Two new compounds named dresigenin B and dresioside I were isolated from the root of Dregea sinensis Hemsl. Their structures were demonstrated as 20-O-(2-methylbutyryl) tomentogenin and dihydrosarcostin 3-O-beta-D-thevetopyranosyl (1-4)-beta-D-oleandropyranosyl (1-4)-beta-D-cymaropyranoside by spectral evidence.