南酸枣的黄烷类成分及其体外抗肿瘤与抗缺氧活性

目的 阐明南酸枣Choerospondias axillaries (Roxb.) Burtt. et Hill.树皮中黄烷类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，根据理化性质和波谱数据鉴定结构，利用MTT法测评抗肿瘤及抗缺氧活性，采用纸片法测定抗菌活性。结果 从南酸枣树皮中分离鉴定了3个黄烷类化合物 (+)-儿茶素（1）、(+)-儿茶素-7-O-β-D-吡喃葡萄糖苷（2）和 (+)-儿茶素-4’-O-β-D-吡喃葡萄糖苷（3）。化合物1、2 对K562细胞呈一定的抗肿瘤活性，在100.mL^-1质量浓度下的抑制率分别为16.0%和27.3%。在ECV304细胞缺氧损伤保护实验中，化合物1在无细胞毒作用的50 μg.mL^-1质量浓度下呈较强的抗缺氧活性，化合物3未表现出抗肿瘤与抗缺氧活性。化合物1~3在测试浓度下对受试白色念珠菌和金黄色葡萄球菌无抗菌活性。结论 化合物1为南酸枣抗缺氧活性成分的首例报道，其抗缺氧活性也属首次报道。化合物2和3为首次从该属植物中分离得到。

Flavanoidal constituents of Choerospondias axillaries and their in vitro antitumor and anti-hypoxia activities

Aim To investigate flavanoidal constituents of Choerospondias axillaries and their antitumor, anti-hypoxia and anti-bacteria activities. Methods Various chromatographic means were used to obtain pure compounds from the alcoholic extract of Choerospondias axillaries (Roxb.) Burtt. et Hill. Structures of the compounds obtained were investigated by modern spectroscopic methods. MTT method was employed to evaluate their antitumor and anti-hypoxia activities. Antibacterial activities were tested by paper disc method. Results Three flavanoidal compounds 1–3 were isolated from the stem barks of Choerospondias axillaries and they were identified as (+)-catechin (1), (+)-catechin-7-O-β-D-glucopyranoside (2) and (+)-catechin-4’-O-β-D-glucopyranoside (3). Compounds 1 and 2 inhibited the proliferation of K562 cells with the inhibition rates of 16.0% and 27.3% at 100 μg.mL^-1 , respectively. Compound 1 also showed anti-hypoxia effect at lower concentration (50 μg.mL^-1) without showing cytotoxicity on anoxic ECV304 cells. Compounds 1–3 showed no antibacterial effect on Candida albicans ATCC10231 and Staphylococcus aureus ATCC6538 at their concentrations tested each. Conclusions Compound 1 is the first reported anti-hypoxia constituent of Choerospondias axillaries and its anti-hypoxia activity was also assayed for the first time. Compounds 2, 3 were isolated from the genus Choerospondias for the first time.