Synthetic Aurones: New Features for Schistosoma mansoni Therapy

Chem Biodivers. 2021 Nov;18(11):e2100439. doi: 10.1002/cbdv.202100439. Epub 2021 Oct 20.

Abstract

In this work, two synthetic aurones revealed moderate schistosomicidal potential in in vitro and in vivo assays. Aurones (1) and (2) promoted changes in tegument integrity and motor activity, leading to death of adult Schistosoma mansoni worms in in vitro assays. When administered orally (two doses of 50 mg/kg) in experimentally infected animals, synthetic aurones (1) and (2) promoted reductions of 56.20 % and 57.61 % of the parasite load and stimulated the displacement towards the liver of the remaining adult worms. The oogram analysis revealed that the treatment with both aurones interferes with the egg development kinetics in the intestinal tissue. Seeking an action target for compounds (1) and (2), the connection with NTPDases enzymes, recognized as important therapeutic targets for S. mansoni, was evaluated. Molecular docking studies have shown promising results. The dataset reveals the anthelmintic character of these compounds, which can be used in the development of new therapies for schistosomiasis.

Keywords: NTPDases; Schistosoma mansoni; SmATPDase; anthelmintic; flavonoids.

MeSH terms

  • Administration, Oral
  • Animals
  • Anthelmintics / administration & dosage
  • Anthelmintics / chemistry
  • Anthelmintics / pharmacology*
  • Benzofurans / administration & dosage
  • Benzofurans / chemistry
  • Benzofurans / pharmacology*
  • Dose-Response Relationship, Drug
  • Female
  • Mice
  • Molecular Structure
  • Schistosoma mansoni / drug effects*
  • Schistosomiasis / drug therapy*

Substances

  • Anthelmintics
  • Benzofurans
  • aurone