ABSTRACT
Jervine, a novel steroidal alkaloid from Veratrum nigrum L., exhibits both antitumor effect and potential toxicity. The aim of study was to characterize the pharmacokinetic behaviors and enterohepatic circu-lation of jervine in rats. A rapid and simple ultra-high performance liquid chromatography-tandem mass spectrometric method was developed and validated for quantification of jervine and alpinetin (internal standard) in rat plasma. After extraction from rat plasma by a simple protein-precipitation method, the analyte was separated on a C18 column (2.1 mm × 50 mm, 1.7μm) using water with 0.1％formic acid and acetonitrile as the mobile phase delivered at a flow rate of 0.4 mL/min. Jervine and alpinetin were determined in the positive mode with multiple reaction monitoring (MRM) of the ion transitions at m/z 426.3→108.8 and m/z 271.0→166.9, respectively. Molecular docking method was used to investigate the binding of jervine to p-glycoprotein and dehydroepiandrosterone sulfotransferase. The method was well validated within acceptance limits including specificity, matrix effect, recovery, precision, accuracy, and stability, and was successfully applied to the pharmacokinetic study of jervine after oral and intravenous administration to rats. Jervine presented a small volume of distribution, fast absorption, high oral bioavailability, and enterohepatic circulation. The enterohepatic circulation was first observed in veratrum alkaloids, and was further investigated by molecular docking studies, which was related to the binding of jervine to p-glycoprotein and dehydroepiandrosterone sulfotransferase. The pharmacokinetic properties and enterohepatic circulation of jervine in rats provided a significant basis for the drug-drug interaction and toxicity study in the future.
ABSTRACT
Objective To predict the value of advanced glycation end products (AGEs) in the risk and severity of coronary heart disease in diabetic patients.Methods Totally 120 cases were divided into 3 groups.Group A had no diabetes mellitus (DM) and no coronary atherosclerotic heart disease (CAD).Group B had DM without CAD.Group C had DM with CAD.The levels of AGEs,low density lipoprotein cholesterol (LDL-C),glycosylated hemoglobin,and the severity of coronary stenosis were detected.Receiver operating characteristic (ROC) curve was used to evaluate the sensitivities and specificities of AGEs for the diagnosis of DM with CAD.Results The highest level of AGEs,LDL-C,glycosylated hemoglobin and carotid plaque was in the C group,with a statistically significant difference (P ＜ 0.05).The severity of AGEs was significantly correlated with the severity of CAD and the Gensini score of AGEs (r =0.445).ROC curve showed that the sensitivity,specificity and area under ROC curve of AGEs determination of DM with CAD were 80.0％,75.0％,and 0.86,respectivity.Conclusions The level of AGEs is significantly correlated with atherosclerosis and prognosis in DM.The severity of CAD was higher in the patients with higher AGEs,and the incidence and severity of restenosis increased.
ABSTRACT
In China,there are no standard and good modes for the chemistry courses taught in English for the international medical students.On the basis of the experience achieved in teaching the chemistry courses for overseas students,with the intenti on of the science development,the system of chemistry courses with Chinese characteristic has been programmed.
ABSTRACT
Object To investigate the chemical constituents from the whole plant of Notoseris gracilipes Shih Methods Compounds were isolated by various column chromatography and identified by spectral analysis Results Eight sesquiterpene lactones and four other compounds were isolated and identified as jacquilenin (Ⅰ), scorzoside (Ⅱ), ixerisoside D (Ⅲ), austricin (Ⅳ), notoserolide A (Ⅴ), crepidiaside A (Ⅵ), crepidiaside B (Ⅶ), and lactuside B (Ⅷ) The other four were 6, 7 dihydroxycoumarin (Ⅸ), cichoriin (Ⅹ), luteolin 7 glucoside (Ⅺ), and daucosterol ( ⅩⅡ ) Among them, compounds Ⅰ and Ⅱ showed antibacterial activity against Bacillu cereus AS 1 1688 Conclusion All compounds were isolated from this plant for the first time