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6. Bioassay-guided isolation of leishmanicidal cucurbitacins from Momordica charantia.

Author

Silva Marques, Maria Carolina, Cristiane Yoshida, Nídia, Torres-Santos, Eduardo Caio, Rodrigues Garcez, Fernanda, and Silva Garcez, Walmir

Subjects
NEGLECTED diseases, MOMORDICA charantia, LEISHMANIASIS, PERITONEAL macrophages, CYTOTOXINS, MEDICINAL plants, BIOLOGICAL assay
Abstract

Introduction: Leishmaniasis, a neglected tropical parasitic disease, is regarded as a major public health problem worldwide. The first-line drugs for leishmaniasis suffer from limitations related to toxicity and the development of resistance in certain parasitic strains. Therefore, the discovery of alternative treatments for leishmaniasis is imperative, and natural products represent a valuable source of potential therapeutic agents. Methods: The present study aimed at finding new potential antileishmanial agents from the aerial parts of the medicinal plant Momordica charantia. This study was based on bioassay-guided fractionation of the M. charantia extract against promastigotes and amastigotes of Leishmania (Leishmania) amazonensis. The cytotoxicity of the extract, fractions, and isolated compounds were evaluated against peritoneal murine macrophages by employing the MTT assay for assessing cell metabolic activity. Results: Antileishmanial assay-guided fractionation of the M. charantia extract led to the bioactive cucurbitacin-enriched fraction and the isolation of four bioactive cucurbitacin-type triterpenoids, which exhibited significant antileishmanial activity, with IC50 values between 2.11 and 3.25 μg.mL−1 against promastigote and amastigote forms, low toxicity and selectivity indexes ranging from 8.5 to 17.2. Conclusion: Our findings demonstrate that the fractions and cucurbitacin-type triterpenoids obtained from the aerial parts of M. charantia are promising natural leishmanicidal candidates. [ABSTRACT FROM AUTHOR]

Published
2024
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8. Chemical Composition and Evaluation of Antibacterial, Antibiofilm and Mutagenic Potentials of a Propolis Sample from the Atlantic Forest of Midwest Brazil

Author

Rodrigues Garcez, Fernanda, primary, da Silva Mirowski, Patrick, additional, da Silva Coutinho de Araújo Bueno, Gabriela, additional, Rodrigues, Vitória Elsner, additional, Fernandes Barros, Thayná, additional, Grangeiro da Costa Jr, Alberto, additional, Yoshida, Nídia Cristiane, additional, da Rosa Guterres, Zaira, additional, and Silva Trentin, Danielle, additional

Published
2023
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10. 7.1′,8.3′- and 7.3′,8.5′-Connected Bicyclo[3.2.1]octanoids and Oxabicyclo[3.2.2]nonane-Type Neolignans from Ocotea aciphylla: Structures and Absolute Configurations.

Author

Totini dos Santos, Carlos Henrique, Petrica, Edith Eunice Arthur, Nastri de Luca Batista, Andrea, Delphino Rodrigues, Edilene, Garcez, Walmir Silva, Ferreira de Albuquerque, Ana Carolina, dos Santos Jr., Fernando Martins, Batista Jr., João Marcos, and Garcez, Fernanda Rodrigues

Published
2024
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19. Evaluation of in vitro and in vivo Anti-neuroinflammatory and Genotoxic Activities of the Alkaloid Tryptophol-5-O-β-D-glucopyranoside from Ocotea minarum.

Author

de Araújo Boleti, Ana Paula, de Oliveira Cardoso, Pedro Hernique, Frihling, Breno Emanuel Farias, da Rosa Guterres, Zaira, da Silva, Ana Francisca Gomes, de Rezende, Alexandre Azenha Alves, Garcez, Fernanda Rodrigues, Garcez, Walmir Silva, Graf, Ulrich, Spanó, Mário Antônio, da Silva, Lillian May Grespan Estodutto, and Migliolo, Ludovico

Subjects
ALKALOIDS, INDOLE alkaloids, DROSOPHILA melanogaster, CERRADOS, CHEMICAL species, ISOQUINOLINE alkaloids, LIPOPOLYSACCHARIDES
Abstract

Ocotea minarum (Nees & Mart.) Mez is a tree belonging to the Lauraceae family and found in the Brazilian Cerrado ecosystem. Although the chemical composition of this species has already been described, little is known about the biological activities of one of the constituents of its fruits-the alkaloid tryptophol-5-O-β-D-glucopyranoside. In the present study, we assessed the anti-neuroinflammatory, mutagenic and recombinogenic properties of this indole alkaloid. Cytotoxicity and anti-inflammatory activities were performed using a model of LPS-stimulated microglia BV-2. Mutation detection and somatic recombination were performed in Drosophila melanogaster wing cells. The results showed that tryptophol-5-O-β-D-glucopyranoside was not cytotoxic to BV-2 cells at the concentrations tested. The results also showed that this alkaloid inhibited by 75% the inflammatory response induced by LPS at the concentration of 189 μM with IC50 = 12.07±0.35 μM. The analysis of the MH offspring showed that different concentrations of the alkaloid did not induce statistically significant increases in the frequencies of mutant spots when compared to those observed in the negative control. With these results, we can conclude that tryptophol-5-O-β-D-glucopyranoside presents therapeutic potential for the treatment of neurodegenerative diseases with no mutagenic effects. [ABSTRACT FROM AUTHOR]

Published
2023
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21. Chemical constituents from Terminalia glabrescens

Author

Garcez Fernanda R., Garcez Walmir S., Miguel Daniel L. S., Serea Alessandro A. T., and Prado Fabiana C.

Subjects
Terminalia glabrescens, Combretaceae, triterpenes, 3beta,6beta,23,28-tetrahydroxyolean-12-ene, stigmastane-3beta,6alpha-diol, Chemistry, QD1-999
Abstract

A new oleanane-type triterpene (3beta,6beta,23,28-tetrahydroxyolean-12-ene) was isolated from the leaves of Terminalia glabrescens, together with ursolic, 2alpha-hydroxyursolic, oleanolic, maslinic, arjunolic, sumaresinolic and asiatic acids, squalene, phytol, sitosterol-3-O-beta-D-glucopyranoside and n-alkanes. Friedelin, taraxerol, lupeol, lupenone, betulin, betulone, betulinic acid, arjunglucoside I, stigmastane-3beta,6alpha-diol, beta-sitosterol, (-) catechin,beta-D-pyranotagatose, beta-D-furanofructose and alpha-D-furanofructose were obtained from the trunk bark.

Published
2003

23. Evaluation of in vitroand in vivoAnti-neuroinflammatory and Genotoxic Activities of the Alkaloid Tryptophol-5-O-β-D-glucopyranoside from Ocotea minarum

Author

de Araújo Boleti, Ana Paula, de Oliveira Cardoso, Pedro Hernique, Frihling, Breno Emanuel Farias, da Rosa Guterres, Zaira, da Silva, Ana Francisca Gomes, de Rezende, Alexandre Azenha Alves, Garcez, Fernanda Rodrigues, Garcez, Walmir Silva, Graf, Ulrich, Spanó, Mário Antônio, da Silva, Lillian May Grespan Estodutto, and Migliolo, Ludovico

Abstract

AbstractOcotea minarum(Nees & Mart.) Mez is a tree belonging to the Lauraceae family and found in the Brazilian Cerrado ecosystem. Although the chemical composition of this species has already been described, little is known about the biological activities of one of the constituents of its fruits-the alkaloid tryptophol-5-O-β-D-glucopyranoside. In the present study, we assessed the anti-neuroinflammatory, mutagenic and recombinogenic properties of this indole alkaloid. Cytotoxicity and anti-inflammatory activities were performed using a model of LPS-stimulated microglia BV-2. Mutation detection and somatic recombination were performed in Drosophila melanogasterwing cells. The results showed that tryptophol-5-O-β-D-glucopyranoside was not cytotoxic to BV-2 cells at the concentrations tested. The results also showed that this alkaloid inhibited by 75% the inflammatory response induced by LPS at the concentration of 189 μM with IC50= 12.07±0.35 μM. The analysis of the MH offspring showed that different concentrations of the alkaloid did not induce statistically significant increases in the frequencies of mutant spots when compared to those observed in the negative control. With these results, we can conclude that tryptophol-5-O-β-D-glucopyranoside presents therapeutic potential for the treatment of neurodegenerative diseases with no mutagenic effects.

Published
2023
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24. Cytotoxicity and antibacterial activity of scutellarein and carajurone-enriched fraction obtained from the hydroethanolic extract of the leaves of Fridericia chica (Bonpl.) L.G. Lohmann

Author

Violante, Ivana M. P., Carollo, Carlos A., Silva, Larissa I., Oliveira, Adna Q. C., Pardinho, Flavia C., Garcez, Walmir Silva, Garcez, Fernanda R., Arunachalam, Karuppusamy, and de Oliveira Martins, Domingos Tabajara

Abstract

The hydroethanolic extract obtained from the dry leaves of Fridericia chica (HEFc) underwent several fractionations by different chromatographic techniques. The ethyl acetate and dichloromethane fraction were subjected to phytochemical analysis, resulting in the identification and isolation of scutellarein (1) and in a fraction rich in carajurone (2). They were tested for cytotoxicity in CHO-K1 and the antibacterial activity and mode of action by in vitro assays. The HEFc and scutellarein (1) presented no cytotoxicity. The results showed good antibacterial effect of HEFc against Streptococcus pyogenes and Staphylococcus aureus and moderate activity for Staphylococcus epidermidis, Pseudomonas aeruginosa and Salmonella typhimurium. The fraction containing the compound carajurone (2) showed good activity against Staphylococcus aureus and Staphylococcus epidermidis and moderate activity against Streptococcus pyogenes. Scutellarein (1) showed no activity against the bacteria tested. HEFc antibacterial mode of action appeared to be associated with changes in the permeability of bacterial membranes and nucleotide leakage.

Published
2020
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25. Antitrypanosomal butanolides from Aiouea trinervis

Author

Nunes, Felipe Oliveira, de Almeida, Júlio Menta, Ferreira, Alda Maria Teixeira, da Cruz, Letícia Alves, Jacob, Camila Mareti Bonin, Garcez, Walmir Silva, and Garcez, Fernanda Rodrigues

Subjects
in silico ADMET properties, anti-Trypanosoma activity, Aiouea trinervis, Trypanosoma cruzi, butanolides
Abstract

In a search for new antitrypanosomal agents in the Brazilian flora, the ethanol extract of the xylopodium from Aiouea trinervis (Lauraceae) exhibited in vitro activity against the epimastigote forms of Trypanosoma cruzi, the etiological agent of Chagas disease. Bioassay-guided chromatographic fractionation of the ethanol extract afforded three butanolides, isoobtusilactone A (1), epilitsenolide C2 (2), and epilitsenolide C1 (3). Butanolides 1 and 3 were more active against T. cruzi epimastigotes than the reference drug benznidazole (by 8.9-fold and 3.2-fold, respectively), while 2 proved inactive. Compounds 1 and 3 showed low cytotoxicity in mammalian Vero cells (CC50> 156 μmol L-1) and high selectivity index (SI) values for epimastigotes (SI = 56.8 and 28.6, respectively), and 1 was more selective than benznidazole (SI = 46.5). Butanolide 1 at 24 μmol L-1 also led to cell cycle alterations in epimastigote forms, and inhibited the growth of amastigote cells in more than 70 %. In silico ADMET properties of 1 were also analyzed and predicted favorable drug-like characteristics. This butanolide also complied with Lipinski’s rule of five and was not predicted as interference compound (PAINS). This is the first report on the isolation of these bioactive butanolides under the guidance of in vitro trypanocidal activity against T. cruzi., EXCLI Journal;Vol. 19 2020

Published
2020
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26. Myricitrin fromCombretum lanceolatumExhibits Inhibitory Effect on DNA-Topoisomerase Type IIαand Protective Effect AgainstIn VivoDoxorubicin-Induced Mutagenicity

Author

Perdomo, Renata Trentin, primary, Defende, Camila Pineze, additional, da Silva Mirowski, Patrick, additional, Freire, Talita Vilalva, additional, Weber, Simone Schneider, additional, Garcez, Walmir Silva, additional, da Rosa Guterres, Zaira, additional, de Fátima Cepa Matos, Maria, additional, and Garcez, Fernanda Rodrigues, additional

Published
2021
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27. Synergistic effect and ultrastructural changes in Trypanosoma cruzi caused by isoobtusilactone A in short exposure of time

Author

de Almeida, Júlio Menta, primary, Nunes, Felipe Oliveira, additional, Ceole, Lígia Fernanda, additional, Klimeck, Tabata D’Maiella Freitas, additional, da Cruz, Letícia Alves, additional, Tófoli, Danilo, additional, Borges, Beatriz Santana, additional, Garcez, Walmir Silva, additional, Tozetti, Inês Aparecida, additional, Medeiros, Lia Carolina Soares, additional, Garcez, Fernanda Rodrigues, additional, and Ferreira, Alda Maria Teixeira, additional

Published
2021
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28. Repeated Administration of Clinically Relevant Doses of the Prescription Opioids Tramadol and Tapentadol Causes Lung, Cardiac, and Brain Toxicity in Wistar Rats

Author

Barbosa, Joana, primary, Faria, Juliana, additional, Garcez, Fernanda, additional, Leal, Sandra, additional, Afonso, Luís Pedro, additional, Nascimento, Ana Vanessa, additional, Moreira, Roxana, additional, Pereira, Frederico C., additional, Queirós, Odília, additional, Carvalho, Félix, additional, and Dinis-Oliveira, Ricardo Jorge, additional

Published
2021
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29. Therapeutic Effects of Morinda citrifolia Linn. (Noni) Aqueous Fruit Extract on the Glucose and Lipid Metabolism in High-Fat/High-Fructose-Fed Swiss Mice

Author

Inada, Aline Carla, primary, Silva, Gabriela Torres, additional, Silva, Laleska Pâmela Rodrigues da, additional, Alves, Flávio Macedo, additional, Filiú, Wander Fernando de Oliveira, additional, Asato, Marcel Arakaki, additional, Junior, Wilson Hino Kato, additional, Corsino, Joaquim, additional, Figueiredo, Patrícia de Oliveira, additional, Garcez, Fernanda Rodrigues, additional, Garcez, Walmir Silva, additional, Silva, Renée de Nazaré Oliveira da, additional, Santos-Eichler, Rosangela Aparecida dos, additional, Guimarães, Rita de Cássia Avellaneda, additional, Freitas, Karine de Cássia, additional, and Hiane, Priscila Aiko, additional

Published
2020
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30. Chemical profile and gastroprotective effect of Jatropha elliptica (Pohl) Oken roots

Author

Coelho, Izabela Pereira, primary, Santos, Larissa Bianca Barbosa Dos, additional, Kato Junior, Wilson Hino, additional, Corsino, Joaquim, additional, Cordeiro, Kátia Wolf, additional, Boeing, Thaise, additional, Coelho, Julice Medeiros, additional, Garcez, Fernanda Rodrigues, additional, Garcez, Walmir Silva, additional, de Andrade, Sérgio Faloni, additional, and Figueiredo, Patrícia de Oliveira, additional

Published
2020
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31. Antimicrobial Potential of Essential Oils from Cerrado Plants against Multidrug−Resistant Foodborne Microorganisms

Author

de Jesus, Genilson Silva, primary, Micheletti, Ana Camila, additional, Padilha, Rafael Gonçalves, additional, de Souza de Paula, Jessica, additional, Alves, Flavio Macedo, additional, Leal, Cassia Rejane Brito, additional, Garcez, Fernanda Rodrigues, additional, Garcez, Walmir Silva, additional, and Yoshida, Nidia Cristiane, additional

Published
2020
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34. Cytotoxicity and antibacterial activity of scutellarein and carajurone-enriched fraction obtained from the hydroethanolic extract of the leaves of Fridericia chica (Bonpl.) L.G. Lohmann

Author

Violante, Ivana M. P., primary, Carollo, Carlos A., additional, Silva, Larissa I., additional, Oliveira, Adna Q. C., additional, Pardinho, Flavia C., additional, Garcez, Walmir Silva, additional, Garcez, Fernanda R., additional, Oliveira, Ruberlei Godinho de, additional, Arunachalam, Karuppusamy, additional, and de Oliveira Martins, Domingos Tabajara, additional

Published
2020
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37. Cytotoxicity and antibacterial activity of scutellarein and carajurone-enriched fraction obtained from the hydroethanolic extract of the leaves of Fridericia chica (Bonpl.) L.G. Lohmann.

Author

Violante, Ivana M. P., Carollo, Carlos A., Silva, Larissa I., Oliveira, Adna Q. C., Pardinho, Flavia C., Garcez, Walmir Silva, Garcez, Fernanda R., Oliveira, Ruberlei Godinho de, Arunachalam, Karuppusamy, and de Oliveira Martins, Domingos Tabajara

Subjects
ANTIBACTERIAL agents, BACTERIAL cell walls, STREPTOCOCCUS pyogenes, STAPHYLOCOCCUS epidermidis, STAPHYLOCOCCUS aureus
Abstract

The hydroethanolic extract obtained from the dry leaves of Fridericia chica (HEFc) underwent several fractionations by different chromatographic techniques. The ethyl acetate and dichloromethane fraction were subjected to phytochemical analysis, resulting in the identification and isolation of scutellarein (1) and in a fraction rich in carajurone (2). They were tested for cytotoxicity in CHO-K1 and the antibacterial activity and mode of action by in vitro assays. The HEFc and scutellarein (1) presented no cytotoxicity. The results showed good antibacterial effect of HEFc against Streptococcus pyogenes and Staphylococcus aureus and moderate activity for Staphylococcus epidermidis, Pseudomonas aeruginosa and Salmonella typhimurium. The fraction containing the compound carajurone (2) showed good activity against Staphylococcus aureus and Staphylococcus epidermidis and moderate activity against Streptococcus pyogenes. Scutellarein (1) showed no activity against the bacteria tested. HEFc antibacterial mode of action appeared to be associated with changes in the permeability of bacterial membranes and nucleotide leakage. [ABSTRACT FROM AUTHOR]

Published
2021
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42. Relación entre el médico y los pacientes ancianos en el cine: visiones de atención

Author

Lobo, Mariana de Oliveira, Garcez, Fernanda Caroline Moura, Bezerra, Armando José China, and Gomes, Lucy

Subjects
Medical care, Educação médica, Atención médica, Idoso, Anciano, Cuidados médicos, Physician-patient relations, Relações médico-paciente, Prejuicio, Educatión médica, Medical Education, Preconceito, Prejudice, Aged, Relaciónes médico-paciente
Abstract

Resumo Este artigo objetiva descrever diferentes visões de atendimento da relação médico-paciente idoso abordada em filmes de ficção. Pesquisou-se filmografia nacional e internacional, buscando filmes de longa-metragem que exibissem cenas em que a relação médico-paciente idoso fosse retratada de diferentes formas. Foi possível identificar nos dez filmes analisados expectativas referentes ao atendimento do paciente idoso, tanto na visão do paciente quanto na de seus familiares, evidenciando sentimentos e valores socioculturais presentes na inter-relação estabelecida durante o exercício profissional da medicina. Concluiu-se que a linguagem cinematográfica é útil para a formação do médico, que deve se preocupar com o sentido humano de seu trabalho, bem como para interpretar elementos que envolvem a complexa relação médico-paciente, particularmente com o idoso. Abstract This article aims to describe different views of care through the doctor-elderly patient relationship as addressed in feature films. Research was carried out based on national and international filmography, seeking films containing scenes in which the doctor-elderly patient relationship was portrayed in different ways. In the ten films analyzed, it was possible to identify expectations regarding the care of the elderly patient, both from the patient’s and their family’s view, describing the feelings and socio-cultural values present in the interrelationship established during the professional practice of medicine. It was concluded that cinematographic language is useful for the training of physicians, who should be concerned with the human aspect of their work, as well as for the interpretation of elements involving the complex doctor-patient relationship, particularly among the elderly. Resumen El objetivo de este artículo es describir las diferentes visiones de atención, abordadas en películas de ficción, sobre la relación entre el médico y los pacientes ancianos. Se investigó la filmografía nacional e internacional, buscando películas de larga duración que exhibieran escenas en las que la relación entre el médico y el paciente anciano se retratara de diferentes formas. En las diez películas analizadas, fue posible identificar expectativas referentes a la atención del paciente anciano, tanto en la visión del paciente como en la de sus familiares, evidenciando sentimientos y valores socioculturales presentes en la interrelación establecida en el ejercicio profesional de la medicina. Se concluyó que el lenguaje cinematográfico es útil para la formación del médico, quien debe preocuparse del sentido humano de su trabajo, para interpretar elementos que involucran la relación compleja entre el médico y el paciente, particularmente el anciano.

Published
2017

44. ANTITRYPANOSOMAL BUTANOLIDES FROM AIOUEA TRINERVIS.

Author

Oliveira Nunes, Felipe, de Almeida, Júlio Menta, Teixeira Ferreira, Alda Maria, da Cruz, Letícia Alves, Bonin Jacob, Camila Mareti, Silva Garcez, Walmir, and Rodrigues Garcez, Fernanda

Subjects
CHAGAS' disease, TRYPANOSOMA cruzi, CELL cycle, CELL growth, FORECASTING
Abstract

In a search for new antitrypanosomal agents in the Brazilian flora, the ethanol extract of the xylopodium from Aiouea trinervis (Lauraceae) exhibited in vitro activity against the epimastigote forms of Trypanosoma cruzi, the etiological agent of Chagas disease. Bioassay-guided chromatographic fractionation of the ethanol extract afforded three butanolides, isoobtusilactone A (1), epilitsenolide C2 (2), and epilitsenolide C1 (3). Butanolides 1 and 3 were more active against T. cruzi epimastigotes than the reference drug benznidazole (by 8.9-fold and 3.2-fold, respectively), while 2 proved inactive. Compounds 1 and 3 showed low cytotoxicity in mammalian Vero cells (CC50> 156 μmol L-1) and high selectivity index (SI) values for epimastigotes (SI = 56.8 and 28.6, respectively), and 1 was more selective than benznidazole (SI = 46.5). Butanolide 1 at 24 μmol L-1 also led to cell cycle alterations in epimastigote forms, and inhibited the growth of amastigote cells in more than 70 %. In silico ADMET properties of 1 were also analyzed and predicted favorable drug-like characteristics. This butanolide also complied with Lipinski’s rule of five and was not predicted as interference compound (PAINS). This is the first report on the isolation of these bioactive butanolides under the guidance of in vitro trypanocidal activity against T. cruzi. [ABSTRACT FROM AUTHOR]

Published
2020
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45. Antiproliferative Activity of Extracts of Campomanesia adamantium (Cambess.) O. Berg and Isolated Compound Dimethylchalcone Against B16-F10 Murine Melanoma

Author

Lima e Silva, Magalli C.B., primary, Bogo, Danielle, additional, Alexandrino, Caroline A.F., additional, Perdomo, Renata T., additional, Figueiredo, Patrícia de O., additional, do Prado, Pamela R., additional, Garcez, Fernanda R., additional, Kadri, Monica C.T., additional, Ximenes, Thalita V.N., additional, Guimarães, Rita de Cassia A., additional, Sarmento, Ulana C., additional, and Macedo, Maria Lígia R., additional

Published
2018
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