Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica
نویسندگان
چکیده
Infection with Fasciola hepatica (liver fluke) causes fasciolosis (or fascioliasis) and poses a considerable economic as well welfare burden to both the agricultural animal health sectors. Here, we explore ex vivo anthelmintic potential of synthetic derivatives hederagenin, isolated in bulk from Hedera helix. Thirty-six compounds were initially screened against F. newly excysted juveniles (NEJs) Italian strain. Eleven these active NEJs selected for further study, using adult derived local abattoir (provenance unknown). From eleven compounds, six demonstrated activity assessed immature liver flukes Subsequently, most (n = 5) evaluated dose response experiments strain flukes. Overall, MC042 was identified molecule EC50 obtained fluke assays (at 24 h post co-culture) are estimated 1.07 μM 13.02 μM, respectively. When compared vitro cytotoxicity MDBK bovine cell line, highest selectivity (44.37 3.64 flukes). These data indicate that modified hederagenins display properties suitable investigations candidate flukicides.
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We examined the in vivo activity of tribendimidine against selected trematodes. A single 150 mg/kg dose of tribendimidine achieved a 99.1% reduction of Clonorchis sinensis in rats. 400 mg/kg tribendimidine reduced Opisthorchis viverrini in hamsters by 95.7%. High doses of tribendimidine showed no activity against Schistosoma mansoni and Fasciola hepatica.
متن کاملEvaluation of the in vivo activity of tribendimidine against Schistosoma mansoni, Fasciola hepatica, Clonorchis sinensis, and Opisthorchis viverrini.
We examined the in vivo activity of tribendimidine against selected trematodes. A single 150-mg/kg dose of tribendimidine achieved a 99.1% reduction of Clonorchis sinensis in rats. A 400-mg/kg dose of tribendimidine reduced Opisthorchis viverrini in hamsters by 95.7%. High doses of tribendimidine showed no activity against Schistosoma mansoni and Fasciola hepatica.
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ژورنال
عنوان ژورنال: Pharmaceutics
سال: 2023
ISSN: ['1999-4923']
DOI: https://doi.org/10.3390/pharmaceutics15071869