Cytotoxic and antibacterial aspidofractinine alkaloids from Kopsia hainanensis

The ethanol extract of the twigs and leaves of Kopsia hainanensis afforded six new aspidofractinine alkaloids, kopsiahainanins A-F (1-6), among which alkaloids 1 and 2 possessed a lactone bridge with novel regiochemistry. The structures of the isolated compounds were established based on 1D and 2D (¹H¹H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated compounds were tested in vitro for cytotoxic activity against seven tumor cell lines and antibacterial activities against two Gram-positive bacteria and five Gram-negative bacteria. As a result, alkaloids 1 and 2 exhibited cytotoxic activities (IC₅₀ values <20 μM) against all tested tumor cell lines and significant antibacterial properties (MIC values from 0.12 to 0.26 mM).