AIM:To investigate whether Notch1 changes stemness and chemotherapeutic sensitivity in human glioma U251 cells.METHODS: The lentiviral vectors, which expressed Notch1-shRNA or Notch1 intracellular domain ( NICD) , were transfected into U251 cells .Western blot and immunofluorescence staining were applied to monitor the va-lidity of the cells, down-regulation of Notch1 expression or over-expression of NICD.The proportion of CD133 +cells was analyzed by flow cytometry.The expression of nestin and GFAP was identified by immunofluorescence staining.The forma-tion rate of tumor cell spheres and the implanted tumor growth in SCID mice were observed.MTT assay was performed to e-valuate the chemotherapeutic sensitivity to VM-26 and BCNU of the cells with different treatments.RESULTS:Stemness was significantly enhanced in the cells over-expressing NICD.For example, the proportion of CD133 +cells was increased, the expression of nestin was up-regulated, the expression of GFAP was down-regulated, and the formation rate of tumor cell spheres and implanted tumor growth were increased.The chemotherapeutic sensitivity to VM-26 and BCNU of the cells was decreased.In the cells with Notch1 gene down-regulation by RNAi, the stemness was inhibited and chemotherapeutic sensi-tivity was increased.CONCLUSION:Notch1, which leads to the change of stemness and chemotherapeutic sensitivity in human glioma U251 cells, is likely to be a potential molecular target for treatment of glioma.

To investigate the delivery mechanism of micro-porous osmotic pump tablets ( MPOP), taking tramadol hydrochloride ( TR) as the model drug, tramadol hydrochloride micro-porous osmotic pump tablets (TR MPOP) were prepared with compressible starch as diluent, cellulose acetate as coating material, polyethylene glycol 400 as pore-forming agents. The equilibrium solubility and osmolality of TR were determined. The effects of fillers in tablet cores, coating levels, and osmotic pressures of release media on expansion behavior of preparations were described. The influences of the category, osmolality, and pH value of release media, release methods, and release conditions on release curves of tablets were evaluated. Based on several models, the delivery pattern of TR MPOP was fitted. The equilibrium solubility in water and osmolality of TR were (775.8 +/- 17.7) g x L(-1) and 4.036 Osmol x kg(-1), respectively. During the drug-release period, it was observed that the tablets expanded markedly in response to the expansion characteristics of compressible starch and the osmotic pressure difference across the membrane. When osmotic pressure of release media increased, the significant change of the equilibrium solubility of TR was not found, but the release rates of TR MPOP decreased significantly. The delivery rate was not influenced by the pH of release mediums, dissolution methods and paddle stirring rates. The drug release profile conformed to the model of zero order in 8 h. The pore-forming agents were dissolved in release medium, which caused micro-pores. The expansion of tablets made the size of micropores bigger, and then the drug-releasing pores were obtained. It was proved that the drivers of drug delivering from TR MPOP were mainly the difference of osmotic pressure, and secondly the difference of solubility. TR MPOP were the controlled-release preparation.
Analgesics, Opioid ; administration & dosage ; chemistry ; Cellulose ; analogs & derivatives ; chemistry ; Delayed-Action Preparations ; Drug Carriers ; Drug Delivery Systems ; methods ; Drug Stability ; Osmosis ; Osmotic Pressure ; Polyethylene Glycols ; chemistry ; Porosity ; Solubility ; Starch ; chemistry ; Tablets, Enteric-Coated ; Technology, Pharmaceutical ; methods ; Tramadol ; administration & dosage ; chemistry ; pharmacokinetics

Objective To study the relationship between the clinical manifestations and changes of pituitary magnetic resonance imaging(MRI) in short stature children with growth hormone deficiency(GHD).Methods The pituitary MRI finding in 38 cases of short stature children diagnosed as GHD(males 23,females 15;5-14 years old,10 children were in pubertas and Tanner Ⅱ-Ⅲ) were analyzed,and the pituitary morphology,size,signal and pituitary stalk's shape and location were observed.SPSS 12.0 soffware was used to analyze the data.Results The forms of pituitery were plaque in 20 children(53%),cupped in 17 children(45%),and carinate in 1 children.In the 22 cases of completely GHD,18 cases had different levels of anterior pituitary dysplasia,abnormal pituitary stalk and/or pituitary signal changes,5 cases without posterior lobe disappeared high signal and 4 cases with pituitary stalk interruption syndrome;the other 4 cases had completely normal pituitary.In the 16 cases of partially GHD,7 cases had varying degrees of pituitary size and/or abnormal pituitary stalk,8 cases had completely normal pituitary,and 1 case had pituitary adenoma.Conclusion Pituitary MRI could assist diagnosis and evaluate pituitary function in short stature children.

Brain Neoplasms ; metabolism ; pathology ; surgery ; Diagnosis, Differential ; Humans ; Infant ; Magnetic Resonance Imaging ; Male ; Neoplasm Recurrence, Local ; Nestin ; metabolism ; Neuroectodermal Tumors, Primitive ; metabolism ; pathology ; surgery ; Temporal Lobe ; Vimentin ; metabolism

The main chemical constituents in plants of genus pteris include diterpenoids, diterpenoid glycosides, flavonoids, flavonoid glycosides, sesquiterpenoids and volatile oils, etc. Some of extracts show the following activities, such as antitumor, antifungi and antibacteria. Some of compounds have inhibitory effect on platelet aggregation and antiinflamatory action. The latest progress on chemical constituents and pharmacological activity were reviewed in the paper. Main problems and study directions in future of pteris were indicated.
Animals ; Anti-Bacterial Agents ; isolation & purification ; pharmacology ; Antifungal Agents ; isolation & purification ; pharmacology ; Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; Diterpenes ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Flavonoids ; chemistry ; isolation & purification ; Humans ; Molecular Structure ; Plants, Medicinal ; chemistry ; Pteris ; chemistry ; Sesquiterpenes ; chemistry ; isolation & purification

OBJECTIVETo establish the quality standard of PsL injections containing mainly 5F (ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid).

METHODThe identification of PsL was performed by thin-layer chromatography, and the content was determined by HPLC. The column was Hypersil C18 (4.6 mm x 250 mm, 5 microm), the mobile phase was the mixture of methane-water-acitic acid (55:45: 0.045) with a flow rate of 1.0 mL x min(-1), the detective wavelength was 254 nm, and the column temperature was maintained at 35 degrees C. The pH value and K+ content of the three batchs injection were determined with pH meter and flame photometric meter, and the contents of tannin, protein, oxalic acid salt and heavy metals were detected by deferent methods.

RESULTThe TLC method was suitable for the identification of PsL5F. The linearity for 5F was obtained over the range of 30-240 microg x mL(-1) (r = 0.999 8), the average recovery of 5F was 99.8%. The injections were of pH value range from 7.80 to 8.20, K+ contents less than 10 mmol x L(-1), and the contents of tannin, protein, oxalic acid salt and heavy metals were qualified with the Chinese pharmacopoeia, respectively.

CONCLUSIONIt's sensitive and reliable that can be used as quality control methods of PsL5F injections.

Chromatography, High Pressure Liquid ; Chromatography, Thin Layer ; Diterpenes ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Injections ; Reproducibility of Results

OBJECTIVETo understand the prevalence of HBV core promoter mutant (T1762 A1764 mutant) isolated from asymptomatic carriers from areas with higher and lower incidence of hepatocellular carcinoma (HCC) in Guangxi.

METHODSA nested polymerase chain reaction (nPCR) was used for amplification of HBV DNA core promoter in sera, and then HBV DNA nPCR products were sequenced by direct sequencing.

RESULTSThe results show that 50.6% (39/77) of all HBV asymptomatic carriers were positive for HBV DNA HBV DNA positive rates of the samples from HCC higher incidence area, Longan County, and from lower incidence area, Guilin city were 55.6% (20/36) and 46.3% (19/41), respectively. HBV core promoter mutants could be seen in 35% in Longan positive samples and 47.4% in Guilin. The common mutations in both regions were all double mutations (nt 1,762 A-->T; nt 1,764 G-->A), accounting for 25% and 21%, respectively. The difference of the double mutant between Longan County and Guilin city was not significant (P>0.05).

CONCLUSIONSThese data implicated that the prevalence of HBV core promoter mutant isolated from asymptomatic carriers may not be correlated with the incidence of HCC in Guangxi.

Adolescent ; Adult ; Carcinoma, Hepatocellular ; virology ; Carrier State ; virology ; DNA, Viral ; genetics ; Female ; Hepatitis B ; virology ; Hepatitis B Core Antigens ; genetics ; Hepatitis B virus ; genetics ; Humans ; Liver Neoplasms ; virology ; Male ; Middle Aged ; Point Mutation ; Promoter Regions, Genetic ; genetics

OBJECTIVETo explore the relationship between HBV core promoter mutations and liver damage or HBeAg status.

METHODSNested polymerase chain reaction (nPCR) was used for amplification of HBV DNA core promoter in 59 sera from patients with chronic hepatitis B in Guangxi, then the HBV DNA positive products were sequenced by direct sequencing.

RESULTSThe HBV DNA positive rate of was 59.3%(35/59). All the patients were infected by mutants. The commonest mutation was the double mutation (A --> T at nt1762 and G --> A at nt1764), counting for 57.1% (20/35). The next was C --> G at nt1799, counting for 54.4% (19/35), but this was no function. A --> G at nt1752 (resulting in isoleucine to valine) was seen in 37.1% (13/35) of the HBV DNA positive patients, and T --> C at nt1753 was seen in 20% (7/35). The significant difference in the frequency of T1762A1764 mutant was found between HBeAg positive patients (31.3%) and negative patients (79.0%).

CONCLUSIONSHBV core promoter mutations are common among patients with chronic hepatitis B in Guangxi. T1762A1764 mutant is associated with HBeAg status and chronic hepatitis.

Adolescent ; Adult ; Female ; Hepatitis B Core Antigens ; genetics ; Hepatitis B e Antigens ; blood ; Hepatitis B virus ; genetics ; isolation & purification ; Hepatitis B, Chronic ; virology ; Humans ; Liver ; pathology ; Male ; Middle Aged ; Point Mutation ; Promoter Regions, Genetic ; genetics

The effects of cephradinum and ceftazidime on the metabolism of Escherichia coli (E. coli) DH5alpha was determined by microcalorimetry. The microbial activity was recorded as power-time curves through an ampoule method with a TAM Air Isothermal Microcalorimeter at 37 degrees C. The parameters such as the growth rate constant (k), inhibitory ratio (I), the maximum power output (Pm) and the time (tm) corresponding to the maximum power output were calculated. The results show that the ceftazidime has a better inhibitory effect on E. coli DH5alpha than cephradinum.
Anti-Bacterial Agents ; administration & dosage ; pharmacology ; Calorimetry ; methods ; Ceftazidime ; administration & dosage ; pharmacology ; Cephradine ; administration & dosage ; pharmacology ; Escherichia coli ; drug effects ; growth & development ; metabolism ; Microbial Sensitivity Tests

Adolescent ; Adult ; Aged ; China ; epidemiology ; Female ; Humans ; Hypertension ; epidemiology ; etiology ; Male ; Mass Screening ; Middle Aged ; Risk Factors ; Rural Health ; statistics & numerical data ; Sampling Studies