AIM:To select an optiomal formulation of liposome entrapped alkanin prepared with ethanol injection in the combination of orthogonal design and central composite design/Response surface method.METHODS:Five influencing factors,including ratio of alkanin to liposome and soyabean lecithin to cholesterol,volume ratio of ethanol phase to water phase,soybean concentration and mannitol concentration were chosen as indices by orthogonal design.Then the method utilized the central composite design,which fitted multivariate linear and second/third order nonlinear regression equation,to find out the optimal formulation.RESULTS:Third order regression equation gained made the good prediction about entrapment(85.4%) and alkanin load(5.16%),and exhibited no significant difference between theoretic value and measured value.CONCLUSION:The combination of orthogonal design with central composite design is a feasible and convenient method to optimize the prescription of alkanin-lipo-some.

AIM:To select an optiomal formulation of liposome entrapped alkanin prepared with ethanol injection in the combination of orthogonal design and central composite design/Response surface method.METHODS:Five influencing factors,including ratio of alkanin to liposome and soyabean lecithin to cholesterol,volume ratio of ethanol phase to water phase,soybean concentration and mannitol concentration were chosen as indices by orthogonal design.Then the method utilized the central composite design,which fitted multivariate linear and second/third order nonlinear regression equation,to find out the optimal formulation.RESULTS:Third order regression equation gained made the good prediction about entrapment(85.4%)and alkanin load(5.16%),and exhibited no significant difference between theoretic value and measured value.CONCLUSION:The combination of orthogonal design with central composite design is a feasible and convenient method to optimize the prescription of alkanin-liposome.

Berberine is an isoquinoline alkaloid isolated from Rhizoma Coptidis and Cortex Phellodendri,which has a long medical history in China.Recent studies have indicated that berberine has multiple pharmacological activities including anti-inflammatory,anti-microorganisms,anti-cancer,cardiac protection,glucose lowering,regulating lipid metabolism and immune suppression.Berberine has been used for the treatment of intestinal infectious diseases for many years.With the continuous progress of the research,it is reported that berberine has many new clinical applications,including treatment of the cardiovascular disease,metabolic syndrome and its complications,cancers,abdominal adhesions and chlamydia trachomatis infection.This review is intended to introduce the role of berberine in various aspects of pharmacological effects,molecular mechanisms and clinical applications.

The intracellular hepatitis B surface antigen (HBsAg) content per cell was increased by 7.2-fold in the culture with 1.5% dimethyl sulfoxide (DMSO) compared with that in the control without DMSO, while the extracellular HBsAg production and specific productivity were only improved by 70% and 3.2-fold, respectively. Electron microscope has been employed to reveal large dilated structures within recombinant CHO cells in the presence DMSO. The dilated structures have a distribution within whole cytoplasm, and some dilated areas were engulfed in the nucleus. These large, dilated structures were not observed in the control. Immunogold labeling was used to discover the accumulated HBsAg was localized within these dilated areas, and some HBsAg-specific labels were detected in the nucleus membrane, owing to the encroachment of the dilated areas upon nucleus. The result could help to reveal the mechanism of intracellular HBsAg accumulation in the presence of DMSO.

Objective To investigate the affecting factors of interventricular septum (IVS) swing by study of the mechanical model of the respiration-driven variation of cardiac function using echocardiography.Methods In present study,the equivalent mechanical model of septal swing in previous study was used.By changing the end-diastolic pressure difference between the simulated right and left ventricles and simulated intrapericardial pressure,the subsequent influences on IVS swing using echocardiography were observed.Results Under the rhythmic respiratory intrathoracic pressure change(RIPC)(0--4 mm Hg,1 mm Hg =0.133 kPa),the swing amplitude of simulated IVS increased with decrease of the simulated end-diastolic pressure difference between the simulated right and left ventricles (2.2-17.6 mm).With increasing of the simulated intrapericardial pressure,the simulated right ventricle and left ventricle collapsed in succession,the swing amplitude of simulated IVS also increased to a maximal amplitude of 22.4 mm.Conclusions The affecting factors of IVS swing including the magnitude of RIPC,the end-diastolic pressure difference between the two ventricles and the intrapericardial pressure.

Objective To observe the peripheral arterial Doppler flow velocity curve changes and elucidate the blood flow characteristics by adding extra pressure on the limbs,and to provide evidence for better diagnosis of peripheral arterial diseases by ultrasound.Methods Color Doppler ultrasound instrument was used to record the brachial artery(BA),radial artery(RA),common femoral artery(CFA) and popliteal artery(POA) Doppler flow velocity curves both at rest and under different grades of distal and proximal limb pressuring in 40 randomly selected healthy adults.The peak systolic and early diastolic reverse flow velocity(PSV,PRV) and the resistance index (RI) were measured and analyzed.Results Three-phase waveform was seen at rest.Significant changes were noticed in PRV and RI under distal pressuring,while no significant difference was seen in PSV between groups.Conclusions Normal peripheral arteries show pulsed step-by-step blood flow pattern along with the cardiac cycles.Peripheral arterial Doppler flow curves changes regularly with limb grading pressuring.

The epieardial adipose tissue in 210 subjects with or without metabolic syndrome (MS) was measured by echocardiography.The thickness of epicardial adipose tissue in male with MS group was significantly greater than that in men without MS [(9.10?3.59) mm vs (6.82?3.00) mm,P

To study the effect of Tibetan medicine Zuotai on the activity, protein and mRNA expression of CYP1A2 and NAT2, three different doses (1.2, 3.8 and 12 mg x kg(-1)) of Zuotai were administrated orally to rats once a day or once daily for twelve days, separately. Rats were administrated orally caffeine (CF) on the second day after Zuotai administration, and the urine concentration of CF metabolite 5-acetylamino-6-formylamino-3-methyl-uracil (AFMU), 1-methyluric acid (1U), 1-methylxanthine (1X), 1, 7-dimethylxanthine (17U) at 5 h after study drug administration was determined by RP-HPLC. The activity of CYP1A2 and NAT2 was evaluated by the ratio of metabolites (AFMU+1X+1U)/17U and the ratio of AFMU/(AFMU+1X+1U), respectively. The protein and mRNA expression of CYP1A2 and NAT2 were determined by ELISA and RT-PCR method, respectively. After single administration of Zuotai 3.8 mg x kg(-1) and repeated administration of Zuotai 3.8 and 12 mg x kg(-1), the activity of CYP1A2 and NAT2 decreased significantly compared with control group and there was no significant difference between other dose group and control group. The protein expression of CYP1A2 was significant lower than that in control group after repeated administration of Zuotai 12 mg x kg(-1), and the mRNA expression of CYP1A2 decreased significantly compared with that of control group after single administration of Zuotai 3.8 mg x kg(-1) and repeated admistration of Zuotai 12 mg x kg(-1), separately. The protein expression of NAT2 decreased significantly compared with that of control group after single and repeated administration of Zuotai 3.8 mg x kg(-1), respectively, and the mRNA expression of CYP1A2 decreased significantly compared with control group after single administration of Zuotai 3.8 mg x kg(-1). This study found that Tibetan medicine Zuotai had significant effect on the activity, protein and mRNA expression of CYP1A2 and NAT2.
Administration, Oral ; Animals ; Arylamine N-Acetyltransferase ; genetics ; metabolism ; Caffeine ; metabolism ; urine ; Cytochrome P-450 CYP1A2 ; genetics ; metabolism ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; Female ; Male ; Medicine, Tibetan Traditional ; RNA, Messenger ; metabolism ; Rats ; Rats, Sprague-Dawley ; Theophylline ; urine ; Uracil ; analogs & derivatives ; urine ; Uric Acid ; analogs & derivatives ; urine ; Xanthines ; urine

OBJECTIVETo observe the uptake of tiliani in Caco-2 Cell.

METHODA human intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study the kinetics of uptake, transport and efflux kinetics of tiliani at small intestine. The effect of time, pH, drug concentration and inhibitors on the uptake of tiliani were investigated. The determination of tiliani was performed by HPLC.

RESULTTiliani in Caco-2 cell uptake was time-dependent. Tiliani in Caco-2 cell uptake was concentration-dependent at 4-16 mg x L(-1) consistent with passive diffusion process. The acid condition was good for the uptake of tiliani at pH 5-8. Compared with the control group, tiliani cell uptake was significantly higher after additional treatmeant with verapamil (1.545 +/- 0.010) mg x g(-1), (P < 0.05), and tiliani cell uptake was significantly lower after additional treatmeanet with sodium azide (0.994 +/- 0.003) mg x g(-1) (P < 0.05), with 2,4-dinitrophenol (1.174 +/- 0.030) mg x g(-1) (P < 0.05), and with phloridzin (1.098 +/- 0.021) mg x g(-1) (P < 0.05). Compared with the control group, tiliani cell uptake was not significantly after additional treatmeant with lactose (1.470 +/- 0.025) mg x g(-1), Papp of Basolateral to Apical was much more than that of Apical to Basolateral (1.10 Fold).

CONCLUSIONP-glycoproteins and SGLT1 participate in the conveying process of tiliani in Caco-2 cells. The uptake of tiliani has no relationship to LPH. passive transport and carrier-mediated transport participate in the uptake process of tiliani in Caco-2 cells.

Biological Transport ; drug effects ; Caco-2 Cells ; Chromatography, High Pressure Liquid ; Flavonoids ; pharmacokinetics ; Glycosides ; pharmacokinetics ; Humans ; Intestinal Absorption ; Kinetics ; Verapamil ; pharmacology

We predicted the anti-hepatitis B virus (HBV) active components and mechanism of Salvia miltiorrhiza based on network pharmacology. The active components of S. miltiorrhiza were obtained through TCMSP, PubChem database and literature research. The potential targets of the active components and HBV infection were predicted by SwissTargetPrediction and GeneCards databases, respectively. The protein-protein interaction (PPI) network was constructed by String database. Cytoscape software was adopted to construct a visual network of active component-disease target and perform topological analysis. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were performed using DAVID platform. The molecular docking of key components and core targets was carried out by AutoDock Vina software. We screened out a total of 38 active components and 178 disease-component overlapping targets. Enrichment analyses obtained 405 related GO items and 68 signaling pathways, such as T/B cell receptor signaling pathways, PI3K/AKT signaling pathway, and mTOR signaling pathway. According to the results of molecular docking, most characteristic components of S. miltiorrhiza (miltionone Ⅱ, miltirone, protocatechuic acid, lithospermic acid, protocatechualdehyde) showed good affinity with the key targets (PIK3CA, APP, STAT3,AKT1 and mTOR). Furthermore, the anti-HBV activity of lithospermic acid, the representative active component of S. miltiorrhiza, and its regulation on PI3K/AKT and mTOR signaling pathways were investigated in an HBV replicating mouse model. Animal welfare and experimental procedures follow the regulations of the Animal Ethics and Welfare Committee of Hubei University. The results showed that lithospermic acid significantly inhibited HBV DNA replication, reduced serum HBsAg and HBeAg levels, and decreased the phosphorylation protein expression levels of AKT and mTOR in liver, indicating that lithospermic acid might exert the anti-HBV activity by regulating PI3K/AKT and mTOR signaling pathways.