Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

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.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11946004PMC
http://dx.doi.org/10.3390/plants14060954DOI Listing

Publication Analysis

Top Keywords

trypanocidal activity
8
canthin-6-one alkaloids
8
exploring anti-chagas
4
anti-chagas activity
4
activity seedlings
4
seedlings metabolomics
4
metabolomics protein-ligand
4
protein-ligand docking
4
docking publication
4
publication reports
4

Similar Publications

Sertraline as a Scaffold for Antitrypanosoma Cruzi Drug Development: Design of Novel Derivatives and Computational Target Screening.

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 PDF

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.

View Article and Find Full Text PDF

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 PDF

Analysis of the Behavior of Trypanosoma cruzi in Culture Against Different Dosage Forms of Benznidazole: Experimental Insights.

Acta 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.

View Article and Find Full Text PDF

Palladium-Catalyzed C-H Arylation of Quinoidal Scaffolds Through Homogeneous and Heterogeneous Pathways: Advancing Toward Trypanocidal Prototypes.

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.

View Article and Find Full Text PDF