1.Permeability increase of prostate cancer cells membrane under low intensity ultrasound in vitro
Ji-zhen, ZHANG ; E, SHEN ; Bing, HU
Chinese Journal of Medical Ultrasound (Electronic Edition) 2010;07(12):2025-2030
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.
2.Study on preparation of sagittatoside B with epimedin B converted from cellulase.
Feng-Juan XU ; E SUN ; Zhen-Hai ZHANG ; Li CUI ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2014;39(2):235-239
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
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metabolism
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Drug Compounding
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methods
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Flavonoids
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chemistry
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Hydrogen-Ion Concentration
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Hydrolysis
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Temperature
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Time Factors
3.Study on preparation of salvianolic acid phospholipid compound.
Xiao-Yun CHEN ; Zhen-Hai ZHANG ; Dan LIU ; Dan-Hong YU ; E SUN ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2014;39(2):216-221
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
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chemistry
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metabolism
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Chemical Phenomena
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Chemistry, Pharmaceutical
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methods
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Intestinal Absorption
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Phospholipids
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chemistry
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Polyphenols
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chemistry
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metabolism
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Soybeans
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chemistry
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Temperature
4.Study on oral absorption enhancers of astragalus polysaccharides.
Xiao-Yun CHEN ; Xiao-Bin TAN ; E SUN ; Dan LIU ; Xiao-Bin JIA ; Zhen-Hai ZHANG
China Journal of Chinese Materia Medica 2014;39(7):1243-1247
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
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Astragalus Plant
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chemistry
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Biological Transport
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Caco-2 Cells
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Fluorescein-5-isothiocyanate
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chemistry
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Fluorescent Dyes
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chemistry
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Humans
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Plant Extracts
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chemistry
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pharmacokinetics
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Polysaccharides
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chemistry
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pharmacokinetics
5.Studies on hydroxyapatite applicatied in coprecipitate of total salvianolic acids phospholipid complex.
Xiao-Yun CHEN ; Zhen-Hai ZHANG ; Dan LIU ; E SUN ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2014;39(6):992-996
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
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chemistry
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Chemical Precipitation
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Chemistry, Pharmaceutical
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methods
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Durapatite
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chemistry
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Phospholipids
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chemistry
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Polyphenols
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chemistry
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Time Factors
6.Study on totai flavonoids of Epimedium assisted with soybean polysaccharide spray-drying powder.
Hong-mei YAN ; Xiao-bin JIA ; Zhen-hai ZHANG ; E SUN ; Jia-hui DENG
China Journal of Chinese Materia Medica 2015;40(15):2994-2998
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
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chemistry
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Flavonoids
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analysis
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Particle Size
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Polysaccharides
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chemistry
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Powders
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Soybeans
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chemistry
7.Clinicopathological analysis on renal primitive neuroectodermal tumor.
Shilan LI ; Hai LI ; Zhen WANG ; Minhong PAN ; Qinhe FAN ; Zhihong ZHANG
Chinese Journal of Pathology 2015;44(11):788-789
8.Study on solid dispersion of precipitated calcium carbonate-based oleanolic acid.
Hong-mei YAN ; Zhen-hai ZHANG ; Xiao-bin JIA ; Yan-rong JIANG ; E SUN
China Journal of Chinese Materia Medica 2015;40(10):1935-1938
Oleanolic acid-precipitated calcium carbonate solid dispersion was prepared by using solvent evaporation method. The microscopic structure and physicochemical properties of solid dispersion were analyzed using differential scanning calorimetry and scanning electron microscopy (SEM). And its in vitro release also was investigated. The properties of the precipitated calcium carbonate was studied which was as a carrier of oleanolic acid solid dispersion. Differential scanning calorimetry analysis suggested that oleanolic acid may be present in solid dispersion as amorphous substance. The in vitro release determination results of oleanolic acid-precipitated calcium carbonate (1: 5) solid dispersion showed accumulated dissolution rate of.oleanolic acid was up to 90% at 45 min. Accelerating experiment showed that content and in vitro dissolution of oleanolic acid solid dispersion did not change after storing over 6 months. The results indicated that in vitro dissolution of oleanolic acid was improved greatly by the solid dispersion with precipitated calcium carbonate as a carrier. The solid dispersion is a stabilizing system which has actual applied value.
Calcium Carbonate
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chemistry
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Calorimetry, Differential Scanning
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Chemistry, Pharmaceutical
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Drug Carriers
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chemistry
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Drug Stability
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Microscopy, Electron, Scanning
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Oleanolic Acid
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chemistry
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Plant Extracts
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chemistry
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Solubility
9.Study on porous starch as solid dispersion carrier of total Epimedium flavonoids.
Hong-mei YAN ; Xiao-bin JIA ; Zhen-hai ZHANG ; E SUN ; Yi-hao XU
China Journal of Chinese Materia Medica 2015;40(9):1723-1726
In order to evaluate the characteristic of porous starch (PS) as the solid dispersions carrier of the total Epimedium flavonoids (TEF), the PS was used. The dissolution of icariin was selected as an indicator to analyze the differences of dissolution between TEF and its solid dispersion. TEF was characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). Solid dispersion was irregular block and no powder characteristics of TEF and PS could be seen in SEM, DSC and XRD analysis suggested that TEF may be present in solid dispersion as amorphous substance. The dissolution rate of icariin has been improved significantly when the proportion of TEF and PS was 1:2. PS as a traditional solid dispersion carrier is worthy of further study.
Calorimetry, Differential Scanning
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Chemistry, Pharmaceutical
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Drugs, Chinese Herbal
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chemistry
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Epimedium
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chemistry
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Flavonoids
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chemistry
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Porosity
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Solubility
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Starch
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chemistry
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X-Ray Diffraction
10.Solidification of volatile oil with graphene oxide.
Hong-Mei YAN ; Xiao-Bin JIA ; Zhen-Hai ZHANG ; E SUN ; Yi-Hao XU
Acta Pharmaceutica Sinica 2015;50(2):222-226
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
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Clove Oil
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chemistry
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Curcuma
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chemistry
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Eugenol
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Graphite
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chemistry
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Microscopy, Electron, Scanning
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Oils, Volatile
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chemistry
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Oxides
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chemistry
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Plant Extracts
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chemistry
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Powders
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Sesquiterpenes