Two new compounds, piperoside (1) and isoheptanol 2(S)-O-beta-D-xylopyranosyl (1 -> 6)-O-beta-D-glucopyranoside (11), along with 10 known compounds 3,4-dihydroxyallylbenzene (2), 1,2-di-O-beta-D-glucopyranosy14-allylbenzene (3), tachioside (4), benzyl-O-beta-D-glucopyranoside (5), icariside F2(6), dihydrovomifolio1-3'-O-beta-D-glucopyranoside (7), isopropyl 0-6-o-glucopyranoside (8), isopropyl primeveroside (9), n-butyl O-beta-D-glucopyranoside (10), isoheptanol 2(S)-O-beta-D-apiofuranosyl-(1 -> 6)-O-beta-D-glucopyranoside (12), were isolated from the leaves of Piper retrofractum. Their structures were determined from 1D-NMR, 2D-NMR, and HR-ESI-MS spectral, a modified Masher's method, and comparisons with previous reports. All of the isolated compounds showed modest oc-glucosidase inhibitory (4.60 1.74% to 11.97 3.30%) and antioxidant activities under the tested conditions. (C) 2014 Elsevier Ltd. All rights reserved.