作者: Lhais Araujo Caldas , Meire L Yoshinaga , Marcelo JP Ferreira , Joao HG Lago , Adriana B de Souza
DOI: 10.1016/J.BIOORG.2018.10.059
关键词: Chemistry 、 Mechanism of action 、 Ultrastructure 、 Sesquiterpene 、 Biochemistry 、 Cytotoxicity 、 Miltefosine 、 Asteraceae 、 EC50 、 Amastigote
摘要: Abstract Bioactivity-guided fractionation of antileishmanial active CH2Cl2 phase MeOH extract from leaves Calea pinnatifida led to isolation two sesquiterpene lactones calein C (1) and calealactone (2), which structures were stablished on the basis spectroscopic analysis. Compounds 1 2 displayed potent activity against Leishmania amazonensis promastigotes with EC50 1.7 4.6 µg mL−1, respectively. Compound presented low cytotoxicity for J774 macrophages amastigote forms L. similar miltefosine CC50 values 31.73 27.18 µg mL−1, Additionally, compounds caused ultrastructural changes in leading a loss their classical structural morphology, as evidenced by electron microscopy. Also compound decreased mitochondria membrane potential. To best our knowledge, this is first occurrence C. pinnatifida. The results obtained highlighted importance studying isolated terms activity, order understand mechanism action amazonensis.