Studies On Anti-tumor Metastatic Constituents From Ardisia Crenata

Ardisia Crenata Sins. f hortensis (Migo) is the variant of A. Crenata Sins. in family of Myrsinaceae, which is widely distributed in the east and southeast of China. As a Chinese folk medicine, it has been used in preventing sore throat, bruises in clinic. It also has the properties of anti-HIV, anti-tumor, anti-fertility and so on.In order to search for new bioactive constituents from natural source, the 95% ethanol extract of Ardisia Crenata revealed significant anti-tumor metastasis effect in MDA-MB-231 cell lines. The metastatic inhibition ratio of value on MDA-MB-231 was 92.5% at the concentration of 1.0μg/ml. We started to study the anti-tumor metastatic chemical consitituents from Ardisia Crenata. By repeated column chromatography, including Silica gel, Toyopearl HW-40 and preparative HPLC, nine compounds were isolated from extract of A. Crenata. By analysis of MS,'H-NMR, 13C-NMR,1H-1H COSY, HMBC and HSQC spectra, the structures of nine compounds were identified as follows:Asperuloside acid (1), ardisiacrispins B (2), (+)-Bergenin (3), n-butyl-a-D-fructofuranoside (4), n-butyl-β-D-fructofuranoside (5), methyl-a-D-fructofuranoside (6), Syringic acid (7), ethyl-β-D-fructopyranoside (8),5-hydroxymethyl-2-furalclehyde (9). Compounds 1 and 4～9 were isolated from A. Crenata for the first time.MTT was used to determine the non-cytotoxic concentrations for the extract and isolated compounds. Then transwell chemotaxis was used to evaluating the role of inhibition of tumor cell migration. Compounds 1-9 showed positive anti-tumor cell migration effects, and compounds 2,4, and 9 showed significant anti-tumor cell migration effects. The metastatic inhibition ratio of value on MDA-MB-231 was 93.8% at the concentration of 0.8μg/ml of compound 4. The above result indicated that the active compounds may be have potentical anti-tumor metastatic effect.