Bupleurum chinense is a plant of the Apiaceae family. Bupleurum is a primary ingredient an ancient Chinese medicinal formula known as Xiao Chai Hu Tang. The ingredients are: Bupleurum (root)16%; Paeonia lactiflora (peony root) 16%; Pinellia ternata (a rhizome) 14%; Zingiber officinale (ginger rhizome) 11%; Zizyphus jujuba var. inermis (jujube fruit) 11%; Panax ginseng (Asian ginseng root) 8%; Scutellaria baicalensis (Chinese skullcap root) 8%; Glycyrrhiza uralensis (licorice) 5%. A new megastigmane sesquiterpene glucoside named chaihuxinoside A (1), and a new indole diglucoside named chaihuxinoside B (9) were isolated from the aerial parts of Bupleurumchinense DC. along with eight known compounds. Chaihuxinosides A and B were characterized as 11-hydroxyl-4-en-3,9-dioxo- megastigmane-11-O-β-D-glucopyranoside (1), and 3-carboxy-indole-10-O-β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl ester (9), respectively.