| Summary: | Six new coumarin glycosides, genglycoside A–F (<b>1</b>–<b>6</b>), were isolated from the aerial parts of <i>Gendarussa vulgaris</i>, along with ten known analogues (<b>7</b>–<b>16</b>). Their structures were unambiguously established on the basis of extensive spectroscopic data and HPLC analysis. The cytotoxic activities of all isolated compounds were evaluated by MTT assay. Compound <b>12</b> showed the most potent cytotoxicity in Eca-109, MCF-7, and HepG2 cell lines. By the preliminary structure–activity relationships, it was firstly discovered that the glycosylation or esterification at 7,8-dihydroxy or 7-hydroxy drastically reduced the cytotoxic activity of the parent coumarin.
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