In addition to the plant sterols β-sitosterol and daucosterol, a new bisabolane-typed sesquiterpene glycoside and three bioactive compounds (artemetin, geniposide and 6β-hydroxygeniposide) were characterized from the whole plant ofBiebersteinia heterostemonendemic to the Tibetan area. The structure determination of the novel glycoside and identification of the known phytochemicals were accomplished by a combination of modern spectroscopic methods. Tests of all isolates for the antimicrobial activity indicated that the new sesquiterpene glycoside exhibited pronounced antibacterial activities againstBacillus subtilis, Staphylococcus aureusandPseudomonas sp.with MICs at 50, 50 and 70 μg/ml, respectively.