Aim To study pharmacokinetics and bioavailablity of domestic penicillin V dispersion tablet in healthy volunteers. Methods According to the crossover design, each volunteer in two groups was orally given a single dose ( 0.75 g ) of domestic penicillin V dispersion tablet or imported penicillinV tablet alternately and the plasma concentrations were determined by RP HPLC. The pharmacokinetic parameters were obtained by using ATPK program and calculated on the basis of open single compartment model. Results After a single oral dose( 0.75 g ), the t 1/2(ke) was ( 0.75 ? 0.10 ) h and ( 0.70 ? 0.14 ) h ,the c max was( 8.44 ? 2.40 ) mg?L -1 and ( 8.75 ? 3.04 ) mg?L -1 at ( 0.56 ? 0.11 ) h and ( 0.63 ? 0.17 ) h and AUC 0～4 was( 8.44 ? 2.40 ) mg?h?L -1 and ( 8.75 ? 3.04 ) mg?h?L -1 for two formulations, respectively. Relative bioavailability of domestic penicillin V dispersion tablet was ( 90.50 ? 8.84 )%. Conclusion The result shows that the two formulations are bioequivalent.

Objective To investigate the association between single nucleotide polymorphisms (SNPs)in cytokine IL-6, IL- 10 genes and HBV-related hepatocellular carcinoma(HCC). Methods A hospital-based case-control study was conducted in 381 cases with HBV-related HCC, 340 HBsAg carriers and 359 non-tumor controls. Genotypes of-572 site of IL-6 gene and-819, -592 sites of IL-10 gene were determined by real-time polymorphism chain reaction. Unconditional logistic regression was used to estimate the odds ratios(ORs)and 95 confidence intervals(C/s). Results For the G/C alleles of -572 loci on IL-6 gene, there were significant differences between the three groups(P＜0.05). Compared with CC genotype, GG genotype increased the risk of HBV infection (OR=2.171,95% Ch 1.068-4.415), but did not seem to be associated with HCC. For the alleles of-819 and -592 site of IL-10 gene, there were significant differences between the three groups(P＜0.05). Compared with CC genotype, TT genotype increased the risks of both HCC(OR=2.791,95%CI:1.326-5.874), and HCC in HBsAg carriers(0R=3.522,95%CI: 1.707-7.266). When compared with CC genotype on -592 site, the AA genotype reduced the risk of both HCC(OR=0.389, 95% CI:0.173-0.875), and HCC in HBsAg carriers(OR=0.336, 95% CI: 0.154-0.734). Conclusion The SNPs in -572 site of IL-6 gone might be associated with the risk of HBV infection. The SNPs in -819 site of IL-10 gene increased the risk of HCC, but -592 site of IL-10 gene decreased the risk of HCC.

10.3969/j.issn.1007-3969.2013.04.005

AIM: To analyze the difference of endonuclease domain containing 1 (ENDOD1) expression be-tween benign prostatic hyperplasia ( BPH ) tissues and prostate cancer ( PCa ) tissues and to investigate the effect of ENDOD1 on the biological function of human prostate cancer cells .METHODS: The BPH samples ( n=20 ) and PCa samples (n=21) were processed and analyzed according to the instruction of immunohistochemical (IHC) staining.The mRNA and protein levels of ENDOD 1 in the normal prostate epithelial cells and prostate cancer cells were evaluated by RT -qPCR and Western blot , respectively .The recombinant plasmids pCMV-N-Flag-ENDOD1 was constructed and was trans-fected into the human prostate cancer cells .The proliferation , apoptosis , migration and invasion abilities of the prostate cancer cells were evaluated by MTT assay , flow cytometry, Transwell migration and Matrigel invasion assays , respectively. RESULTS:The analysis of variance of the immunoreactivity score showed that PCa tissues with high Gleason score dis -played significantly lower ENDOD1expression than that with low Gleason score and BPH (P<0.05).The expression of ENDOD1 at mRNA and protein levels in PC3 cells and DU145 cells was significantly lower than that in the LNCap cells (P<0.05).The proliferation of DU145 transfected with ENDOD1 was inhibited.The flow cytometry indicated that ENDOD1 over-expression in the DU145 cells resulted in a notable increase in G0/G1 phase arrest (P<0.05), but the ap-optotic rates showed no statistical difference .The results of Transwell assay showed that migration and invasion abilities of the cells were also inhibited after transfection with over-expressing ENDOD1 plasmid (P<0.05).CONCLUSION: The expression of ENDOD1 significantly decreased in prostate cancer with high Gleaon score .Meanwhile, the ENDOD1 is spe-cifically down-regulated in androgen independent prostate cancer (AIPC) cell lines.Over-expression of ENDOD1 remark-ably inhibits the proliferation , migration and invasion abilities of AIPC .

Objective To investigate the clinical effect of vagus nerve preserving pericardial devascularization plus subtotal splenectomy in treating portal hypertension with a history of variceal bleeding.Methods The clinical data of 33 cases of portal hypertension with variceal hemorrhage treated with vagus nerve preserving selective pericardial devascularization plus subtotal splenectomy from April 2004 to December 2013 (study group) were compared with that of 34 cases treated with pericardial devascularization plus splenectomy (control group).Results There was no mortality in two groups.The postoperative gastric drainage during the first 72 h were(1 525 ±30) ml in the study group and (2 130 ±40) ml in control group(P ＜0.05).Portal vein thrombosis developed in one case in the study group and 15 cases in the control group(P ＜ 0.05).Postoperative 3-year recurrent gastroesophageal varices hemorrhage was 15％ in the study group and 25％ in the control group (P ＜ 0.05).Postoperative 5-year variceal hemorrhage recurrence rate were 28％ in the study group and 30％ in the control group (P ＞ 0.05).Conclusions Maitaining vagus nerve selective pericardial devascularization plus subtotal splenectomy is of less postoperative complication and lower portal vein thrombosis rate and better patients' survival compared with pericardial devascularizatim plus total splenectomy.

Aim To study relative bioavailablity of cefaclor effervescent tablets in healthy volunteers. Methods According to the crossover design, A volunteers were each orally given a single does of the 0.75 g cefaclor effervescent tablets and cefaclor capsules with an interval of 5 days between the two formulations.The plasma concentrations of the drug were determined by RP-HPLC.Pharmacokinetic parameters were obtained by ATPK programe,and calculated on the basis of open single compartment model.Results After a single oral dose, the peak levels in plasma averaged Cmax(31.27?5.81)?g?ml-1 and(30.56?5.25) ?g?ml-1 at (0.58?0.12)h and(0.73?0.17)h and AUC0～4(35.48?4.65) ?g?h?ml-1 and (35.89?2.90) ?g?h?ml-1 for tablet and capsule,respectively. Conclusion The result shows that two formulations are bioequivalence.

Objective To study the effects of Androsace umbellata extract on bone wound healing in rats.Methods A total of 32 rats were selected,and the rat femur bone trauma model was established.The Androsace umbellata was administrated to rats in treatment groups (including high-dose Androsace umbellata group and low-dose Androsace umbellata group,8 rats in each group)continuously for 10 days,while rats in the fake operation control group (8 rats)and bone trauma model group (8 rats) were treated with corresponding volume of solvent by body weight.The growth of body weight and wound healing of rats were recorded.The serum levels of calcium and phosphorus,activity of alkaline phosphatase (ALP),bone density and bone biomechanics were examined.The X-ray photograph was carried out to observe the effects of Androsace umbellata on bone wound healing,Results Compared with the bone trauma model group,serum levels of calcium and phosphorus,calcium-phosphorus product and activity of ALP were significantly increased in treatment groups,there were statistically significant differences (P＜0.05).Compared with the bone trauma model group,bone density of trauma place in the high-dose Androsace umbellata group was significantly decreased (P＜0.05),bending energy in the low-dose Androsace umbellata group was increased (P＜0.05),while no statistically significant difference was found in the other skeletal biomechanical properties (P＞0.05).The results of X-ray films indicated that the treatment groups shown better effects on bone wound healing compared with the bone trauma model group.Conclusion Androsace umbellata extract could effectively promote bone wound healing in rats.

To study the relationship between the interleukin (IL)6 -572G/C polymorphism and risk of hepatocellular carcinoma (HCC) in men.A hospital-based case-control study was conducted with 500 male HCC patients without tumor history in other organs and 590 healthy male controls without history of tumors or chronic diseases. All HCC cases were diagnosed by histopathology. The controls were recruited from the Department of Orthopedic Trauma and Ophthalmology at the same hospital. The IL-6 promoter -572G/C polymorphism and its genotype variants were detected by real-time fluorescence quantitative PCR. The Chi-squared test and unconditional logistic regression analyses were applied to determine the risk of HCC among men carrying the different genotype variants.The frequencies of alleles and distribution of genotypes in the -572G/C loci were not significantly different between the HCC cases and controls (P more than 0.05). The Chi-squared test indicated that the polymorphisms of the loci were not associated with HCC in our male population. However, after adjusting by multivariate logistic regression, the odds ratio (OR) of HCC for the G allele (CG + GG genotypes) carriers was 1.31 (95% confidence interval (CI): 1.00 - 1.71) compared with the CC genotype. Among the male HBV carriers, the CG genotype increased HCC risk significantly (OR = 1.60, 95% CI: 1.14 - 2.24) compared with the CC genotype. A trend test indicated that HCC risk was significantly increased with the numbers of G alleles (P trend less than 0.05). Breslow-Day tests of homogeneity of the ORs indicated an interaction between hepatitis B virus (HBV) infection and polymorphisms of IL-6 (P less than 0.05). The synthetic odds ratio (OReg) of HBV infection and harboring a G allele was 5.95 (95% CI: 3.99-8.87), which represented a super multiplication interaction.Polymorphism of the IL-6 promoter -572 loci may be associated with HCC occurrence in men. Moreover, there is a super multiplication interaction for HCC risk between HBV infection and harboring the IL-6 G allele.
Adult ; Alleles ; Carcinoma, Hepatocellular ; genetics ; pathology ; Case-Control Studies ; Genotype ; Humans ; Interleukin-6 ; genetics ; Liver Neoplasms ; genetics ; pathology ; Male ; Middle Aged ; Polymorphism, Single Nucleotide ; Promoter Regions, Genetic ; Risk Factors

AIMTo investigate the effects of shivering on airway rewarming.

METHODSThe hypothermic dog model without shivering was established by immersing an anesthetized dog in cold water and administering atracurium to inhibit the dog shivering. The model dog respired warm fully humidified (40-45 degrees C, RH 99.9%) air and room temperature air(19 +/- 1 degrees C, RH 30% - 75%) to rewarm each for 2 hours, the priority of different temperature air respired was arranged randomly. After rewarming for 4 hours, the relaxed dog breathed warm humidified air by positive pressure ventilation in order to restore its spontaneous respiratory. Then the dog continued to respire warm humidified air spontaneously until the esophageal (Te) and rectal temperature (Tr) of the dog achieved the same degrees as the dog was immersed in the water. The metabolic heat production was detected by indirect calorimetry during the experiment.

RESULTS(1) When the shivering was inhibited, inhaling warm humidified air for 2 hours made the Tr and Te of the dogs increase 0.26-0.39 degrees C and 0.44-1.11 degrees C per hour respectively, inhaling air at room temperature for 2 hours made Tr and Te of the dogs decrease 0.24-0.51 degrees C and 0.58-0.67 degrees C per hour, respectively. And the changes in Tr and Te of the dogs were unrelated to the priority of inhaling air at different temperature. (2) When the dog with shivering respired spontaneously warm humidified air, the rewarming rates of Tr and Te were 2.26-2.33 degrees C/h and 1.96-2.38 degrees C/h respectively, quicker than those of the dogs whose shivering was inhibited. (3) Compared with metabolic heat production of the unshivering dog respiring warm humidified air by positive pressure ventilation, that of the shivering dog respiring warm humidified air spontaneously increased outstandingly, shivering thermogenesis made the rewarming rates increased obviously.

CONCLUSIONAirway rewarming is a method conducive to rewarming of hypothermia. When the body is shivering, the metabolic heat production increases obviously, that makes the rewarming rate increase markedly. So the shivering must be inhibited in order to eliminate the interference of shivering thermogenesis when the effects of airway rewarming are detected.

Animals ; Body Temperature Regulation ; Cold Temperature ; Dogs ; Hypothermia ; physiopathology ; therapy ; Hypothermia, Induced ; Male ; Respiratory Physiological Phenomena ; Shivering

AIMTo investigate the role of ICAM-1 on the surface of vascular endothelial cell (VEC) in freezing/thawing injury of VEC, in order to elucidate the pathogenesis of freezing/thawing injury.

METHODSVEC separated and cultured from rat aorta and PMN separated from rat peripheral blood were selected as experiment materials. The frozen/thawed VEC model was founded by freezing VEC with the type WKL-V rate cooling instrument and then rewarming them in a water bath. ICAM-1 expression on the surface of frozen/thawed VEC was detected at 4, 12 and 24 h after freezing/thawing with immunohistochemical method. After coincubating frozen/thawed VEC with normal PMN, the adhesion of VEC to PMN was monitored with rose bengal staining assay and the injury level of VEC was indicated by measuring LDH activity in nutrient solution.

RESULTSThe ICAM-1 expression on the surface of VEC increased from 13.2% +/- 3.6% before freezing/thawing of VEC to 22.3% +/- 4.4% at 4 hour after freezing/thawing, and reached the peak (37.9% +/- 2.5%) at 12 hour after freezing/thawing of VEC. After coincubation of frozen/thawed VEC with normal PMN, the adherence of frozen/thawed VEC to PMN increased from group control 0.204 +/- 0.025 to 0.363 +/- 0.022 (P < 0.01), LDH activity in nutrient solution increased from group control 104.64 +/- 20.14 U/L to 162.33 +/- 27.88 U/L (P < 0.01), monoclonal antibody against ICAM-1 (ICAM-1 Mab) could partially block the adherence of frozen/thawed VEC to PMN (0.270 +/- 0.021, P < 0.01), and diminish LDH activity in nutrient solution (125.39 +/- 22.26 U/L, P < 0.05).

CONCLUSIONThe freezing/thawing of VEC can elicit an increase in ICAM-1 expression on the surface of VEC, and then proceed to VEC-PMN adherence and lead to VEC injury.

Animals ; Cells, Cultured ; Endothelial Cells ; metabolism ; Endothelium, Vascular ; cytology ; Freezing ; Intercellular Adhesion Molecule-1 ; metabolism ; Neutrophils ; cytology ; Rats