Administration of a single oral dose of oltipraz (5-(2-pyrazinyl)-4 methyl-1,2 dithiol-3-thione) to mice infected with Schistosoma mansoni resulted in the elimination of the parasites. Oltipraz is a slow-acting drug and approximately 2 months are required until its full schistosomicidal effect becomes evident. One of the earliest effects of the drug is a reduction of the glutathione stores of the worms. The antischistosomal activity of oltipraz is lowered when drug metabolism is stimulated by pretreatment with phenobarbital or butyl-hydroxyanisole (BHA). By contrast, administration of L-cysteine is synergistic with the antischistosomal effect of oltipraz. Evaluation of a limited number of oltipraz analogs revealed among dithiolthiones rather stringent structural requirements for antischistosomal activity.
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Acta Trop
January 2025
Centre of Excellence for Pharmaceutical Sciences (Pharmacen(TM)), North-West University, Private Bag X6001, Potchefstroom 2520, South Africa. Electronic address:
Praziquantel is currently the only effective treatment for schistosomiasis, but several limitations underscore the need for new therapeutic agents. Recent promising in vitro results with Artemisia species and the success of A. annua and its active compound artemisinin in treating parasitic infections warrant the need for further studies.
View Article and Find Full Text PDFMolecules
January 2025
Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, Santo André 09280-560, SP, Brazil.
In the present study, the hexane extract from branches of (Winteraceae) displayed potent activity against parasites (100% mortality of the worms at 200 μg/mL). Bioactivity-guided fractionation afforded, in addition to the previously reported bioactive sesquiterpene 3,6-epidioxy-bisabola-1,10-diene, two chemically related drimane sesquiterpenes-polygodial () and 9-deoxymuzigadial (). The anti- effects for compounds and were determined in vitro, with compound demonstrating significant potency (EC value of 10 μM for both male and female worms), while was inactive.
View Article and Find Full Text PDFFront Parasitol
February 2024
Department of Cell Biology, Neurobiology & Anatomy, Medical College of Wisconsin, Milwaukee, WI, United States.
Infections caused by parasitic flatworms impart a significant disease burden. This is well exemplified by the neglected tropical disease schistosomiasis, which afflicts millions of people worldwide. The anti-schistosomal activity of various chemotypes has been known for decades, but the parasite targets of many of these remain undefined.
View Article and Find Full Text PDFExp Parasitol
January 2025
Faculty of Pharmacy, Department of Pharmaceutical Sciences, Federal University of Juiz de Fora, Juiz de Fora, MG, 36036-900, Brazil. Electronic address:
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.
View Article and Find Full Text PDFEur J Med Chem
February 2025
Swiss Tropical and Public Health Institute, Kreuzstrasse 2, 4123, Allschwil, Switzerland; University of Basel, P.O. Box CH-4003, Basel, Switzerland. Electronic address:
For over three decades, praziquantel (PZQ) has been the mainstay chemotherapy for prevention and treatment of schistosomiasis. The excessive use of PZQ, coupled with the lack of advanced drug candidates in the current anti-schistosomiasis drug development pipeline, emphasizes the genuine need for new drugs. In the current work, we investigated the antischistosomal potential of a new series of compounds derived from the privileged benzimidazole scaffold, which exhibited low micromolar IC potency in the range of 1.
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