, we monitored this event in the annexin-A1 null mice in comparison with littermate wild-type controls. METHODS: Radiographic and densitometry methods were used for the assessment of bone in annexin-A1 null mice at a gross level. We used whole-skeleton staining, histological analysis, and Western blotting techniques to monitor changes at the tissue and cellular levels. RESULTS: There were no gross differences in the appendicular skeleton between the genotypes, but an anomalous development of the skull was observed in the annexin-A1 null mice. This was characterized in the newborn annexin-A1 null animals by a delayed intramembranous ossification of the skull, incomplete fusion of the interfrontal suture and palatine bone, and the presence of an abnormal suture structure. The annexin-A1 gene was shown to be active in osteocytes during this phase and COX-2 was abundantly expressed in cartilage and bone taken from annexin-A1 null mice. CONCLUSIONS: Expression of the annexin-A1 gene is important for the normal development of the skull in mice, possibly through the regulation of osteoblast differentiation and a secondary effect on the expression of components of the cPLA2-COX-2 system. © 2007 Wiley-Liss, Inc.

Expenditures, investment and financing for sustainable development in Trinidad and Tobago

Includes bibliography

Internationalization and technology in MERCOSUR

Includes bibliography

Cellular responses in the Malpighian tubules of Scaptotrigona postica (Latreille, 1807) exposed to low doses of fipronil and boric acid

Studies of sub-lethal effects of pesticide residues on stingless bees are scarce and morphological analysis of organs would add information to toxicological analysis in order to clarify the continuous exposure of Scaptotrigona postica to insecticides. The aim of this study was to evaluate the morphology and histochemistry of the Malpighian tubules (excretory organ) of S. postica exposed to fipronil or boric acid to detect cellular responses that indicate toxicity or adaptative mechanisms to stress induced by exposure of worker bees to low doses of these chemical compounds. Newly emerged bees were submitted to toxicological bioassays and morphological analyses by optical microscopy and Transmission Electron Microscopy, as well as histochemical methods, were performed to detect proteins and glycoconjugates. Additionally, immunohistochemical detection of DNA fragmentation and HSP70 (70-kDa Heat shock protein) were performed to detect cell death and stress response, respectively. Statistical analysis, for the bioassays conducted with ingestion of contaminated diet with boric acid at 0.75% (w/w) or with fipronil at 0.1μg/kg of food, showed that the survival of bees that ingested the contaminated diets were significantly different to the survival rate presented by the control group (P<0.0001). Although some characteristics indicative of initiation of cell death were observed, the cells remained metabolically active in the processes of excretion and inactivation of chemical compounds. The data from this study reinforce the importance of research on sublethal effects of low doses of pesticides on bees in an attempt to assess a possible realistic dose and evaluate the risk assessment of stingless bee S. postica foraging in the vicinity of cultivated fields and/or in green urban areas. © 2013 Elsevier Ltd.