Antifungals and acetylcholinesterase inhibitors from the stem bark of Croton heliotropiifolius

作者：Queiroz M M F; Queiroz E F; Zeraik M L; Marti G; Favre Godal Q; Simoes Pires C; Marcourt L; Carrupt P A; Cuendet M; Paulo M Q; Bolzani V S; Wolfender J L^*

来源：Phytochemistry Letters, 2014, 10: LXXXVIII-xciii.

DOI：10.1016/j.phytol.2014.08.013

• Croton heliotropiifolius
• HPLC-PDA-ESI-MS
• HPLC-TOF-HRMS
• Acetylcholinesterase inhibition
• Antifungal
• Candida albicans

The ethanolic extract of the stem bark of Croton heliotropiifolius Kunth (Euphorbiaceae) showed significant in vitro inhibition of acetylcholinesterase using a dilution spectrophotometric assay and antifungal activity against Candida albicans with a thin layer chromatography (TLC) bioautographic assay. In order to isolate the active compounds, bioassay-guided fractionation was undertaken using HPLC to localize the active compounds. Different zones of the HPLC-UV chromatogram were linked to acetylcholinesterase inhibition or to antifungal activities. In parallel to this HPLC-based activity profiling, HPLC-PDA-ESI-MS and HPLC-TOF-HRMS were used for the early identification of some of the compounds present. The targeted isolation of the active compounds was performed by medium pressure liquid chromatography (MPLC-UV) and further semi-preparative HPLC. Using this approach, nine compounds were isolated, one of them being a new indole alkaloid derivative. The structures of the isolated compounds were elucidated by spectroscopic methods including UV, NMR, MS and HRMS.

• 出版日期2014-12