Pharmacokinetics of ginsenoside Rb1 in lincomycin-induced gut microbiota dysbiosis rats / 中国药科大学学报

@#Gut microbiota-mediated deglycosylationplays an important role in the metabolism of ginsenoside Rb1. Thus, a lincomycin-induced gut microbiota dysbiosis rat model was selected to explored the pharmacokinetics and deglycosylation metabolism of ginsenoside Rb1. An UPLC-MS/MS analytical method was developed to detect ginsenoside Rb1 and its deglycosylated metabolite, Rd in rat plasma. The triple quadruple mass spectrometer was set in negative electrospray ionization mode by multiple reaction monitoring. The method was validated to meet the requirements of biological applications, by evaluating specificity, linearity, lower limits of quantification(LLOQ), precision, accuracy, matrix effect, recovery and stability. Gut microbiota dysbiosis rats were induced by oral administration of lincomycin(5 000 mg/kg)for 7 continuous days. The in vitro and in vivo results reveal that the reduced β-D-glucosidase activity significantly decreases the Rd formation rate in lincomycin-induced gut microbiota dysbiosis rats, leading to the pharmacokinetic alteration of ginsenoside Rb1 and Rd in gut microbiota dysbiosis rats.

Analysis of metabolites of daphnetin in the intestinal wall of rats by liquid chromatography and quatrupole-time of flight mass spectrometry / 药学学报

In this study, daphnetin and its major metabolites in the intestinal wall of rats were identified by liquid chromatography and quatrupole-time of flight mass spectrometry. Perfusion fluid of duodenum, jejunum, ileum and colon were collected separately for 2 hours from the rat intestine following perfusion with daphnetin. The metabolites of daphnetin in the perfusion fluid of different intestine segments were analyzed by the liquid chromatography and quatrupole-time of flight mass spectrometry. It is shown that the parent drug daphnetin and four metabolites were found in the perfusion fluid of duodenum, jejunum and ileum. However, no metabolites were found in the colon. Among the four metabolites, two daphnetin sulfates (m/z 257) were first discovered as the phase II metabolites of daphnetin in rats, which revealed a new way of daphnetin metabolism in rats.

Advances in studies on absorption and metabolism of natural coumarins / 中国中药杂志

Natural coumarins have strong pharmacological activities. In this paper, the absorption and metabolism of natural coumarins were introduced by analyzing and summarizing the related literature in recent years. The research of absorption and metabolism will be propitious to further understand their pharmacological mechanism and provide basis for developing new drugs of coumarins.

Effects of glycyrrhiza extract on pharmacokinetics property of daphnetin in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To research the influence of glycyrrhiza extract on the pharmacokinetics characteristic parameters of daphnetin, which was aimed to explore the rationality of concert application of drugs.</p><p><b>METHOD</b>The rats received intragastric administration of daphnetin and glycyrrhiza extract containing the same daphnetin respectively. The blood concentration of daphnetin was assayed by LC-MS. The data was processed by program DAS2.1.1.</p><p><b>RESULT</b>Glycyrrhiza extract can reduce the t(1/2), tmax and Ke of daphnetin, while increased the Ka and AUC(0-infinity).</p><p><b>CONCLUSION</b>Glycyrrhiza extract promoted the oral absorption of daphnetin, slowed down the elimination and increased the biological availability.</p>

Investigation of research method of fingerprint pharmacodynamics of traditional Chinese medicines / 中国中药杂志

Fingerprinting techniques play a increasingly important role in the quality control standards of traditional Chinese medicines (TCM), research and establish the fingerprint about spectral-efficiency could improve the quality control of TCM. The necessity of the fingerprint pharmacodynamics research and the analysis and evaluation of the research methods in the existing literature at home and abroad were reviewed in this article, Combined with the author's laboratory research, we proposed the research methods of fingerprint pharmacodynamics of TCM and provided the basis for effectively promoting the the establishment and development of fingerprint pharmacodynamics of Chinese medicine compound preparations.

Determination of Three Kinds of Phenylpropanoids in Stem Rind of Daphne giraldii by HPLC / 中国中医药信息杂志

Objective To establish a HPLC method for the determination of daphnetin, 7-OH coumarin and syringing in Zushima. Methods The separation was performed on YMC-Pack ODS (4.6 mm?250 mm, 5 ?m) column with a mobile phase consisting of methanol-0.5% acetic acid-water (19︰8︰1) as gradient elution at the flow rate of 1.0 mL/min. The dual detective wavelength was set at 327 nm and 266 nm. The column temperature was 30 ℃. Results Baseline separation was achieved for the analysis of the three index components. The average recoveries were 98.4%～100.2%. Conclusion This method is convenient, rapid and accurate. It can be used for quality control in production of Zushima.

Determination of the Physical Chemistry Constants of Total Cumarin / 中国中医药信息杂志

Objective To determine pH value, the solubility in different solvents and the oil-water partition coefficients of cumarin. Method UV spectrophotometry was used to determine the content of cumarin. Shake-flask method was developed to determine the oil-water partition coefficients of cumarin. Result The higher solubility values of cumarin were 2 044,2015 and 1969 ?g/mL in acetone , methanol and ethanol, it was almost indiscerptible in water, the limit solubility was 1096.9 ?g/mL, which become stable while the whisk time reached to 8 hours. The oil/water detached coefficient was 11.210, which was higher in acid solvent. Conclusion The method is simple, rapid and reliable.

Establishment of fingerprint of Cortex Eucommiae and its mutual mode by HPLC / 中草药

Objective To establish the fingerprints for analysis of Cortex Eucommiae by HPLC. Methods The column of Lichroshper C18(250 mm?4.6 mm, 5 ?m) was used. The mobile phase consisted of methanol-0.1% phosphoric acid with gradient elution. The detective wavelength was 230 nm, the column temperature was 30 ℃, and the flow rate was 1.0 mL/min. Results The fingerprint consisted of 11 common peaks. The mutual mode of HPLC fingerprints was set up and the similar degrees to the crude drugs from different habitats were compared by Similarity Evaluation System for Chromatographic Fingerprint of CMM (Version 2004A), and the range of similarity for ten balches of Cortex Eucommiae 0.574—0.958. The standard HPLC fingerprint of Cortex Eucommiae was established too. ConclusionThis method is accurate and reliable, and provides a scientific basis for the quality control of Cortex Eucommiae.