Astragalus polysaccharides was lounded to 4-(2-aminoethylphenol), followed by labeling the APS-Tyr with fluorescein-5-isothiocyanate (FITC) at the secondary amino group. The absorption enhancement effects of low molecular weight chitosan and protamine on astragalus polysaccharides were evaluated via Caco-2 cell culture model. The results show that the fluorecent labeling compound has good stability and high sensitivity. On the other hand low molecular weight chitosan and protamine also can promoted absorption of the astragalus polysaccharides without any cytotoxity, and the absorption increase was more significant with increasing the amount of low molecular weight chitosan and protamine. At the same time, the low molecular weight chitosan has slightly better effect. The transepithelial electric resistance (TEER) of Caco-2 cells show that absorption enhancers could improve its membrane transport permeability by opening tight junctions between cells and increasing the cell membrane fluidity.
Absorption ; Astragalus Plant ; chemistry ; Biological Transport ; Caco-2 Cells ; Fluorescein-5-isothiocyanate ; chemistry ; Fluorescent Dyes ; chemistry ; Humans ; Plant Extracts ; chemistry ; pharmacokinetics ; Polysaccharides ; chemistry ; pharmacokinetics

The difference between three representative components of total salvianolic acids in pharmacodynamic activity were compared by three different pharmacological experiments: HUVECs oxidative damage experiment, 4 items of blood coagulation in vitro experiment in rabbits and experimental myocardial ischemia in rats. And the effects of contribution rate of each component were calculated by multi index comprehensive evaluation method based on CRITIC weights. The contribution rates of salvianolic acid B, rosmarinic acid and Danshensu were 28.85%, 30.11%, 41.04%. Apparent oil/water partition coefficient of each representative components of total salvianolic acids in n-octyl alcohol-buffer was tested and the total salvianolic acid components were characterized based on a combination of the approach of self-defined weighting coefficient with effects of contribution rate. Apparent oil/water partition coefficient of total salvianolic acids was 0.32, 1.06, 0.89, 0.98, 0.90, 0.13, 0.02, 0.20, 0.56 when in octanol-water/pH 1.2 dilute hydrochloric acid solution/ pH 2.0, 2.5, 5.0, 5.8, 6.8, 7.4, 7.8 phosphate buffer solution. It provides a certain reference for the characterization of components.
Animals ; Benzofurans ; chemistry ; pharmacology ; Cinnamates ; chemistry ; pharmacology ; Depsides ; chemistry ; pharmacology ; Lactates ; chemistry ; pharmacology ; Male ; Rabbits ; Rats ; Rats, Sprague-Dawley ; Solubility

To evaluate the properties of solidifying volatile oil with graphene oxide, clove oil and zedoary turmeric oil were solidified by graphene oxide. The amount of graphene oxide was optimized with the eugenol yield and curcumol yield as criteria. Curing powder was characterized by differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The effects of graphene oxide on dissolution in vitro and thermal stability of active components were studied. The optimum solidification ratio of graphene oxide to volatile oil was 1:1. Dissolution rate of active components had rare influence while their thermal stability improved after volatile oil was solidified. Solidifying herbal volatile oil with graphene oxide deserves further study.
Calorimetry, Differential Scanning ; Clove Oil ; chemistry ; Curcuma ; chemistry ; Eugenol ; Graphite ; chemistry ; Microscopy, Electron, Scanning ; Oils, Volatile ; chemistry ; Oxides ; chemistry ; Plant Extracts ; chemistry ; Powders ; Sesquiterpenes

OBJECTIVETo optimize Supper Critical CO2 extracting technical (SFE-CO2) methods for extraction of anti-cancer active components of Fig Residues and to investigate the anti-cancer effect of the extract in vitro and in vivo.

METHODThe anti-cancer activity of extracted compound was measured on U937,95D and AGS cancer cells in vitro by MTT method. The anti-cancer effect of the extraction of Fig Residues was studied on mice transplant liver cancer in vivo.

RESULTThe SFE-CO2 condition for extraction of the anti-cancer components of Fig Residues was optimized as follows: granularity was 100, the extraction pressure was 30 MPa, the extraction temperature was 45 degrees C, the extraction time was 6 h and the CO2 flux was 12 L x h(-1); The IC50 of anti-cancer active components of Fig Residues on U937, 95D and AGS cells were 70.125 microg x mL(-1), 127.957 microg x mL(-1), 116.000 microg x mL(-1); The anti-cancer active components of Fig Residues inhibited 49.3% of the transplanted liver cancer in the mice.

CONCLUSIONThe method for extracting the anticancer active components of Fig Residues is stable and reasonable, and the extract from Fig Residues is of the anticancer effect.

Animals ; Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Chromatography, Supercritical Fluid ; methods ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Female ; Ficus ; chemistry ; Fruit ; chemistry ; Humans ; Inhibitory Concentration 50 ; Liver Neoplasms ; pathology ; Male ; Mice ; Neoplasm Transplantation ; Plants, Medicinal ; chemistry ; Stomach Neoplasms ; pathology ; U937 Cells ; drug effects

In this paper, the action of suet oil in the preparation of self-assembled micelles of the active flavonoids in Epimedium in the simulated human environment was researched. Twelve suet oil samples were collected from different growing areas and different positions of sheep or goat to simulate the formation of micelles. Then the effects of the fatty acids in suet oil on the preparation of self-assembled micelles were studied furthermore. The results showed that the micelles had a dispersed state and spherical smooth surface. To compare the diameter, potential, encapsulation efficiency and drug loading of the 12 batches micelles, the micelles prepared by the suet oil from Qinghai were more stable and had a higher encapsulation efficiency. The fatty acids in suet oil could promote the formation of self-assembled micelles, but the whole suet oil had a better effect. Above all the study, we confirmed that the suet oil promoted the formation of self-assembled micelles of the flavonoids in Epimedium, it laid foundation for further research about increasing the efficacy of Epimedium and improved the absorption of the active flavonoids in Epimedium.
Animals ; Chemistry, Pharmaceutical ; methods ; China ; Drug Carriers ; chemistry ; Electric Conductivity ; Epimedium ; chemistry ; growth & development ; Fatty Acids ; chemistry ; Flavonoids ; chemistry ; Geography ; Goats ; Humans ; Micelles ; Oils ; chemistry ; Sheep

The formulation for sustained release tablet of Epinedium component was selected and the evaluation equation of in vitro release was established. The liquidity of component was improved with the help of colloidal silica aided by spray drying, which would be the main drug in the sustained release tablets. Dissolution was selected as an evaluation index to investigate skeletal material type, fillers, impact porogen, lubricants and other materials on the quality of sustained release tablet. The sustained release tablets were prepared by dry compression. Formulation of sustained release preparations was main drug 35%, HPMC K(4M) 20% and HPMC K(15M) 10% as skeleton material, MCC 31% as filler, PEG6000 2% as porogen and magnesium stearate 2% as lubricant. The sustained release tablets released up to 80% in 8 h. The zero order equation, primary equation and Higuchi equation could simulate the release characteristics of sustained release tablets in vitro, the correlation coefficients r were larger than 0.96. The primary equation was most similar in vitro release characteristics and its correlation coefficient r was 0.9950. The preparation method is simple and the results of formulation selection are reliable. It can be used to guide the production of Epimedium component sustained release preparations.
Chemistry, Pharmaceutical ; methods ; Delayed-Action Preparations ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Epimedium ; chemistry ; Kinetics ; Tablets ; chemistry

In order to evaluate the characteristics of the spray drying of total flavonoids of Epimedium extracts assisted with soybean polysaccharide, a certain percentage of soybean polysaccharide or polyvidone were added to the total flavonoids of Epimedium extract to conduct the spray drying. The effect of soybean polysaccharides against the wall sticking effect of the spray drying was detected, as well as the powder property of total flavonoids of Epimedium spray drying powder and the dissolution in vitro behavior of the effective component. Compared with the total flavonoids of Epimedium spray drying powder, soybean polysaccharide revealed a significant anti-wall sticking effect. The spray drying power which had no notable change in the grain size made a increase in the fluidity, improvement in the moisture absorption and remarkable rise in the dissolution in vitro behavior. It was worth further studying the application of soybean polysaccharide in spray drying power of traditional Chinese medicine.
Epimedium ; chemistry ; Flavonoids ; analysis ; Particle Size ; Polysaccharides ; chemistry ; Powders ; Soybeans ; chemistry

With low molecular weight chitosan and poloxamer 188 as the joint carriers, ginsenoside Rg3 solid dispersions were prepared by using the solvent evaporation method for an in vitro dissolution test. Subsequently, differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray diffraction (X-RD) were adopted for a phase analysis. The results showed that the 60 min in vitro cumulative dissolution rate of ginsenoside Rg3 solid dispersions prepared with low molecular weight chitosan and poloxamer 188 at the ratio of 2:1 exceeded 90%, and the drug was dispersed in carriers in an amorphous state. Therefore, ginsenoside Rg3 solid dispersions prepared with low molecular weight chitosan and poloxamer 188 could help significantly improve the drug dissolution, with a practical application value.
Chitosan ; chemistry ; Drug Compounding ; methods ; Ginsenosides ; chemistry ; Molecular Weight ; Poloxamer ; chemistry ; Solvents ; chemistry

Objective To explore the relationship between insulin resistance and other metabolic disorders in patients with essential hypertension (EH).Methods Glucose metabolism rate (GMR) was measured by euglycemic insulin clamp technique,and salt sensitivity was tested by increase in blood pressure after salt load and its decreases alter depletion of sodium in 26 healthy subjects and 84 patients with EH.Results GMR lowered significantly in patients with EH than that in healthy subjects,P

Objectives To study the level and development of serum specific antibody against severe acute respiratory syndrome coronavirus(SARS-CoV)of different populations in SARS pestilence district after SARS outbreak in a general hospital.Discuss SARS sub-clinical infection and protective action of the IgG antibody.Methods Seroepidemiology method,enzyme-linked immunosorbent assay (ELISA)and indirect immunfluorescence assay(IFA)were employed to investigate the changing level of serum antibody to SARS-associated coronavirus in non-SARS population in SARS pestilence district during and after SARS outbreak.The development of IgM and IgG antibody in patients with SARS in 6 weeks after the onset of SARS was studied qualitatively.The level changing of IgG antibody in con- valescent patients with SARS in 82 weeks after the onset was observed dynamically.Results The ELISA test outcome of IgG antibody was negative in 200 non-SARS people who were random samples of normal mass in SARS pestilence district and common community.The positive rate was 0.41% in 487 SARS high risk population tested by ELISA,but showed negative when retested by IFA.The A value level of IgG antibody existed significant difference in non SARS mass during and after SARS outbreak and the later's was higher them the former's(P