Abstract
Bioassay-guided fractionation of a hexane extract prepared from the roots of the Chinese drug Angelica dahurica (Bai Zhi) led to the isolation of the polyacetylenic natural product falcarindiol (1). The absolute stereochemistry of this compound was confirmed by careful 1H NMR analysis of its (R)- and (S)-Mosher ester derivatives as the 3(R), 8(S) isomer. Activity was tracked using a Mycobacterium fortuitum screening assay and the purified product was evaluated against multidrug-resistant and methicillin-resistant strains of Staphylococcus aureus (MRSA). The minimum inhibitory concentrations (MIC) of this metabolite ranged from 8 to 32 μg/ml highlighting the potential of the acetylene natural product class as antibiotic-lead compounds. These MIC values compare favourably with some of the newest agents in development for the treatment of MRSA infection and indicate that further evaluation of the antibiotic activity of acetylenes is warranted.
Bioassay-guided isolation of a hexane extract of the roots of Angelica dahurica (Apiaceae) led to the isolation of 3(R), 8(S)-falcarindiol as the active anti-bacterial principle. This compound displayed minimum inhibitory concentrations of 8–32 μg/ml against multidrug-resistant (MDR) and methicillin-resistant Staphylococcus aureus (MRSA).
Bioassay-guided isolation of a hexane extract of the roots of Angelica dahurica (Apiaceae) led to the isolation of 3(R), 8(S)-falcarindiol as the active anti-bacterial principle. This compound displayed minimum inhibitory concentrations of 8–32 μg/ml against multidrug-resistant (MDR) and methicillin-resistant Staphylococcus aureus (MRSA).
Original language | English |
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Pages (from-to) | 331-335 |
Number of pages | 5 |
Journal | Phytochemistry |
Volume | 65 |
Issue number | 3 |
DOIs | |
Publication status | Published - 1 Feb 2004 |