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This publication reports the controlled cultivation of var. Engl. (Rutaceae) in several growth substrates under controlled greenhouse conditions. This plant is well-known for its anti-Chagas (trypanocidal) activity, related to the presence of several β-carboline alkaloids. The metabolomic study of seedlings over two years of growth (2018-2020) was performed using comprehensive two-dimensional gas chromatography time-of-flight mass spectrometry (GC × GC-TOFMS). The canthin-6-one alkaloids, canthin-6-one and 5-methoxy-canthin-6-one, were putatively identified in extracts. Finally, in vitro and in silico studies of trypanocidal activity were performed, suggesting that canthin-6-one alkaloids could interact with the main pharmacological targets against , cruzain protease, dihydroorotate dehydrogenase, lanosterol 14-alpha-demethylase, farnesyl diphosphate, and squalene synthases.
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http://dx.doi.org/10.3390/plants14060954 | DOI Listing |
ChemMedChem
September 2025
Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, Caracas, 1041-A, Venezuela.
Due to the advantages of drug repurposing, the discovery of new chemotherapeutic agents for the treatment of Chagas disease based on approved drugs has become a strategy for identifying new candidates. In this work, the antidepressant drug sertraline is reported, with an IC of 7.8 ± 1.
View Article and Find Full Text PDFActa Parasitol
September 2025
Région du Centre, Université Joseph Ki-Zerbo, Rue Thomas Sankara, O3 BP 7021, Ouagadougou, Burkina Faso.
Introduction: The objective of the World Health Organization is to achieve the interruption of human African trypanosomiasis (HAT) transmission by 2030.
Methods: This review aims to update knowledge on HAT, through a synthesis on the epidemiology, diagnostic tools and drugs of HAT.
Results: From 1960 to 2024 approximately 132,063 cases of HAT have been reported across Africa.
J Inorg Biochem
September 2025
Área Química Inorgánica, Facultad de Química, Universidad de la República, Montevideo, Uruguay. Electronic address:
Chagas disease, caused by Trypanosoma cruzi, remains a major public health concern with limited therapeutic options and significant toxicity associated with current treatments. In this work, eight novel heteroleptic complexes of the type [M(L)(phen)], where M = Cu(II) or Zn(II), L = coumarin-thiosemicarbazone hybrid ligands, and phen = 1,10-phenanthroline, were synthesized and fully characterized in the solid state and in solution. For comparison, some homoleptic [Cu(HL)₂], [Zn(HL)₂], and [CuCl(HL)] complexes were also prepared.
View Article and Find Full Text PDFActa Parasitol
September 2025
LADISER Inmunología y Biología Molecular, Edificio D, Facultad de Ciencias Químicas, Universidad Veracruzana (UV), Prolongación de Oriente 6 #1009, Colonia Rafael Alvarado, C.P. 94340, 86039, Orizaba, Veracruz, Mexico.
Introduction: This study aimed to investigate the influence of benznidazole (BZN) origin on its in vitro potency against various Trypanosoma cruzi strains.
Methods: Pure BZN, purified BZN, and the pharmaceutical formulation Abarax were evaluated for their activity against several parasite strains.
Results: Results demonstrated significant variability in BZN's effectiveness, contingent upon both its specific form and the T.
ACS Omega
August 2025
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, Minas Gerais 31270-901, Brazil.
A Pd-mediated C-H activation methodology was developed for the direct arylation of quinoidal skeletons, both by means of homogeneous catalysis and heterogeneous catalysis using metal-decorated carbon nanotubes, enabling the direct functionalization of quinones in moderate to excellent yields. The derivatives obtained were tested against trypomastigote forms of , showing promising biological activity.
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