Galloyl glucosidic constituents of Choerospondias axillaries and their in vitro anti-tumor, anti-hypoxia and anti-bacteria activities / 国际药学研究杂志

ABSTRACT

Objective To investigate gallic acid-derived chemical constituents of Choerospondias axillaries (Roxb.) Burtt. et Hill., and evaluate their in vitro anti-tumor, anti-hypoxia and anti-bacteria activities. Methods The aimed chemical constituents were isolated by various chromatographic means, and their structures were identified by physicochemical and spectroscopic data. MTT method was employed to evaluate anti-tumor and anti-hypoxia activities. Antibacterial activities were tested by paper disc method. Results Seven compounds 1-7 were isolated from the stem barks of Choerospondias axillaries (Roxb.) Burtt. et Hill. and identified as gallic acid(1), gallic acid ethyl ether(2), 1-O-galloyl-β-D-glucose(3), 1,6-di-O-galloyl-β-D-glucose(4), 1,4-di-O-galloyl-β-D-glucose(5), 1,4,6-tri-O-galloyl-β-D-glucose(6), and 1,3,4,6-tetra-O-galloyl-β-D-glucose(7). Compounds 1, 2 and 4-6 significantly inhibited K562 cells with the IC50 values of 2.9, 14.6, 39.1, 40.2, 41.2 μg/ml, respectively, and 3 and 7 also showed a slight inhibition of the K562 cells with the inhibition rate of 20.8% and 30.1% at 100 μg/ml respectively. Compounds 1-7 showed protective effects on anoxia-induced injury in cultured ECV304 and PC12 cells at the concentrations showing no significant cytotoxicity, and 5-7 also showed an antibacterial effect on Staphylococcus aureus ATCC6538 to a certain extent. Conclusion Compounds 2-7 were isolated from the genus Choerospondias for the first time. It was the first time to report 1-7 as anti-tumor and anti-hypoxia constituents of Choerospondias axillaries, and the anti-hypoxia activity for 1-7 was also recorded for the first time in the present study.