Twelve new dihydroagarofuran sesquiterpene polyol esters, triptersinines A-L (1-12), and eight known sesquiterpene pyridine alkaloids were isolated from the leaves of Tripterygium wilfordii. Their structures were elucidated on the basis of spectroscopic analyses, including UV, IR, and NMR experiments ((1)H-(1)H COSY, NOESY, HSQC, and HMBC). Furthermore, in an in vitro bioassay, compounds 1, 9, 11, 13, 14, and 18 showed moderate inhibitory effects on nitric oxide production in LPS-induced macrophages at 5 μM; all compounds were inactive when tested against five human cancer cell lines (IC(50) values >1 μM).