黔产钩藤茎、叶化学成分及抗肿瘤活性研究

Chemical constituents of stems and leaves from Uncaria rhynchophylla in Guizhou and their antitumor activities

关键词:  钩藤, 化学成分, 分离纯化, 结构鉴定, 抗肿瘤活性

Key words:  Uncaria rhynchophylla, chemical constituents, isolation and purification, structure identification, antitumor activity

摘要:

钩藤富含生物碱类成分且资源丰富,具有清热平肝、息风定惊等作用。为明确钩藤茎、叶的物质基础,该文采用硅胶柱色谱、Sephadex LH-20及半制备 HPLC 等色谱技术对其进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构,并采用 MTT 法对人白血病细胞株 K562、HEL 进行体外抗肿瘤活性筛选。从钩藤茎中分离得到7个化合物,分别鉴定为3,4,5-三甲氧基苯酚(1),东莨宕素(2),异去氢钩藤碱(3),去氢钩藤碱(4),Vallesiachotamine(5),异钩藤碱(6),钩藤碱(7)。从钩藤叶中分离得到12个化合物,分别鉴定为二十八烷醇(8),β-谷甾醇(9),三十烷酸(10),2-methyl-5,7-dihydroxy-chromone-7-O-β-D-glucopyranoside(11),齐墩果酸(12),槲皮素(13),常春藤苷元(14),山柰酚(15),(6R, 9R)-9-hydroxymegastigman-4-en-3-one(16),熊果酸(17),表儿茶素(18),大黄素甲醚(19)。结果表明:(1)化合物3、5对HEL细胞有抑制作用,IC₅₀值分别为17.96、73.01 μg·mL^-1; 化合物5对K562细胞有抑制作用,IC₅₀值为16.45 μg·mL^-1,表明钩藤茎化学成分有一定的抗肿瘤活性。(2)化合物1, 8, 10, 16均为首次从钩藤植物中分离得到。该研究可为钩藤植物资源的合理开发与可持续利用提供科学依据。

Abstract:

Uncaria rhynchophylla contains large amount of alkaloids and abounds in natural resources, and has the function of heat-clearing for calming liver and wind-calming for calming frightened. In order to make clear the material basis of stems and leaves of U. rhynchophlla, in this paper, the chemical constituents of stems and leaves from U. rhynchophylla and their antitumor activities were studied. The extracts were isolated and purified by using silical gel, Sephadex LH-20, semi-HPLC, and the structures of the compounds were identified by physicochemical property and spectrum analysis. The antitumor activities of chemical constituents against K562, HEL cell lines were assessed by MTT method. Seven compounds were isolated and identified from stems of U. rhynchophylla as 3, 4, 5-trimethoxyphenol(1),scutellarin(2), isohydrohydrogenine(3), dehydroramine(4), Vallesiachotamine(5), isorhynchophylline(6), rhynchophylline(7). Twelve compounds were isolated and identified from leaves of U. rhynchophylla as octadecanol(8), β-sitosterol(9), tridecanoicacid(10), 2-methyl-5,7-dihydroxy-chroone-7-O-β-D-glucopyranoside(11), oleanolic acid(12), quercetin(13), ivy aglycone(14), kaempferol(15),(6R, 9R )-9-hydroxymegastigman-4-en-3-one(16), ursolic(17), epicatechin(18), emodin methylether(19). The results of antitumor activities were as follows:(1)Compounds 3 and 5 inhibited the activities of HEL cell lines, and IC₅₀ values were 17.96 and 73.01 μg·mL^-1; Compound 5 inhibited the activities of K562 cell lines, and IC₅₀ values were 16.45 μg·mL^-1, which indicate that some compounds from stems of U. rhynchophylla have certain antitumor activities.(2)Compounds 1, 8,10 and 16 were isolated from this plant for the first time. This study shed the scientific light on reasonable utilization and sustainable development of plant resources.