In Vivo and in Silico Trypanocidal Activity Evaluation of (-)-Cubebin Encapsulated in PLGA Microspheres as Potential Treatment in Acute Phase

Chem Biodivers. 2021 Jun;18(6):e2100052. doi: 10.1002/cbdv.202100052. Epub 2021 Apr 27.

Abstract

In this study, the trypomastigotes of a Y strain of Trypanosoma cruzi were inoculated intraperitoneally into male BALB/c mice weighing approximately 25 g each, which were divided into groups for evaluation of the trypanocidal activity. For the treatment of experimental groups, encapsulated and unencapsulated (-)-cubebin, Benznidazole, and two groups as negative controls were used. The encapsulated (-)-cubebin showed a 68.1 % encapsulation efficiency. The parasitemia peak of substances remained around the 9th day after the observed reduction in the number of circulating trypomastigotes. The encapsulated (-)-cubebin and (-)-cubebin unloaded showed a decrease of 61.3 % and 58.5 % in the number of parasites as compared to the negative control, respectively. Moreover, animals treated with encapsulated (-)-cubebin had a higher survival time as compared to the other groups. In conclusion, the results obtained were more promising for encapsulated (-)-cubebin as compared to unloaded particles.

Keywords: (−)-cubebin; Chagas disease; PLGA; lignans; molecular docking.

MeSH terms

  • Animals
  • Capsules
  • Injections, Intraperitoneal
  • Lignans / administration & dosage
  • Lignans / chemistry
  • Lignans / pharmacology*
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Microspheres*
  • Molecular Docking Simulation
  • Parasitic Sensitivity Tests
  • Trypanocidal Agents / administration & dosage
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma cruzi / drug effects*

Substances

  • Capsules
  • Lignans
  • Trypanocidal Agents
  • cubebin