Mostrando recursos 1 - 1 de 1

  1. Examination of the cytotoxic and embryotoxic potential and underlying mechanisms of next-generation synthetic trioxolane and tetraoxane antimalarials

    Copple, I. M.; Mercer, A. E.; Firman, J.; Donegan, G.; Herpers, B.; Wong, M. H.; Chadwick, J.; Bringela, A.; Cristiano, Maria Lurdes Santos; Van De Water, B.; Ward, Stephen A.; O'Neill, Paul M.; Park, B. K.
    Semisynthetic artemisinin-based therapies are the first-line treatment for P. falciparum malaria, but next-generation synthetic drug candidates are urgently required to improve availability and respond to the emergence of artemisinin-resistant parasites. Artemisinins are embryotoxic in animal models and induce apoptosis in sensitive mammalian cells. Understanding the cytotoxic propensities of antimalarial drug candidates is crucial to their successful development and utilization. Here, we demonstrate that, similarly to the model artemisinin artesunate (ARS), a synthetic tetraoxane drug candidate (RKA182) and a trioxolane equivalent (FBEG100) induce embryotoxicity and depletion of primitive erythroblasts in a rodent model. We also show that RKA182, FBEG100 and ARS...
    - 09-nov-2017

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