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黑籽重楼化学成分及其抗肿瘤活性研究

Chemical constituents from Paris thibetica and their antitumor activities

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目的 研究黑籽重楼Paris thibetica根状茎的化学成分及其抗肿瘤活性.方法 综合运用正相硅胶、Sephadex LH-20、ODS-C18等柱色谱以及半制备高效液相色谱等方法进行分离纯化,并通过MS、1H-NMR、13C-NMR等波谱学方法进行结构鉴定.采用MTT法研究化合物的体外抗肿瘤活性.结果 从黑籽重楼根状茎的乙醇提取物中分离得到14个化合物,分别鉴定为重楼皂苷Ⅴ(1)、重楼皂苷Ⅰ(2)、重楼皂昔Ⅱ(3)、重楼皂苷Ⅵ(4)、偏诺皂苷元-3-O-α-L-呋喃阿拉伯糖基(1→4)-β-D-吡喃葡萄糖苷(5)、重楼皂苷H(6)、偏诺皂苷元-3-O-α-L-吡喃鼠李糖基(1→4)-[α-L-吡喃鼠李糖基(1→2)]-β-D-吡喃葡萄糖苷(7)、重楼皂苷Ⅶ (8)、parisyunnanoside G(9)、trikamsteroside E(10)、豆甾醇-3-O-β-D-吡喃葡萄糖(11)、β-谷甾醇棕榈酸酯(12)、β-香树脂醇(13)、4-羟基-5-甲基呋喃-3-羧酸(14).结论 所有化合物均为首次从黑籽重楼中分离得到,化合物10、12~14为首次从重楼属植物中分离得到.化合物1~8对人肝癌细胞BEL-7402有细胞毒活性,其中化合物3活性最好,IC50为0.48μmol/L.
Objective To investigatethe chemical constituents from Paris thibetica and their antitumor activities.Methods The separations and purifications were taken by column chromatography over silica gel,Sephadex LH-20,ODS-C18,and semi-preparative HPLC.The in vitro antitumor activities of the isolated compounds were studied by MTT method.Results Fourteen compounds were isolated from ethanol extract of the rhizomes ofP thibetica,which were identified as paris saponin Ⅴ (1),paris saponin Ⅰ (2),paris saponin Ⅱ (3),paris saponin Ⅵ (4),pennogennin-3-O-α-L-arabinofuranosyl-(1→4)-β-D-glucopyranoside (5),paris saponin H (6),pennogennin-3-O-α-L-rhamnopyranosyl-(1→4)-[α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranoside (7),paris saponin Ⅶ (8),parisyunnanoside G (9),trikamsteroside E (10),stigmasterol-3-O-β-D-glucopyranoside (11),β-sitosteryl palmitate (12),β-amyrin (13),and 4-hydroxy-5-methylfuran-3-carboxylic acid (14).Conclusion All compounds are furstly reported from P.thibetica,and this is the first report of compounds 10 and 12-14 from the genus Paris L.Compounds 1-8 show cytotoxicities against BEL-7402.Among the tested compounds,compound 3 exhibits the strongest cytotoxicity with IC50 value of 0.48 μmol/L.

Paris thibetica Franchsteroidal saponinsparis saponin Ⅰparis saponin Ⅱantitumor activities

景松松、王颖、李雪娇、李霞、黄璐琦、肖培根、高文远

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天津大学药物科学与技术学院现代药物传递及功能高效化重点实验室,天津300072

天津中医药大学中药学院,天津300193

中国中医科学院中药资源中心道地药材国家重点实验室培育基地,北京100700

中国医学科学院中国协和医科大学药用植物研究所,北京 100093

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黑籽重楼 甾体皂苷 重楼皂苷Ⅰ 重楼皂苷Ⅱ 抗肿瘤活性

国家自然科学基金资助项目国家自然科学基金资助项目国家自然科学基金资助项目

811734878137390481673535

2017

中草药
天津药物研究院,中国药学会

中草药

CSTPCDCSCD北大核心
影响因子:1.632
ISSN:0253-2670
年,卷(期):2017.48(6)
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