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Gardenia is a genus of about 140 different plant species of the Rubiaceae family. Previous studies have shown that terpenes and phenolics extracted from Gardenia sp. showed numerous potential bioactivities. In this study, the chemical constituents of G. angkorensis, their cytotoxic and αglucosidase inhibition activities were investigated. The phytochemical investigation of the dichloromethane extract of G. angkorensis leaves growing in Vietnam has led to the isolation of 19α-hydroxyoleanolic acid 3-Ο-β-D-glucuronopyranoside (1), chikusetsusaponin IVa, 3 β, 16 β, 21 β, 23, 24-pentahydroxy urs-12,18,20-trien-28-oic acid-γ-lactone (3), linalool glucoside and linalyl 6-O-α-L-arabinopyranosyl-β-D-glucopyranoside (5). The identities of the compounds were based on the analysis of their NMR data. Compound 1 showed moderate inhibition against αglucosidase with IC50 value of 58.01 ± 4.45 µM while compounds 3 (IC50 186.60 ± 4.68 µM) and 5 (IC50 239.53 ± 7.22 µM) exhibited weak cytotoxicity against the KB cell line and Hep G2 cell line (IC50 values 180.80 ± 7.16 µM, 253.95 ± 8.14 µM). [ABSTRACT FROM AUTHOR]