Assay of Antiparasitic Compounds Targeting Tubulin in Schistosoma Mansoni Cultures
Abstract
Schistosomiasis is a neglected tropical disease that affects over 250 million people. It is caused by trematodes of the genus Schistosoma spp., the conventional treatment is praziquantel (PZQ), an antiparasitic agent effective against the adult stages of the parasite. However, PZQ has limited efficacy against juvenile forms, and over time, cases of drug resistance have been reported. This highlights the need to develop new antiparasitic compounds targeting all parasite life cycle stages. This study evaluated antiparasitic compounds that are effective against all stages of Schistosoma mansoni. The parasite’s life cycle was maintained in the laboratory using mice as definitive hosts and snails as intermediate hosts. A total of 26 compounds were tested on juveniles (schistosomula) and adult worms, and their viability was assessed using techniques such as microscopy and artificial intelligence. These compounds, designed by the Department of Pharmaceutical Chemistry at the Faculty of Pharmacy (USAL), target tubulin by inhibiting its polymerization. Furthermore, they were previously tested on a human cell line and showed no significant cytotoxic effects. Among the results, Compound 1 exhibited 100% lethality at both stages of the parasite, with promising lethal concentration (LC50) values. In conclusion, one of the compounds showed promising in vitro results for both parasite developmental stages. However, further in vivo studies are required for a more comprehensive evaluation.
Keywords: schistosomiasis; drug resistance; tubulin; in vitro assays
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