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The Ivermectin Related Compound Moxidectin Can Target Apicomplexan Importin α and Limit Growth of Malarial Parasites.
Cells
January 2025
Nuclear Signaling Laboratory, Monash Biomedicine Discovery Institute, Department of Biochemistry and Molecular Biology, Monash University, Clayton, VIC 3800, Australia.
Signal-dependent transport into and out of the nucleus mediated by members of the importin (IMP) superfamily is crucial for eukaryotic function, with inhibitors targeting IMPα being of key interest as anti-infectious agents, including against the apicomplexan species and , causative agents of malaria and toxoplasmosis, respectively. We recently showed that the FDA-approved macrocyclic lactone ivermectin, as well as several other different small molecule inhibitors, can specifically bind to and inhibit and IMPα functions, as well as limit parasite growth. Here we focus on the FDA-approved antiparasitic moxidectin, a structural analogue of ivermectin, for its IMPα-targeting and anti-apicomplexan properties for the first time.
View Article and Find Full Text PDFGossypol is a natural product with good antimalarial activity against Plasmodium falciparum clinical isolates.
Sci Rep
January 2025
West African Centre for Cell Biology of Infectious Pathogens, University of Ghana, Accra, Ghana.
Gossypol has demonstrated significant antimalarial activity against chloroquine-resistant and susceptible Plasmodium falciparum parasites. However, data on its potency in clinical isolates of P. falciparum remains limited.
View Article and Find Full Text PDFEmerging nanotechnology-driven drug delivery solutions for malaria: Addressing drug resistance and improving therapeutic success.
Int J Pharm
January 2025
Centre for Transgenic Plant Development, Department of Biotechnology, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi 110062, India. Electronic address:
Malaria remains the fifth deadliest parasitic infection worldwide, despite significant advancements in technology. A major challenge in combating this disease lies in the growing resistance of malaria parasites to antimalarial drugs and insect vectors to insecticides. The emerging inefficacy of artemisinin-based combination therapies (ACTs) further exacerbates the issue.
View Article and Find Full Text PDFPHYLOGENETIC ANALYSIS OF AEDES AEGYPTI IN TAIF AND JEDDAH GOVERNORATES, SAUDI ARABIA.
J Am Mosq Control Assoc
January 2025
Department of Biological Sciences, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
With their diverse species, mosquitoes are known to transmit the causal agents of diseases such as malaria, dengue, and yellow fever. Their high adaptability, attraction to humans, and variable adult behaviors make them a significant health concern. The focus on Aedes aegypti is significant for reducing vector-human contacts, monitoring insecticide resistance, and developing innovative vector management strategies.
View Article and Find Full Text PDFDesign, synthesis and in vitro evaluation of primaquine and diaminoquinazoline hybrid molecules against the malaria parasite.
Chem Asian J
January 2025
Birla Institute of Technology and Science - Pilani Campus: Birla Institute of Technology & Science Pilani, Pharmacy, BITS Pilani, Pilani campus, Vidya Vihar, 333031, Pilani, INDIA.
In this study, we built on the known inhibitory potential of diaminoquinazolines (DAQs) against different stages of Plasmodium development and designed a convenient two-step synthesis to combine DAQ with the primaquine (PQ) pharmacophore. The PQ-DAQ hybrids displayed potent in vitro activities in the low nanomolar range (IC50 of 135.20-398.
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