Biological Activity of Coumarin Derivatives as Anti-Leishmanial Agents

PLoS One. 2016 Oct 21;11(10):e0164585. doi: 10.1371/journal.pone.0164585. eCollection 2016.

Abstract

Cutaneous leishmaniasis affects nearly 0.7 to 1.3 million people annually. Treatment of this disease is difficult due to lack of appropriate medication and the growing problem of drug resistance. Natural compounds such as coumarins serve as complementary therapeutic agents in addition to the current treatment modalities. In this study, we have performed an in-silico screening of the coumarin derivatives and their anti-leishmanial properties has been explored both in-vitro and in-vivo. One of the compounds (compound 2) exhibited leishmanicidal activity and to further study its properties, nanoliposomal formulation of the compound was developed. Treatment of cutaneous lesions in BALB/c mice with compound 2 showed significantly reduced lesion size as compared to the untreated mice (p<0.05) suggesting that compound 2 may possess anti-leishmanial properties.

MeSH terms

  • Animals
  • Antiprotozoal Agents / pharmacology
  • Antiprotozoal Agents / therapeutic use*
  • Cell Line
  • Coumarins / pharmacology
  • Coumarins / therapeutic use*
  • Female
  • Leishmaniasis, Cutaneous / drug therapy*
  • Liposomes
  • Membrane Potential, Mitochondrial / drug effects
  • Mice
  • Mice, Inbred BALB C

Substances

  • Antiprotozoal Agents
  • Coumarins
  • Liposomes

Grants and funding

Vineetha Mandlik acknowledges the financial support as Senior Research Fellow of Department of Biotechnology, Government of India; and Shailza Singh received the funding BT/PR6037/GBD/27/372/2012, Department of Biotechnology, Government of India. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.