| Summary: | <i>Gynostemma pentaphyllum</i> (thumb.) Makino is a functional herbal tea commonly used in Asian countries and regions to reduce blood lipid levels. <i>G. pentaphyllum</i> saponin is the main component, but there are still a large number of components with lipid-lowering activity that have not been found. In this study, 10 novel dammarane-type saponins, (<b>1</b>–<b>10</b>) and a known one (<b>11</b>) were isolated from <i>G. pentaphyllum</i>. Ten new compounds were identified and named as yunnangypenosides A-J (<b>1</b>–<b>10</b>), and another known one (<b>11</b>) was also obtained. Their chemical structures were determined by MS, NMR spectroscopic analyses. Moreover, the cytotoxicities on human HepG-2 hepatocellular carcinoma cells of these isolates were evaluated, and the results showed that compounds <b>1</b>–<b>11</b> had no obvious cytotoxicity. Finally, all these compounds were evaluated for their lipid-lowering effect by means of the oil red O staining method. Ten compounds could significantly reduce lipid levels except of <b>2</b>, especially <b>8</b> exhibite the strongest hypolipidemia activity.
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