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Acta tropica v.167, 2017년, pp.163 - 173   SCI SCIE
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Antiparasitic activity of menadione (vitamin K3) against Schistosoma mansoni in BABL/c mice

Kapadia, Govind J. (Department of Pharmaceutical Sciences, College of Pharmacy, Howard University, Washington, DC 20059, USA ); Soares, Ingrid A.O. (Research Group on Natural Products, Center for Research in Sciences and Technology, University of Franca, Franca, Brazil ); Rao, G. Subba (Global Biotechnology Resource Center, 145 Rosewood Drive, Streamwood, IL 60107, USA ); Badoco, Fernanda R. (Research Group on Natural Products, Center for Research in Sciences and Technology, University of Franca, Franca, Brazil ); Furtado, Ricardo A. (Research Group on Natural Products, Center for Research in Sciences and Technology, University of Franca, Franca, Brazil ); Correa, Mariana B. (Research Group on Natural Products, Center for Research in Sciences and Technology, University of Franca, Franca, Brazil ); Tavares, Denise C. (Research Group on Natural Products, Center for Research in Sciences and Technology, University of Franca, Franca, Brazil ); Cunha, Wilson R. (Research Group on Natural Products, Center for Research in Sciences and Technology, University of Franca, Franca, Brazil ); Magalhães, Lizandra G. (Research Group on Natural Products, Center for Research in Sciences a );
  • 초록  

    Abstract Schistosomiasis is one of the neglected tropical diseases affecting nearly quarter of a billion people in economically challenged tropical and subtropical countries of the world. Praziquantel (PZQ) is the only drug currently available to treat this parasitic disease in spite being ineffective against juvenile worms and concerns about developing resistance to treat reinfections. Our earlier in vitro viability studies demonstrated significant antiparasitic activity of menadione (MEN) (vitamin K 3 ) against Schistosoma mansoni adult worms. To gain insight into plausible mechanism of antischistosomal activity of MEN, its effect on superoxide anion levels in adult worms were studied in vitro which showed significant increases in both female and male worms. Further confirmation of the deleterious morphological changes in their teguments and organelles were obtained by ultrastructural analysis. Genotoxic and cytotoxic studies in male Swiss mice indicated that MEN was well tolerated at the oral dose of 500mg/kg using the criteria of MNPCE frequency and PCE/RBC ratio in the bone marrow of infected animals. The in vivo antiparasitic activity of MEN was conducted in female BALB/c mice infected with S. mansoni and significant reductions ( P P P S. mansoni infection in humans. Highlights LC 50 of menadione (MEN) against S. mansoni adult worms in vitro was 10.49±1.02μM at 24h. MEN induced alterations on tegument and organelles of S. mansoni adult worms in vitr o. MEN increased superoxide anion levels in S. mansoni adult worms in vitro . MEN reduced the number of worms and egg formation in S. mansoni -infected mice in vivo . Above effects of MEN compared reasonably well to currently used drug, praziquantel. Graphical abstract [DISPLAY OMISSION]


  • 주제어

    Menadione .   Naphthoquinone .   Schistosoma mansoni .   Vitamin K3.  

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