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益母草(Leonurus japonicus Houtt)为唇型科(labiatae)益母草属(Leonurus)植物,主要分布于河南、河北、安徽等地。益母草为传统中药,其药用历史悠久,具有调经、活血调瘀、利尿消肿之功效的。为了进一步阐明益母草发挥其药理活性的药效物质基础,本课题对益母草的水溶性部分进行了系统的化学成分研究。益母草30%的乙醇/水提取物经大孔吸附树脂柱层析,用乙醇/水为流动相进行梯度洗脱,得到六个洗脱部分。本实验对其中15%与30%两个洗脱部分进行了系统的化学成分分离,采用了多种柱色谱手段分离得到41个单体化合物,并通过理化常数测定、光谱分析对分离得到的化合物进行了结构鉴定,其中8个为新化合物。这41个化合物包括：leonoside C (1*), leonoside D (2*), verbascoside (3), isoacteoside (4),2-(3,4-dihydroxyphenethy)-O-a-L-arabinopyranosyl-(1→2)-α-L-rh amnopyranosyl-(1→3)-6-O-β-D-glucopyranoside (5), lavandulifolioside (6), leonoside E (7*), cistanoside E (8), leonoside F (9*), tyrosol8-O-β-D-glucopyranoside (10), tyrosol (11), phenethyl O-a-L-arabinopyranosyl-(1→6)-β-D-glucopyranoside (12),2-(2-hydroxyethyl)-4-methoxybenzoic acid (13),3-hydroxyl-l-(4-hydroxy-3,5-dimethoxyphenyl)-1-propanone (14), vanillic acid (15), syringic acid (16), caffeic acid (17),4-hydroxy-2,6-dimethoxyphenol1-O-β-D-glucoside (18),2-(hydroxymethyl) phenol (19), coniferyl alcohol (20), vanillyl alcohol (21),4-formyl-2,6-dimethoxybenzoic acid (22), staphylionoside E (23), citroside A (24), blumenol A (25),9-hydroxymegastigma-4,7-dien-3-one-9-O-β-D-glucopyranoside (26),7α (H),10α-eudesm-4-en-3-one-2β,12-triol (27),7α (H)-eudesmane-4,11(12)-diene-3-one-2β-hydroxy-13-β-D-glucopyranoside (28*), leonurine (29), transtorine (30), N, N, N-trimethyl tryptophan (31), tryptophan (32), adenosine (33),3/4-feruloyl-4/3-syringic glucaric acid (34*),2/5-feruloyl-4/3-syringic glucaric acid (35*),2/5-syringic-4/3-feruloyl glucaric acid (36*), rutin (37),2,6-dimethoxybenzoquinone (38), chlorogenic acid (39),β-sitosterol (40), daucosterol (41)。在药理活性方面,本实验采用多种药理模型对益母草地上部分的各个提取物和单体进行了活性筛选。结果显示,30%的乙醇/水洗脱部分在剂量为50mg/kg时皮下注射给药对巴豆油致小鼠耳部炎症的抑制率为37.7%；95%乙醇/水洗脱部分对人肝癌细胞、人胃癌细胞、人肺腺癌细胞、人卵巢癌细胞具有细胞毒活性,ICso分别为33.44μg/mL,26.71μg/mL,20.76μg/mL,22.77μg/mL。化合物18在10.5M浓度水平对小鼠腹腔巨噬细胞NO的生成有一定的抑制作用,抑制率为40.0%；化合物1,3,7-9,11,18,23-27,35,37对D-Ga1N引起的肝细胞损伤有保护作用(在浓度1×10.5M时,细胞成活率为36～74%)；化合物8,37对ROT损伤的PC12细胞有保护作用(在浓度1×10-5M时,细胞成活率为107.67和109.04%)。