Lucielli Savegnago

Universidade Federal de Pelotas

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Diego Alves

Universidade Federal de Pelotas

Eder J. Lenardão

Universidade Federal de Pelotas

Cristina W. Nogueira

Universidade Federal de Santa Maria

Angela Maria Casaril

The University of Texas MD Anderson Cancer Center

Mariana G. Fronza

Universidade Federal de Pelotas

Tiago Collares

Universidade Federal de Pelotas

Fabiana K. Seixas

Universidade Federal de Pelotas

Cristiano R. Jesse

Universidade Federal do Pampa

Raquel G. Jacob

Universidade Federal de Pelotas

Paloma T. Birmann

Universidade Federal de Pelotas

Cooperative Institutions

Universidade Federal de Pelotas

205

Universidade Federal de Santa Maria

Universidade Federal do Rio Grande do Sul

Universidade de São Paulo

Universidade Federal do Pampa

Universidade Federal de Santa Catarina

Universidade Federal do Rio Grande

Instituto de Ciências Farmacêuticas

Universidade de Caxias do Sul

Universidade Federal de São Carlos

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2′-Hydroxychalcones as an alternative treatment for trichomoniasis in association with metronidazole

Parasitology Research (2019)

Raquel Nascimento das Neves Ângela Sena-Lopes Mirna Samara Dié Alves Bárbara da Rocha Fonseca Caroline Carapina da Silva

Trichomoniasis

Vero cell

10.1007/s00436-019-06568-4

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Citations (9)

Selenylated Analogs of Tacrine: Synthesis, in Silico and in Vitro Studies of Toxicology and Antioxidant Properties

Chemistry - An Asian Journal (2024)

Manoela Sacramento Roberto B. Morais Ariana Silveira Lima Giuliana P. Zugno Renata L. de Oliveira

We present our results on the synthesis and preliminary in silico and in vitro studies of the toxicology and antioxidant properties of selenylated analogs of Tacrine. Initially, we synthesized 2-aminobenzonitriles containing an organic selenium moiety, resulting in sixteen compounds with various substituents linked to the portion derived from diorganyl diselenide. These compounds were then used as substrates in reactions with cyclic ketones, in the presence of 1.4 equivalents of trifluoroboroetherate as a Lewis acid, to synthesize selenylated analogs of Tacrine with yields ranging from 20 % to 87 %. In silico studies explored computational parameters related to antioxidant activity and hepatotoxicity. In vitro studies elucidated the antioxidant effects of Tacrine and its selenium hybrid (TSe) in neutralizing ABTS radicals, scavenging DPPH radicals, and reducing iron ions. Additionally, the acute oral toxicity of one synthesized compound was evaluated.

Tacrine

10.1002/asia.202400637

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Citations (0)

Mechanisms involved in the antidepressant-like action of orally administered 5-((4-methoxyphenyl)thio)benzo[c][1,2,5]thiadiazole (MTDZ) in male and female mice

Psychopharmacology (2024)

Karline da Costa Rodrigues Meliza da Conceição Oliveira Beatriz F. dos Santos Nélson Domingues Mariana G. Fronza

Thio-

Mechanism of Action

10.1007/s00213-024-06647-0

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Quinolines-1,2,3-triazolylcarboxamides exhibits antiparasitic activity in Trichomonas vaginalis

Biotechnology Research and Innovation (2019)

Ângela Sena-Lopes Raquel Nascimento das Neves Mirna Samara Dié Alves Gelson Perin Diego Alves

Increased prevalence of metronidazole-resistant infections has resulted in a search for alternative drugs for the treatment of trichomoniasis. In the present study, we report the evaluation of in vitro activity of three quinolines-1,2,3-triazolylcarboxamides (QTCA-1, QTCA-2 and QTCA-3) against Trichomonas vaginalis, evaluation of cytotoxicity in CHO cells and expression of genes related to hydrogenosome by real time PCR. Nine concentrations of these compounds were analyzed for in vitro activity against ATCC 30236 isolate of T. vaginalis. QTCA-2 reported a cytotoxic effect against 100% of T. vaginalis trophozoites at a final concentration of 80 μM with an IC50 of 50 μM. The kinetic growth curve of trophozoites indicated that QTCA-2 reduced the growth by 70% at a concentration of 80 μM after an exposure of 12 h, and induced complete parasite death at 24 h. QTCA-2 induced less than 30% of cytotoxicity in CHO-K1 cells at 80 μM and data showed this concentration and lower ones had no significant cytotoxic effect when compared to the control. There was no significant difference in gene expression (pyruvate-ferredoxin oxidoreductase A and B; Malic enzyme D; Hydrogenase; β-tubulin) when compared to control and MTZ. Further in silico analysis showed that QTCA-2 had significant binding free energy with T. vaginalis lactate dehydrogenase (−9.3 kcal/mol), purine nucleoside phosphorylase (−9.1 kcal/mol) and triosephosphate isomerase (−7.3 kcal/mol). The present study offers new perspectives for exploring the potential of this class of molecules as an additional option for the treatment of trichomoniasis.

Antiparasitic

Trichomonas

Antiparasitic agent

10.1016/j.biori.2019.06.003

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Citations (1)

Convenient Michael addition/β-elimination approach to the synthesis of 4-benzyl- and 4-aryl-selenyl coumarins using diselenides as selenium sources

Tetrahedron Letters (2017)

Gustavo Padilha Paloma T. Birmann Micaela Domingues Teodoro S. Kaufman Lucielli Savegnago

Michael reaction

Tandem

10.1016/j.tetlet.2017.01.084

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Citations (20)

Protective effects of octylseleno-xylofuranoside in a streptozotocin-induced mouse model of Alzheimer's disease

European Journal of Pharmacology (2021)

Rodolfo Baldinotti Mariana G. Fronza Jenifer Fetter Luana Aparecida Alves da Silva Camila Bonemann Bender

10.1016/j.ejphar.2021.174499

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Citations (4)

Antidepressant-like effect of a new selenium-containing compound is accompanied by a reduction of neuroinflammation and oxidative stress in lipopolysaccharide-challenged mice

Journal of Psychopharmacology (2017)

Angela Maria Casaril Micaela Domingues Mariana G. Fronza Beatriz Vieira Karine R. Begnini

Organoselenium compounds and indoles have gained attention due to their wide range of pharmacological properties. Depression is a recurrent and disabling psychiatric illness and current evidences support that oxidative stress and neuroinflammation are mechanisms underlying the pathophysiology of this psychiatric condition. Here, we evaluated the effect of 3-((4-chlorophenyl)selanyl)-1-methyl-1H-indole (CMI) in lipopolysaccharide (LPS)-induced depressive-like behaviour, neuroinflammation and oxidative stress in male mice. CMI pre-treatment (20 and 50 mg/kg, intragastrically) significantly attenuated LPS (0.83 mg/kg, intraperitoneally)-induced depressive-like behaviour in mice by reducing the immobility time in the tail suspension test (TST) and forced swimming test (FST). CMI pre-treatment ameliorated LPS-induced neuroinflammation by reducing the levels of interleukin (IL)-1β, IL-4 and IL-6 in the hippocampus and prefrontal cortex, as well as markers of oxidative damage. Additionally, we investigated the toxicological effects of CMI (200 mg/kg, i.g.) in the liver, kidney and brain through determination of the activity of aspartate aminotransferase (AST), alanine aminotransferase (ALT), δ-aminolevulinate dehydratase (δ-ALA-D) and creatinine levels. These biomarkers were not modified, indicating the possible absence of neuro-, hepato- and nephrotoxic effects. Our results suggest that CMI could be a therapeutic approach for the treatment of depression and other neuropsychiatric disorders associated with inflammation and oxidative stress.

Tail suspension test

10.1177/0269881117711713

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Citations (64)

Phenylselanyl-1H-1,2,3-triazole-4-carbonitriles: synthesis, antioxidant properties and use as precursors to highly functionalized tetrazoles

RSC Advances (2015)

Lucielli Savegnago Manoela Sacramento Lucimar M. Pinto Brod Mariana G. Fronza Natália Seus

We describe herein our results on the synthesis, antioxidant properties and chemical diversification of phenylselanyl-1H-1,2,3-triazole-4-carbonitriles.

Triazole

10.1039/c5ra22445d

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Citations (29)

Selenium compounds in Click Chemistry: copper catalyzed 1,3-dipolar cycloaddition of azidomethyl arylselenides and alkynes

Tetrahedron (2012)

Natália Seus Maiara T. Saraiva Eduardo E. Alberto Lucielli Savegnago Diego Alves

Sodium ascorbate

10.1016/j.tet.2012.07.019

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Citations (30)

Effect of oral administration of diphenyl diselenide on antioxidant status, and activity of delta aminolevulinic acid dehydratase and isoforms of lactate dehydrogenase, in streptozotocin-induced diabetic rats