Copper salisylaldoxime (CuSAL) imparts protective efficacy against visceral leishmaniasis by targeting Leishmania donovani topoisomerase IB.
Exp Parasitol
; 175: 8-20, 2017 Apr.
Article
en En
| MEDLINE
| ID: mdl-28174102
ABSTRACT
In vitro and in vivo anti-leishmanial efficacy of copper salisylaldoxime (CuSAL), a transition metal complex, was evaluated and the underlying mechanism was studied. In vitro studies revealed that 30 µM of CuSAL causes 96% reduction in parasite burden in infected macrophages. CuSAL is least toxic in host cells. A dose of 5 mg/kg bodyweight per mice on alternate days (5 doses) gives â¼97% protection in both liver and spleen. Moreover, CuSAL potentially inhibits the catalytic activity of LdTOPILS and causes apoptosis of Leishmania parasites through induction of intracellular ROS generation and activation of caspase-like proteases. Interestingly, CuSAL does not inhibit the catalytic activity of human topoisomerase I. The present study illuminated that CuSAL, has potent anti-leishmanial activity, which selectively targets LdTOPILS; and is a safe for human. Therefore, this compound might be highly promising candidate to develop the rational approaches for chemotherapy of human leishmaniasis.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Oximas
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Leishmania donovani
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Complejos de Coordinación
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Leishmaniasis Visceral
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Antiprotozoarios
Límite:
Animals
Idioma:
En
Año:
2017
Tipo del documento:
Article