Physicochemical properties Safflower yellow pigments are quinone chalketone compounds, which are A mixture of a variety of water-soluble components, mainly including safflower yellow pigment A (saffloryellowA), Safflower yellow pigment B (saffloryellowB), HSYA, AHSYB, etc., promoting blood circulation and removing blood stasis, promoting pulse and relieving pain. It is used for stable fatigue angina pectoris of grade I, II and III caused by blood blood stasis. The symptoms are chest pain, chest tightness, palpitation, shortness of breath, etc. The pharmacokinetic study showed that the blood concentration-time curve of rats with HSYA had a double-peak phenomenon, which speculated that HSYA degraded in the gastrointestinal tract and had bile effection effect. The oral absorption of HSYA was poor, and the maximum blood concentration (Cmax) was reached in 20-50min, and the absolute bioavailability (F) was 1.2%. The bioavailability of HSYA was improved after the combination of the compound. For example, the absorption of HSYA was slightly faster and the areaunderthecurve (AUC) was significantly increased during administration of safflower extract, suggesting that non-chalcone components in safflower extract affected the absorption of HSYA in safflower yellow pigment. The cmax, AUC0-T and AUC0-∞ of HSYA after intragastric administration of compound Naodesheng tablets were significantly higher than those of HSYA monomer group and safflower extract group. Pharmacological effects Safflower yellow pigment is extracted from Safflower, A traditional Chinese medicine, and consists of a mixture of water-soluble chalketone components. The main pharmacological active ingredient is hydroxyl Chemicalbook Safflower Yellow pigment A(HSYA), which has the effect of activating blood circulation, removing blood stasis and relieving pain. Modern pharmacological studies have shown that safflower yellow pigment has the effect of expanding microarteries, increasing tissue hemoperfusion flow and improving microcirculation. At the same time, it can resist platelet aggregation, reduce blood viscosity, anticoagulation, inhibit thrombosis, regulate blood lipids, remove harmful oxygen free radicals, prevent excessive cell oxidation and play an antioxidant role, which is suitable for coronary heart disease, vascular embolic diseases, hypertension, diabetes complications. The detection and structural identification of prototype drugs and their metabolites in the body are the basis of revealing the pharmacodynamic substances of traditional Chinese medicine. After injecting HSYA into rat tail vein, a total of 18 metabolites were detected, including 4 in plasma, 9 in urine and 5 in feces. Their metabolic reactions were mainly reduction, hydrolysis, methylation, deglycosylation, glucosylation and sulfonation. A total of 17 HSYA-related metabolites were identified in plasma and urine of rats after intragastric administration of safflower extract, including 6 in plasma and 11 in urine. In rats, HSYA is first hydrolyzed by glycoside bonds to provide glycoside ligands, and then further binds to glucuronic acid and/or sulfonyl groups to produce polyhydroxy-chalcone type and 4-hydroxy-cinnamic acid type phase II metabolites, of which polyhydroxy-chalcone type metabolites are more than 4-hydroxy-cinnamic acid type metabolites. In addition, LiJR et al. found that glutathione and sulfate conjugates could also be detected in bile after rats were given HSYA solution.
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