Studies On The Active Constituents From Stellaria Media (L.) Cyr

Stellaria media (L.) Cyr. belongs to Stellaria L. genus (Caryophyllaceae). As a Chinese folk herb medicine, the whole herb possesses the functions of heat-clearing and detoxicating, promoting blood circulation to arrest pain, detumescence, etc. It is used for dysentery, ulcerative carbuncle, mammary abscess, periappendicular abscess, injury from fall and celiodynia after parturition. It is used as the folk antihyperlipidemic medicine in Guizhou province. No researches had been reported on the antihyperlipidemic activity and bioactive constituents of the plant. To provide scientific theoretical evidence for Stellaria media (L.) Cyr. using as antihyperlipidemic medicine, the pharmacological action of antihyperlipidemic and chemical constituents of this plant were investigated in this thesis .The hypercholesterolemia SD rats were experimented to observe the antilipidemic effect of the glycosylflavones (FL) obtained from Stellaria media (L.) Cyr.. FL in the high dose could reduce triglyeride and total cholesterol very remarkably, comparing to the model group. The result showed that FL possessed antihyperlipidemic activity, suggesting that Stellaria media (L.) Cyr. possessed antihyperlipidemic effects.Compound l¹0 were isolated from the 70% EtOH extract of Stellaria media (L.) Cyr., using various column chromatography and semi-preparative HPLC. The structures of the compounds obtained were determined by modern spectroscopic methods (IR, UV, ¹H-NMR, ¹³C-NMR, HMBC, ESI-MS). 1-7 were obtained form Stellaria L. genus for the first time.A HPLC method had been set up for qualitative and quantitative analysis of the main flavone glycosides of Stellaria media (L.) Cyr., using a 35% aqueors MeOH (including 0.01% AcOH), a flow rate of 1mL/min and UV absorbance at 335 nm. The column temperatrure was maintained at 25°C. The regress equations for both of the compounds were Y=3.12×10^-5X+5.47 (r = 0.999703) and Y=2.11×10^-5X+9.31 (r =0.999487), respectively. This method was good reproducible, easy to carry out and sensitive. The average contents of compound 1,2 in FL are 12.05%, 11.31%, respectively. RSD are 2.23%, 3.62%, respectively.In conclusion, it is proved that FL possessed antihyperlipidemic activity, using the hypercholesterolemia SD rats model, which provides the modern pharmacological support for Stellaria media (L.) Cyr as a folk herb medicine, and provided good bases for its further R& D. Ten compounds were isolated from 70% EtOH extract. The structures of nine of these compounds were determined by spectral analysis. Compounds 1～5, 10, whose aglycones are all apigenins, were isolated from the active site (FL). These flavones, which may be the effective active components for antihyperlipidemic from the active site of Stellaria media (L.) Cyr., may be developed as drugs or as the lead compounds. The flavone C-glycosides are more difficult to be metabolized to aglycones than O-glycosides, which shows that these compounds may produce a marked effect as original forms of the other metabolizions, instead of aglycones. So it may have an important significance for the research of the pharmacokinetics of these compounds.