The protozoan parasite Leishmania donovani is the causative agent of visceral leishmaniasis, a disease potentially fatal if not treated. Current available treatments have major limitations, and new and safer drugs are urgently needed. In recent years, advances in high-throughput screening technologies have enabled the screening of millions of compounds to identify new antileishmanial agents. However, most of the compounds identified in vitro did not translate their activities when tested in in vivo models, highlighting the need to develop more predictive in vitro assays. In the present work, we describe the development of a robust replicative, high-content, in vitro intracellular L. donovani assay. Horse serum was included in the assay media to replace standard fetal bovine serum, to completely eliminate the extracellular parasites derived from the infection process. A novel phenotypic in vitro infection model has been developed, complemented with the identification of the proliferation of intracellular amastigotes measured by EdU incorporation. In vitro and in vivo results for miltefosine, amphotericin B, and the selected compound 1 have been included to validate the assay.
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http://dx.doi.org/10.1128/AAC.01781-15 | DOI Listing |
J Biol Chem
January 2025
Department of Microbiology, University of Delhi South Campus, New Delhi, India.
SET proteins are lysine methyltransferases. In investigating Leishmania donovani SET29, we found depletion of LdSET29 by two-thirds did not affect promastigote growth, nor alter the parasite's response to UV-induced or HU-induced stress, but made it more tolerant to HO-induced oxidizing environment. The deviant response to oxidative stress was coupled to lowered accumulation of reactive oxygen species, which was linked to enhanced scavenging activity.
View Article and Find Full Text PDFExp Parasitol
January 2025
Natural Products Chemistry Laboratory, State University of Ceará, Fortaleza, Brazil. Electronic address:
The current treatment of leishmaniasis is confronted with significant challenges, including limited efficacy, adverse effects, and parasite resistance to drugs. The search for alternative therapeutic options, including the utilization of natural products, has demonstrated considerable promise. In this study, the antileishmanial activity of the flavonoid hesperetin against Leishmania donovani, the causative agent of visceral leishmaniasis, was reported for the first time.
View Article and Find Full Text PDFBMC Infect Dis
January 2025
Aklilu Lemma Institute of Pathobiology, Addis Ababa University, Addis Ababa, Ethiopia.
Background: Visceral leishmaniasis is endemic in Ethiopia and caused by Leishmania donovani. Although the disease manifests with significant clinical variability, a substantial number of individuals are asymptomatic. These individuals can serve as reservoirs, complicating control efforts.
View Article and Find Full Text PDFExp Parasitol
January 2025
Department of Biotechnology, Savitribai Phule Pune University, 411007, Pune, India. Electronic address:
Visceral leishmaniasis (VL) is an opportunistic infection in HIV patients with higher relapse and mortality rate. The number of HIV-VL patients is comparatively higher in areas where both infections are endemic. However, the conventional chemotherapeutic agents have limited success due to drug toxicity, efficacy variance and overall cost of treatment.
View Article and Find Full Text PDFCell Biol Int
January 2025
Laboratory of Leishmaniasis, Department of Parasitology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, Brazil.
Leishmaniases affect millions of people around the world, caused by Leishmania parasites. Leishmania are transmitted by female sandflies from Phlebotominae subfamily during their blood meals. In mammals, promastigotes are phagocytosed mainly by macrophages, differentiate into amastigotes and multiply.
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