HepG2 ceils were treated with various concentrations of tumor necrosis factor-or (TNF-α) for 24 hours. RT-PCR and Western blot were used to measure protein tyrosine phosphatase-1 B(PTP-1B)expression, and luciferase reporter assay was used to detect NF-kB activity. The results showed that treatment of HepG2 cells with TNF-α for 24 hours led to upregulation of PTP-1B and NF-kB activity in a dose-dependent manner. Inhibition of NF-kB by PI)TC significantly attenuated TNF-α-induced PTP-IB expression in HepG2 cells. Thus, the transactivation of NF-kB seems to play an important role in the expression of PTP-1B in HepG2 cells induced by TNF-α.

A lactoferrin-containing PEGylated liposome system (Lf-PLS) was developed and tested in vitro as a hepatoma-targeting drug delivery system. PEGylated liposomes (PLS) were successfully prepared using the thin film hydration method with peglipid post insertion. Lf was covalently conjugated onto the carboxyl terminal of DSPE-PEG2000-COOH on liposomes. Coumarin-6 was used to trace Lf-PLS with fluorescence. The cellular uptake of this system was carried out in asialoglycoprotein receptor (ASGPR) positive HepG2 cells via confocal microscopy and flow cytometry. The Lf-PLS liposome was observed as spherical or oval vesicles with the particle size around 130 nm, zeta potential about -30 mV and encapsulation efficiency more than 80%. The confocal microscopy images and flow cytometry data demonstrated that Lf-PLS resulted in significantly higher cell association by ASGPR positive HepG2 cells compared to PLS. The association between Lf-PLS and cells were dependent on the concentration, time and temperature, which was inhibited by pre-incubation with excessive free Lf. The results suggest that Lf-PLS has a good targeting effect on HepG2 cells in vitro. The targeting mechanism may be related to the specific binding of Lf and ASGPR on HepG2 cells, which guides Lf-PLS to the cell surface to induce an active endocytosis process. All these results demonstrated that Lf-PLS might be a potential drug delivery system in targeting hepatocellular carcinoma, which deserves more research on its targeting ability, antitumor efficiency, and metabolism in vivo for treatment of hepatomacellular carcinoma.
Asialoglycoprotein Receptor ; metabolism ; Carcinoma, Hepatocellular ; pathology ; Coumarins ; Drug Delivery Systems ; Endocytosis ; Hep G2 Cells ; drug effects ; Humans ; Lactoferrin ; pharmacology ; Liposomes ; Liver Neoplasms ; pathology ; Particle Size ; Phosphatidylethanolamines ; Polyethylene Glycols ; Thiazoles

Objective To evaluate and analyse the effectiveness of surgical treatment for fibrous dysplasia in proximal femur with severe varus deformity.Methods A retrospective study was performed in 21 patients (24 femora)of fibrous dysplasia who were treated in our hospital between August 2000 and May 2009.All patients had severe femoral varus deformity.The four-step procedures were performed orderlv as valgus osteotomy,lesion curettage,impacting of massive bone allograft,and fixation by femoral intramedullary nail.There were 6 patients with monostotic disease,15 with polyostotic diseases,including 12 males and 9 females with a mean age of 22.7 years(range,14-39 years).The average neck-shaft angle and femoral varus angle was 75°(range 55°-105°)and 30°(range,18°-45°),respectively.The average length of thigh shortened 3.4 cm(range,2.0-4.5 cm)compared with the contralateral thigh.Results All of the 21 patients were followed up from 21 months to 7 years with an average period of 3 years and 4 months.There were 30 osteotomy sites in 24 femurs,28 osteotomy sites showed bone union after 3-6 months from surgery.Two distal location of the double-level osteotomy showed nonunion,which received bone grafting again and got bone union after 3 months finally.The femoral mechanical alignments of the 21 patients had been recriticd.The average neck-shaft angle was 118°(range,95°-135°)postoperatively,the femoral varus angle disappeared.The average extremity lengthening was 2.8 cm(range,1.8-3.6 cm)postoperatively.There were no infection,recurrent fracture and progression of deformity.The visual analogue scales(VAS)score of 17 patients decreased to zero postoperatively from 7-10 preoperatively,and that of the other 4 patients decreased to 3-4 postoperatively from 8-10 preoperatively.The result of Harris hip functional score was excellent in 12 cases,good in 6,and fair in 3.Conclusion The valgus osteotomy can rectify varus deformity effectively.The reconstract nail of the fumer can support the stability of femur.Impacting of massive bone allograft can improve the capacity of the femur.

ObjectiveTo compare the neonatal outcomes between infants of assisted conception (AC) and natural conception (NC). Methods A prospective case-control study was conducted.Eligible mothers were invited to this study at 28 weeks of gestation and were followed up to delivery.All newborns were examined by pediatricians right after birth.Data including gestational age,birth weight,admission to neonatal intensive care unit (NICU),and presence of any major malformation were collected.Statistical analysis was performed with SPSS 13.0.Difference between two groups was compared by x2 test. ResultsSix hundred and seventy-three newborns were enrolled into this study,including 325 in AC group and 348 in NC group.There were no differences between the demographic characteristics of the two groups,including maternal age,parents' education,family income and proportion of primipara (P＞0.05).The incidences of twins (32.62％ vs 3.45％,x2 =98.88),preterm birth (30.46％ vs 7.76％,x2=56.92),low birth weight infant (32.31％ vs 8.91％,x2 =57.07)and admission to neonatal intensive care unit (27.38％ vs 8.91％,x2 =39.16) and proportion of cesarean birth (62.77％ vs 21.55％,x2=117.64) in AC group were significantly higher than in NC group (all P＜0.01),except for the incidence of birth defect (4.62％ vs 2.59％,x2=2.01,P＞ 0.05).However,no significant differences was found in the above items when only singletons were compared between the two groups (P＞0.05),except for the cesarean section rate (61.18％ vs 22.03％,x2 =100.93,P＜0.01).There were no difference in any of the above neonatal outcomes when different assisted reproductive technologies applied were compared(in vitro fertilization-embryo transfer,intracytoplasmic sperm injection and frozen embryo transfer) (P＞0.05).Conclusions Neonatal outcome after assisted conception is a bit worse than natural conception,which might mainly due to the large proportion of multiple pregnancy after assisted conception.In order to improve neonatal outcome after assisted conception,the number of embryos transferred should be limited.

Cranial Fossa, Anterior ; Humans ; Liposarcoma, Myxoid ; diagnostic imaging ; metabolism ; pathology ; Magnetic Resonance Imaging ; Male ; Middle Aged ; S100 Proteins ; metabolism ; Skull Base Neoplasms ; diagnostic imaging ; metabolism ; pathology ; Tomography, X-Ray Computed

Objective To investigate the value of MR diffusion weighted imaging (DWI) in the pathological grading of glioma. Methods Thirty patients who were confirmed pathologically with glioma were examined by MR DWI. The values of apparent diffusion coefficient (ADC) and relative ADC (rADC) were measured. All those values were analyzed statistically. Results The 30 glioma patients were divided into lower-grade and higher-grade glioma groups. The lower-grade glioma group included 14 cases (1 case of WHO Ⅰ, tricholeukocyte astrocytoma; 13 cases of WHO Ⅱ, 11 astrocytomas with 1 case of post-operative reenrrence, 1 ependymoma, 1 oligodendroglioma); the higher-grade group included 16 cases (! I cases of WHOm, anaplastic astrocytoma with 1 case of post-operative recurrence; 5 cases of WHO Ⅳ, 4 multiforme glioblastomas, 1 ependymoma). The ADC and rADC values of lower-grade gliomas were (1.36±0.16)×10-3 mm2/s and 1.76±0.23, and the values of higher-grade glioma were (1.08±0.10)×10-3 mm2/s and 1.36±0.16, respectively. The values of ADC and rADC were significantly different between the 2 groups (P<0.05). The accuracy rates were 86.7% and 83.3% when the thresholds of ADC and rADC were 1.20×10-3 mm2/s and 1.53. Conclusion The values of ADC and rADC have high accuracy for pathological grading of the glioma.

Objective To investigate the value of perfusion-weighted magnetic resonanceimaging (MRI) in the grading ofgliomas. Methods Thirty patients with pathologically confirmedglioma underwent perfusion-weighted MRI. Of the 30 glioma patients, 14 patients had low-grade and 16had high-grade gliomas. The low-grade glioma patients included 1 with WHO grade Ⅰ glioma (pilocyticastroeytoma) and 13 with WHO grade Ⅱ gliomas; in the WHO grade Ⅱ patients, 11 had astrocytomaincluding I with postoperative recurrence, 1 with epeudymoma, and 1 with oligodendroglioma. Of the 16patients with high-grade gliomas, 11 had WHO grade Ⅲ gliomas identified as anaplastic astrocytoma(including 1 with postoperative recurrence) and 5 had WHO Ⅳ gliomas (including 4 with glioblastomamultiforme and 1 with ependymoma). The relative cerebral blood volume (rCBV), rMSD and relativemean transit time (rMTT) were measured and statistically analyzed in these patients. Results TherCBV, rMSD and rMTT were 1.99±1.0, 1.83±0.78, and 1.10±0.08 in the patients with low-grade gliomas,as compared to those in the high-grade giioma patients of 4.95±2.04, 3.59±1.13, and 1.03±0.61,respectively, showing significant differences in the rCBV and rMSD between the two groups (P<0.05).The diagnostic accuracy of rCBV and rMSD was 83.3% and 80% for the gliomas using their upper limits(2.99 and 2.61, respectively) as the diagnostic thresholds. Conclusion The values ofrCBV and rMSDhave high accuracy in the grading of brain gliomas.

AIMTo observe the role of melatonin receptor and GABAA receptor in sleeping time prolonged by melatonin in mice.

METHODSThe absence of the righting reflex was considered as the sleep onset and the duration of the loss of the righting reflex was recorded as the sleeping time. The effects of receptor agonist and antagonist on hypnotic activity of melatonin were studied in the paper.

RESULTSPrazosin hydrochloride, the blocker of melatonin 3 receptor, didn't affect the sleeping time prolonged by melatonin in mice. GABA, the endogenous agonist of GABA receptor, significantly potentiated the hypnotic activity of melatonin. When picrotoxin, the ligand of picrotoxin site on GABAA receptor, used together with melatonin, it significantly antagonized the sleeping time prolonged by melatonin, however, bicuculline, the specific antagonist of GABA binding site in GABAA receptor, didn't affect the hypnotic activity of melatonin in mice.

CONCLUSIONMelatonin does not exhibit its potentiation sleeping time in mice through melatonin 3 receptor. Hypnotic activity of melatonin may be mediated through picrotoxin site on GABAA receptor.

Animals ; Bicuculline ; pharmacology ; Male ; Melatonin ; physiology ; Mice ; Mice, Inbred Strains ; Picrotoxin ; pharmacology ; Prazosin ; pharmacology ; Receptors, GABA-A ; physiology ; Receptors, Melatonin ; physiology ; Sleep ; physiology

·AIM: To evaluate the effects of two series of enantiomers [(R, R)-XY-1 through (R, R)-XY-12 and (S,S)-XY-1 through (S, S)-XY-12] on ocular blood flow in rabbits.·METHODS; Colored microsphere technique was used for in vivo experiments to determine the ocular blood flow in various tissues of ocular hypertensive (40mmHg) rabbit eyes.·RESULTS; Of the twelve compounds of ( R, R)-XY series examined, four increased choroidal blood flow at 10g/L, 50uL instilled into eyes. All compounds of (S, S)-XY series were not effective on ocular blood flow.·CONCLUSION; Some compounds of (R, R)-XY series increased the ocular blood flow, which might be useful for the prevention and treatment of ocular blood flow related eye diseases. Among all twenty-four compounds, (R, R)-XY-1and (R, R)-XY-9 seem to be the most potent ones.KEYWORDS; ocular blood flow; ischemia; enantiomer

AIM: The effects of ZX-5, as nitric oxide (NO) donor, on ocular blood flow has been investigated using colored microsphere technique in previous study. The relationship between the production of NO by ZX-5 and ocular blood flow has been evaluated. ZX-5 has been shown to have strong positive effect on increasing choroidal blood flow. However,the effect of ZX-5 on retinal function recovery, the effects of its optical isomers, (R, R)-ZX-5 and (S, S)-ZX-5, on choroidal blood flow and retinal function recovery have not been studied and merit investigation.METHODS: Colored microsphere technique was used for in vivo experiments to determine choroidal blood flow of ocular hypertension (40mmHg) in rabbit eyes. Electroretinography was used to measure the b-wave recovery as an indication of retinal function recovery.RESULTS: (R, R)-ZX-5 increased choroidal blood flow at 10g/L, 50μL instillation into eyes at all time points (P＜0.05).(S, S)-ZX-5 was not effective in increasing choroidal blood flow. ZX-5 and (R, R)-ZX-5 showed significant effects in retinal function recovery after ischemia of the retina at all time points (P＜0.05); whereas (S, S)-ZX-5 did not show significant effect on recovery of b-wave after ischemia at most time points except at 120 and 240 minutes.CONCLUSION: ZX-5 and (R, R)-ZX-5 have high potency in increasing the choroidal blood flow and improving the retinal function recovery. It is hoped that they could be used for the prevention/treatment of ocular blood flow related eye diseases.