Objective To prepare the cleavable PEG and RGD co-modified liposome for tumor targeting.Methods Liposomes were prepared by film-ultrasonic method.The particle size,Zeta potential and stability in FBS were evaluated.Cellular uptake by HepG2 cell was explored.MTT assay was used to evaluate the cytotoxicity of blank liposomes. Results The particle diameter of C/RGD-LP was (104.8 ±5.5 )nm with the Zeta potential of (-4.45 ±1.75 )mV.The cellular uptake of C/RGD-LP increased 2.8 times after Cys was added.The C/RGD-LP showed little cytotoxicity to HepG2 cell.Conclusion Cleavable PEG and RGD co-modified liposomes were easy to prepare and has a special application value for targeting tumor.

Polycystic ovary syndrome (PCOS) is one of the most popular diseases in obstetrics and gynecology research at internal and abroad at present, traditional Chinese medicine(TCM)in the clinical treatment of the disease have the advantage. Clinical epidemiological study of descriptive research method this research adopts investigation, observation of TCM syndromes and improper diet through 401 cases in Jiangsu Province confirmed PCOS patients, to explore the relationship between TCM syndrome type distribution and improper diet factors, and to provide the clinical basis for further etiology of this disease research. TCM syndrome type distribution of the disease is kidney deficiency, phlegm stagnation syndrome, qi stagnation and blood stasis syndrome, syndrome of dampness heat of liver channel and is composed of 4 basic syndromes and formed complex syndrome, and the composite and syndrome type (60.85%); combined with the analysis of traditional Chinese medicine dialectical, Pure empirical syndrome this disease (46.88%), followed by the actual card (45.39%), pure deficiency is rare. Improper diet factors associated with the disease, in which improper diet with different TCM syndrome type distribution significantly related. Stagnation of phlegm dampness syndrome is the main syndrome of the disease type, improper diet factors and every syndrome PCOS type distribution is as follows: the partial eclipse fatness greasy with basic syndromes of phlegm dampness stagnation of kidney deficiency syndrome, the nephrasthenia syndrome is less; eating spicy stimulation by basic syndromes of stagnation of Qi and blood stasis; eating cold people the basic certificate type of qi stagnation and blood stasis; The diet of patients are more prone to stagnation of phlegm dampness syndrome.
Adolescent ; Adult ; China ; Diagnosis, Differential ; Diet ; Eating ; Female ; Humans ; Medicine, Chinese Traditional ; Polycystic Ovary Syndrome ; diagnosis ; metabolism ; physiopathology ; Young Adult

Objective To synthesize 628F-Py-AMD3465,to investigate its biodistribution in mice and to perform the microPET/CT imaging on mice bearing human lung cancer cell (A549).Methods AMD3465 quaternary ammonium salt precursor was directly labeled with 18F,then 628F-Py-AMD3465 was synthesized through nucleophilic reaction,hydrolysis,neutralization and the product was purified using HPLC.The labeling yield and radiochemical purity were analyzed by HPLC.Fifteen Kunming mice were injected with 5.55 MBq of 628F-Py-AMD3465 and sacrificed at 5,20,40,60 and 120 min postinjection.The selected tissues were harvested and weighed,and the radioactivity in the tissues was measured by an automated γ-spectrometer.The ％ID/g was calculated.MicroPET/CT studies were performed on A549-bearing mice after injecting 6-18F-Py-AMD3465 through vena caudal.Paired t test was used.Results 6-18F-Py-AMD3465 was successfully synthesized with the labeling yield of (9.0±2.0)％,the total synthesis time was about 60 min,and the radiochemical purity was more than 98％.Biodistribution studies showed that the radiouptake was higher in the kidneys and bladder of normal mice,which demonstrated that 6-18 F-Py-AMD3465 was mainly excreted through the kidneys.Biodistribution in A549-bearing mice was similar to that in normal mice.The tumor/muscle ratio at 40 min was 5.0,but the radiouptake of the tumor was still lower than that of the normal lung:(8.05±0.35) ％ID/g vs (9.33±0.66) ％ID/g;t=5.26,P＜0.05.MicroPET/CT imaging showed that the high-uptake location of 6-18F-Py-AMD3465 in tumor-bearing mice was similar to the normal mice,and the tumor uptake reached the maximum level at 45 min post-injection (SUV 0.67).Conclusions 6-18F-Py-AMD3465 can be synthesized by a simple method.A lower uptake could be shown in the tumor compared to that in the lung and the tracer has limited diagnostic value for lung cancer.

Objective To determine the prognostic factors after radical resection (RR) for hepatocellular carcinoma (HCC).Methods Altogether 144 patients who had undergone RR for HCC from 1988 through 1995 were included for a univariate and a Cox multivariate analysis.Nineteen factors contributing to overall survival rate (SR) and disease-free SR were analysed.Results The 5-year SR and disease-free SR (N=144) were 47.3% and 23.9%,separately.Multivariate analysis revealed that classification of RR was the signficant factor to overall SR,and presence of vessel invasion was the signficant factor to disease-free SR.The 5-year SR and disease-free SR in the patholngically RR and clinically RR groups were 60.2%,29.0% and 14.0%,0%,respectively.The 5-year disease-free SR in the group without (or with) vessel invasion was 27.8% (or 0%).Conclusions The classification of RR is the determinative prngnostie factor.Pathologically RR is the first option for patients with in- dications.It is essential to improve adjuvant therapy to decrease postoperative recurrence and metastasis rates.

Objective To investigate the pathogen distribution and drug sensitivity in childhood bacillary dysentery,and to guide clinically the selection of reasonable antibiotics.Methods Bacterial drug susceptibility test was performed by standard Kirby-Bauer method.The results were interpreted according to NCCLS 2002.Results Of the 98 cases,there were two types of positive bacterial species:sh.flexneri(n = 77)and sh.sonnei(n = 21).Both sh.flexneri and sh.sonnei were sensitive to cefoperazone,eeftazidime,ceftriaxone,cefoperazone/sulbactam and fura- zolidone,and insensitive to ampicillin and co-trimoxazole.Conclusion sh.flexneri was the major pathogen of child- hood bacillary dysentery.The third generation cephalosporins were the first choice for shigella infections.

Seven sinapine analogs (6a-6g) were synthesized using cinnamon acid or benzoic acid and their derivatives as starting materials, which obtained from substituted benzaldehyde and malonate. The structures of target compounds were characterized by IR, 1H NMR and elemental analysis. The effects of compounds 6a-6g on the smooth muscle of intestine isolated from rabbit were studied, and the experimental results showed that compounds 6a, 6d and 6g had diastolic action, while 6f had contractile action.

Objective To investigate the antitumor effects on ovarian cancer using recombinant adenoviruses expressing autocatalytic caspase-3 driven by amplified human telomerase reverse transcriptase promoter (AdHTVP2G5-rev-casp3) combined with flavopiridol. Methods Following the treatment with AdHTVP2G5-rev-casp3 combined with flavopiridol, cell survival rate was measured by cell counting kit 8;cell apoptotic rate and cell cycle distribution were detected by flow cytometry. Western blot was performed to observe the expression of p17, the active subunit of caspase-3, and p85, the cleavage segment of substrate of caspase-3, in AO cells. The mice survival rates were measured for abdominally metastatic tumor models and the volume of tumor nodules were determined for subcutaneous tumor models following the treatments of AdHTVP2G5-rev-casp3 combined with flavopiridol. HE staining was used to detect the histopathological changes of various organs, and the serum level of alanine transaminase (ALT) and aspartate aminotransferase (AST) were measured to monitor liver damages following the intraperitoneal administration of AdHTVP2G5-rev-casp3 and flavopiridol. Results There was no significant cell-killing effects or apoptosis in AO cells following treatments with AdHTVP2G5-rev-casp3 or flavopiridol at low dosage alone (apoptotic rate all ＜ 11% ), whereas significant synergism of their sequential combination was observed in AO cells. This sequential treatment of AdHTVP2G5-rev-casp3 [multiplicity of infection (MOI) was 20]infection for 72 hours, followed by flavopiridol ( 300 nmol/L) for 48 hours, could result in the most substantial cell death, and AO cells survival rate and apoptotic rate were 73. 5% and 11.6%, respectively.Following treatments with AdHTVP2G5-rev-casp3 at low doses ( MOI = 10), there was a significant increase in cell number with S-phase content ( 62. 5% ), which resulted in the most marked apoptosis induced by sequential treatments with flavopiridol. The sequential combination could induce significantly higher levels of p17 and p85 expression than that when their applications alone. Combined AdHTVP2G5-rev-casp3 and flavopiridol treatment prolonged mouse survival [ mean survival time of ( 286 ± 6) days ] and suppressed tumor growth significantly (tumor growth suppression rate of 81% ), when compared with treatment using either alone. The levels of serum ALT and AST were not significantly elevated and no obvious lesions were found in any organs in treatments with AdHTVP2G5-rev-casp3 of low doses combined with flavopiridol.Conclusions AdHTVP2G5-rev-casp3 at low doses results in a significant increase in cell number with Sphase content, which significantly enhanced the sensitivity of cells to flavopiridol. Treatments of autocatalytic caspase-3 combined at low doses with flavopiridol result in significant synergistic antitumor effects,significant tumor growth suppression and prolonged survival of mice. When compared with normal dose flavopiridol alone, the combination could resulted in minimal liver toxicity.

Objective To investigate the analgesic effect of adenosine A1 receptor agonist R( - )-N6-(2-phenylisopropyl)-adenosine (R-PIA) administered into the brainstem medial pontine reticular formation (mPRF) and the underlying mechanism. Methods Sixty male SD rats aged 8-10 weeks weighing 250-300 g were used in this study. The animals were anesthetized with intraperitoneal 10% chloral hydrate 300 mg?kg-1 .A 24-gauge stainless steel cannula was inserted into mPRF on one side using a stereotaxic apparatus. One week after operation the animals were randomly divided into 12 groups ( n=5 each) : groupⅠcontrol; groupⅡR-PIA 0.5?g; groupⅢR-PIA 1.0?g; groupⅣR-PIA 2.0?g; groupⅤtheophylline (an adenosine receptor antagonist) 5.0?g; groupⅥ8-cyclopentyl-1 ,3-dipropylxanthine (DPCPX, an adenosine A, receptor antagonist) 1.0?g; groupⅦglibenclamide (an ATP-sensitive K+ channel blocker) 5.0?g; groupⅧ4-aminopyridine (4-AP, a voltage dependent K+-channel blocker) 5.0?g; groupⅨtheophylline 5.0?g + R-PIA 2.0?g; groupⅩDPCPX 1.0?g + R-PIA 2.0?g; groupⅪglibenclamide 5.0?g + R-PIA 2.0?g and groupⅫ4-AP 5.0?g + R-PIA 2.0?g. All the drugs were injected into mPRF in 0.3?l of normal saline. In groupⅨ-ⅫR-PIA 2.0?g was administered 15 min after pretreatment with theophylline, DPCPX, glibenclamide or 4-AP. Analgesia was determined using the tailflick latency (TFL) (the time between the onset of the radiant heat stimulus and voluntary tail withdrawal) at 5, 15, 30, 45, 60 and 90 min after R-PIA injection into mPRF. The pain threshold was expressed as percentage of the maximal possible effect ( MPE) : MPE = (TFL after drug - baseline TFL)/( 10.0 -baseline TFL)?100% .Results R-PIA 0.5-2.0?g injected into mPRF produced significant analgesia in a dose-dependent manner. Pretreatment with theophylline or DPCPX completely reversed the analgesic effect of R-PIA while pretreatment with glibenclamide or 4-AP only partially reversed the analgesic effect of R-PIA.Conclusion R-PIA administered into mPRF produces analgesia through activation of both ATP-sensitive and voltage-dependent K+ -channel in mPRF.

Objective To investigate the distribution of ligustrazine hydrochloride in guinea pig blood, cerebrospinal fluid and perilymph fluid afte intramuscular injection. Methods The HPLC was used for determination of ligustrazine hydrochloride in guinea pig blood, cerebrospinal fluid and perilymph fluid afte intramuscular injection by internal and external standard method.Results Ligustrazine hydrochloride could be absorbed into blood rapidly after intramuscular administration in guinea pig. The concentration reach its high level in 20 min.It was 357.76 ?g/ml. It decreased to low level 2 h after injection.It could be found in cerebrospinal fluid 10 min after injection. The concentration reached its high level in 20 min.It was 120.50 ?g/ml.It decreased to low level 70 min after injection. The ligustrazine hydrochloride could be found in perilymph fluid 5 min later.Its high level in 20 min was 215.79 ug/ml.It decreased to low level 70 min after injection.The results indicated that ligustrazine hydrochloride was rapidly absorbed and eliminated after intramuscular administration in guinea pig.Conclusion Ligustrazine hydrochloride can be absorbed into blood, enter cerebrospinal fluid and perilymph fluid. It can pass through blood-brain barrier and blood-labyrinth barrier. The results indicates that ligustrazine hydrochloride is rapidly absorbed and eliminated after intramuscular administration in guinea pig.

Objective To investigate the metabolic rules of surfactant protein A and D(SP- A,SP- D )in bronchoalveolar lavage fluid(BALF)in human fetal lungs during gestational ages. Methods BALF with 30 mL saline was performed on clinically collected human fetus with induction of labor by water- bag Their BALF was respectively retrieved [total retrieval rate(85. 6% ? 13 1)% ]for analysis of protein content. The BALF SP - A and SP - D from fetus of various gestational ages or newboms were detected by RPHA and ELISA. Results The total protein in BALF gradually increased since 10th week to newborn peak during lung development. And SP - A and SP D were respectively updated from(0.34 ?0.07 ) ,(0.05?0.01) ng/L to newborn climax[ (6 42 ? 0 36),(1.22 ? 0 13)ng/L] .Conclusions The protein in BALF gradually increases with fetal growth and lung development. SP-A and SP- D may reach prenatal climax and become the main indicator of newborn lung maturity.