peoniflorin and puerarin

Dan-Lou tablet (DLT) is developed from the traditional Chinese medicine (TCM) formula Gualou Xiebai Baijiu Tang which has been used for at least 2000 years in China. DLT has been widely used in clinical practice to treat cardiovascular diseases.. This study aimed to uncover the pharmacological mechanism of the compounds absorbed into the blood of Dan-Lou tablet (DLT) on coronary heart disease (CHD) using a network pharmacology integrated pharmacokinetics strategy.. A rapid and sensitive method was developed for the simultaneous determination of the six compounds (puerarin, formononetin, calycosin, paeoniflorin, cryptotanshinone and tanshinone IIA) in rat plasma by liquid chromatography tandem mass spectrometry (LC-MS/MS). Then, the pharmacology network was established based on the relationship between five compounds absorbed into the blood targets (puerarin, formononetin, calycosin, cryptotanshinone and tanshinone IIA) and CHD targets.. The intra-and inter-day precision were less than 11% and the accuracy ranged from 88.2% to 112%, which demonstrated that the LC-MS/MS method could be used to evaluate the pharmacokinetic feature of the six compounds in rats after oral administration of DLT. The pathway enrichment analysis revealed that the significant bioprocess networks of DLT on CHD were positive regulation of estradiol secretion, negative regulation of transcription from RNA polymerase II promoter, lipopolysaccharide-mediated signaling pathway and cytokine activity.. The proposed network pharmacology integrated pharmacokinetics strategy provides a combination method to explore the therapeutic mechanism of the compounds absorbed into the blood of multi-component drugs on a systematic level.

Topics: Abietanes; Administration, Oral; Animals; Chromatography, Liquid; Coronary Disease; Drugs, Chinese Herbal; Glucosides; Isoflavones; Male; Monoterpenes; Myocardium; Pharmacology; Phenanthrenes; Protein Interaction Maps; Rats, Sprague-Dawley; Tandem Mass Spectrometry

Our objective of this research was (1) to investigate the transport characteristics of puerarin through MDCK-MDR1 and MDCK cells and (2) to evaluate the effects of paeoniflorin and menthol on puerarin transport so as to (3) explore the enhancement mechanism.. The cytotoxicity of drugs on MDCK and MDCK-MDR1 was evaluated by the MTT assay, and the transport studies were performed in both directions. The membrane fluidity was evaluated by fluorescence recovery after photobleaching, and the membrane potential was estimated by the accumulation of DiBAC4(3) in the cells.. Puerarin showed relatively poor absorption and purely passive diffusion. However, the efflux ratio of puerarin was <2 in MDCK-MDR1 models, which suggested puerarin was not P-gp substrates so as to the P-glycoprotein activity determination of puerarin. With the existence of menthol, the transcellular transport of puerarin increased and puerarin transport significantly increased when co-administrated with paeoniflorin and menthol.. The enhancing effect of paeoniflorin and menthol may be attributed to the significant enhancement on cell membrane fluidity, the decrease in membrane potential. Immunostaining results indicated that menthol behaved as transport enhancer by disassembly effect on tight junction integrity.

Topics: Animals; Biological Transport; Blood-Brain Barrier; Cell Survival; Dogs; Drug Interactions; Glucosides; Isoflavones; Madin Darby Canine Kidney Cells; Membrane Fluidity; Membrane Potentials; Menthol; Models, Biological; Monoterpenes

The aim of this research is to investigate the effects of paeoniflorin and menthol on the physiological function of Calu-3 cell membrane during the transport of puerarin. Calu-3 cell was used as the

Topics: Calcium-Transporting ATPases; Cell Line, Tumor; Cell Membrane; Glucosides; Humans; Isoflavones; Membrane Fluidity; Menthol; Monoterpenes; Sodium-Potassium-Exchanging ATPase

Topics: Administration, Intranasal; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Drug Delivery Systems; Epithelial Cells; Fluorescent Antibody Technique; Glucosides; Isoflavones; Male; Menthol; Monoterpenes; Nasal Mucosa; Permeability; Rats; Rats, Sprague-Dawley; Tissue Distribution

Nasal administration is a high-potential delivery system, particularly because it can provide a pathway from the nose to the brain. The objective of this research is to characterize puerarin transport across a Calu-3 cell monolayer used as a model of the nasal mucosa and to evaluate the influence of puerarin in combination with paeoniflorin and menthol to explore the enhanced mechanism of the permeability at the cell level. The apparent permeability coefficients (P app) of puerarin bidirectional transport were both <1.5×10(-6) cm/s, and the efflux ratio was <1.5, indicating that puerarin alone exhibited poor absorption and that its transport primarily occurred by passive diffusion through the cell monolayer. When puerarin was coad ministered with paeoniflorin, the P app was not changed (P>0.05). However, the addition of menthol significantly (P<0.05) improved the P app of puerarin in both directions. Moreover, based on immunofluorescence experiments and transepithelial electrical resistance measurements, the data indicated that the drug compatibility opened tight junctions and weakened the barrier capabilities of epithelial cells, thereby promoting the permeability of puerarin.

Topics: Biological Transport; Cell Survival; Cells, Cultured; Dose-Response Relationship, Drug; Glucosides; Humans; Isoflavones; Menthol; Models, Biological; Monoterpenes; Nasal Mucosa; Permeability; Structure-Activity Relationship

A liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) method was developed and validated for simultaneous determination of seven constituents including puerarin, daidzin, daidzein, paeoniflorin, albiflorin, liquiritin and liquiritigenin in rat plasma using schisandrin as the internal standard (IS). The plasma samples were pretreated by a one-step direct protein precipitation with acetonitrile. The chromatographic separation was carried out on a C18 column with a gradient mobile phase consisting of acetonitrile and water (containing 0.1% formic acid and 5mM ammonium acetate). All analytes and IS were quantitated through electrospray ionization in positive ion multiple reaction monitoring (MRM) mode. The mass transitions were as follows: m/z 417.5→297.2 for puerarin, m/z 417.1→255.2 for daidzin, m/z 255.2→152.4 for daidzein, m/z 498.1→179.3 for paeoniflorin, m/z 481.1→197.3 for albiflorin, m/z 436.2→257.3 for liquiritin, m/z 257.2→137.3 for liquiritigenin and m/z 415.0→384.2 for IS, respectively. All calibration curves exhibited good linearity (r>0.9979) over a wide concentration range for all components. The intra-day and inter-day precisions (RSD) at three different levels were both less than 14.3% and the accuracies (RE) ranged from -13.2% to 14.8%. The extraction recoveries of the seven compounds ranged from 72.9% to 117.4%. The validated method was successfully applied to pharmacokinetic study of the seven components in female rat plasma after oral administration of Ge-Gen Decoction aqueous extract.

Topics: Animals; Bridged-Ring Compounds; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavanones; Glucosides; Isoflavones; Monoterpenes; Rats; Spectrometry, Mass, Electrospray Ionization; Tandem Mass Spectrometry

An HPLC-photodiode array (PDA) detection method was established for the simultaneous determination of 12 components in Xiao-Yao-San-Jia-Wei (XYSJW): geniposide, puerarin, paeoniflorin, ferulic acid, liquiritin, hesperidin, naringin, paeonol, daidzein, glycyrrhizic acid, honokiol, and magnolol. These were separated in less than 70 min using a Waters Symmetry Shield RP 18 column with gradient elution using (A) acetonitrile, (B) water, and (C) acetic acid at a flow rate of 1 ml/min, and with a PDA detector. All calibration curves showed good linear regression (r(2)>0.9992) within the test ranges. The method was validated for specificity, accuracy, precision, and limits of detection. The proposed method enables in a single run the simultaneous identification and determination for quality control of 12 multi-structural components of XYSJW forming the basis of its therapeutic effect.

Topics: Acetophenones; Benzoates; Biphenyl Compounds; Bridged-Ring Compounds; Coumaric Acids; Drugs, Chinese Herbal; Flavanones; Glucosides; Glycyrrhizic Acid; Hesperidin; Iridoids; Isoflavones; Lignans; Medicine, Chinese Traditional; Molecular Structure; Monoterpenes; Quality Control; Reference Standards; Reproducibility of Results; Sensitivity and Specificity

We report a high-performance liquid chromatographic method to determine the quantities of puerarin, daidzin, paeoniflorin, liquiritin, cinnamic acid, cinnamaldehyde and glycyrrhizin in Kampo medicine. All seven compounds were separated in less than 30 min with a Wakosil-II 5C18 AR column by linear gradient elution using 0.01% (v/v) phosphoric acid acetonitrile (0 min 90:10, 10 min 88:12, 22 min 70:30, 30 min 30:70) as the mobile phase at a flow-rate of 1.0 ml/min(-1), and detection at 250 nm. The detection limits of these compounds are 0.15-0.3 microM with response linearity. This method was applied to determine the quantities in eight Kampo decoctions; Mao-to, Makyo-yokukan-to, Makyo-kanseki-to, Yokuinin-to, Sho-seiryu-to, Keima-kakuhan-to, Kakkon-to and Kakkon-to-ka-senkyu-sin'i. Glycyrrhizin content was lower in both the decoction and the methanol-diluted decoction of Sho-seiryu-to compared with the others. Low pH due to organic acids of Schisandrae fructus in the decoction caused inhibition for glycyrrhizin dissolution in Sho-seiryu-to.

Topics: Acrolein; Benzoates; Bridged-Ring Compounds; Calibration; Chromatography, High Pressure Liquid; Cinnamates; Drugs, Chinese Herbal; Glucosides; Glycyrrhizic Acid; Isoflavones; Medicine, Kampo; Monoterpenes; Regression Analysis; Reproducibility of Results; Sensitivity and Specificity; Spectrophotometry, Ultraviolet