The new pyrrolizidine alkaloid glycoside 1, and the three new highly oxygenated bisabolane sesquiterpenes 4-6, together with the two known pyrrolizidine alkaloids 2 and 3, were isolated from the roots of Ligularia cymbulifera (W. W SMITH) HAND.-MAZZ. Their structures were established on the basis of spectroscopic analysis, especially 1D- and 2D-NMR data. ne cytotoxic activities of compounds 1, 2, and 4-6 were evaluated against hepatoma (BEL-7402), human leukemia (HL-60), human ovarian carcinoma (HO-8910), and nasopharyngeal carcinoma (KB) cell lines (Tables 1-3). Compound 6 showed weak cell-growth inhibition of BEL-7402 cell.