空心莲子草化学成分及抗癌活性研究

Constituents from Alternanthera philoxeroides and their antitumor activity

目的:研究空心莲子草Alternanthera philoxeroides正丁醇提取物的抗肿瘤活性成分。方法:以硅胶柱、凝胶柱色谱分离,制备HPLC纯化,采用MS,NMR等波谱方法以及酸水解进行结构鉴定,以MTT法测试石油醚、醋酸乙酯、正丁醇萃取物以及各化合物的细胞毒活性。结果:从正丁醇提取部位分离得到7个化合物:齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸苷(olean-olic acid 3-O-β-D-glucuropyranoside,1),齐墩果酸-28-O-β-D-吡喃葡萄糖苷(oleanolic acid 28-O-β-D-glucopyranoside,2),齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸苷-6′-O-甲酯(oleanolic acid 3-O-β-D-glucuronopyranoside-6′-O-methyl ester,3),竹节参苷IV a甲酯(chikusetsusaponin IV a methyl ester,4),常春藤皂苷元-3-O-β-D-吡喃葡萄糖醛酸苷-6′-O-甲酯(hederagenin 3-O-β-D-glucuro-nopyranoside-6′-O-methyl ester,5),4,5-二羟基布卢姆醇(4,5-dihydroblumenol,6),(6S,7E,9R)-6,9-dihydroxymegastigma-4,7-dien-3-one-9-O-β-D-glucopyranoside(7),化合物1在30 mg.L-1剂量时对Hela和L929抑制率分别为91.3%和92.9%。结论:化合物4,5,7首次从该属植物中分得,化合物1在30 mg.L-1剂量时对Hela和L929具有显著抑制活性。

Objective： To investigate antitumor constituents from n-butyl alcohol extract of Alternanthera philoxeroides. Method：The constituents were isolated with silica gel, gel permeation chromatography, and purified by HPLC. Their structures were elucidated by spectroscopy and acid hydrolysis. The antitumor effects of extracts and isolated compounds were tested by MTT method in vitro. Result： Seven compounds were isolated and elucidated as followings： oleanolic acid 3-O-β-D-glucuronopyranoside （1）, oleanolic acid 28-O-β-D-glucopyranoside （2）, oleanolic acid 3-O-β-D-glucuronopyranoside-6＇-O-methyl ester （ 3 ）, chikusetsusaponin Ⅳ a methyl ester （ 4 ）, hederagenin 3 -O-β-D-glucuronopyranoside- 6 ＇-O-methyl ester （ 5 ）, 4,5-dihydroblumenol （ 6 ）, 6S, 7E, 9R-6,9-dihydroxymegastigma-4,7-dien-3-one-9-O-β-D-glucopyranoside （7）. Compound 1 showed significant inhibitory effect against Hela and L929 with inhibitive ratios 91.3% and 92. 9% at 30 mg ·L^-1, respectively. Conclusion： Compounds 4, 5 and 7 were isolated from this genus for the first time. Compound 1 showed significant inhibitory effect against Hela and L929 at 30 mg ·L^-1.