The bark of Ruyschiaphylladenia was collected from Monteverde, Costa Rica, and extracted with acetone. Bioactivity-directed chromatographic separation of the crude acetone bark extract of R. phylladenia led to isolation and identification of lupeol, betulinic acid, and isofraxidin. Lupeol and betulinic acid showed in-vitro cytotoxic activity to MCF-7, MDA-MB-231, and 5637 human tumor cell lines. Isofraxidin was not cytotoxic, but did show antileishmanial activity to Leishmania amazonensis promastigotes.
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Chem Biodivers
December 2024
Universidad Nacional de Colombia, Antioquia, carrera 65 59a-110, 3840, Medellín, COLOMBIA.
Coumarin-chalcone hybrids are promising compounds that could be used as lead structures in the fight against parasitic diseases. In this work, sixteen hybrids of coumarin-chalcone (3-cinnamoyl-2H-chromen-2-ones) were synthesized, and their in vitro biological activity was evaluated against intracellular amastigotes of Leishmania braziliensis and Trypanosoma cruzi; as well as their cytotoxicity in the U-937 cell line. Compounds (E)-3-(3-(3-ethoxy-4-hydroxyphenyl)acryloyl)-7-methoxy-2H-chromen-2-one (H25) and (E)-7-(diethylamino)-3-(4-(methoxyphenyl)acryloyl)-2H-chromen-2-one (H12) showed the highest antileishmanial activity with EC50 values of 18.
View Article and Find Full Text PDF3 Biotech
January 2025
Cell and Molecular Biology Laboratory, Department of Zoology, Soban Singh Jeena University, Campus Almora, Almora, Uttarakhand India.
Unlabelled: Visceral leishmaniasis (VL), caused by , remains challenging to treat due to severe side effects and increasing drug resistance associated with current chemotherapies. Our study investigates the anti-leishmanial potential of from Uttarakhand, India, with extracts prepared from leaves and stems using ethanol and hexane. Advanced GC-MS analysis identified over 100 bioactive compounds, which were screened using molecular docking to assess their binding to LdHEL-67, a DDX3-DEAD box RNA helicase of donovani.
View Article and Find Full Text PDFFuture Microbiol
December 2024
Department of Biology, Faculty of Biological Sciences, Falavarjan Branch, Islamic Azad University, Isfahan, Iran.
Aim: Leishmaniasis is a globally prevalent parasitic disease that has drawn significant attention. Killer yeasts offer a novel biological control method, presenting a potential alternative for treating leishmaniasis. This study evaluates the antileishmanial activity of and killer toxins against .
View Article and Find Full Text PDFChemMedChem
December 2024
Nantes Université: Nantes Universite, Chimie Thérapeutique UR 1155 - IICiMed, IRS2 22 Boulevard Bénoni Goullin, 44200, Nantes, FRANCE.
Our research group previously discovered CTN1122, an imidazo[1,2-a]pyrazine compound with promising antileishmanial activity against intramacrophage amastigotes of Leishmania major and L. donovani strains. CTN1122 effectively targets Leishmania casein kinase 1 (L-CK1.
View Article and Find Full Text PDFParasite Immunol
December 2024
Department of Epidemiology and Biostatistics, Shahrekord University of Medical Sciences, Shahrekord, Iran.
The mechanistic study of new pharmaceutical compounds is crucial for evaluating their efficacy, identifying potential side effects, and optimising drug formulations. This study aimed to investigate the mechanism of action of trigonelline on the promastigote and amastigote stages of Leishmania major (MRHO/IR/75/ER). An initial in silico study was conducted to examine the pharmacological effects of trigonelline using molecular docking to evaluate the potential binding affinity of trigonelline with nitrate, a crucial molecule in the macrophage immune response against Leishmania.
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