| Safflower injection is a traditional Chinese patent medicine prepared from thecrude drug safflower. It has the functions of activating and promoting blood circulation, and is commonly used for treatment of coronary heart disease, angiitis, cerebral vascular occlusive diseases. It has a therapeutic effect for cardiovascular diseases in clinical use. Most of studies are more focused on the fields of pharmacology, toxicology, clinical use, but there is little definite bioactive component aboutit. Previous study showed that flavonoids and safflower yellow were the effectivecomponents that cured the diseases, so it was necessary that we should pay muchmore attention to the bioactive components.Referred to previous research results, we adopted various modern analyticalmethods (polyamide, Sephadex LH-20, ODS, HPLC and LC-MSnetc.), and we choosed proper pharmacological models those were linked with its functions to uncover the compounds that showed anti-platelet aggregation activities. As the contentof safflower yellow parts was little, unstable and couldn’t be separated easily. Thecharacteristic chromatogram of safflower pigments was established by us, and weidentified four chromatographic peaks. Based on the results of anti-platelet aggregation activities of the isolated compounds, a high performance liquid chromatography method was established. The main results were listed as followed:1. The chemical constituents of Safflower injection were isolated and purified.As a result, sixteen compounds were isolated. Based on the spectral data analysis,their structures were elucidated as scutellarin (1), kaempferol-3-O-β-rutinoside (2),hydroxysafflor yellow A (3), rutin (4), coumalic acid (5), adenosine (6), syringoside (7),(3E)-4-(4’-hydroxyphenyl)-3-buten-2-one (8),(8Z)-decaene-4,6-diyne-1-O-β-D-glucopyranoside (9),4-hydroxybenzaldehyde (10),(2E，8E)-tetradecadiene-4,6-diyne-1,12,14-triol-1-O-β-D-glucopyranoside (11), kaem-pferol-3-O-β-sophorose(12),uridine (13), roseoside (14), cinnamic acid (15), and kaempferol (16). And compounds1,2,7,9,11and12were isolated from the Safflower injection for the first time.2. The anti-platelet aggregation activities of the isolated compounds were assayed. The results indicated that all the tested compounds exhibited potent activity e xcept for5, while2,3,9and12showed strong activity against platelet aggregation.3. Based on the present quality standards, we pretreated the Safflower injection first and imported Safflower injection chromatograms into the Chinese medicine chromatographic fingerprint evaluation system (national pharmacopoeia committee,2010edition). The characteristic chromatogram of safflower pigments was established, there were13common peaks in the chromatographic picture. Through LC-MS analysis online, we identified the structures of four compounds and elucidated the cracking ways. By analyzing the data from fingerprint of Safflower injection,we could draw the conclusion that this method could successfully assess the quality of Safflower injection, the characteristic chromatogram estalibished could give us a preliminary understanding of quinochalcone in Safflower injection, and it could be a method to evaluate the quality of Safflower injection.4. Based on the results of anti-platelet aggregation activities of the isolated compounds, a high performance liquid chromatography method was established to evaluate the quality of Safflower injection through a simultaneous quantitation of three compounds, hydroxysafflor yellow A, syringoside,(8Z)-decaene-4,6-diyne-1-O-β-D-glucopyranoside, and this method was applied to quantify the compounds in9batches of Safflower injection from the same factory. We found that there were no variations between batches, which indicated that the production process was relatively stable. Compared with the method that quantify the content of hydroxysafflor yellow A only, this method could provide a basis for overall assessment on quality of Safflower injection. |
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