ABSTRACT
ABSTRACT β-Glucuronidase inhibitors are suggested as potential hepatoprotective agents. Swertia chirayita (Roxb.) Buch.-Ham. ex C.B. Clarke, Gentianaceae, is known for its hepatoprotective and anti-hepatotoxic activity in Ayurvedic system of medicine for ages. This plant is substituted by other species like S. decussata Nimmo ex C.B. Clarke and S. bimaculata (Siebold & Zucc.) Hook. f. & Thomson ex C.B. Clarke. The aim of the study was to compare metabolite profile and β-glucuronidase inhibitory activity of these three important species of Swertia and to identify the active constituents. S. chirayita (IC50 210.97 µg/ml) and S. decussata (IC50 269.7 µg/ml) showed β-glucuronidase inhibitory activity significantly higher than that of silymarin, the known inhibitor of the enzyme. The activity of S. bimaculata was low. The metabolites present in the three species were analyzed by HPLC and GC-MS based metabolomics approach. Five amino acids, twenty one organic acids, one inorganic acid, eight fatty acids, twenty one phenols including xanthones, eight sugars, seven sugar alcohols, five terpenoids and amarogentin were identified. Activities of the xanthones mangiferin (IC50 16.06 µg/ml), swerchirin (IC50 162.84 µg/ml), decussatin (IC50 195.11 µg/ml), 1-hydroxy-3,5,8-trimethoxy xanthone (IC50 245.97 µg/ml), bellidifolin (IC50 390.26 µg/ml) were significantly higher than that of silymarin (IC50 794.62 µg/ml). Quinic acid (IC50 2.91 mg/ml), O-acetylsalicylic acid (IC50 48.4 mg/ml), citric acid (IC50 1.77 mg/ml), D-malic acid (IC50 14.82 mg/ml) and succinic acid (IC50 38.86 mg/ml) also inhibited the enzyme β-glucuronidase. The findings suggest that constituents, in addition to the xanthones, probably also contribute to the bioactivity of different Swertia species by synergistic effect. Further in vivo study is required to support the claim.