In Vitro, In Vivo, and In Silico Studies of Cumanin Diacetate as a Potential Drug against Trypanosoma cruzi Infection.

ABSTRACT: The sesquiterpene lactones cumanin, helenalin, and hymenin and their semisynthetic derivatives were evaluated against Trypanosoma cruzi epimastigotes. The cytotoxicity of the compounds was evaluated on murine splenocytes. Cumanin diacetate was one of the most active and selective compounds [IC₅₀ = 3.20 ± 0.52 μg/mL, selectivity index (SI) = 26.0]. This sesquiterpene lactone was selected for its evaluation on trypomastigote and amastigote forms of the parasite. The diacetylated derivative of cumanin showed moderate activity on trypomastigotes (IC₅₀ = 32.4 ± 5.8 μg/mL). However, this compound was able to efficiently inhibit parasite replication with an IC₅₀ value of 2.2 ± 0.05 μg/mL against the amastigote forms. Cumanin diacetate showed selectivity aga

SUBMITTER: Sanchez Alberti A 

PROVIDER: S-EPMC8757452 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature