南酸枣中没食子酰葡萄糖苷类化学成分及其体外抗肿瘤抗缺氧抗菌活性

Galloyl glucosidic constituents of Choerospondias axillaries and their in vitroanti-tumor,anti-hypoxia and anti-bacteria activities

目的：阐明南酸枣中没食子酸衍生物类化学成分及其体外抗肿瘤、抗缺氧、抗菌活性。方法利用各种色谱技术分离化学成分，根据理化性质和光谱数据鉴定结构，利用MTT法测评抗肿瘤与抗缺氧活性，用纸片法测定抗菌活性。结果从南酸枣树皮中分离鉴定了没食子酸（1）、没食子酸乙酯（2）、1-O-没食子酰基-β-D-吡喃葡萄糖（3）、1，6-二-O-没食子酰基-β-D-吡喃葡萄糖（4）、1，4-二-O-没食子酰基-β-D-吡喃葡萄糖（5）、1，4，6-三-O-没食子酰基-β-D-吡喃葡萄糖（6）、1，3，4，6-四-O-没食子酰基-β-D-吡喃葡萄糖（7）等7个没食子酸衍生物类化合物。化合物1、2、4～6对K562细胞呈较强抗肿瘤活性，IC50分别为2.9、14.6、39.1、40.2和41.2μg /ml；化合物3和7活性较弱，在100μg /ml浓度下对K562细胞的抑制率分别为20.8%和30.1%。在对ECV304和PC12细胞的缺氧损伤保护实验中，1～7在无明显细胞毒作用的浓度下呈较强的抗缺氧活性。化合物5～7还对受试金黄色葡萄球菌显示一定的抗菌活性。结论化合物2～7为首次从南酸枣属植物分离得到。化合物1～7作为南酸枣中抗肿瘤、抗缺氧活性成分系首次报道，其抗缺氧活性也属首次报道。

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.