hydroxysafflor-yellow-a and protocatechualdehyde

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.. 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.. 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 (t1/2) 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 (Cmax; p > 0.05).. 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.

Topics: Animals; Anticoagulants; Benzaldehydes; Cardiotonic Agents; Catechols; Chalcone; Drugs, Chinese Herbal; Hyperlipidemias; Lipids; Male; Quinones; Random Allocation; Rats; Rats, Sprague-Dawley

To study the pharmacokinetics-pharmacodynamics correlation of protocatechuic aldehyde and hydroxysafflor yellow A alone or their combination use in rats with hyperlipidemia. In this study, the hyperlipidemia model was established by intravenous injection of protocatechuic aldehyde (20 mg•kg⁻¹) and hydroxysafflor yellow A (12 mg•kg⁻¹). The HPLC-DAD method was applied to determine the plasma concentration of protocatechuic aldehyde and hydroxysafflor yellow A at different time points and draw the drug effect-time curve. Meanwhile, the platelet activating factors (PAF) and plasma a granule membrane protein (GMP-140) contents were determined at different time points to draw the time-effect curve. Then DAS 3.2.6 software was used to process the data, analyze their correlation, and compare the difference of pharmacokinetics and pharmacodynamics of protocatechuic aldehyde and hydroxysafflor yellow A in hyperlipidemia rats after alone or their combined application, so as to evaluate the effect of protocatechuic aldehyde and hydroxysafflor yellow A on hyperlipidemia rats. According to the result, the pharmacokinetics and pharmacodynamics process of protocatechuic aldehyde and hydroxysafflor yellow A in hyperlipidemia rats after alone or their combination were consistent to the three-compartment model. In model group, the plasma PAF and GMP-140 were significantly increased, and the PAF and GMP-140 in vivo contents were decreased in a certain time after treatment. The effects of protocatechuic aldehyde and hydroxysafflor yellow A against the pharmacodynamic action may be related with their level in vivo, and their plasma concentration was positively related to the PAF and GMP-140 contents. The pharmacodynamic indexes were better after the combined use of protocatechuic aldehyde and hydroxysafflor yellow A, with certain influence on each other in hyperlipidemia rats; at the same time, it also reflected the rationality of protocatechuic aldehyde and hydroxysafflor yellow A combined application.

Topics: Animals; Benzaldehydes; Catechols; Chalcone; Hyperlipidemias; Quinones; Rats

The application of near infrared (NIR) spectroscopy for on-line quantitative monitoring of alcohol precipitation of the Danhong injection was investigated. For the NIR measurements, two fiber optic probes designed to transmit NIR radiation through a 2mm path length flow cell were applied to collect spectra in real-time. Particle swarm optimization- (PSO-) based least square support vector machines (LS-SVM) and partial least squares (PLS) models were developed for quantitative analysis of the critical intermediate quality attributes: the soluble solid content (SSC) and concentrations of danshensu (DSS), protocatechuic aldehyde (PA), hydroxysafflor yellow A (HSYA) and salvianolic acid B (SAB). The optimal models were then used for on-line quantitative monitoring of alcohol precipitation. The results showed that the PSO-based LS-SVM with a radial basis function (RBF) kernel was slightly better than the conventional PLS method, even though both methods exhibited satisfactory fitting results and predictive abilities. In this study, successful models were built and applied on-line; these models proffer real-time data and instant feedback about alcohol precipitation.

Topics: Benzaldehydes; Benzofurans; Catechols; Chalcone; Chemical Precipitation; Drugs, Chinese Herbal; Ethanol; Lactates; Least-Squares Analysis; Microfluidic Analytical Techniques; Online Systems; Quinones; Spectroscopy, Near-Infrared; Support Vector Machine

We aimed to detect optimal ratio of cardioprotection-dependent absorbed bioactive compounds (ABCs) as quality control of guan-xin-er-hao (GXEH) formula extracted by various processings.. Ferulic acid (F), tanshinol (T), hydroxysafflor yellow A (A), protocatechualdehyde (P) and paeoniflorin (E) in GXEH formula and FTA in blood from rat with acute myocardial infarction (AMI) were first identified by HPLC-MS/MS, and FTAPE in GXEH formulae with various herbs, extraction times and extraction water volumes were then quantitated only by HPLC.. FTAPE in various GXEH were determined. FTA were selected as GXEH's ABCs. Ratios of FTA were determined, suggesting the high (1:6.1:15.6), medium (1:1.7:15.2) and low (1:0.2:15.3) ratios. Three FTA ratios and their parent formulae ratio-dependently reduced infarct size, myocardial apoptosis and caspase-3 activity.. There is the optimal ratio of F:T:A among various formulae, contributing to the best cardioprotection. This FTA ratio was developed as quality control of GXEH formula.

Topics: Animals; Apoptosis; Benzaldehydes; Benzoates; Bridged-Ring Compounds; Cardiotonic Agents; Caspase 3; Catechols; Chalcone; Chemistry, Pharmaceutical; Coumaric Acids; Drugs, Chinese Herbal; Ethnopharmacology; Glucosides; Male; Monoterpenes; Myocardial Infarction; Phytotherapy; Quality Control; Quinones; Rats; Rats, Sprague-Dawley

We have used microarray technology to detect the effect of Guanxin No.2 decoction on gene expression in different areas of the myocardial infarcted heart of rats.. Male Sprague-Dawley rats (180-200 g) were randomly divided into three groups: sham-operated; coronary artery ligation; and coronary artery ligation plus administration of Guanxin No.2 decoction (10.0 g raw materials/kg per day by gavage). The experiment was carried out on day seven after ligation.. We found that the gene expression using microarray technology showed many differences in the border infarcted left ventricular area compared with the remote noninfarcted left ventricular area after administration of Guanxin No.2 decoction.. Guanxin No.2 decoction has a long history in treating ischaemic cardiomyopathy in China, but the molecular mechanism has been unclear. In this study we found that some important genes may have contributed to the cardioprotective effect of Guanxin No.2 decoction.

Topics: Animals; Benzaldehydes; Benzoates; Benzofurans; Bridged-Ring Compounds; Cardiotonic Agents; Carthamus tinctorius; Catechols; Chalcone; Coumaric Acids; Dalbergia; Drugs, Chinese Herbal; Gene Expression; Gene Expression Profiling; Glucosides; Heart Ventricles; Hydroxybenzoates; Lactates; Ligusticum; Male; Monoterpenes; Myocardial Infarction; Oligonucleotide Array Sequence Analysis; Paeonia; Plant Extracts; Quinones; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Polymerase Chain Reaction; Salvia miltiorrhiza