We describe herein a new approach to prepare unprecedented bioactive indolizine motifs decorated with organosulfur and organoselenium groups. A total of 12 1sulfanylindolizines and 2 1-selanylindolizines were prepared in excellent yields by an intramolecular annulation of easily prepared chalcogen-containing pyridinium salts. The reaction is fast (1 h at 70 °C or 5 min under sonication) and transitionmetal-free, using glycerol as a green solvent.
The monoaminergic dysfunction plays a central role in major depressive disorder (MDD), a mental disturbance associated with constant feeling of sadness and lack of interest. The available treatments do not present a desirable efficacy and some of them provoke several adverse effects. In this context, organoselenium compounds and molecules containing the indolizine nucleus have demonstrated interesting pharmacological properties, including antidepressant-like effects. In this study, the antidepressant-like effect of 2-phenyl-1-(phenylselanyl)indolizine (SeI), a selenium-containing indolizine derivative, was investigated on the forced swimming test (FST) and on the tail suspension test (TST) in male Swiss mice. The involvement of the serotonergic system in this effect was also accessed. The selenium compound SeI (10−100 mg/kg, intragastrical (i.g.)) was administered 0.5 h before the behavioral tests, and it diminished the immobility on both FST and TST experiments, which is an indication of antidepressant-like effect. No changing in the locomotor motion was observed in the open-field test (OFT). The anti-immobility effect of SeI was not altered by the preadministration of the selective serotonergic receptor antagonists ondansetron (1 mg/kg, intraperitoneally (i.p.), antagonist of 5-HT 3 receptor) and WAY100635 (0.1 mg/kg, subcutaneous route (s.c.), antagonist of 5-HT 1A receptor). In contrast, the preadministration of ketanserin (1 mg/kg, i.p., antagonist of 5-HT 2A/C receptor) blocked this effect, demonstrating that the antidepressant-like effect of SeI involves 5-HT 2A/C . In addition, molecular docking studies showed a strong interaction between SeI and the receptors of 5-HT 2A and 5-HT 2C . The toxicological results demonstrated that SeI has low potential to cause adverse effects in mice. It was found that the antidepressant-like effect of SeI is related to modulation of the serotonergic system, and this selenium compound could be included in new treatment approaches for MDD.
A Botânica é negligenciada no ensino de Biologia para o ensino fundamental e médio. Dessa forma, o Projeto de Ensino Jogos Botânicos, do Laboratório de Sistemática e Evolução de Plantas da Universidade Federal de Pelotas, foi criado para abordar o ensino de Botânica de forma lúdica, buscando tornar os assuntos relacionados ao reino das plantas mais interessantes e próximos da comunidade. Nesse sentido, foram elaborados jogos didáticos com intuito de apresentar os assuntos de forma simples e atraente aos estudantes. O jogo Enraizando foi inspirado em um tabuleiro dinâmico de xadrez, tornando o ensino de fisiologia vegetal mais interessante aos alunos. Da mesma forma, o jogo Batalha Algal foi inspirado no jogo batalha naval, dinamizando os conteúdos referentes às algas. Este trabalho apresenta propostas didáticas no ensino de Botânica, a fim de auxiliar os professores, do ensino fundamental e médio, em uma transposição didática mais efetiva e de maneira lúdica.
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