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Background: Schistosomiasis is a neglected tropical disease caused by Schistosoma sp., and praziquantel (PZQ) is the first-line treatment. However, traditional PZQ formulations have low solubility and fast metabolism, limiting its effectiveness.

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Introduction: Schistosomiasis has for many years relied on a single drug, praziquantel (PZQ) for treatment of the disease. Immense efforts have been invested in the discovery of protein kinase (PK) inhibitors; however, given that the majority of PKs are still not targeted by an inhibitor with a useful level of selectivity, there is a compelling need to expand the chemical space available for synthesizing new, potent, and selective PK inhibitors. Small-molecule inhibitors targeting the ATP pocket of the catalytic domain of PKs have the potential to become drugs devoid of (major) side effects, particularly if they bind selectively.

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Schistosomiasis stands as one of the most significant parasitic diseases on a global scale, with approximately 250 million infections worldwide. It is imperative to address this pressing issue by developing new antischistosomal drugs. Chalcones have emerged as a promising class of natural compounds, demonstrating noteworthy effects observed in vitro experiments with Schistosoma mansoni, and demonstrating the ability to inhibit SmNTPDases and apyrase from potatoes.

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LC-MS/MS Analyzing Praziquantel and 4-Hydroxypraziquantel Enantiomers in Black Goat Plasma and Mechanism of Stereoselective Pharmacokinetics.

Biomed Chromatogr

February 2025

Guangdong Provincial key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, South China Agricultural University, Guangzhou, China.

Praziquantel (PZQ) is the most effective treatment for schistosomiasis, commonly administered as a racemic mixture of the two enantiomers. Despite many reports on the pharmacokinetics of PZQ, the stereoselective pharmacokinetics of PZQ and its major metabolite 4-hydroxypraziquantel (4-OH-PZQ) remain poorly understood in goats. In this study, the chiral LC-MS/MS method was further optimized for separating and quantifying PZQ, trans-4-OH-PZQ, and cis-4-OH-PZQ and their enantiomers and then applied for the molecular pharmacokinetics of three analytes in black goat plasma.

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Development and Application of an In Vitro Drug Screening Assay for Schistosomula Using YOLOv5.

Biomedicines

December 2024

Infectious and Tropical Diseases Research Group (e-INTRO), Biomedical Research Institute of Salamanca, Research Centre for Tropical Diseases at the University of Salamanca (IBSAL-CIETUS), Faculty of Pharmacy, University of Salamanca, 37007 Salamanca, Spain.

Background: Schistosomiasis impacts over 230 million people globally, with 251.4 million needing treatment. The disease causes intestinal and urinary symptoms, such as hepatic fibrosis, hepatomegaly, splenomegaly, and bladder calcifications.

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