OBJECTIVE: To develop RP-HPLC method for the rapid determination of resveratrol in serum and tissue homogenates (in some organs) of mice.METHODS:HPLC determination was performed using Kromasil C18 column,the mobile phase consisted of methanol - water (48∶ 52) with a flow rate of 1ml/min,the column was under room temperature with its pressure at 12kPa,the detection wavelength was 303nm and the sample size was 20?l. RESULTS: The linear range for resveratrol was 0.25～25?g/ml, with minimal detectable drug concentration at 0.1?g/ml (S/N=3). The average absolute rec_overy of the samples was above 88% and the methodological recovery rates of which ranged from 96% to 100%,RSD were below 10%. CONCLUSIONS: The established determination method is economical, reliable, simple and rapid, and suitable for the blood concentration determination of resveratrol and the study of its distribution in animal body.

Objective To compare the oxygen saturation between the blood of superior vena cava and mixed venous in lung transplantation and provide reference for monitoring method in anesthesia. Methods 30 patients who received lung transplantation were placed central venous catheter into superior vena cava and flotation catheter into the pulmonary artery in turn. The blood samples were collected from the superior vena cava and pulmonary artery for blood gas analysis simultaneously at the time of just followed the catheter placement (T1), before the resection of the first bad lung (T2), after the reperfusion of the first donor lung (T3), before the resection of the second bad lung (T4), after the reperfusion of the second donor lung (T5), before the end of the operation (T6). The oxygen saturation were compared between the blood of the superior vena cava and mixed venous. Results From T1 to T6, Bland-Altman analysis showed that the mean of deviation between the SpO2 measured in blood of superior vena cava and mixed venous were 0.5, 3.4, 2.3, 0.5, 0.27,-2.9, respectively, and the incidence beyond the upper and lowed limits of consistency zone was 3.3%, 0%, 0%, 3.3%, 3.3%, 0%respectively. The incidence of SpO2 within the consistent limits was 96.7%, 100%, 100%, 96.7%, 96.7%, 100% respectively. Conclusions The SpO2 of superior vena cava may be approximately reference as SpO2 of mixed venous during lung transplantation.

Objective To assess the application value of disposable syringe of low resistance (SLR) in epidural puncture.Methods One hundred and thirty-two patients scheduled to undergoing selective operation under epidural or combined epidural-spinal anesthesia were divided into glass syringe (GS) group and SLR group with 66 cases each by random digits table method.GS was applied in local anesthesia and epidural puncture with loss of resistance in GS group.While SLR was used in SLR group.The defect of the syringes' appearance was evaluated.The fastness between each sub-unit during the procedure was observed.The rupture,dropping,leakage,air leakage and blockage were also estimated.The heart rate,blood pressure,oxygen saturation and other adverse events were also observed.Results In SLR group,syringe excepted 1 case of slight resistance but did not affect the use,the rest of the components connected firmly,surface without defects,clear scale uniform color,not observed rupture,air leakage,leakage and blockage phenomenon,pump liquid and air resistance was small.In GS group,syringe surface without defects,clear scale uniform color,3 cases had loose connection,1 case with rupture when using,5 cases with air leakage and leakage,3 cases of pumping liquid or dry air resistance to 0.9％ sodium chloride and moist after use.There was significant difference in appearance and usage between two groups (x2 =10.324 5,P =0.001 3).There was no significant difference in a puncture success,first three puncture success and inject air negative pressure sensitivity between two groups (P ＞ 0.05).Conclusion SLR is worth to be applied in epidural puncture.

Objective To analyse the relative factors of the linear growth velocity(GV)in girls with central precocious puberty(CPP)during gonadotropin-releasing hormone analog(GnRHa)therapy,and to investigate the factors affecting the height gain during two-year GnRHa treatment.Methods In 86 girls aged (8.04?1.28)years with CPP treated with GnRHa for more than 2 years,the data including target height,age of onset,pubertal course,chronological age,bone age,linear GV,serum estradiol level and mature index of vaginal smear were analyzed,then the correlations and stepwise regression were performed.Results During GnRHa therapy,GV decreased year by year.The GV in the second year(GV_(2nd))was negatively correlated with the age of onset,bone age(BA_0,BA_2)and chronologic age(CA_0,CA_2)at the onset and by the end of the first year of GnRHa therapy(r=-0.37,-0.59,-0.57,-0.51 and-0.52,respectively,all P

Gardeniae Fructus contains volatile ingredients, however, the species and proportions in different processed products of Gardeniae Fructus are different. In this experiment, volatile ingredients were separated by steam distillation with content of 1.2, 1.0, 0.9, 0.7 µL · g(-1) in Gardeniae Fructus, fried Gardeniae Fructus, stir-baked Gardeniae Fructus, Gardeniae Fructus fried into carbon respectively. One hundred and twenty-four kinds of volatile components were identified by GC-MS. Fifty-three kinds of volatile ingredients consisted in Gardeniae Fructus accounting for 93.85%, 54 kinds in fried Cardeniae Fructus accounting for 92.01%, 32 kinds in stir-baked Cardeniae Fructus accounting for 91.59% and 43 kinds in Gardeniae Fructus fried into carbon accounting for 90.81%. In this paper, analysis of Gardeniae Fructus by GC-MS provides a scientific basis for elucidating the mechanism of different processed products.
Chemistry, Pharmaceutical ; Drugs, Chinese Herbal ; chemistry ; Gardenia ; chemistry ; Gas Chromatography-Mass Spectrometry ; Molecular Structure ; Volatile Organic Compounds ; chemistry

Processed Chinese medicine is the core of traditional Chinese medicine (TCM) industry chain,which directly affects the clinical efficacy and. safety of Chinese patent medicine and clinical formula Decoction pieces. Studied the variation of effective substance in vivo Chinese medicine processing before and after processed, clarifying the effective substance and processing principle is a top priority of the development of Chinese medicine processing. The traditional research method chiefly focus on the variation about chemicals in vitro of processed Chinese medicine, it cannot reveal that the integrity and complexity of processed Chinese medicine efficacy changes, so the change process is the focus of future research in vivo on the base of effective substance of TCM This paper described the research on the base of effective substance of TCM and Processed Chinese medicine research status in vitro, discussed the analytical methods (plasma chemistry, pharmacokinetics, metabonomics) of the dynamic process in vivo about processed Chinese medicine, and pointed out development and related problems in process in vivo on the base of effective substance of TCM, which could provided research ideas and methods for in-depth interpretation of Chinese medicine processing mechanism.
Animals ; Drugs, Chinese Herbal ; analysis ; pharmacokinetics ; Humans ; Medicine, Chinese Traditional

OBJECTIVETo study the impact of the chloride channel dysfunction of the cystic fibrosis transmembrane conductance regulator (CFTR) on the cytoskeleton of Sertoli cells in the mouse.

METHODSTM4 Sertoli cells were cultured and treated with CFTR(inh)-172 at the concentrations of 1, 5, 10 and 20 μmol/L for 48 hours. Then the cytotoxicity of CFT(inh)-172 was assessed by CCK-8 assay, the expressions of F-actin and Ac-tub in the TM4 Sertoli cells detected by immunofluorescence assay, and those of N-cadherin, vimentin and vinculin determined by qPCR.

RESULTSCFTR(inh)-172 produced cytotoxicity to the TM4 Sertoli cells at the concentration of 20 μmol/L. The expressions of F-actin and Ac-tub were decreased gradually in the TM4 Sertoli cells with the prolonging of treatment time and increasing concentration of CFTR(inh)-172 (P < 0.05). The results of qPCR showed that different concentrations of CFTR(inh)-172 worked no significant influence on the mRNA expressions of N-cadherin, vimentin and vinculin in the Sertoli cells.

CONCLUSIONThe CFTR chloride channel plays an important role in maintaining the normal cytoskeleton of Sertoli cells. The reduced function and expression of the CFTR chloride channel may affect the function of Sertoli cells and consequently spermatogenesis of the testis.

Actins ; metabolism ; Animals ; Benzoates ; pharmacology ; Chloride Channels ; physiology ; Cystic Fibrosis Transmembrane Conductance Regulator ; antagonists & inhibitors ; Cytoskeleton ; drug effects ; Male ; Mice ; Sertoli Cells ; drug effects ; metabolism ; Spermatogenesis ; Thiazolidines ; pharmacology ; Time Factors

OBJECTIVETo prepare cryptotanshinone (CT)-cyclodextrin inclusion compound and improve dissolution of CT.

METHODInclusion ratio was determined by plotting the phase solubility curve of CT versus hydroxypropyl-beta-cyclodextrin (HPCD). CT-cyclodextrin inclusion compound was made by wet grinding method. Properties of the inclusion compound was investigated by in vitro dissolution test, DTA and IR spectrum.

RESULTInclusion ratio of CT versus HPCD was 1:1. Dissolution of CT-HPCD inclusion compound at 45 min was 21.6 times of material drug.

CONCLUSIONDissolution of CT was improved remarkably in CT-HPCD inclusion compound. The complexation force of the inclusion compound was hydrogen bond formed by carbonyl group of CT and hydroxyl group of HPCD.

2-Hydroxypropyl-beta-cyclodextrin ; Biological Availability ; Drug Carriers ; Drugs, Chinese Herbal ; chemistry ; Phenanthrenes ; chemistry ; isolation & purification ; Salvia miltiorrhiza ; chemistry ; Solubility ; Technology, Pharmaceutical ; methods ; Time Factors ; beta-Cyclodextrins ; chemistry

BACKGROUNDCandida albicans is the most frequently seen opportunistic human fungal pathogen. Terbinafine is an allylamine antifungal agent that has been proven to have high clinical efficacy in the therapy of fungal infections, the mechanism of action of terbinafine involves the specific inhibition of fungal squalene epoxidase, resulting in ergosterol deficiency and accumulation of intracellular squalene. We used cDNA microarray analysis technology to monitor global expression profile changes of Candida albicans genes in response to terbinafine treatment, and we anticipated a panoramic view of the responses of Candida albicans cells to the representatives of allylamine antifungal agents at the molecular level in an effort to identify drug class-specific and mechanism-independent changes in gene expression.

METHODSCandida albicans strain ATCC 90028 was exposed to either medium alone or terbinafine at a concentration equivalent to the 1/2 minimal inhibitory concentrations (MICs, 4 mg/L) for 90 minutes. RNA was isolated and gene expression profiles were compared to identify the changes in the gene expression profile using a cDNA microarray analysis. Differential expression of 10 select genes detected by cDNA microarray analysis was confirmed by semi-quantitative reverse transcription-polymerase chain reaction (RT-PCR).

RESULTSA total of 222 genes were found to be responsive to terbinafine, including 121 up-regulated genes and 101 down-regulated genes. These included genes encoding membrane transport proteins belonging to the members of the ATP-binding cassette (ABC) or major facilitator superfamily (MFS; CDR1, AGP2, GAP6, PHO84, HOL3, FCY23, VCX1), genes involved in stress response and detoxification (CDR1, AGP2, HOL3), and gene involved in the ergosterol biosynthesis pathway (ERG12). The results of semi-quantitative RT-PCR were consistent with that of the cDNA microarray analysis.

CONCLUSIONSThe up-regulation of the gene encoding the multidrug resistance efflux pump CDR1 may contribute to the terbinafine resistance in Candida albicans. However, the precise roles of other affected genes remain unclear, further studies of these genes and their respective products that play roles in the context of antifungal resistance are warranted.

Antifungal Agents ; pharmacology ; Candida albicans ; drug effects ; genetics ; Ergosterol ; biosynthesis ; Fungal Proteins ; genetics ; Gene Expression Profiling ; Genome, Fungal ; Membrane Transport Proteins ; genetics ; Naphthalenes ; pharmacology ; Oligonucleotide Array Sequence Analysis

Chitosan microsphere has been wildly researched in controlled release of protein and peptide drug because of its excellent mucoadhesive and permeation enhancing effect across the biological surfaces. The control of the size and size distribution of microspheres is necessary in order to improve reproducibility, bioavailability, and repeatable release behavior. In this work, uniform-sized chitosan microspheres containing insulin were prepared by a novel membrane emulsification technique combined with glutaraldehyde crosslinking method. In order to prepare uniform-sized chitosn microspheres, it is necessary to modify hydrophilic membrane into hydrophobicity. It is found that there exists a linear relationship between the size of chitosan microspheres and pore size of the membrane used, so it is easy to control the size of microspheres by using membranes with different pore size. In this study, the effect of different amount of crosslinker and crosslinking time on microspheres' morphology, encapsulation efficiency (EE) and release profile of drug in vitro were investigated. It is shown that the morphology of microspheres is more smooth and spherical, and the release rate is slower with the increase of amount of glutaraldehyde and prolongation of crosslinking time. When the molar ratio of amino group of chitosan to aldehyde group of glutaraldehyde is 1:0.7, and crosslinking time is 1 h, the highest EE was obtained (about 65%). Date obtained suggest that chitosan microspheres prepared by this new method would be a promising system for controlled release of protein drugs.
Biocompatible Materials ; chemistry ; Chitosan ; chemistry ; Cross-Linking Reagents ; Delayed-Action Preparations ; chemical synthesis ; Drug Carriers ; chemical synthesis ; Emulsions ; Glutaral ; chemistry ; Humans ; Insulin ; pharmacokinetics ; Microspheres ; Particle Size