Article
Chemistry, Inorganic & Nuclear
Felipe Figueiroa Moreira, Juliana de Araujo Portes, Nathalia Florencia Barros Azeredo, Christiane Fernandes, Adolfo Horn Jr, Cristina Pinheiro Santiago, Bruna Barriquel Segat, Giovanni Finoto Caramori, Leticia Maria Pequeno Madureira, Dalber Ruben Sanchez Candela, Marcelo Monteiro Marques, Jackson Antonio Lamounier Camargos Resende, Wanderley de Souza, Renato Augusto DaMatta, Sergio Henrique Seabra
Summary: Chagas disease, caused by Trypanosoma cruzi, is a neglected tropical disease predominantly affecting Latin America. Two new mu-oxo Fe(iii) dinuclear complexes show promising anti-parasitic effects on T. cruzi epimastigotes in vitro, with low cytotoxicity and high selectivity indexes.
DALTON TRANSACTIONS
(2021)
Review
Biochemistry & Molecular Biology
Carlos Garcia-Estrada, Yolanda Perez-Pertejo, Barbara Dominguez-Asenjo, Vanderlan Nogueira Holanda, Sankaranarayanan Murugesan, Maria Martinez-Valladares, Rafael Balana-Fouce, Rosa M. Reguera
Summary: Due to the lack of specific vaccines, neglected tropical diseases caused by trypanosomatids, such as sleeping sickness, Chagas disease and leishmaniasis, rely solely on pharmacological treatments. The current drugs have drawbacks including adverse effects, parenteral administration, chemical instability, and high costs. However, the discovery of new drugs for these diseases is rare due to the lack of interest from big pharmaceutical companies. Nitroheterocyclic compounds, such as benznidazole and nifurtimox, have provided potent effects against Chagas disease, and fexinidazole has been developed as a new drug against African trypanosomiasis. Despite being initially discarded due to their mutagenic potential, nitroheterocycles now show promise as a source of inspiration for developing oral drugs to replace existing ones.
Article
Biology
Lorraine Martins Rocha Orlando, Leonardo da Silva Lara, Guilherme Curty Lechuga, Giseli Capaci Rodrigues, Omar Ginoble Pandoli, Druval Santos de Sa, Mirian Claudia de Souza Pereira
Summary: Therapeutic alternatives for Chagas disease are urgently needed due to limitations and adverse effects of current drugs. Triazole analogues show promise in treating T. cruzi.
Article
Biochemistry & Molecular Biology
Diego Rodney Rodrigues de Assis, Alexandre Almeida Oliveira, Samuel Luiz Porto, Rayane Aparecida Nonato Rabelo, Eduardo Burgarelli Lages, Viviane Correa Santos, Matheus Marques Milagre, Stenio Perdigao Fragoso, Mauro Martins Teixeira, Rafaela Salgado Ferreira, Carlos Renato Machado, Lucas Antonio Miranda Ferreira, Nivaldo Lucio Speziali, Heloisa Beraldo, Fabiana Simao Machado
Summary: (English Summary:)
This study investigated the potential antichagasic activities of thiosemicarbazones and hydrazones as new anti-T. cruzi drug candidates. Compounds C1 and C3 showed anti-parasitic activity in macrophages without toxicity to host cells, and were also effective in directly killing trypomastigotes. Moreover, C1 and C3 attenuated parasitemia in T. cruzi-infected mice and maintained anti-T. cruzi activity in vivo when loaded in a lipid nanocarrier system.
BIOORGANIC CHEMISTRY
(2021)
Article
Infectious Diseases
Mikael Boberg, Monica Cal, Marcel Kaiser, Rasmus Jansson-Lofmark, Pascal Maser, Michael Ashton
Summary: The study showed that the compound L-eflornithine was more potent than D-eflornithine in inhibiting the growth of parasites in vitro, potentially offering an improved treatment option for late-stage Gambian human African trypanosomiasis.
PLOS NEGLECTED TROPICAL DISEASES
(2021)
Article
Biochemistry & Molecular Biology
Sheila C. Araujo, Fernanda S. Sousa, Thais A. Costa-Silva, Andre G. Tempone, Joao Henrique G. Lago, Kathia M. Honorio
Summary: The phytochemical study of n-hexane extract from Nectandra leucantha flowers yielded six known neolignans and one new metabolite. The new compound exhibited potent activity against T. cruzi with no observed mammalian cytotoxicity, and molecular modeling techniques were employed to design new neolignan-based compounds with higher activity. The integration of experimental and computational techniques was found to be a powerful tool for discovery of new drug prototypes.
Article
Multidisciplinary Sciences
Roger Espinosa, Sara Robledo, Camilo Guzman, Natalia Arbelaez, Lina Yepes, Gilmar Santafe, Alex Saez
Summary: The synthesized styrylquinoline-like compounds exhibited promising in vitro antitrypanosomal activity and showed significant therapeutic effects in a mouse infection model, indicating a potential for treatment.
Article
Chemistry, Medicinal
Sheila Cruz Araujo, Rafaela Molina de Angelo, Henrique Barbosa, Thais Alves Costa-Silva, Andre Gustavo Tempone, Joao Henrique Ghilardi Lago, Kathia Maria Honorio
Summary: Chagas disease remains a major public health problem, particularly in Latin America and other endemic regions. Current drug treatments have limitations, and there is an urgent need for new therapeutic options. This study utilized virtual screening techniques to identify 11 potential inhibitors with significant activity against T. cruzi.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Simone I. Schulz, Dieter Lang, Gabriele Schmuck, Michael Gerisch, Michaela Bairlein, Robert Fricke, Heino Stass
Summary: This study aimed to better understand the fate of oral nifurtimox in vivo through investigating its exposure and excretion pathways in rats and humans. The results showed that nifurtimox was rapidly absorbed and eliminated in rats, and it yielded six predominant metabolites in urine and plasma. In patients with Chagas disease, only two metabolites achieved relevant exposure levels, and the total amount of excreted metabolites was higher in fed patients. No potential drug-drug interactions were identified in vitro. This analysis expands the understanding of nifurtimox and its metabolism.
CURRENT DRUG METABOLISM
(2023)
Article
Immunology
Faustino Torrico, Joaquim Gascon, Lourdes Ortiz, Jimy Pinto, Gimena Rojas, Alejandro Palacios, Fabiana Barreira, Bethania Blum, Alejandro Gabriel Schijman, Michel Vaillant, Nathalie Strub-Wourgaft, Maria Jesus Pinazo, Graeme Bilbe, Isabela Ribeiro
Summary: The study found that fexinidazole may be a potential drug for the treatment of chronic indeterminate Chagas disease. In the 12-month follow-up after treatment, all treated patients with available data showed clearance of parasites, while no patients in the placebo group achieved this effect. Further analysis suggested that low dosages of fexinidazole may be safe and effective.
CLINICAL INFECTIOUS DISEASES
(2023)
Review
Chemistry, Medicinal
Diogo de Freitas Paiva, Ana Paula dos Santos Matos, Denise de Abreu Garofalo, Tatielle do Nascimento, Mariana Sato de Souza de Bustamante Monteiro, Ralph Santos-Oliveira, Eduardo Ricci-Junior
Summary: Chagas disease, a neglected tropical disease, is caused by a parasitic protozoan and primarily transmitted to humans through vector insects. The traditional drugs for treating the disease have limitations and adverse effects. However, the use of nanocarriers as an alternative treatment has shown promising results in increasing drug stability, selectivity, and efficacy against the parasite.
Article
Chemistry, Medicinal
Marina M. Marcos Valdez, Octavio E. Fandino, Sonia N. Faudone, Alejandro P. Ayala, Mino R. Caira, Norma R. Sperandeo
Summary: This study investigated the polymorphism of the compound 1-(4-acetamide-benzenesulfonyl)-benzimidazole (PABZI) and selected the most stable form I for further preclinical studies.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Chemistry, Medicinal
Aldo S. de Oliveira, Lucas dos S. Mello, Camila H. Ogihara, Thiago H. Doring, David L. Palomino-Salcedo, Simone Michelan-Duarte, Leonardo L. G. Ferreira, Julia M. Souza, Maria Jose Davila-Rodriguez, Jose W. da Cruz Junior, Edward R. Dockal, Adriano D. Andricopulo
Summary: A total of 27 Schiff bases derived from diaminomaleonitrile were synthesized in high yields, with one analog showing potential as a potent cruzain inhibitor in molecular docking studies. A strong correlation was observed between IC50 values and binding energies, with robust 2D quantitative structure-activity relationship models for the dataset. These novel cruzain inhibitors serve as promising starting points for further Chagas disease drug discovery programs.
FUTURE MEDICINAL CHEMISTRY
(2021)
Article
Microbiology
Ramendra P. Pandey, Marilda Savoia Nascimento, Caio Haddad Franco, Karina Bortoluci, Marcelo Nunes Silva, Bianca Zingales, Daniel Gibaldi, Leda Castano Barrios, Joseli Lannes-Vieira, Leonardo Moro Cariste, Jose Ronnie Vasconcelos, Carolina Borsoi Moraes, Lucio H. Freitas-Junior, Jorge Kalil, Laura Alcantara, Edecio Cunha-Neto
Summary: The study investigated the effects of repurposed drugs chloroquine and colchicine on the treatment of Chagas disease, and found that the combination of chloroquine and benznidazole could enhance the trypanocidal activity of benznidazole, reducing the required dosage. In vivo experiments in mice also showed the effectiveness of the combination therapy.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Parasitology
Patricia M. L. Pereira, Priscila G. Camargo, Bruna T. Fernandes, Luiz A. P. Flores-Junior, Luiza R. S. Dias, Camilo H. S. Lima, Phileno Pinge-Filho, Lucy M. Y. Lioni, Sueli F. Yamada-Ogatta, Marcelle L. F. Bispo, Fernando Macedo
Summary: Three benzoylthioureas derivatives exhibited promising activity against the epimastigote form of Trypanosoma cruzi, as shown by in vitro studies. Molecular docking studies indicated that these compounds have the potential to interact with two main enzymatic targets effectively.
PARASITOLOGY INTERNATIONAL
(2021)
Article
Chemistry, Multidisciplinary
Aline Meireles Coelho, Isabela Ferreira Queiroz, Wanderson Geraldo Lima, Andre Talvani, Luiza Oliveira Perucci, Melina Oliveira de Souza, Daniela Caldeira Costa
Summary: Paracetamol-induced hepatotoxicity causes severe and potentially irreversible liver damage. Early treatment and alternative therapies are necessary to mitigate the acute liver injury caused by this toxicity.
DRUG AND CHEMICAL TOXICOLOGY
(2023)
Article
Immunology
Gabriela Rodrigues Leite, Denise da Gama Jaen Batista, Ana Lia Mazzeti, Rosemeire Aparecida Silva, Ademar Benevolo Lugao, Maria de Nazare Correia Soeiro
Summary: The synthetic peptides PepA and PepB were found to reduce the intracellular parasitism of T. cruzi in macrophages (PMM), but were ineffective against cardiac cells. However, they did not exhibit trypanocidal effects on bloodstream trypomastigotes, nor showed in vivo efficacy when administered after parasite inoculation.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Nutrition & Dietetics
Thalles de Freitas Castro, Natalia Alves de Matos, Ana Beatriz Farias de Souza, Guilherme de Paula Costa, Luiza Oliveira Perucci, Andre Talvani, Silvia Dantas Cangussu, Rodrigo Cunha Alvim de Menezes, Frank Silva Bezerra
Summary: Maternal protein restriction during pregnancy has adverse effects on the lungs of offspring, including decreased body weight, inflammation and oxidative stress, and simplification of lung structure.
Article
Biotechnology & Applied Microbiology
Pamela Felix da Silva, Natalia Alves de Matos, Camila de Oliveira Ramos, Thalles de Freitas Castro, Natalia Pereira da Silva Araujo, Ana Beatriz Farias de Souza, Guilherme de Paula Costa, Silvia Dantas Cangussu, Andre Talvani, Akinori Cardozo Nagato, Frank Silva Bezerra
Summary: Short-term exposure to e-cigarettes leads to more severe respiratory inflammation and lung damage compared to cigarette smoke.
BIOMED RESEARCH INTERNATIONAL
(2022)
Review
Immunology
Priscilla Vilela dos Santos, Debora Nonato Miranda de Toledo, Debora Maria Soares de Souza, Tatiana Prata Menezes, Luiza Oliveira Perucci, Zolder Marinho Silva, Daniela Caldas Teixeira, Ed Wilson Rodrigues Vieira, Valter Ferreira de Andrade-Neto, Nathalia Sernizon Guimaraes, Andre Talvani
Summary: This study evaluated the available information on inflammatory and regulatory plasma mediators in pregnant women diagnosed with toxoplasmosis. Eight studies were included in the analysis, and the results showed that infected pregnant women had higher levels of IL-5, IL-6, IL-8, IL-17, CCL5, and IL-10 in their plasma. These findings suggest that the immune status of pregnant women determines the course of T. gondii infection, and the balance between inflammatory and regulatory cytokines mitigates the adverse effects on the placenta and fetus.
FRONTIERS IN IMMUNOLOGY
(2023)
Article
Biotechnology & Applied Microbiology
Lucas M. M. Oliveira, Fallon S. S. Siqueira, Michelle T. T. Silva, Jose V. C. Machado, Cleydson F. F. Cordeiro, Livia F. Diniz, Marli M. A. Campos, Lucas L. L. Franco, Thiago B. B. Souza, Jamie A. A. Hawkes, Diogo T. T. Carvalho
Summary: Molecular hybridisation, a well-known technique in pharmaceutical research, has been used to create novel hybrid compounds by combining known pharmacophoric subunits. This study focused on the development of molecular hybrids based on eugenol and chloramphenicol pharmacophores, and evaluated their antimicrobial potential. The results showed significant improvement in the antimicrobial activity of the hybrid compounds against multidrug-resistant Pseudomonas aeruginosa, methicillin-resistant Staphylococcus aureus (MRSA), and rapidly growing mycobacteria.
FOLIA MICROBIOLOGICA
(2023)
Article
Immunology
Luiza Oliveira Perucci, Sirlaine Pio Gomes da Silva, Eduardo Bearzoti, Kelerson Mauro de Castro Pinto, Patricia Nessralla Alpoim, Melina de Barros Pinheiro, Lara Carvalho Godoi, Lauro Angelo Goncalves de Moraes, Lirlandia Pires de Sousa, Luci Maria Sant Ana Dusse, Andre Talvani
Summary: This study discovered that neuroserpin levels are decreased, while levels of inflammatory mediators (IL-17A, IL-33, and CXCL-16) are increased during severe preeclampsia. Neuroserpin may serve as a potential biomarker for early-onset severe preeclampsia, and the imbalance among neuroserpin, IL-17A, IL-33, and CXCL-16 levels may be associated with the pathogenesis of preeclampsia, regardless of maternal age.
Article
Chemistry, Medicinal
Stefan Biendl, Cecile Haeberli, Gong Chen, Wen Wang, Longjin Zhong, Jessica Saunders, Thao Pham, Xiaofang Wang, Jianbo Wu, Susan A. Charman, Jonathan L. Vennerstrom, Jennifer Keiser
Summary: Researchers conducted an in-depth characterization of the antischistosomal activity and pharmacokinetics of ozonide carboxylic acids. These ozonides showed rapid and consistent activity against schistosomula and adult schistosomes in vitro. The most active compound in vivo was ethyl ester OZ780, which achieved significant efficacy against both adult and juvenile Schistosoma mansoni.
ACS INFECTIOUS DISEASES
(2023)
Article
Pharmacology & Pharmacy
Ana Lia Mazzeti, Karolina R. Goncalves, Patricia Ferreira Boasquivis, Jamile Barbosa, Bruno G. Pereira, Maria de Nazare Correia Soeiro, Vanessa Carla Furtado Mosqueira, Maria Terezinha Bahia
Summary: The design and development of biodegradable benznidazole (BZ) subcutaneous (SC) implants based on poly-e-caprolactone (PCL) are proposed in this study to improve the treatment for Chagas disease. The implants showed controlled release of BZ and maintained safe BZ concentrations in plasma, leading to a cure for all mice in the experimental model. These results provide a promising option to optimize human Chagas disease treatment regimens by reducing failures related to poor adherence to treatment and improving patient comfort.
Editorial Material
Microbiology
Andre Talvani, Mauro Martins Teixeira
Article
Nutrition & Dietetics
Giulia Valente Ciriaco, Luiz Antonio Alves de Menezes-Junior, Wandeir Wagner de Oliveira, Andre Talvani, Silvana Mara Luz Turbino Ribeiro
Summary: This study aimed to assess the clinical and nutritional risk factors associated with the occurrence of pressure ulcers (PUs) in patients admitted to an Intensive Care Unit (ICU). A retrospective cohort study was conducted by analyzing the medical records of ICU patients, including sociodemographic, clinical, dietary, and anthropometric data, as well as information on mechanical ventilation, sedation, and use of noradrenaline. Multivariate Poisson's regression was used to estimate the relative risk (RR) according to the explanatory variables and identify the significant factors associated with PUs.
CLINICAL NUTRITION ESPEN
(2023)
Article
Parasitology
Priscilla Vilela dos Santos, Debora Nonato Miranda de Toledo, Nathalia Sernizon Guimaraes, Luiza Oliveira Perucci, Valter Ferreira de Andrade-Neto, Andre Talvani
Summary: This study examined the association between Toxoplasma gondii seropositivity and plasma markers (CCL2, CXCL16, IL-17, and IL-33) in pregnant women in Brazil. The results showed that the concentrations of CCL2, CXCL16, and IL-33 were higher in T. gondii-seropositive women, while IL-17 levels were lower. Additionally, multiparous women were more likely to be infected with T. gondii than primiparous women.
Article
Chemistry, Medicinal
Fernanda Karoline Vieira da Silva Torchelsen, Tamiles Caroline Fernandes Pedrosa, Michelle Peixoto Rodrigues, Alex Ramos de Aguiar, Fabricio Marques de Oliveira, Giovanni Wilson Amarante, Policarpo Ademar Sales-Junior, Renata Tupinamba Branquinho, Sirlaine Pio Gomes da Silva, Andre Talvani, Silvane Maria Fonseca Murta, Felipe Terra Martins, Rodrigo Ligabue Braun, Robson Ricardo Teixeira, Vanessa Carla Furtado Mosqueira, Marta de Lana
Summary: A novel diamide was synthesized and shown to have activity against Trypanosoma cruzi both in vitro and in vivo.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Infectious Diseases
Vitoria Louise, Bianca Alves Almeida Machado, Washington Martins Pontes, Tatiana Prata Menezes, Fernanda Carolina Ribeiro Dias, Luiz Otavio Guimaraes Ervilhas, Kelerson Mauro de Castro Pinto, Andre Talvani
Summary: Theracurmin, a nanoparticle formulation derived from curcumin, has immunomodulatory and trypanocidal effects on T. cruzi infection. It reduces parasitemia and protects against weight loss. However, further investigations are needed to understand its effects on leukocyte infiltration and inflammatory factors.
TROPICAL MEDICINE AND INFECTIOUS DISEASE
(2023)
Correction
Chemistry, Medicinal
Elkin Jose Torres Sierra, Cleydson Finotti Cordeiro, Livia de Figueiredo Diniz, Ivo Santana Caldas, Jamie Anthony Hawkes, Diogo Teixeira Carvalho
REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY
(2022)