黔产钩藤茎、叶化学成分及抗肿瘤活性研究
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。目前对钩藤茎、叶的化学成分及生物活性方面的报道较少，为了明确钩藤茎、叶的物质基础，以及为该植物资源的合理开发与可持续利用提供科学依据。该文研究了钩藤茎、叶的化学成分及抗肿瘤活性的筛选。采用硅胶柱色谱、Sephadex LH-20及半制备 HPLC 等色谱技术进行分离纯化，根据理化性质和波谱数据鉴定化合物的结构；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），钩藤碱（6），异钩藤碱（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：化合物3和5对HEL细胞有抑制作用，IC50值分别为17.96 μg·mL-1和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。其中，化合物1, 8, 10, 16为首次从钩藤植物中分离得到，钩藤茎化学成分有一定的抗肿瘤活性。
Uncaria rhynchophylla contains large amounts of alkaloids and abounds in natural resources, which has the the function of heat-clearing for calming liver and wind-calming forcalming frightened. In this paper, the chemical constituents of stems and leaves from Uncaria rhynchophylla and their antitumor activities were studied. The extracts were isolated and purified by using silical gel, Sephadex LH-20, semi-HPLC, 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 Uncaria rhynchophylla as: 3,4,5-trimethoxyphenol (1), scutellarin (2), isohydrohydrogenine (3), dehydroramine (4), Vallesiachotamine (5), rhynchophylline (6), isorhynine (7). Twelve compounds were isolated and identified from leaves of Uncaria rhynchophylla as: octadecanol (8), -sitosterol (9), tridecanoicacid (10), 2-methyl-5,7-dihydroxy-chroone-7-O--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 showed that compound 3 and 5 inhibited the activities of HEL cell lines, IC50 values were 17.96 gmL-1 and 73.01 gmL-1. Compound 5 inhibited the activities of K562 cell lines, IC50 values were 16.45gmL-1. Compounds 1, 8, 10 and 16 were isolated from this plant for the first time. Some compounds from stems of Uncaria rhynchophylla have certain antitumor activities. Key words: Uncaria rhynchophylla, chemical constituents, isolation and purification, struct-ure identification, antitumor activity.
刘扬、王苗苗、 潘卫东、张妮、 罗俊
药学肿瘤学生物科学研究方法、生物科学研究技术
钩藤化学成分分离纯化结构鉴定抗肿瘤活性
刘扬,王苗苗, 潘卫东,张妮, 罗俊.黔产钩藤茎、叶化学成分及抗肿瘤活性研究[EB/OL].(2020-05-28)[2025-08-11].https://chinaxiv.org/abs/202005.00079.点此复制
评论