| Leonurus japonicus Houtt.(family labiatae) is distributed in Hebei, Henan, and Anhui Provinces of the People’s Republic of China. The dried aerial part of the plant is used as a tradtional Chinese Medicine for regulating menstrual disturbance, invigorating blood circulation, diuretics and dispel edema. In order to clarify the active substance from the Leonurus japonicus Houtt., we carried out the chemical investigation of high-polar fraction of the plant.The30%(Ⅴ/Ⅴ) extract of the plant was subjected to HP-20macroporous resin using a H2O-EtOH step gradient to give six fractions.15%and30%fractions were further subjected to column chromatography and preparative HPLC to yield41compounds, including8new compounds, were identified on the basis of the physical constants and spectroscopic analysis. The structures of these compounds were characterized as followings:leonoside C (1*), leonoside D (2*), verbascoside (3), isoacteoside (4),2-(3,4-dihydroxyphenethy)-O-a-L-arabinopyranosyl-(1→2)-α-L-rha mnopyranosyl-(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-α-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).Furthermore, bioacitivities of some fractions and compounds from Leonurus japonicus Houtt. were screened by various pharmaceutical models. The30%(Ⅴ/Ⅴ) extract of Leonurus japonicus Houtt. showed obvious anti-flammatory activity against croton oil-induced rat ear edema with a inhibitory rate of37.7%at50mg/kg;95%fraction showed selective cytotoxicities, with IC50values of33.44μg/mL against Bel-7402,26.71μg/mL against BGC-823,20.76μg/mL against A549and22.77μg/mL against A2780, respectively; compound18displayed inhibitory effects on nitric oxide production by macrophages stimulated with LPS, with inhibitory rate of40.0%, at a concentration of10-5M; compounds1,3,7-9,11,18,23-27,35and37showed hepatoprotective effects against D-galactosamine-induced toxicity in HL-7702Cells, with cell survival rates of36～74%at1×10-5M; compounds8and37exhibited protective effects of compounds against ROT-induced toxicity in PC12Cells with cell survival rates of107.67and109.04%at1×10-5M. |
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