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• W3136551495 endingPage "2766" @default.
• W3136551495 startingPage "2755" @default.
• W3136551495 abstract "Abstract Schistosoma mansoni is a parasitic flatworm causing schistosomiasis, an infectious disease affecting several hundred million people worldwide. Schistosomes live dioeciously, and upon pairing with the male, the female starts massive egg production, which causes pathology. Praziquantel (PZQ) is the only drug used, but it has an inherent risk of resistance development. Therefore, alternatives are needed. In the context of drug repurposing, the cancer drug imatinib was tested, showing high efficacy against S. mansoni in vitro. Besides the gonads, imatinib mainly affected the integrity of the intestine in males and females. In this study, we investigated the potential uptake and distribution of imatinib in adult schistosomes including its distribution kinetics. To this end, we applied for the first time atmospheric-pressure scanning microprobe matrix-assisted laser desorption/ionization mass spectrometry imaging (AP-SMALDI MSI) for drug imaging in paired S. mansoni . Our results indicate that imatinib was present in the esophagus and intestine of the male as early as 20 min after in vitro exposure, suggesting an oral uptake route. After one hour, the drug was also found inside the paired female. The detection of the main metabolite, N-desmethyl imatinib, indicated metabolization of the drug. Additionally, a marker signal for the female ovary was successfully applied to facilitate further conclusions regarding organ tropism of imatinib. Our results demonstrate that AP-SMALDI MSI is a useful method to study the uptake, tissue distribution, and metabolization of imatinib in S. mansoni . The results suggest using AP-SMALDI MSI also for investigating other antiparasitic compounds and their metabolites in schistosomes and other parasites. Graphical abstract" @default.
• W3136551495 created "2021-03-29" @default.
• W3136551495 creator A5010321935 @default.
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• W3136551495 date "2021-03-15" @default.
• W3136551495 modified "2023-10-01" @default.
• W3136551495 title "High-resolution AP-SMALDI MSI as a tool for drug imaging in Schistosoma mansoni" @default.
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• W3136551495 doi "https://doi.org/10.1007/s00216-021-03230-w" @default.
• W3136551495 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8007518" @default.
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• W3136551495 hasPublicationYear "2021" @default.
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