Nitrergic pathways and L-type calcium channel of MnPO influencing cardiovascular homeostasis

The median preoptic nucleus (MnPO) is one of most important site of the lamina terminalis implicated in the regulation of hydro electrolytic and cardiovascular balance. The purpose of this study was to determine the effect of L-Type calcium channel antagonist, nifedipine, on the increase of median arterial blood pressure (MAP) induce by angiotensin II (ANG II) injected into the MnPO. The influence of nitric oxide (NO) on nifedipine antipressor action has also been studied by utilizing N W-nitro-L-arginine methyl ester (L-NAME) (40 μg 0.2 μL -1) a NO synthase inhibitor (NOSI), 7-nitroindazole (7-NIT) (40 μg 0.2 μL -1), a specific neuronal NO synthase inhibitor (nNOSI) and sodium nitroprusside (SNP) (20 μg 0.2 μL -1) a NO donor agent. We have also investigated the central role of losartan and PD123349 (20 nmol 0.2 μL -1), AT 1 and AT 2, respectively (selective non peptide ANG II receptor antagonists), in the pressor effect of ANG II (25 pmol 0.2 μL -1) injected into the MnPO. Male Wistar rats weighting 200-250 g, with cannulae implanted into the MnPO were utilized. Losartan injected into the MnPO, prior to ANG II, blocked the pressor effect of ANGII. PD 123319 only decreased the pressor effect of ANG II. Rats pre-treated with either 50 μg 0.2 μL -1 or 100 μg 0.2 μL -1 of nifedipine, followed by 25 pmol 0.2 μL -1 of ANG II, decreased ANG II-pressor effect. L-NAME potentiated the pressor effect of ANG II. 7-NIT injected prior to ANG II into the MnPO also potentiated the pressor effect of ANGII but with less intensity than that of L-NAME. SNP injected prior to ANG II blocked the pressor effect of ANG II. The potentiation action of L-NAME and 7-NIT on ANG II-pressor effect was blocked by prior injection of nifedipine. The results described in this study provide evidence that calcium channels play important roles in central ANG II-induced pressor effect. The structures containing NO in the brain, such as MnPO, include both endothelial and neuronal cells, which might be responsible for the influence of nifedipine on the pressor effect of ANG II. These data have shown the functional relationship between L-Type calcium channel and a free radical gas NO in the MnPO, on the control of ANG II-induced pressor effect acting in AT 1 and AT 2 receptors.

Effects of nitric oxide and arginine vasopressin on water intake induced by central angiotensin II. Part 1

We determined the effects of AT 1 and AT 2 (selective no peptides antagonists angiotensin receptors), arginine vasopressin V 1 receptor antagonist as well as L-arginine, a nitric oxide donor and N W-nitro-L-arginine methyl ester (L-NAME), a nitric oxide synthase inhibitor, injected into supraoptic nucleus (SON) on water and sodium intake induced by the injection of angiotensin II (ANGII). Male Holtzman rats weighing 200-250 g with canulae implanted into the SON were used. The drugs were injected in 0.5 μL over 30-60 sec. The water intake after injection of saline SAL+SAL 0.15 M NaCl was 0.40±0.1 mL 2 h -1; SAL+ANGII increase water intake. Losartan decreased the water intake induced by ANGII. PD123319 injected prior to produce no change in water intake induced by ANGII. AVPA prior to ANGII reduced the water intake with a less intensity than losartan. L-arginine prior to ANGII decreases the water intake at a same intensity than losartan. L-NAME prior to ANGII potentiated the dipsogenic effect of ANGII. Losartan injected simultaneously with L-arginine prior to ANGII blocked the dipsogenic effect of ANGII. These results confirm the importance of SON in the control of water intake and strongly suggest that AT 1, V 1 receptors interact with nitrergic pathways within the SON influencing the dipsogenic effect of ANGII.

Natural chromenes and chromene derivatives as potential anti-trypanosomal agents

The aim of the study was to investigate the anti-trypanocidal activities of natural chromene and chromene derivatives. Five chromenes were isolated from Piper gaudichaudianum and P. aduncum, and a further seven derivatives were prepared using standard reduction, methylation and acetylation procedures. These compounds were assayed in vitro against epimastigote forms of Trypanosoma cruzi, the causative agent of Chagas disease. The results showed that the most of the compounds, especially those possessing electron-donating groups as substituents on the aromatic ring, showed potent trypanocidal activity. The most active compound, [(2S)-methyl-2-methyl-8-(3″-methylbut-2″-enyl)-2- (4′-methylpent-3′-enyl)-2H-chromene-6-carboxylate], was almost four times more potent than benznidazole (the positive control) and showed an IC 50 of 2.82 μM. The results reveal that chromenes exhibit significant anti-trypanocidal activities and indicate that this class of natural product should be considered further in the development of new and more potent drugs for use in the treatment of Chagas disease. © 2008 Pharmaceutical Society of Japan.

Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases

Amino acids are well known to be an important class of compounds for the maintenance of body homeostasis and their deficit, even for the polar neuroactive aminoacids, can be controlled by supplementation. However, for the amino acid taurine (2-aminoethanesulfonic acid) this is not true. Due its special physicochemical properties, taurine is unable to cross the blood-brain barrier. In addition of injured taurine transport systems under pathological conditions, CNS supplementation of taurine is almost null. Taurine is a potent antioxidant and anti-inflammatory semi-essential amino acid extensively involved in neurological activities, acting as neurotrophic factor, binding to GABA A/glycine receptors and blocking the excitotoxicity glutamate-induced pathway leading to be a neuroprotective effect and neuromodulation. Taurine deficits have been implicated in several CNS diseases, such as Alzheimer's, Parkinson's, epilepsy and in the damage of retinal neurons. This review describes the CNS physiological functions of taurine and the development of new derivatives based on its structure useful in CNS disease treatment.&; 2012 by the authors; licensee MDPI, Basel, Switzerland.

Dynamics and Conformational Studies of TOAC Spin Labeled Analogues of Ctx(Ile21)-Ha Peptide from Hypsiboas albopunctatus

Antimicrobial peptides (AMPs) isolated from several organisms have been receiving much attention due to some specific features that allow them to interact with, bind to, and disrupt cell membranes. The aim of this paper was to study the interactions between a membrane mimetic and the cationic AMP Ctx(Ile21)-Ha as well as analogues containing the paramagnetic amino acid 2,2,6,6-tetramethylpiperidine-1-oxyl-4-amino-4-carboxylic acid (TOAC) incorporated at residue positions n = 0, 2, and 13. Circular dichroism studies showed that the peptides, except for [TOAC13]Ctx(Ile21)-Ha, are unstructured in aqueous solution but acquire different amounts of α-helical secondary structure in the presence of trifluorethanol and lysophosphocholine micelles. Fluorescence experiments indicated that all peptides were able to interact with LPC micelles. In addition, Ctx(Ile21)-Ha and [TOAC13]Ctx(Ile21)-Ha peptides presented similar water accessibility for the Trp residue located near the N-terminal sequence. Electron spin resonance experiments showed two spectral components for [TOAC0]Ctx(Ile21)-Ha, which are most likely due to two membrane-bound peptide conformations. In contrast, TOAC2 and TOAC13 derivatives presented a single spectral component corresponding to a strong immobilization of the probe. Thus, our findings allowed the description of the peptide topology in the membrane mimetic, where the N-terminal region is in dynamic equilibrium between an ordered, membrane-bound conformation and a disordered, mobile conformation; position 2 is most likely situated in the lipid polar head group region, and residue 13 is fully inserted into the hydrophobic core of the membrane. © 2013 Vicente et al.

Environmental ageing studies of chemically modified micro and nanofibril phenol formaldehyde composites

Cellulose micro and nano fibrils were extracted from banana macro fibres and chemically modified using sodium hydroxide, formic acid, 3-methacryloxy propyltrimethoxy silane. These untreated and chemically treated fibrils were incorporated into PF resin and the specimens were prepared. The composites were subjected to long-term water ageing, thermal ageing soil burial and outdoor weathering. The mechanical properties are reduced under all ageing conditions. The present study investigates the effects of different types of ageing on macro fibre, microfibril and nanofibril reinforced PF composites. The effect of chemical modifications of fibres on the degradability of the composites at different environments also has been analysed. © 2013 Elsevier B.V.

Síntese em fase sólida e estudos comformacionais de análogos contendo TOAC de um peptídeo de rã Hypsiboas albopunctatus

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Síntese do complexo ferro (III) com ácido pirazina tetracarboxílico e aplicação como catalisador em reação fenton

The amount of waste generated by industries has increased gradually in recent years. The proper disposal of residues has been an area of study of many researchers. Several organic compounds are considered potential contaminants of natural waters due to their high toxicity, difficult natural degradation and long persistence in the environment. Ways of recovery and reutilization as well as concepts that minimize the generation of wastes have been increasing widely. Organometallic compound of pyrazine carboxylic acid has proven to be of great interest in many areas. Herein, we studied the use of pyrazine tetracarboxylic acid ligand for complex formation with iron (Fe). The binder (C 8H4N2O8) was synthetized with the addition of Fe (complex) and tested as a catalyst in oxidation reactions of the organic model compound methylene blue (MB). Tetramethyl pyrazine was used in the synthesis, which was oxidized with potassium permanganate in order to form the ligand. The ligand (C 8H4N2O8) was then characterized to validate its formation. For the complex solution, it was used (C 8H4N2O8) and Fe (NO3)3.9H2O 0,01molL-1. After preliminary tests, it was found that the best ratio of Fe and the ligand was 2: 1. Through the oxidation tests, it could be seen that the complex has great potential for the degradation of different concentrations of MB. During only 20 minutes of reaction, approximately 60% of MB 500 mgL -1 was oxidized. The use of the complex was found to be an attractive alternative for oxidation of effluents with high organic compounds levels and contributes to the minimization of organic contaminants hazards in the environment.

Síntese, caracterização e estudo do comportamento térmico dos 2-metoxibenzoatos de Mn(II), Co(II), Ni(II), Cu(II) e Zn(II) no estado sólido

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Síntese, caracterização e estudo do comportamento térmico dos 2-metoxicinamalpiruvatos de lantanídeos (III), exceto promécio, e ítrio (III) no estado sólido

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Dicroísmo circular vibracional e eletrônico na determinação da configuração absoluta de benzopiranos de Peperomia obtusifolia e Piper gaudichaudianum (Piperaceae): implicações biológicas e biossintéticas

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Estudo químico e biológico dos fungos endofílicos associados com a espécie vegetal Alibertia macrophylla (Rubiaceae)

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Uso sustentável de biodiversidade brasileira - prospecção químico-farmacológica em plantas superiores: Alchornea glandulosa, Alchornea triplinervia (Euphorbiaceae), Indigofera truxillensis e Indigofera suffruticosa (Fabaceae)

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Estudo da atividade antibacteriana do picolinato de sacarose em Escherichia coli.Escherichia coli.

Os sucroésteres são empregados como surfactantes, tensoativos, substitutos de gordura e antibióticos. Este trabalho tem como objetivo sintetizar um novo sucroéster derivado do ácido picolínico (ácido 2-piridinocarboxílico), o picolinato de sacarose, e estudar sua atividade antibacteriana in vitrosobre a bactéria Gram-negativa patogênica Escherichia coli. A síntese do picolinato de sacarose foi processada a partir da transesterificação da sacarose com picolinato de metila em condição anidra à 80oC, utilizando dimetil sulfóxido (DMSO) como solvente e K2CO3 como catalisador. A separação dos isômeros formados foi realizada por HPLC no modo semipreparativo e cinco frações cromatográficas foram coletadas e aplicadas em testes de atividade antibacteriana, por disco-difusão em meio sólido, nas concentrações de 150; 300; 450; 600; 750 e 900 μg/mL. As frações 2, 4 e 6 foram ativas contra E.coli. e a fração 4 (900 μg/mL) foi a mais eficiente, sendo selecionada para testes em sinergia com EDTA nas concentrações de 250, 500 e 750 μg/mL, com melhor resultado quando empregado EDTA em 750 μg/mL. Neste caso, os discos apresentaram halos de inibição de crescimento igual ao da Tetraciclina (30 μg/mL) e superior aos produzidos pelos discos com Gentamicina (10 μg/mL). A fração 4 foi caracterizada por FTIR e espectrometria de massas (ESI-MS) e os resultados indicam que se trata sucroéster monossubstituído. Palavras-chave:Sucroquímica. Sucroéster. Sacarose. Picolinato de sacarose. Escherichia coli. Antibiograma por disco-difusão. ABSTRACT Study of antimicrobial activity of sucrose picolinate against Escherichia coli Sucrose esters are generally used as surfactants, fat substitutes and antibiotics. The aim of the present study was to synthesize new sucrose esters derived from picolinic acid (2-pyridine carboxylic acid) and study in vitro antimicrobial activity on the Gramnegative pathogenic bacterium Escherichia coli. The synthesis of sucrose picolinate was performed through the transesterification of sucrose with methyl picolinate under anhydrous conditions at 80 oC using dimethyl sulfoxide (DMSO) as the solvent and K2CO3as the catalyst. The separation of the formed isomers was performed by HPLC in a semi-preparative chromatograph system. Five fractions were collected and applied to a disc-diffusion antibiogram in solidmedium tests at concentrations of 150, 300, 450, 600, 750 and 900 μg/mL. Fractions 2, 4 and 6 were active against E. coli. Fraction 4 (900 μg/mL) was the most efficient and was selected for the determination of antimicrobial activity in synergistic tests with EDTA at concentrations of 250, 500 and 750 μg/mL. The best result was obtained with 750 μg/mL of EDTA. Fraction 4 was characterized as a monosubstituted sucrose ester by FTIR and mass spectrometry (ESI-MS). Keywords: Sucrochemistry. Sucrose. Chromium picolinate sucrose. Escherichia coli. Susceptibility testing by disk diffusion.

Prospecção química e biológica do fungo endofítico Saccharicola sp. isolado de Eugenia jambolana

Pós-graduação em Química - IQ