| Steroidal saponins are important components with biological activities in natural plants. The contents are richer in the diascoreaceae plant. The modern Pharmacology research indicated that the steroid saponins compounds have various activities of anti-tumor, anti- platelet aggregation, conquer blood pressure, immunity and so on. So this kind of components has highly potential medical composes and the development value.Dioscorea nipponica Makino is a kind of traditional Chinese medicine. There are plenty of diosgenin series compounds which are important source to make the steroid hormone raw material in the plant. In order to find out antithrombotic leading compounds, we carried out system's studies of chemical compositions. We have obtained 9 monomer compounds from the n-butyl alcohol spot of the D. nipponica Makino rhizome with the methods of the silica gel, the preparation thin layer, half preparation HPLC, and so on. Based on the data of MS, NMR, 9 steroid saponins were identified as follows : gracillin (1) , dioscin (2) , pseudoprotodioscin (3) , diosgenin (4) , diosgenin 3-O-β-D-glucopyranoside (5) , diosgenin 3-O-[α-L- rhamnopyranosyl(1→2)]-β-D-glucopyranoside (6) , diosgenin 3-O-[α-L-rhamnopyr anosyl (1→4) ]-β-D-glucopyranoside (7) , 26-O-β-D-glucopyranosyl-3→,26-diol- 25(R) -Δ5,20(22)-diene-furosta-3-O-[α-L-rhamnopyranosyl(1→2)]-β-D- glucopyranoside (8) , 26-O-→-D-glucopyranosyl-3→,26-diol-25(R)-Δ5,20(22)-diene- furosta-3-O- [α-L-rhamnopyranosyl (1→4)]-β-D-glucopyranoside (9) .Through the pharmacology experiment, we appraised the antithrombotic activity and analysed the structure-activity relationship of partial compounds. The results indicate that 2 and 5 have some activity. The antithrombotic activity is affected by spirostane aglycon and substitution of 3-OH. On the ground of the results ,we designed and synthesized two diosgenin monosugar derivatives : diosgenin 3-O-β-D-galactopyranoside (10) , diosgenin 3-O-β-L-rhamnopyranoside (11) . |
PDF Full Text Request