| Safflower (Carthamus tinctorius L.) belongs to the family Compositae and is widely distributed in the Xinjiang Uygur Autonomous Region, Zhejiang, Henan, and Sichuan province of China. The flowers of this plant are used as a remedy for dysmenorrheal, wound, coronary disease, angina pectoris, and hypertension in Chinese folk medicine. Various bioactives of Safflower have been confirmed by modern pharmacology, especially the cadiovascular bioactivities. Now, hydroxysafflor yellow A as a main constituents of safflower are in Clinical Trials. Because this compound has an especial frame of quinochalcone, they have been paid more attentions gradually. The purpose of this dissertation was to study constituents of safflower systematically. Furthermore, the emphasis was to study quinochalcone glycosides so as to elucidate the relationship between the quino-structure and their bioactivity.In the course of our study, 46 compounds were isolated and identified by chromatograms (silica gel, ODS, sephadex LH-20 and HPLC et al) and spectroscopic (IR, UV, MS, 1D-NMR and 2D-NMR) methods, of which 8 compounds were new, which were as follows: saffloquinoside A (1*), saffloquinoside B (2*), saffloquinoside C (3*), saffloquinoside D (4*), saffloquinoside E (5*), safflospermidine A (11*), safflospermidine B (12*), 2Z-decaene-4,6-diyn-1-O-β-D-glucopyranoside (46*), the others were known compounds, including safflomin C (6), safflor yellow A (7), cartormin (8), hydroxysafflor yellow A (9), anhydrosafflor yellow B (10), N1,N5,N10-(Z)-tri-p-coumaroylspermidine (13), N1,N5,N10-(E)-tri-p-coumaroylspermidine (14), 6-hydroxy kaempferol 3,6-di-O-β-D-glucoside-7-O-β-D-glucuronide (15), 6-hydroxykaempferol 3-β-rutinoside-6-β-D-glucoside (16), 6-hydroxykaempferol 3-β-rutinoside (17), 6-hydroxy kaempferol 3,6-di-O-β-D-glucoside (18), 6-hydroxykaempferol 3-O-β-D-glucoside (19), kaempferol 3-O-β-sophoroside (20), kaempferol 3-β-rutinoside (21), kaempferol 3-O-β- D-glucoside (22), kaempferol (23), quercetin 3-O-β-rutinoside (24), quercetin 3-O-β-D-glucoside (25), quercetin (26), 6-hydroxyapigenin (27), apigenin (28), neocarthamin (29), safflochalconeside (30), uridine (31), adenosine (32), 7,8-dimethyl pyrazino[2,3-g]quinazolin-2,4-(1H,3H)- dione (33), adenine (34), thymine (35), uracil (36), p-coumaric acid (37), p-hydroxybenzoic acid (38), succinic acid (39), 4-O-β-D-glucopyranosyloxy-benzoic acid (40), fat acid (41), sitosterol (42), daucosterol (43), dihydrophaseic acid 3-O-β-D-glucopyranoside (44), roseoside (45). Among all of these 46 compounds, 10 compounds were quinochalcone glycosides, whereas 5 were new compounds. The structrue of 1 were comprised by ketose and a quinocycle, and they were fused as five-member dioxaspirocycle, while 2 and 4 included cyclohexatrione. The novel structures of 1, 2, and 4 have enriched new frameworks of quinochalcone glycosides. In addition, the spectral characteristic of NMR and the sorts of quinocycle segment of quinochalcone glycosides were summarized.Extracts evaluating in vitro: The petroleum ether layer, EtOAc layer, and water layer of ethanol extract and water extract were tested in vitro with antithrombotic methods. The petroleum ether, and water layer of ethanol extract and water extract exhibited antithrombotic activities. At the same time, the 5%, 30%, and 50% ethanol eluates of water extract in chromatographing over porous polymer column were evaluated in vitro with hepatoprotection, antioxidant, and cyteprotection model, the results exhibited no activities. But the 5% and 30% parts of ethanol eluates showed activities by evaluating in vitro with antiplatelet aggregate model.Compound evaluating in vitro: Compound 3*, 4*, 11*, 12*, 13, and 14 were evaluated in vitro to study the effect on releasing of TNFαof mice peritoneal macrophage and the result exhibited no antiinflammatory activities of these compounds; Compound 3*, 4*, 12*, 13, and 14 were evaluated in vitro using HCT-8, Bel-7402, BGC-823, A-549, and A2780 model and the results exhibited no anti-tumor activities; Compound 1* and 9 were evaluated in vitro and exhibited no cadiovascular activities; Compound 1*, 2*, 3*, 4*, 7, 8, 9, and 10 were evaluated in vitro and the results exhibited no hepatoprotection, and antioxidant activities; Compound 1*, 4*, 7, 8, 11*, and 12* were evaluated in vitro and the results exhibited no antivirus activities; Compound 1*, 2*, 3*, 4*, 5*, 6, 7, 8, 9, and 10 were evaluated in vitro and the results exhibited no cyteprotection activities; Compound 1*, 2*, 3*, 4*, 5*, 6, 7, 8, 9, 10, and 30 were evaluated in vitro and the results exhibited that compound 1*, 2*, and 4* have antiplatelet aggregate activities; Compound 1*, 2*, 3*, 4*, 7, 8, 9, and 10 were evaluated in vitro to study the inhibitory effect on releasing ofβ-glucuronidase from rat PMNs induced by PAF, and the results showed compound 2* and 8 exhibiting good antiinflammatory activities and the inhibitory rates were 54.3% (10-5mol/L) and 63.4% (10-5mol/L), respectively.
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