OBJECTIVE:To domminate the quality of Fushuye,the contents of baicalin in Fushuye was determined by HPLC.METHOD:Baicalin was separated on Spherisorb C18 column and detected at 278 nm,by using methanol-4g.L-1 phosphoric acid (50∶50) as mobile phase.RESULTS:The resolution was 4.5.The number of theoretical plates calculaled for baicalin peak was 3800.The standard curve was linear over the range of 20 ng～900ng,with the correlation coefficient 0.999 9.The average recovery was 99.88% with RSD=1.54%(n=5). CONCLUSION:The method is simple and fast,and can be used for quantitative analysis of Fushuye.

ObjectiveTo study the therapeutic effect and feasibility of endoscopic thyroidectomy via breast areola approach. MethodEndoscopic thyroidectomy via breast areola approach was performed in 62 patients, including 16 cases of adenoma, 43 cases of nodular goiter, and 3 cases of thyroid carcinoma.ResultsEndoscopic thyroidectomy was succeeded in 62 patients, 2 cases of cutaneous emphysema, 1 case of light skin bum which diameter was 0.5 cm, 1 case of transient hoarse voice,and 1 case of puncture sinus tract bleeding. There was no converted to open surgery,no hypercapnia, no damage of recurrent laryngeal nerve or parathyriod glands. ConclusionEndoscopic thyroidectomy via breast areola approach is safe and effective,and has good cosmetic results.

AIM: To study pattern recognition of the fingerprint of Polygonum orientale from Guizhou Province. METHODS: 20 batches of samples,Polygonum orientale,come from different producing areas and harvest time were carried out to gain fingerprints by HPLC-DAD,as compared with retention time and ultraviolet spectra of standard substances.The pattern recognition of the characteristic fingerprint of Polygonum orientale,known as cluster analysis and principal component analysis,formed. RESULTS: The fingerprint of 20 batches of Polygonum orientale showed 12 characteristic peaks,in which 9 common peaks were confirmed.the samples were grouped into 3 types of harvest time. CONCLUSION: The quality of Polygonum orientale in Guizhou Province is stable,the pattern recognition of the fingerprint provides the experimental basis for manufacture and quality control of Polygonum orientale.

AIM: To study and establish the fingerprint of raw Herba Polygoni Orientalis by RP-HPLC. METHODS: The chromatographic conditions were as follow: an Inersil-ODS-3 column was used;the mobile phase was composed of acetontrile and 0.1% phosphoric acid with gradient elution;the flow was 1.0 mL?mim~(-1) and the UV absorbance detection was set at 300 nm. RESULTS: Under the selected chromatographic conditions. Similarity of 10 batches of good HPLC fingerprint of raw Herba Polygoni Orientalis were obtained. no less than 0.9.( CONCLUSION): Quality of raw Herba Polygoni Orientalis can be controlled effectively by HPLC-UV fingerprint.

Aims To establish a UPLC-MS method for quantifying protocatechuie acid,kaempferol-3-O-β-D-glucoside and quercitrin and to investigate the pharma-cokinetics of three indix components in flower of Poly-gonumorientale L.in rat plasma.Methods The anal-ysis was achieved by BEH C18 column (2.1 mm ×100 mm,1.7 μm)with a mobile phase composed of 0.1%formic acid using step gradient elution.A TQD tandem mass spectrometry equipped with electrospray ionization source was used as detector and operated by selected ion recording(SIR)mode.Results In the selected linear range,calibration curves of the three markers components showed good linearity.Extraction recovery rate,precision,accuracy and stability reached the de-termination request.The parameters of Tmax (h ) in three index components were 0.46 ±0.1,0.79 ±0.33 and 2.63 ±4.6,respectively;Cmax (μg·L -1 )in three index components were 463.8 ±207.81,18.53 ±7.82 and 137.38 ±71.09,respectively.Conclusion The fully validated UPLC-MS method has been successfully applied to the pharmacokinetic study of the three index components in flower of Polygonumorientale L.in rat plasma.

Objective To assess the correlation between magnetic resonance imaging (MRI)and clinical staging of pelvic organ prolapse (POP)by using pubococcygeal line (PCL)and midpubic line (MPL)respectively.And to determine which(MRI)reference line for staging pelvic organ prolapse had the highest agreement with clinical staging.Methods A retrospective study of 32 women with pelvic organ prolapse who underwent dynamic pelvic MRI from Jan 2013 to May 2013 was conducted.One radiologist staged descent on MRI for each pelvic compartment (anterior,middle,posterior),using PCL and MPL lines.Agreement between MRI and clinical staging was estimated respectively.Results Thirty-two women were included.Agreement between clinical and MPL staging was morderate in the anterior (κ=0.44,SE=0.13)and middle compartment (κ=0.46,SE=0.12),but fair in the posterior com-partment (κ=0.23,SE=0.10).Agreement between clinical and PCL staging was poor in all compartments of pelvic.Conclusion MPL appeared more reliable and simple than the PCL for the evaluation of pelvic prolapse on MRI.

A series of adefovir mono-L-amino acid esters, mono non-steroidal anti-inflammatory drugs carboxylic ester prodrugs with more potent anti-HBV activity and lower nephrotoxicity were designed and synthesized. Adefovir bis (L-amino acid) ester was used as lead compound, according to pathological and pharmacological findings that non-steroidal anti-inflammatory drugs can effectively inhibit the organic anion transporter 1 (hOAT1)-mediated adefovir phosphonic acid pairs of anion transport across tubular basement membrane thereby reducing the nephrotoxicity of adefovir. Flatten design principle was used to introducing non-steroidal anti-inflammatory drugs structural fragments to design and synthesize target adefovir mixture ester prodrugs. HepG2 2.2.15 cell line was used as in vitro anti-HBV activity evaluation model. Five compounds exhibited antiviral activity, and compound 18 showed the most potent anti-HBV activity and relatively high selective index (EC50 3.92 micromol L(-1), SI 9.97). HK-2 cell line was used as in vitro model to evaluate nephrotoxicity. Results suggested the target compounds have lower cytotoxicity than the positive control. Moreover, by analyzing the primary structure and activity relationship of these compounds, it could suggest that mono-L-amino acid ester, mono non-steroidal anti-inflammatory drugs carboxylic ester prodrugs strategy has significant potential in the acyclic nucleoside phosphonates prodrug design.

A simple and selective ultra performance liquid chromatography-electrospray ionization tandem mass spectrometry (UPLC-ESI-MS/MS) assay was developed for the determination of the human plasma protein binding of four bioactive flavonoids (such as orientin and vitexin) in Polygonum orientale. Protein precipitation was used for sample preparation. Equilibrium dialysis technique was applied to determine the plasma protein binding under physiological conditions. The separation was achieved through a Waters C18 column with a mobile phase composed of 0.1%formic acid in acetonitrile and 0.1%aqueous formic acid using step gradient elution at a flow rate of 0.35 mL/min. A Waters ACQUITY?TQD system was operated under the multiple reaction monitoring (MRM) mode of positive electrospray ionization. All of the recovery, precision, accuracy and stability of the method met the requirements. Good correlations (r40.99) of the four compounds were found, which suggested that these compounds can be simultaneously determined with acceptable accuracy. Results showed that the plasma protein bindings of the four bioactive flavonoids were in the range of 74-89% over the six concentrations studied. The binding parameters containing protein binding affinity, protein binding dissociation constant, and protein binding site were studied. The maximum ability to bind with protein was also determined in the assay in order to understand the drug-protein binding of each compound better.

To design and synthesize a series of novel scutellarein 4'-L-amino acid prodrugs with more potent anti-oxidative activity and improved physicochemical properties. Scutellarein was used as lead compound, according to successful experience of improving bioavailability of oral administration drugs by active transport mechanism, principle of hybridization was used to introducing L-amino acid structural fragments at 4'-position of scutellarein to design and synthesize target scutellarein 4'-L-amino acid prodrugs. The synthetic compounds were tested on their physicochemical properties and in vitro anti-oxidative activity against H202 induced oxidative damage in PC12 cells. Five compounds were found to have more potent anti-oxidative activity than positive control VE. Moreover the physicochemical properties of synthesized compounds were evaluated, and the results revealed that L-amino acid ether derivatives are more stable (t1/2 9-92 h) than their corresponding ester derivatives (t1/2 0.5 h). Water solubility of scutellarein 4'-L-amino acid ester and ether derivatives were 1 796-4 100 microg.mL-1 and 27.7-81.1 microg.mL-1 respectively, in comparison with scutellarin, the solubility of compounds 18, 19 and 22, 24-27 increased about 120-280 fold and 2-6 fold respectively. All these results suggested that L-amino acid prodrug strategy has significant potential in scutellarein prodrug design.

OBJECTIVETo establish a UPLC-MS/MS analysical method for simultaneous determination of concentrations of isoorientin, scutellarin and cynaroside in rat plasma and to study their pharmacokinetic characteristics after intravenous injection of 3 doses of Fufang Hongcao in rats.

METHODAcidified plasma samples were precipitated for protein with methanol. Waters Acquity BEH C18 column was adopted for spectrum, with mobile phase as 0. 1% formic acid acetonitrile-0. 1% formic acid-water gradient elution. Detection was carried out by the multiple reaction monitoring (MRM) positive ion mode with ESI ionization source.

RESULTThree flavonoids show a good linear relationship, with the extraction recovery ranging between 78.56% and 101.91% and a high intra-and inter-day precisions and accuracy. The MRT of the three flavonoids were all lower than 22 min in rats.

CONCLUSIONThe above men tioned method is so specific, rapid, sensitive that it is suitable for pharmacokinetic studies of Fufang Hongcao injection in rats.

Animals ; Apigenin ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; pharmacokinetics ; Female ; Glucosides ; blood ; pharmacokinetics ; Glucuronates ; blood ; pharmacokinetics ; Luteolin ; blood ; pharmacokinetics ; Male ; Rats ; Tandem Mass Spectrometry ; methods ; Time Factors