Pharmacokinetic Study on Protocatechuic Aldehyde and Hydroxysafflor Yellow A of Danhong Injection in Rats with Hyperlipidemia

Abstract

Background: Protocatechuic aldehyde (PAL) and hydroxysafflor yellow A (HSYA) are 2 effective ingredients of Danhong Injection, which is extensively used for the clinical treatment of cardio-cerebrovascular diseases. This study aims to investigate the pharmacokinetic differences between single and combined medication of PAL and HSYA and analyze the interaction of the above effective components in hyperlipidemia rats. Methods: Thirty male SD rats were randomly divided into the control group (n = 6) and the model group (n = 24). The hyperlipidemia model was established by feeding with superfatted forage. The successful model rats were then randomly divided into the PAL group (16 mg/kg), the HSYA group (10 mg/kg), and the combination group (16 mg/kg + 10 mg/kg). Administration through tail-vein, and orbital blood was sampled at different time points. The mass concentration of PAL and HSYA was determined by high performance liquid chromatography (HPLC-DAD). Analysis of pharmacokinetic parameters was conducted by using DAS 3.2.6 software and SPSS 19.0 statistical analysis software. Results: According to the parameters of statistical moment of non-compartmental model, there was a significant difference in plasma clearance (CL) between the PAL group and the drug combination group (p < 0.01), as well as in the area under the first moment of the plasma concentration-time curve and the elimination half-life (t_1/2) between the HSYA group and the drug combination group (p < 0.01) but no obvious differences about the blood concentration time curve area, the average dwell time (MRT), and the peak concentration (C_max; p > 0.05). Conclusion: The combined medication of PAL and HSYA could increase the plasma CL significantly and have a great influence on the absorption of HSYA in rats with hyperlipidemia.

Hydroxysafflor Yellow A Together with Blood–Brain Barrier Regulator Lexiscan for Cerebral Ischemia Reperfusion Injury Treatment

“…To further verify the above results, the HPLC was used to detect changes in the content of HSYA in vivo , especially in the brain. 38 The HSYA concentrations in the brain tissue and serum of different groups after administration were detected. The HPLC curves are shown in Figure 5 D,E, and the quantitative analysis is shown in Figure 5 F,G.…”

Gastric floating tablet improves the bioavailability and reduces the hypokalemia effect of gossypol in vivo

“…The pharmacokinetic parameters were determined using the DAS 2.0 software (Chinese Pharmacological Society, China) based on non-compartmental methods ( Liu et al, 2015 , Zhou et al, 2018 ). The analysis of other data was carried out with the Prism 5 software (GraphPad, USA), using Student's t -test for comparison between two groups and one-way ANOVA for comparison among multiple groups ( Liu et al, 2019a , Liu et al, 2020 ).…”

Hydroxysafflor Yellow A Alters Fuel Selection From Glucose to Fat by Activating the PPARδ Pathway in Myocytes

“…For instance, Epigallocatechin gallate promoted glycogen accumulation in skeletal muscle; (−)-Epigallocatechin-3-gallate enhanced the expression of genes related to fat oxidation in the skeletal muscle; Anthocyanins and procyanidins from elderberries increase the oleic acid uptake in human skeletal muscle cells. − Safflower ( Carthamus tinctorius L.), one of the most widely used traditional Chinese herbs all over East Asia, has been widely used as a source of yellow and red dyes for pharmaceuticals and natural food colorants due to its high flavonoid contents. Among these, hydroxysafflor yellow A (HSYA) is the most abundant flavonoid and the cardinal active ingredient in safflower, which has been demonstrated to exhibit many beneficial effects in metabolic diseases with respect to diabetes, obesity, hyperlipidemia, osteoporosis, and so on. − The effects of HSYA on skeletal muscle are rarely reported, and according to our previous study, HSYA could trigger a fast-to-slow myofiber type shift in myocytes. However, the effect of safflower and HSYA in skeletal muscle fuel selection and the underlying mechanism remain unknown.…”