南板蓝根化学成分及其体外抗肿瘤活性研究

Chemical Constituents and In Vitro Antitumor Activities of Baphicacanthus cusia

目的研究药材南板蓝根的化学成分及其抗肿瘤活性。方法采用硅胶柱色谱法、葡聚糖凝胶柱色谱法、高效液相色谱法.等多种色谱手段进行分离纯化得到单体化合物,经核磁共振技术确定化合物的结构,并对化合物进行了抗肿瘤活性的筛选。结果从该药材乙醇提取物中分离鉴定了24个化合物,分别为3-羧基吲哚(1),吲哚-3-乙酸(2),吲哚-3-甲酯(3),色胺酮(4),老鼠簕碱A(5),2(3H)-苯并噁唑啉酮(6),白桦脂醇(7),山香酸A(8),2α-羟基齐墩果酸(9),β-香树脂醇(10),川陈皮素(11),橘皮素(12),胭木二酮(13),(+)-楝叶吴茱萸素B(14),两面针宁(15),(7'S,8'S)-双棱扁担杆素(16),(+)-南烛木树脂酚(17),(+)-丁香脂素(18),啤酒甾醇(19),β-胡萝卜苷(20),1-(4-羟基-3-甲氧基苯基)-3-羟基丙烷-1-酮(21),O-邻苯二甲酸二-(2-乙基癸)-酯(22),1-亚油酰甘油(23)和10,12-十八碳二烯酸-9-羟基甲酯(24)。对所有化合物进行了两种人类肿瘤细胞(HCT116和MGC803)增殖抑制活性的筛选,结果显示化合物3和4对胃癌细胞MGC803的增殖抑制活性的IC_(50)分别为5.53和4.26μmol·L^(-1);对结直肠癌细胞HCT116的增殖抑制活性的IC_(50)分别为23.96和18.86μmol·L^(-1)。结论化合物2,3,5,8~17,19和21~24为首次从该植物中分离得到;化合物3和4对MGC803细胞有较强的增殖抑制活性,对HCT116细胞有一定的增殖抑制活性。

OBJECTIVE To study the chemical constituents and antitumor activity of Baphicacanthus cusia(Nees) Bremek. METHODS The chemical constituents were isolated by column chromatography packed with silica gel, Sephadex LH-20 and HPLC, and the structures of the purified compounds were elucidated by NMR data analysis. RESULTS Twenty-four compounds, namely 3-carboxyindole(1), indole-3-acetic acid(2), methyl indol-3-ylacetate(3), tryptanthrin(4), acanthiline A(5), 2(3H)-benzoxazolinone(6), betulin(7), hyptatic acid-A(8), 2α-hydroxy oleanolic acid(9), β-amyrin(10), nobiletin(11), tangeretin(12), wrightiadione(13),(+)evofolin B(14), nitidanin(15),(7′S,8′S)-bilagrewin(16),(+)-lyoniresinol(17),(+)-syringaresinol(18), cerevisterol(19), β-daucosterol(20), 1-(4-hydroxy-3-methoxyphenyl)-3-hydroxypropan-1-one(21), O-phthalic acid bis-(2-ethyl decyl)-ester(22), 1-linoleoylglycerol(23) and 10,12-octadecadienoic acid-9-hydroxymethyl ester(24) were obtained from the ethanol extract of Baphicacanthus cusia(Nees) Bremek. All of the isolated compounds were screened for antiproliferative activities against two kinds of cancer cell lines(HCT116 and MGC803), and compounds 3 and 4 showed significant inhibitory activity against MGC803 with IC_(50) values of 5.55 and 4.16 μmol·L^(-1), respectively. Meanwhile, these two compounds also showed moderate inhibitory activity against HCT116 with IC50 values of 23.72 and 18.64 μmol·L^(-1), respectively. CONCLUSION Compounds 2,3,5,8-17,19 and 21-24 are isolated from this plant for the first time. Compounds 3 and 4 show significant inhibitory activity against MGC803 and moderate inhibitory activity against HCT116.