Studies On Chemical Constituents Of Traditional Chinese Medicine

Dioscorea nipponica Makino and Ophiopogon japonicus Ker-Gawl contain a large number of steroidal saponins which are important active component and possess significant bioactivities, such as cardio-cerebrovascular, anti-dementia, anti-tumor, anti-inflammatory and anti-fertility activities, etc. Steroidal saponins show favoura-ble officinal value and potential, so it’s necessary to take systematic research on the chemical constituents of the two kinds of traditional Chinese medicine. This paper contains four chapters.Chapter 1 ReviewWe took systematical review on plant resources, composition, pharmacological activity of Dioscorea nipponica Makino and Ophiopogon japonicus. So far,56 compounds from Dioscorea nipponica and 174 compounds from Ophiopogon japonicus were isolated and identified. We elaborated numbers of bioactivities of them. A total of 89 references were cited.Chapter 2 Chemical Constituents and their Activity Research of Dioscorea nipponica MakinoWe used SP825 macroporous adsorptive resins to make the 70% ethanol extract of Dioscorea nipponica Makino get coarse separation by 30%,55% and 85% ethanol. And 28 compounds were isolated by mainly using reversed-phase chromatography from the 55% ethanol fraction. The structures of 25 compounds were identified by using spectroscopic, chromatographic and chemical methods, such as high resolution mass spectrometry, nuclear magnetic resonance spectrum, acid hydrolysis and derivatization.15 of them are new compounds:Diosnipponicoside A-O (1-15); 5 known compounds isolated from genus Dioscorea for the first time (25R-Dracaenoside O,16; 25R-Dracaenoside P,17; anguiviosides XV,19; 3-O-[a-L-rhamnopyranosyl-(1→2)]-[β-D-glucopyranosyl-(1→3)]-β-D-glucopyranosyl 26-0-β-D-glucopyranosyl cholest-5-ene-16,22-dione,20; kushenol O,24),2 compounds were isolated from Dioscorea nipponica Makino for the first time (hypoglaucin G,18; (25R)-26-O-β-D- glucopyranosyl-furost-Δ5(6)-ene-3β 22a,26-triol-3-O-α-L-rhamnopyranosyl-(1→4)-β-D-glucopyranoside,23). After summarizing the chromatographic behaviors and fragmentation pathways of steroidal sapnins, rapid identification was carried out based on UPLC-Q-TOF MSE technology. We confirmed 19 refrencec standards and identified structures of 38 compounds, among them,20 might be the novel compounds and 6 pairs might be the isomers. Finally, we used MTT method to screen the antitumor activity of 12 new steroidal saponins. Inhibition ration of cancer cell (A549, BEL-7402, HCT-8) were all less than 20%, which showed furostanol saponins of Dioscorea nipponica Makino had no cytotoxicity on cancer cell.Chapter 3 Chemical Constituents Research of Ophiopogon japonicusFrom the 95% ethanol extract of Ophiopogon japonicus, by using various chromatographic, spectroscopic and chemical methods,25 compounds were isolated and identified. The compounds contained 6 steroidal saponins,7 phenylpropanoid glycosides,3 homoisoflavones,3 borneol glycosides,2 phenolic glycosides,2 alkaloids,1 cholesterin and 1 sesquiterpenoid glycoside. Among them, there were three new compounds:cryptomeridiol 11-O-β-D-xylopyranosyl-(1→6)-β-D-glucopy-ranoside (49),3,4-dihydroxy-allylbenzene 3-O-β-D-glucopyranosyl-4-O-β-D-apiofu-ranosyl-(1→6)β-D-glucopyranoside (26),3,4,5-trihydroxy-allylbenzene 3-O-β-D-glucopyranosyl-4-O-β-D-glucopyranoside (27) and 22 known compounds (9 compounds were isolated from genus Ophiopogon for the first time):3,4-dihydroxy-allylbenzene-3-O-β-D-glucopyranosyl-4-O-β-D-glucopyranoside, (28); 3,4-dihydroxy-allylbenzene-4-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyranoside, (29); 4-hydroxy-allylbenzene-4-O-β-D-glucopyranoside, (30); caffeic acid 3-O-β-D-glucopyranoside, (31); borneol 7-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyranoside, (43a);p-hydroxy phenylethyl-O-β-D-glucopyranoside, (44); Orcinol glucoside, (45); (3S)-1,2,3,4-Tetrahydro-β-carboline-3-carboxylic acid, (46);L-amygdaloside, (47).Chapter 4 Summary and DiscussionWe used kinds of methods to systematically investigate the chemical constituents of Dioscorea nipponica Makino and Ophiopogon japonicus and get new compounds, then we took a preliminary analysis on unknown steroidal sapnins by suing UPLC-MS. The innovation of this paper was discussed:we did research on high-polar fraction of Dioscorea nipponica Makino and got numbers of new compounds. Then we took rapid identification of unknown constituents by using UPLC-MS; A series of phenylpropanoid glycosides were isolated from the 95% ethanol extract of Ophiopogon japonicus,which include 2 new compounds and 4 known compounds isolated from genus Ophiopogon japonicus for the first time.The ongoing studies were summerized:More compounds in Dioscorea nipponica Makino could be isolated and their new activity should be screened. Phenylpropanoid glycosides in Ophiopogon japonicus needed to be further isolated, and screened.