Article
Immunology
Julian Ernesto Nicolas Gulin, Margarita Maria Catalina Bisio, Daniela Rocco, Jaime Altcheh, Maria Elisa Solana, Facundo Garcia-Bournissen
Summary: This study evaluates the efficacy of Miltefosine (MLT) as a monodrug and combined with benznidazole (BZ) for treating Trypanosoma cruzi infection. MLT showed promising results in inhibiting the parasite in both in vitro and in vivo models, with improved efficacy when combined with BZ. This study provides support for the potential use of MLT in Chagas disease treatment and the exploration of combination therapies.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Chemistry, Medicinal
Yang Zheng, Magali van den Kerkhof, Tiffany van der Meer, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Iwan J. P. de Esch, Marco Siderius, An Matheeussen, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Summary: The discovery of 5-phenylpyrazolopyrimidinone analogs as a novel series of antitrypanosomal agents shows promise for developing new medications to treat Human African Trypanosomiasis (HAT). The most potent compound, 30, has a low toxicity potential and exhibits high in vitro and in vivo antitrypanosomal activity against T. b. brucei.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
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
Chemistry, Medicinal
Ruben Martin-Escolano, Mikel Etxebeste-Mitxeltorena, Javier Martin-Escolano, Daniel Plano, Maria J. Rosales, Socorro Espuelas, Esther Moreno, Manuel Sanchez-Moreno, Carmen Sanmartin, Clotilde Marin
Summary: Chagas disease, caused by Trypanosoma cruzi, is a global public health concern with limited treatment options. Selenium and its derivatives have emerged as an interesting strategy for the treatment of various protozoan diseases, including Chagas disease. Further research on selenium compounds shows potential for the development of new antichagasic agents.
ACS INFECTIOUS DISEASES
(2021)
Article
Biochemistry & Molecular Biology
Kyung-Hwa Baek, Trong-Nhat Phan, Satish R. Malwal, Hyeryon Lee, Zhu-Hong Li, Silvia N. J. Moreno, Eric Oldfield, Joo Hwan No
Summary: SQ109 is an anti-tubercular drug candidate that has shown potent activity against protozoan parasites including Leishmania, Trypanosoma cruzi, and Toxoplasma gondii in vitro. It has demonstrated efficacy in mouse models of T. cruzi and T. gondii infections, but moderate efficacy in models of Trypanosoma brucei and Leishmania donovani infections. Metabolites of SQ109 also exhibit activity against protozoan parasites in vitro.
Article
Microbiology
Sergio Castaneda, Marina Munoz, Peter J. Hotez, Maria Elena Bottazzi, Alberto E. Paniz-Mondolfi, Kathryn M. Jones, Rojelio Mejia, Cristina Poveda, Juan David Ramirez
Summary: Chagas disease is caused by Trypanosoma cruzi and has a profound impact on the gastrointestinal tract. Alterations in the gut microbiome caused by the parasite may play a crucial role in host-parasite interactions and immune responses. Understanding this interaction could provide valuable insights into the pathophysiology of the disease and the development of new treatments.
MICROBIOLOGY SPECTRUM
(2023)
Article
Pharmacology & Pharmacy
Leonardo da Silva Lara, Guilherme Curty Lechuga, Lorraine Martins Rocha Orlando, Byanca Silva Ferreira, Bernardo Araujo Souto, Mauricio Silva dos Santos, Mirian Claudia de Souza Pereira
Summary: Chagas disease is a long-standing disease that primarily affects impoverished populations in Latin America. The available drugs have limited effectiveness and intense side effects. This study explores the biological activity of two new series of pyrazole-thiazoline derivatives with potential therapeutic options against Trypanosoma cruzi. These derivatives show potent activity with good oral bioavailability and low cytotoxicity, making them potential candidates for Chagas disease therapy.
Article
Parasitology
Ruben Martin-Escolano, Maria Jose Rosales, Clotilde Marin
Summary: The T. cruzi Arequipa strain is characterized and evaluated as a model for drug discovery in Chagas disease. The study provides insights into the infection characteristics and benznidazole susceptibility of this strain, suggesting its potential for screening new compounds with anti-parasitic properties.
Article
Immunology
Laura Fraccaroli, Maria Daniela Ruiz, Virginia Gabriela Perdomo, Agustina Nicole Clausi, Dario Emmanuel Balcazar, Luciana Larocca, Carolina Carrillo
Summary: "Chagas disease is an endemic American parasitosis caused by Trypanosoma cruzi. Current therapies have limited efficacy and side effects, leading to the need for new trypanocidal strategies. Ivermectin shows potential as a repurposed drug for Chagas disease, with dose-dependent effects on T. cruzi and other trypanosomatids, and potential novel molecular targets identified in this study."
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Dharaminder Singh, Sudhir P. Deosarkar, Elaine Cadogan, Vikki Flemington, Alysha Bray, Jingwen Zhang, Ronald S. Reiserer, David K. Schaffer, Gregory B. Gerken, Clayton M. Britt, Erik M. Werner, Francis D. Gibbons, Tomasz Kostrzewski, Christopher E. Chambers, Emma J. Davies, Antonio Ramos Montoya, Jacqueline H. L. Fok, David Hughes, Kristin Fabre, Matthew P. Wagoner, John P. Wikswo, Clay W. Scott
Summary: Conventional in vitro model systems fail to replicate the concentration changes of drugs observed in vivo, reducing the predictability of data. This study introduces a novel microfluidic device, the Microformulator, which allows cells to be cultured with in vivo-like pharmacokinetic profiles, improving the understanding of the impact of pharmacokinetics on biological responses.
Review
Microbiology
Eduardo E. Avalos-Borges, Lizette E. Rios, Matilde Jimenez-Coello, Antonio Ortega-Pacheco, Nisha J. Garg
Summary: This article reviews the current knowledge of congenital transmission of Trypanosoma cruzi in humans and compares the placental architecture of humans and different animals. This is important for evaluating the efficacy of new anti-parasite drugs and therapies.
Article
Immunology
Albert Ros-Lucas, Nieves Martinez-Peinado, Jaume Bastida, Joaquim Gascon, Julio Alonso-Padilla
Summary: Chagas disease, caused by Trypanosoma cruzi, is a devastating neglected disease. The discovery of safer and more effective drugs is urgently needed. The AlphaFold Protein Structure Database provides protein models that can help describe new therapeutic approaches and shed light on the molecular mechanisms of known compounds.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Leonardo S. Lara, Guilherme C. Lechuga, Caroline dos S. Moreira, Thais B. Santos, Vitor F. Ferreira, David R. da Rocha, Mirian C. S. Pereira
Summary: Chagas disease remains a serious public health problem in Latin America, with current clinical treatments considered inadequate, emphasizing the need for discovering new effective and safe drugs. Research analyzed a series of naphthoquinone derivatives for biological activity and structure-activity relationship, identifying 1g as a promising compound against Trypanosoma cruzi. However, current compounds were unable to reduce parasite load or prevent mouse mortality in infection.
Article
Chemistry, Medicinal
Cai Lin, Ludmila Ferreira de Almeida Fiuza, Camila Cardoso Santos, Daniela Ferreira Nunes, Otacilio Cruz Moreira, Jakob Bouton, Izet Karalic, Louis Maes, Guy Caljon, Fabian Hulpia, Maria de Nazare C. Soeiro, Serge Van Calenbergh
Summary: The study shows that by modifying the pyrimidine part, the 7-aryl-7-deazapurine nucleoside can retain inhibitory activity against T. cruzi amastigote growth while improving selectivity towards mammalian cells. The 7-(4-chlorophenyl) analogue exhibited promising antitrypanosomal activity in a mouse model.
Article
Biochemistry & Molecular Biology
Michael J. da Silva, Andrey P. Jacomini, Davana S. Goncalves, Karlos Eduardo Pianoski, Julia Poletto, Danielle Lazarin-Bidoia, Helito Volpato, Celso Nakamura, Fernanda A. Rosa
Summary: A novel tetrasubstituted pyrazole derivative was discovered to exhibit potent and selective inhibition against both L. amazonensis and T. cruzi, offering a new approach for the treatment of Chagas disease and Leishmaniasis.
BIOORGANIC CHEMISTRY
(2021)