Evidences for leishmanicidal activity of the naphthoquinone derivative epoxy-α-lapachone

Exp Parasitol. 2014 Dec:147:81-4. doi: 10.1016/j.exppara.2014.10.002. Epub 2014 Oct 13.

Abstract

In this work, we analyze the leishmanicidal effects of epoxy-α-lapachone on Leishmania (Viannia) braziliensis and Leishmania (Leishmania) amazonensis. Promasigotes and amastigotes (inhabiting human macrophages) from both species were assayed to verify the compound's activity over the distinct morphological stages. The incubation with epoxy-α-lapachone led to a significant decrease in the numbers of promastigotes from both species in the cultures, in a dose-and time-dependent fashion. The survival of amastigotes inhabiting human macrophages was also drastically affected by the compound, as shown by the variations in the endocytic index. Our results indicate that the epoxy-α-lapachone has an antiparasitic effect over Leishmania in both morphological stages and may potentially affect a range of species in two distinct subgenera of this parasite.

Keywords: Epoxy-α-lapachone; Leishmania (Leishmania) amazonensis; Leishmania (Viannia) braziliensis; Naphthoquinones.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Humans
  • Leishmania braziliensis / drug effects*
  • Leishmania mexicana / drug effects*
  • Macrophages / drug effects
  • Macrophages / parasitology
  • Naphthoquinones / chemistry
  • Naphthoquinones / pharmacology*
  • Time Factors

Substances

  • 2,2-dimethyl-3,4-dihydrospiro(benzo(g)chromene-10,2'-oxiran)-5(2H)-one
  • Antiprotozoal Agents
  • Naphthoquinones