A new octanordammarane triterpene, 3b, 15a-dihydroxymansumbinol (1) and a novel A-ring contracted oleanane triterpenoid, 2-formyl-(A) 1-19a-hydroxy-1-norolean-2,12-dien-28-oic acid (2) were isolated from the roots extract of Rosa rugosa along with fifteen known compounds (3-17). Their structures were elucidated by extensive spectroscopic analysis, including 1D and 2D NMR, and FTICRMS. The MeOH extract, as well as CH2Cl2 and EtOAc fractions at a concentration of 0.5 mg/mL showed potent sucrase inhibitory activity, with inhibition percentage values of 84.67 +/- 5.37%, 87.50 +/- 2.78%, and 81.91 +/- 2.90%, respectively. In addition, compounds 7-13 (1.0 mM) showed potent sucrase inhibitory activity (61.88 +/- 3.19% to 84.70 +/- 3.07% inhibition), which was comparable to that of the positive control, acarbose, with an inhibition percentage value of 50.96 +/- 2.97%. Compounds 1, 2, 4, and 14-17 showed moderate and/or weak inhibitory activities at the same concentration. The a-glucosidase inhibitory activities of the extracts and purified compounds may provide a novel opportunity to develop a new class of antidiabetic agents. Crown Copyright (C) 2013 Published by Elsevier Ltd. All rights reserved.