Antifungals and acetylcholinesterase inhibitors from the stem bark of Croton heliotropiifolius |
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Institution: | 1. College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, China;2. College of Pharmacy, Harbin University of Commerce, Harbin 150076, China;3. Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Japan;4. School of Medicine, Nankai University, Tianjin 300071, China;1. School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China;2. School of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510006, China |
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Abstract: | 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. |
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Keywords: | HPLC-PDA-ESI-MS HPLC-TOF-HRMS Acetylcholinesterase inhibition Antifungal |
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