| Summary: | The phytochemical study on the leaves of <i>Ligustrum robustum</i>, which have been used as Ku-Ding-Cha, led to the isolation and identification of three new phenylethanoid glycosides and three new phenylmethanoid glycosides, named ligurobustosides R<sub>1</sub> (<b>1b</b>), R<sub>2–3</sub> (<b>2</b>), R<sub>4</sub> (<b>3</b>), S<sub>1</sub> (<b>4b</b>), S<sub>2</sub> (<b>5</b>), and S<sub>3</sub> (<b>6</b>), and five reported phenylethanoid glycosides (<b>7</b>–<b>11</b>). In the bioactivity test, (<i>Z</i>)-osmanthuside B<sub>6</sub> (<b>11</b>) displayed strong fatty acid synthase (FAS) inhibitory activity (IC<sub>50</sub>: 4.55 ± 0.35 μM) as the positive control orlistat (IC<sub>50</sub>: 4.46 ± 0.13 μM), while ligurobustosides R<sub>4</sub> (<b>3</b>) and S<sub>2</sub> (<b>5</b>), ligupurpuroside B (<b>7</b>), <i>cis</i>-ligupurpuroside B (<b>8</b>), ligurobustoside N (<b>9</b>), osmanthuside D (<b>10</b>), and (<i>Z</i>)-osmanthuside B<sub>6</sub> (<b>11</b>) showed stronger ABTS radical scavenging activity (IC<sub>50</sub>: 2.68 ± 0.05~4.86 ± 0.06 μM) than the positive control L-(+)-ascorbic acid (IC<sub>50</sub>: 10.06 ± 0.19 μM). This research provided a theoretical basis for the leaves of <i>L. robustum</i> as a tea with function in treating obesity and diabetes.
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