Highly selective alkylcoumarates and diterpenoids isolated from leaves of Baccharis quitensis : a search for new hit compounds against Trypanosoma cruzi

• Published in: Natural product research 2024-03, p.1-7
• Main Authors: Peres, Nathalia, Silva, Matheus L, Ueno, Anderson K, Antar, Guilherme M, Levatti, Erica V C, Tempone, Andre G, Lago, João Henrique G
• Format: Article
• Language: English
• ISSN: 1478-6419; 1478-6427
• DOI: 10.1080/14786419.2024.2335362

In the present work, the hexane extract of aerial parts of Kunth. was subjected to chromatographic fractionation to afford two alkyl phenylpropanoids: -docosyl ( -coumarate ( ) and -tetracosyl -coumarate ( ) as well as five diterpenes: kaurenoic acid ( ), grandifloric acid ( ), 15β-senecioyl-oxy- -kaur-16-en-19-oic acid ( ), and 15-oxo- -kaurenoic acid ( ). Using an assay with macrophages infected with , compounds and demonstrated high potency against intracellular amastigotes, with EC values of 7.5 and 6.9 µM, respectively. Compound revealed a moderate potency against , with an EC of 25.6 µM, and compounds showed no effectiveness. Additionally, compounds compounds presented no toxicity for mammalian cells to the highest tested concentration of 200 µM. Based on potency and the selectivity indexes of , and , these compounds could be future candidates for optimisation studies for the design of prototypes against Chagas disease.