Metabolic profiling of the hepatotoxicity and nephrotoxicity of Ginkgolic acids in rats using ultra-performance liquid chromatography-high-definition mass spectrometry.

Ginkgolic acids (GAs) are thought to be the potentially hazardous constituents corresponding to the toxic side effects of Ginkgo products. In this study, toxicological and metabolomics studies of GAs were carried out by ultra-performance liquid chromatography-high-definition mass spectrometry (UPLC-HDMS). Significant changes in serum clinical chemistry were observed in the both low (100 mg/kg) and high (900 mg/kg) doses.

Effects of Ziziphus jujuba fruit extracts on cytochrome P450 (CYP1A2) activity in rats.

Drug-drug interactions have become a serious problem in the clinic, since plant-based medicines are extensively used. The present study investigated the effects of Ziziphus jujuba fruit (ZJ) extract on the pharmacokinetics of phenacetin, a typical substrate of a cytochrome P450 enzyme CYP 1A2, in rats. The rats were pretreated with the water extract (1.

Biotransformation and metabolic profile of caudatin-2,6-dideoxy-3-O-methy-β-d-cymaropyranoside with human intestinal microflora by liquid chromatography quadrupole time-of-flight mass spectrometry.

In our previous studies, caudatin-2,6-dideoxy-3-O-methy-β-d- cymaropyranoside (CDMC) was for the first time isolated from Cynanchum auriculatum Royle ex Wightand and was reported to possess a wide range of biological activities. However, the routes and metabolites of CDMC produced by intestinal bacteria are not well understood. In this study, ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) technique combined with Metabolynx(TM) software was applied to analyze metabolites of CDMC by human intestinal bacteria.

Pharmacokinetics and tissue distribution study of caudatin in normal and diethylnitrosamine-induced hepatocellular carcinoma model rats.

Caudatin is a potential antitumor agent isolated from the traditional Chinese medicine "baishouwu", which was the root tuber of Cynanchum auriculatum Royle ex Wight. In our previous studies, caudatin showed selectivity on human hepatoma cell line SMMC7721 among several different tumor cell lines, and further in vivo tests validated the inhibitory action of caudatin against hepatic cancer using an H22 solid tumor model in mice, but to our knowledge, the biopharmaceutical properties of caudatin are largely unknown. In this study, a simple, rapid and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the determination of caudatin in rat plasma and tissues, which kept the run time to detect one sample within 4 min, was developed and validated.

Decreased exposure of simvastatin and simvastatin acid in a rat model of type 2 diabetes.

Aim: Simvastatin is frequently administered to diabetic patients with hypercholesterolemia. The aim of the study was to investigate the pharmacokinetics of simvastatin and its hydrolysate simvastatin acid in a rat model of type 2 diabetes.

Methods: Diabetes was induced in 4-week-old rats by a treatment of high-fat diet combined with streptozotocin.

Chemical constituents of Prunella vulgaris.

Nine compounds were isolated from the spikes of Prunella vulgaris by various kinds of chromatography. Their structures were established on the basis of spectral analysis as polygalacerebroside (1), ursolic acid (2), β-amyrin (3), quercetin (4), quercetin-3-O-β-D-galactoside (5), α-spinasterol (6), stigmasterol (7), β-sitosterol (8), daucosterol (9). Compound 1 was isolated from this genus for the first time.

Discovery of glycyrrhetinic acid as an orally active, direct inhibitor of blood coagulation factor xa.

Introduction: Factor Xa (FXa) plays an important role in blood coagulation. This study investigated glycyrrhetinic acid, a small molecule derived from Chinese herbs, and whether it has a direct inhibitory effect on FXa to display its anticoagulant activity.

Materials And Methods: Enzyme activities of FXa, plasmin, trypsin and thrombin, inhibition of FXa enzyme kinetics and plasma clotting time by glycyrrhentinic acid were performed in vitro.

[Nourishing-yin effect and mechanism of different parts of Cornu Elaphuri Davidiani in rats].

Objective: To investigate nourishing-yin effect and mechanism of different parts of Cornu Elaphuri Davidiani in rats.

Method: The model of yin asthenia rats was built by thy roxine. The substance metabolism, pain threshold, hormone levels and biochemical indicators in serum were measured.

Caudatin-2,6-dideoxy-3-O-methy-β-D-cymaropyranoside 1 induced apoptosis through caspase 3-dependent pathway in human hepatoma cell line SMMC7721.

Caudatin-2,6-dideoxy-3-O-methy-β-D-cymaropyranoside (CDMC), the C-21 steroidal glycoside recently extracted from the traditional Chinese medicinal plant, the root of Cynanchum auriculatum Royle ex Wight (Asclepiadaceae), has been shown to possess potent antitumor properties. However, the bioactivities of CDMC are still largely unknown, especially the antitumor effect and its mechanism. This study investigated the CDMC antitumor effects on human hepatoma cell line SMMC7721 cells by analysis of cell viability, cell cycle phases and apoptosis.

[Effects of three C21 steroidal saponins from Cynanchum auriculatum on cell growth and cell cycle of human lung cancer A549 cells].

Objective: To investigate the inhibition of three C2 steroidal saponins from Cynanchum auriculatum on the cell growth and cell cycle of human lung cancer A549 cells.

Method: A549 cells were exposed to three C21 steroidal saponins of different concentrations (5, 10, 20, 40, 60, 80, 100 micromol L(-1)) for 48 hours. After 48 h, MTT assay was used to evaluate the inhibiting effects of three C21 steroidal saponins on the proliferation of the A549 cells.

[Determination of paeoniflorin in rat plasma by HPLC-MS/MS and its pharmacokinetics].

Objective: An HPLC-MS/MS assay was established to determine paeoniflorin in rat plasma and be used to investigate the effect of pharmacokinetics of paeoniflorin when co-administrated Radix Angelicae Sinensis and Radix Paeoniae Rubra.

Method: HPLC-MS/MS was performed in the multiple reaction monitoring (MRM) mode using target ions at m/z 450 --> m/z 327 for paeoniflorin and m/z 388 --> m/z 225 for jasminoidin. A single dose of Radix Paeoniae Rubra alone and with Radix Angelicae Sinensis was given to rats by ig, the dosage of paeoniflorin was 294.

[Study on Cornu Bos grunniens from Tibet substituting Cornu Rhinoceri].

Objective: Comparing the pyretolysis effect of Cornu Rhinoceri Soup, an ancient prescription of Traditional Chinese Medicine, on fever model of rabbits after Cornu Bos grunniens from Tibet substituting Cornu Rhinoceri, in order to find the succedaneums of Cornu Rhinoceri, a rare animal medicine.

Methods: The fever model was made by over-due Triple-Vaccine i.v.

Four anthraquinones from Hedyotis diffusa.

A new anthraquinone has been isolated from the 95% EtOH extract of Hedyotis diffusa and characterized as 2-hydroxy-3-methoxy-6-methyl-9,10-anthraquinone (1) by extensive spectral analysis. The known compounds isolated for the first time from this plant have been identified as 2-hydroxy-3-methoxy-7-methyl-9,10-anthraquinone (2), 2-hydroxy-6-methylanthraquinone (3), and 1,3-dimethoxy-2-hydroxy-9,10-anthraquinone (4).

[AHP application to study of weighted coefficient on multicriteria optimization of extraction technology about Chinese traditional compound drugs].

Objective: Establishing a subjective and objective method to conform the weighted coefficient in multicriteria optimization of the extraction technology about Chinese traditional compound drugs.

Method: This article used analytic hierarchy process (AHP) to conform the weighted coefficient.

Result: Consistency checking result (CR < 0.

Two new cytotoxic pregnane glycosides from Cynanchum auriculatum.

Two new pregnane glycosides, kidjoranin 3- O- alpha-diginopyranosyl-(1-->4)- beta-cymaropyranoside (1) and kidjoranin 3-O-beta-digitoxopyranoside (2), together with one known compound caudatin 3 -O-beta-cymaropyranoside (3), were isolated from the roots of Cynanchum auriculatum. Their structures were established on the basis of NMR analyses. Compounds 1 - 3 were tested for their in vitro inhibitory activity against the growth of human tumor cell lines SMMC-7721, HeLa and MCF7; all of them displayed marked cytotoxic activities against cells SMMC-7721 and HeLa with IC (50) values ranging from 8.

[Studies of volatile oils from the flowers of Chrysanthemum nankingense and Chrysanthemum indicum].

Chemical constituents of volatile oils from the flowers of Chrysanthemum nankingense and C. indicum were studied by GC-MS. 59, 30 components were identified respectively.