Hemiphragma heterophyllum Wall. is commonly used in traditional Yi herbal medicine for treating bellyache and toothache. In the current study, an unreported monoterpene glucoside, ( S )-thymoquinol O -(6- O -oleuropeoyl)- β -d-glucopyranoside ( 1 ), together with 11 known glucosides were obtained from the whole herb of H. heterophyllum . Their structures were determined based on a detailed analysis of spectroscopic data and acid hydrolysis and methanolysis reactions. Bioassay results showed that compounds 1 and 10 at 40 mg/kg exhibited significant antinociceptive activity in the acetic acid-induced writhing model, with inhibitions of 59.80% and 64.07%, respectively. Moreover, five of the isolates showed moderate anti- α -glucosidase activities with IC 50 values ranging from 5.67 to 46.16 μM.