Objective To investigate the permeability changes of prostate cancer cells membrane under low intensity ultrasound in vitro.Methods The culture of monolayer adherent LNCaP prostate cancer cells in six-well plate was exposed to continuous ultrasound at frequency of 1 MHz.The cells membrane permeability (stained with Calcein)and cells viability(stained with PI)were evaluated by fluorescent microscope (FM) and cells morphological changes were evaluated by scanning electron microscope (SEM) under ultrasound with acoustic intensity of 160 mW/cm2 for 5 s.The rate of cells with increased cells membrane permeability as function of acoustic intensity (80 mW/cm2,120 mW/cm2 and 160 mW/cm2,for 5 s) and exposure duration (5 s,10 s and 15 s,acoustic intensity of 120 mW/cm2) was evaluated by flow cytometry.ResultsAfter low intensity of ultrasound,the cells with increased cell membrane permeability could be clearly shown with Calcein uptake under FM while no cell showed Calcein uptake in the control group.The SEM showed less microvilli on the cells after low intensity of ultrasound exposure and few cells showed holes on the cell membrane.The rate of cells with increased membrane permeability increased with acoustic intensity and exposure duration.Conclusion Low intensity ultrasound alone could increase membrane permeability of prostate cancer cells and cells with increased membrane permeability showed surface plane,uncommon holes on the cells membrane.The rate of cells with increased membrane permeability positively correlated with acoustic intensity and exposure duration.

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

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

Objective To compare the curative effect of high ligation+exfoliation and subfascial endoscopic perforator surgery(SEPS)for superficial varicose veins in calf+invagination spot-striping surgery in great venous varicosity.Methods Study group(42 patients)accepted SEPS+invagination spot-striping surgery and control group (42 patients)accepted traditional surgeries.Operation duration,bleeding volume in operation,the time of beginning movement away from bed after operation,hospitalization duration,the degree of pain,the scar,the recrudescence af- ter operation and the instance of the ulcer heals of two groups were compared.Results Operation duration,bleeding volume in operation,the time of begin movement away from bed after operation and hospitalization durations of study group were significantly lower than those of control group(P0.05).All of the patients in study group recovered without severe syndromes such as venous thrombosis,skin necrosis,lower limb functional disorder etc.They had no recrudesce after 4～16 months and were satisfied with the curative effect.Con- elusions The clinical curative effect of SEPS+invagination spot-striping surgery in great venous varicosity is superi- or to that of traditional operation and it has the advantages such as minor wound,few scars,light pains,short hospi- talization duration,without recrudescence,the ulcer heals quickly and so on.

Baicalin extremely fine powder was made by using ball-mill and the effect of micronization on the micromeritics properties of baicalin was studied and analyzed. The microstructures of baicalin ordinary and extremely fine powder were compared by scanning electron microscope, differential scanning calorimeter and X-ray diffraction and the powder characteristic of them was investigated. The hygroscopicity was studied. The effect of micronization on the dissolution of baicalin was investigated. The results showed that the chemical constituents of baicalin were not changed after micronization with better compressibility. It was confirmed that micronization technology had a certain application value in promoting the insoluble component of baicalin absorption with higher dissolution.
Calorimetry, Differential Scanning ; Drugs, Chinese Herbal ; chemistry ; Flavonoids ; chemistry ; Particle Size ; Solubility ; Wettability ; X-Ray Diffraction

To prepare sagittatoside B with epimedin B Hydrolyzed from cellulase. With the conversion ratio as the index, the effects of pH value, temperature, reaction time, dosage of enzyme and concentration of substrates on the conversion ratio were detected. L9 (3(4)) orthogonal design was adopted to optimize the preparation process. Hydrolyzed products were identified by MS, 1H-NMR, and 13C-NMR. The results showed that the optimum reaction conditions for the enzymatic hydrolysis were that the temperature was 50 degrees C, the reaction medium was pH 5.6 acetic acid-sodium acetate buffer solution, the concentration of substrates was 20 g x L(-1), the mass ratio between enzyme and substrate was 3: 5, and the relative molecular mass of the reaction product was 646.23. NMR data proved that the product was sagittatoside B. The process is simple and reliable under mild reaction conditions, thus suitable for industrial production.
Cellulase ; metabolism ; Drug Compounding ; methods ; Flavonoids ; chemistry ; Hydrogen-Ion Concentration ; Hydrolysis ; Temperature ; Time Factors

To prepare salvianolic acid phospholipid compound. With the compound of salvianolic acids and soybean phospholipid as the index, mono-factor experiment and orthogonal design experiment were conducted to screen its technical parameters. According to the results, the optimal preparation conditions of salvianolic acid phospholipid compound were that THF were taken as the reaction solvent, the concentration time was 3 h, the reactant concentration was 5 g x L(-1), the mass ratio of salvianolic acids and phospholipid was 1: 1.5, and the reaction temperature was 40 degrees C. The oil/water partition coefficient of the prepared salvianolic acid phospholipid compound significant increased in water and buffers with different pH values. The results of phase analysis such as DSC, XRD and FTIR indicated that salvianolic acids existed in phospholipid in an amorphous state.
Alkenes ; chemistry ; metabolism ; Chemical Phenomena ; Chemistry, Pharmaceutical ; methods ; Intestinal Absorption ; Phospholipids ; chemistry ; Polyphenols ; chemistry ; metabolism ; Soybeans ; chemistry ; Temperature

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 purpose of this research was to prepare total salvianolic acids-phytosome-HA coprecipitate to improve drug dissolution and its micromeritic properties. Firstly, the coprecipitate was prepared by solvent method and in vitro dissolution of tripterine was performed with the salvianolic acid B and danshensu as criteria. At the same time, the micromeritic properties was characterizated, the structure of samples was characterized by TEM, DSC, XRD and FTIR. Results showed that when the ratio of drug to HA was 1:2, it had a better dissolution, the accumulative drug-release percent in vitro at 60 min was over 90%. At the same time, it has good liquidity and low moisture absorption. Its micromeritic properties have improved. It is proved that the drug still existed amorphously by microstructure analysis. The preparation process is simple and feasible, it has practical value.
Alkenes ; chemistry ; Chemical Precipitation ; Chemistry, Pharmaceutical ; methods ; Durapatite ; chemistry ; Phospholipids ; chemistry ; Polyphenols ; chemistry ; Time Factors