This investigation describes the synthesis of eugenol analogs presenting 1,2,3-triazole fragments and evaluation of their antileishmanial activity. The alkylation of guaiacol (1) with allyl bromide afforded 1-(allyloxy)-2-methoxybenzene (2) (93% yield). The Claisen rearrangement conducted with 1 gave ortho eugenol (3) (82% yield). Alkylation procedures performed with 3 produced 1-allyl-3-methoxy-2-(prop-2-yn-1-yloxy)benzene (4) (73% yield) and 1-allyl-3-methoxy-2-(pent-4-yn-1-yloxy)benzene (6) (53% yield). The copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) reactions involving alkynes 4 and 6 with different benzylic azides afforded twenty-two eugenol analogs with 1,2,3-triazole functionalities (48-93% yield). We screened the compounds at 10 μmol L 1 against Leishmania braziliensis intracellular amastigotes during macrophage infection. The action of these compounds was compared with the known leishmanicidal drug amphotericin B. None of the analogs were toxic to macrophages at 10 μmol L-1. The cytotoxic concentration at 50% (CC50), effective concentration at 50% (EC50), and selectivity index (SI) were determined to the best compounds 4-((2-allyl-6-methoxy)phenoxymethyl)-1-(4-chlorobenzyl)-1 H-1,2,3-triazole (8c) and 4-((2-allyl-6-methoxy)phenoxymethyl)-1-(4-trifluoromethoxybenzyl)-1 H-1,2,3-triazole (8h). They showed a significant leishmanicidal effect, with EC50 of 28.09 µmol L-1 (8c) and 52.03 µmol L-1 (8h). The SIs were 9.7 for 8c and > 5.7 for 8h. These compounds have the potential as new leishmanicidal agents against L. braziliensis and may represent a starting point for the development of alternative treatments for cutaneous leishmaniasis.

Abstract Introduction Irritability has both mood and behavioral manifestations. These frequently co-occur, and it is unclear to what extent they are dissociable domains. We used confirmatory factor analysis and external validators to investigate the independence of mood and behavioral components of irritability. Methods The sample comprised 246 patients (mean age 45 years; 63% female) from four outpatient programs (depression, anxiety, bipolar, and schizophrenia) at a tertiary hospital. A clinical instrument rated by trained clinicians was specifically designed to capture irritable mood and disruptive behavior dimensionally, as well as current categorical diagnoses i.e., intermittent explosive disorder (IED); oppositional defiant disorder (ODD); and an adaptation to diagnose disruptive mood dysregulation disorder (DMDD) in adults. Confirmatory factor analysis (CFA) was used to test the best fitting irritability models and regression analyses were used to investigate associations with external validators. Results Irritable mood and disruptive behavior were both frequent, but diagnoses of disruptive syndromes were rare (IED, 8%; ODD, 2%; DMDD, 2%). A correlated model with two dimensions, and a bifactor model with one general dimension and two specific dimensions (mood and behavior) both had good fit indices. The correlated model had root mean square error of approximation (RMSEA) = 0.077, with 90% confidence interval (90%CI) = 0.071-0.083; comparative fit index (CFI) = 0.99; and Tucker-Lewis index (TLI) = 0.99, while the bifactor model had RMSEA = 0.041; CFI = 0.99; and TLI = 0.99 respectively). In the bifactor model, external validity for differentiation of the mood and behavioral components of irritability was also supported by associations between irritable mood and impairment and clinical measures of depression and mania, which were not associated with disruptive behavior. Conclusions Psychometric and external validity data suggest both overlapping and specific features of the mood vs. disruptive behavior dimensions of irritability.

Five new withanolides, designated as 15-oxo-nicaphysalin B, 6β,7α-dihydroxynicandrenone 10, 24α,25β-dihydroxy-nicandrenone-2 and a mixture of the epimers 17-(1α/1β-methylpropanone)-nicandrenone, in addition to six known others, were isolated from the leaf acetone extract from Nicandra physalodes. The complete structures of the five new withanolides, particularly their relative stereochemistries, were established by extensive spectroscopic analyses, including 1D and 2D nuclear magnetic resonance (NMR) and high-resolution electrospray ionization mass spectrometry (HRESIMS). The main isolated withanolides were evaluated for their antibacterial, antifungal and larvicidal properties, but, except nicandrenone, which showed marginal larvicidal activity, none of them was active.

Introdução:A dissecção endoscópica da submucosa (ESD) já é procedimento consagrado no tratamento do câncer gástrico e esofagiano em suas fases precoces. As lesões colorre-tais, inicialmente abordadas por mucossectomia, em bloco ou em fragmentos, são o foco atual para a abordagem submucosa, principalmente para os tumores de crescimento lateral superficial a partir de 20 mm de diâmetro. A experiência de centros japoneses, referências em endoscopia terapêutica, demonstram redução no índice de recidiva da doença com esta abordagem e, segundo critérios histopatológicos específicos, podem evitar uma colectomia em alguns casos de neoplasia maligna.1-3Relato de caso:Trata-se de paciente de 50 anos, submetida à dissecção endoscópica da submucosa de lesão de crescimento lateral, com 50 mm, localizada no reto, a 8 cm da margem anal. O procedimento foi realizado sem maiores intercorrências, com apenas dois pontos de afastamento da muscular, sem perfuração grosseira, fechados com clipe. Entretanto, a paciente evoluiu com escape aéreo para peritônio, retroperitônio, mediastino e subcútis, sendo tratada sem intervenção adicional, apenas com manejo clínico.Conclusão:É de fundamental importância conhecer e saber aplicar a técnica da ESD, além de abordar suas complicações, uma vez que, mesmo repleta de benefícios em relação à cirurgia, ela pode apresentar desfechos graves.4,5

Introduction:Endoscopic submucosal dissection (ESD) is an already established procedure in the treatment of gastric and esophageal cancer in its early stages. Colorectal lesions, initially approached by endoscopic mucosal resection en bloc or in fragments, are the current focus for submucosal approach, especially for superficial lateral spreading tumor of 20 mm-diameter. The experience of Japanese centers, which are reference in therapeutic endoscopy, demonstrates reduction in the rate of disease recurrence with this approach and, according to specific histopathological criteria, may avoid colectomy in some cases of malignant neoplasia.1-3Case report:The patient was 50-year-old female. She underwent endoscopic submucosal dissection of a rectal lateral spreading tumor measuring 50 mm, located 8 cm from the anal margin. The procedure was performed without major complications, with just two points for muscle layer detachment, without gross perforation and closed with metal clips. However, the patient developed air leakage to the peritoneum, retroperitoneum, mediastinum and subcutaneous tissue, being only treated with clinical procedures and without additional intervention.Conclusion:It is vital to know and be able to apply the technique of ESD, in addition to addressing its complications, since despite the numerous benefits compared to surgery, ESD can result in serious outcomes.4,5

Nesse trabalho, um método sonoquímico de síntese de nanoestruturas de sulfeto de bismuto em 1D e 3D foi desenvolvido e comparado com uma rota sintética empregando aquecimento sob refluxo. O método sonoquímico monstrou ser mais rápido e eficiente na obtenção de nanoestruturas com alta homogeneidade morfológica. A forma e qualidade dos nanocristais foram dependentes do tipo de solvente empregado na síntese. Superestruturas em 3D semelhantes a flores foram obtidas quando etileno glicol puro foi utilizado como solvente, enquanto estruturas em 1D na forma de nanobastões foram obtidas quando utilizada uma mistura de dimetilsulfóxido e etileno como solvente.

In this work, a sonochemical method to synthesize nanostructures of bismuth sulfide in 1D and 3D framework was developed and compared with a synthetic route with heating under reflux. The sonochemical method showed to be faster and more efficient than refluxing method to obtain nanostructures with high morphological homogeneity. Form and quality of the nanocrystals were dependent on the type of solvent employed in the synthesis procedure. 3D flower-like superstructures were obtained when ethylene glycol was used as solvent, while 1D nanorods were obtained when a mixture of dimethyl sulfoxide and ethylene glycol was used as solvent.

Sulfated polysaccharides were extracted with acetone from brown algae Padina gymnospora. The fraction precipitated with 1.5 volumes of acetone (F1.5) purified in Sephadex G-75 was characterized by infrared and nuclear magnetic resonance of 13C and ¹H, through which the presence of sulfate groups on the C4 of α-L-fucose could be observed. This polysaccharide showed that an MW of 25,000 Da was effective in reducing leukocyte influx into the peritoneal cavity in mice at 10 mg/kg and 25 mg/kg body weight, causing a decrease of 60 and 39%, respectively. In the present study, it was observed that this fucan has anti-inflammatory properties but no cytotoxic action, indicating its potential use in the pharmaceutical industry.

O estudo foi desenvolvido no Parque Estadual de Dois Irmãos, um fragmento de Floresta Atlântica, em Recife - PE, no período de maio/1998 a dezembro/2000. Sabicea cinerea é uma espécie lianescente encontrada na borda da mata, que produz flores por todo ano, com pico de floração na estação seca (setembro a fevereiro). Apresenta flores distílicas, actinomorfas, tubulosas, com pétalas brancas e antese iniciando por volta das 5:00 h, quando o néctar já está disponível; a produção de néctar estende-se até às 16:00 h. O volume médio diário de néctar foi de 8,0 µL e a concentração média de açúcares, de 24%, em ambos os morfos florais. As flores brevistilas possuem a corola e os grãos de pólen maiores em relação às flores longistilas, não havendo, entretanto, diferenças na quantidade dos grãos produzidos entre os dois morfos. Como visitantes florais, foram observados Phaethornis ruber, um dos principais polinizadores, e Amazilia sp., um pilhador. Além desses beija-flores, várias espécies de abelhas Apidae, Anthophoridae e Halictidae, borboletas Hesperiidae e Nymphalidae e moscas Syrphidae, visitavam as flores. A auto-incompatibilidade foi constatada através dos testes de polinização controlada, que resultaram na formação de frutos apenas nos cruzamentos intermorfo. A análise do crescimento dos tubos polínicos confirmou a ocorrência da auto-incompatibilidade esporofítica. A eficiência no transporte de pólen entre os morfos florais é a principal e mais importante função desempenhada pelos polinizadores para que ocorra a manutenção dos agrupamentos de indivíduos de S. cinerea, principalmente por esta espécie apresentar um sistema reprodutivo do tipo xenógamo obrigatório.

The breeding system and pollination biology of Sabicea cinerea were studied at "Parque Estadual Dois Irmãos", a fragment of Atlantic forest, in Recife, State of Pernambuco, Brazil, from May/1998 to December/2000. Sabicea cinerea is a vine found in the forest border and which produces flowers throughout the year, with the flowering peak occurring in the dry season (September to February). It presents distylous, actinomorphic, tubular flowers, with white petals. Anthesis begins about 5.00 a.m. nectar production continues until 4.00 p.m.; the daily mean average volume was 8.0 µL and sugar concentration 24%, in both floral morphs. Short-styled (thrum) flowers possess larger corolla and pollen grains in relation to the long-styled (pin) flowers, but there are no differences in the amount of grains between the morphs. Two species of hummingbird visited S. cinerea flowers, Phaethornis ruber, the main pollinator, and Amazilia sp., a nectar thief. Several species of Apidae, Anthophoridae and Halictidae bees, Hesperiidae and Nymphalidae butterflies and Syrphidae flies were also observed visiting Sabicea cinerea flowers. The self-incompatibility of the species was verified through experiments of controlled pollination in field; fruit set was observed only in the intermorph crossings. The occurrence of the sporophytic selfincompatibility was confirmed with the analysis of pollen tubes growth in both floral morphs. The efficiency in pollen transfer among the floral morphs is the main and more important function carried out by the pollinators in order to maintain the S. cinerea populations, mainly because it presents an obligatory xenogamous reproductive system.