학술논문
Production of Highly Active Antiparasitic Compounds from the Controlled Halogenation of the Arrabidaea brachypodaCrude Plant Extract
Document Type
Article
Author
Source
Journal of Natural Products; September 2020, Vol. 83 Issue: 9 p2631-2640, 10p
Subject
Language
ISSN
01633864; 15206025
Abstract
Direct halogenation of phenolic compounds present in the CH2Cl2extract of the roots of Arrabidaea brachypodawas investigated to enhance chemodiversity. The approach is based on eco-friendly reactions using NaBr, NaI, and NaCl in aqueous media to generate multiple “unnatural” halogenated natural products from crude extracts. The halogenation reactions, monitored by UHPLC-PDA-ELSD-MS, were optimized to generate mono-, di-, or trihalogenated derivatives. To isolate these compounds, the reactions were scaled up and the halogenated analogues were isolated by semipreparative HPLC-UV and fully characterized by NMR and HR-MS data. All of the original 16 halogenated derivatives were evaluated for their antiparasitic activities against the parasites Leishmania amazonensisand Trypanosoma cruzi. Compounds presenting selective antiparasitic activities against one or both parasites with IC50values comparable to the reference were identified.