peoniflorin and 7-3--dihydroxy-4--methoxyisoflavone

Paeoniflorin (PF) and calycosin-7-glucoside (CG,. To investigate the synergistic effects of PF + CG on ischaemia/reperfusion injury. Male Sprague-Dawley rats were subjected to the middle cerebral artery occlusion/reperfusion (MCAO/R). After MCAO/R for 24 h, rats were randomly subdivided into 5 groups: sham, model (MCAO/R), study treatment (PF + CG, 40 + 20 mg/kg), LY294002 (20 mg/kg), and study treatment + LY294002. Males were given via intragastric administration; the duration of the. PF + CG significantly reduced neurobehavioral outcomes (21%), cerebral infarct volume (44%), brain edoema (1.6%) compared with the MCAO/R group. Moreover, PF + CG increased p-PI3K/PI3K (4.69%, 7.4%), p-AKT/AKT (6.25%, 60.6%) and Bcl-2/BAX (33%, 49%) expression. PF + CG showed a synergistic protective effect against ischaemic brain injury, potentially being a future treatment for ischaemic stroke.

Topics: Animals; Brain Ischemia; Glucosides; Glycogen Synthase Kinase 3 beta; Infarction, Middle Cerebral Artery; Ischemic Stroke; Isoflavones; Male; Monoterpenes; Neuroprotective Agents; Phosphatidylinositol 3-Kinases; Proto-Oncogene Proteins c-akt; Rats; Rats, Sprague-Dawley; Reactive Oxygen Species; Reperfusion Injury; Stroke

Naoshuantong capsule (NSTC) is an oral traditional Chinese medicine formula used widely in the clinic for ischemic stroke. The absorbed ingredients and metabolites of NSTC have never been reported before. In this study, a method incorporating rapid resolution liquid chromatography with quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF/MS) was used to identify absorbed ingredients and metabolites after oral administration of NSTC. A total of 15 constituents were detected and identified as prototypes of NSTC. 109 metabolites related to catechin, gallic acid, paeoniflorin, chlorogenic acid, protocatechuate, typhaneoside, β-elemene, calycosin were identified in serum, urine and brain. 19 metabolites of typhaneoside, 3 metabolites of β-elemene, 12 metabolites of calycosin were reported for the first time. This is the first time to explore the absorption and metabolism of NSTC. The work will provide helpful information for further research of the mechanism and application of NSTC.

Topics: Animals; Body Fluids; Brain; Catechin; Chlorogenic Acid; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Gallic Acid; Glucosides; Glycosides; Hydroxybenzoates; Isoflavones; Male; Medicine, Chinese Traditional; Metabolome; Mice; Mice, Inbred C57BL; Monoterpenes; Sesquiterpenes; Tandem Mass Spectrometry

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

Buyang Huanwu Decoction (BYHWD) is a well-known traditional Chinese medicine prescription which is used to treat ischaemic stroke and stroke-induced disabilities. However, the exact mechanism underlying BYHWD's amelioration of ischaemic stroke and its effective constituents remain unclear. The present study aimed to identify the effective constituents of BYHWD and to further explore its action mechanisms in the amelioration of ischaemic stroke by testing the activities of 15 absorbable chemical constituents of BYHWD with the same methods under the same conditions. The following actions of these 15 compounds were revealed: 1) Ferulic acid, calycosin, formononetin, astrapterocarpan-3-O-β-D-glucoside, paeonol, calycosin-7-O-β-D-glucoside, astraisoflavan-7-O-β-D-glucoside, ligustrazine, and propyl gallate significantly suppressed concanavalin A (Con A)-induced T lymphocyte proliferation; 2) Propyl gallate, calycosin-7-O-β-D-glucoside, paeonol, and ferulic acid markedly inhibited LPS-induced apoptosis in RAW264.7 cells; 3) Propyl gallate and formononetin significantly inhibited LPS-induced NO release; 4) Hydroxysafflor yellow A and inosine protected PC12 cells against the injuries caused by glutamate; and 5) Formononetin, astragaloside IV, astraisoflavan-7-O-β-D-glucoside, inosine, paeoniflorin, ononin, paeonol, propyl gallate, ligustrazine, and ferulic acid significantly suppressed the constriction of the thoracic aorta induced by KCl in rats. In conclusion, the results from the present study suggest that BYHWD exerts its ischaemic stroke ameliorating activities by modulating multiple targets with multiple components.

Topics: Animals; Apoptosis; Brain Ischemia; Drugs, Chinese Herbal; Glucosides; Isoflavones; Male; Mice; Mice, Inbred BALB C; Monoterpenes; PC12 Cells; Rats; Rats, Sprague-Dawley; RAW 264.7 Cells; Saponins; Stroke; Triterpenes

To establish an HPLC fingerprint of ethanol extract of QingGuangAn, and to determine the contents of paeoniflorin and calycosin-7-glucosid.. HPLC analysis was performed on an Agilent 1260 Infinity LC system and carried out at 35 degrees C on a column of GRACE Alltima C18 (250 mm x 4.6 mm, 5 μm). A binary gradient elution system was composed of acetonitrile (phase A) and water solution (phase B). Detection was performed at the wavelength of 254 nm, the mobile flow rate was 0.8 mL/min. A matrix including 20 variations (characteristic peaks area) and 10 samples was constructed for similarity evaluation.. The results showed that the collected samples had a good similarity. A specificity fingerprint was produced and 20 characteristic peaks were designated. The content of paeoniflorin and calycosin-7-glucosid was 0.368 and 0.049 mg/g, respectively.. It is a reliable, available and quick method for quality control of QingGuangAn,which provides some reference for the comparison of different extracting methods of QingGuangAn and the differences of pharmacodynamic.

Topics: Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Glucosides; Isoflavones; Monoterpenes; Quality Control

Bu-yang-huan-wu-tang (BYHWT) is a popular Traditional Chinese Medicine formula consisting of seven herbal medicines (Astragalus membranaceus, Angelica sinensis, Paeonia lactiflora, Ligusticum chuanxiong, Carthamus tinctorius, Amygdalus persica and Pheretima aspergillum), that has been used in China for centuries to overcome stroke-induced disability. To ensure the consistency of quality, a reliable analytical method is required, therefore, we developed a liquid chromatography with tandem mass spectrometry (LC-MS/MS) method for quantitative analysis of the major constituents in BYHWT. The herbal ingredients consisting of the cycloartane-type triterpene glycosides of astragaloside I, astragaloside II and astragaloside IV; isoflavones of formononetin, ononin calycosin, calycosin-7-O-β-d-glucoside; ligustilide and paeoniflorin were separated on a C18 column with gradient elution of methanol/10 mM ammonium acetate buffer-formic acid (100:0.1, v/v). This study was performed by a mass spectrometer using electrospray ionization (ESI) with positive ionization ions monitored in the multiple reaction-monitoring (MRM) mode. The linearity, accuracy, precision, limit of detection (LOD) and lower limit of quantification (LLOQ) were validated for this quantification method, and the sensitivity, reliability and reproducibility were all confirmed. The experiments provided a good method for analyzing BYHWT extracts. This study also quantitated the active components in various brands of commercially available products. The results indicated that the pharmaceutical industrial products of BYHWT exhibited considerable variation in their contents of the herbal compounds.

Topics: 4-Butyrolactone; Benzoates; Bridged-Ring Compounds; Chromatography, High Pressure Liquid; Digoxin; Drugs, Chinese Herbal; Glucosides; Humans; Isoflavones; Limit of Detection; Medicine, Chinese Traditional; Monoterpenes; Reproducibility of Results; Saponins; Spectrometry, Mass, Electrospray Ionization; Tandem Mass Spectrometry; Triterpenes