A collection of β-carbolines based on the natural product harmine, a compound known to target the heat shock 90 protein of Plasmodium falciparum, was synthesized and tested for antimalarial activity and potential toxicity. Several of these novel compounds display promising bioactivity, providing a new potential therapeutic with a mode of action that differs versus any currently available clinical treatment.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2023.129410DOI Listing

Publication Analysis

Top Keywords

plasmodium falciparum
8
heat shock
8
shock protein
8
synthesis activity
4
activity β-carboline
4
β-carboline antimalarials
4
antimalarials targeting
4
targeting plasmodium
4
falciparum heat
4
protein collection
4

Similar Publications

The circular genome of the apicoplast contains a complete minimal set of tRNAs, positioning the apicoplast as an ideal model for studying the fundamental factors required for protein translation. Modifications at tRNA wobble base positions, such as xm s U, are critical for accurate protein translation. These modifications are ubiquitously found in tRNAs decoding two-family box codons ending in A or G in prokaryotes and in eukaryotic organelles.

View Article and Find Full Text PDF

The emergence of parasites partially resistant to artemisinins (ART-R) poses a significant threat to recent gains in malaria control. ART-R has been associated with PfKelch13 (K13) mutations, which differ in fitness costs. This study investigates the gametocyte production and transmission fitness of African and Asian isolates with different K13 genotypes across multiple mosquito species.

View Article and Find Full Text PDF

Malian field isolates provide insight into Plasmodium malariae intra-erythrocytic development and invasion.

PLoS Negl Trop Dis

January 2025

Malaria Research and Training Center (MRTC), Université des Sciences, des Techniques et des Technologies de Bamako (USTTB), Bamako, Mali.

Plasmodium malariae is the third most prevalent human malaria parasite species and contributes significantly to morbidity. Nevertheless, our comprehension of this parasite's biology remains limited, primarily due to its frequent co-infections with other species and the lack of a continuous in vitro culture system. To effectively combat and eliminate this overlooked parasite, it is imperative to acquire a better understanding of this species.

View Article and Find Full Text PDF

Genetic diversity of and field isolates from Honduras in the malaria elimination phase.

Curr Res Parasitol Vector Borne Dis

November 2024

Instituto de Investigaciones en Microbiología, Facultad de Ciencias, Universidad Nacional Autónoma de Honduras, Tegucigalpa, 11101, Honduras.

Malaria continues to be a major threat to public health in tropical regions, primarily affecting sub-Saharan Africa but also Asia, the Middle East, and Latin America. Malaria cases in Honduras have seen a significant decline and the country aims to eliminate the disease by 2030. This study examines the genetic diversity of and in Honduras using four molecular markers (, , , and ), and the chloroquine resistance marker in the context of the elimination phase.

View Article and Find Full Text PDF

Unlabelled: Hemozoin (HZ) is a waste product of hemoglobin digestion by and has been implicated in several pathological processes, including inflammation, oxidative stress, endothelial dysfunction, and immune dysregulation. Studying the effects of HZ on the human placenta is essential to understanding the impact of malaria infection during pregnancy. The present study explored the impact of HZ produced by and β-hematin, referred to here as natural HZ (nHZ) and synthetic HZ (sHZ), respectively, on human placental explants exposed .

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!