Asiaticoside induces tumour-necrosis-factor-α-mediated nitric oxide production to cure experimental visceral leishmaniasis caused by antimony-susceptible and -resistant Leishmania donovani strains

J Antimicrob Chemother. 2012 Apr;67(4):910-20. doi: 10.1093/jac/dkr575. Epub 2012 Jan 18.

Abstract

Objectives: The aim of this study was to investigate and characterize the efficacy of asiaticoside in an experimental model of visceral leishmaniasis caused by antimony-susceptible (AG83) and -resistant (GE1F8R and K39) Leishmania donovani.

Methods: The effect of asiaticoside was evaluated by microscopic counting of intracellular amastigotes in cultured macrophages stained with Giemsa. The antileishmanial effect of the compounds was assessed in infected BALB/c mice by estimation of splenic and liver parasite burdens in Leishman Donovan units. Cytokines were measured by real-time PCR and ELISA. Intracellular tumour necrosis factor-α (TNF-α) was measured by fluorescence-activated cell sorting. Nitric oxide was measured by the Griess reaction.

Results: Besides effectively inhibiting in vitro replication of the parasite within macrophages, asiaticoside treatment resulted in almost complete clearance of the liver and splenic parasite burden when administered at a dose of 5 mg/kg × 10 starting on day +30 of challenge with antimony-susceptible (AG83) and -resistant (GE1F8R and K39) L. donovani. Asiaticoside treatment was associated with a switch in the host from a Th2- to a Th1-type immune response accompanied by the induction of TNF-α-mediated nitric oxide production, all of which are important elements for macrophage function in antileishmanial defence mechanisms.

Conclusions: These results suggest that oral therapy with asiaticoside shows promising antileishmanial efficacy in animals infected by antimony-susceptible (AG83) and -resistant (GE1F8R and K39) L. donovani.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimony / pharmacology
  • Antiprotozoal Agents / administration & dosage*
  • Antiprotozoal Agents / pharmacology
  • Disease Models, Animal
  • Drug Resistance
  • Enzyme-Linked Immunosorbent Assay
  • Female
  • Leishmania donovani / immunology*
  • Leishmaniasis, Visceral / drug therapy*
  • Liver / parasitology
  • Macrophages / parasitology
  • Mice
  • Mice, Inbred BALB C
  • Microscopy
  • Nitric Oxide / immunology
  • Nitric Oxide / metabolism*
  • Polymerase Chain Reaction
  • Spleen / parasitology
  • Treatment Outcome
  • Triterpenes / administration & dosage*
  • Tumor Necrosis Factor-alpha / immunology
  • Tumor Necrosis Factor-alpha / metabolism*

Substances

  • Antiprotozoal Agents
  • Triterpenes
  • Tumor Necrosis Factor-alpha
  • Nitric Oxide
  • Antimony
  • asiaticoside