The inter-species differences of estradiol metabolism were investigated in human, Beagle dog and rat liver microsomes by comparing enzyme kinetics of parent drug and the formation of its major metabolites. The incubation systems of estradiol with liver microsomes of the three species were optimized in terms of estradiol concentration, microsomal protein content and incubation time. The concentrations of estradiol and its metabolites were measured by LC-MS/MS method. The t1/2, CLint, CLh, Km and Vmax of estradiol incubated with male human liver microsomes were 40.02 +/- 8.32 min, 41.39 +/- 6.57 mL x min(-1) x kg(-1), 13.81 +/- 12.36 mL x min(-1) x kg(-1), 26.8 +/- 6.99 micromol x L(-1) and 0.75 +/- 0.92 micromol x L(-1) x min(-1), respectively. The corresponding parameters of female human were 44.71 +/- 10.21 min, 29.85 +/- 8.97 mL x min(-1) x kg(-1), 0.01 +/- 0.68 mL x min(-1) x kg(-1), 44.2 +/- 7.73 micromol x L(-1) and 1.27 +/- 4.41 micromol x L(-1) x min(-1), that of male dog were 21 +/- 7.33 min, 165.53 +/- 29.33 mL x min(-1) xkg(-1), 26.01 +/- 8.39 mL x min(-1) x kg(-1), 19.5 +/- 7.34 micromol x L(-1) and 1.6 +/- 0.65 micromol x L(-1) x min(-1), that of female dog were 25.5 +/- 5.32 min, 135.11 +/- 42.34 mL x min(-1) x kg(-1), 0.24 +/- 3.18 mL x min(-1) x kg(-1), 8.33 +/- 6.32 micromol x L(-1) and 0.51 +/- 2.15 micromol x L(-1) x min(-1), that of male rat were 5.11 +/- 3.84 min, 485.63 +/- 36.52 mL x min(-1) x kg(-1), 49.57 +/- 15.29 mL x min(-1) x kg(-1), 62 +/- 13.74 micromol x L(-1) and 19.16 +/- 9.67 micromol x L(-1) x min(-1), and that of female rat were 7.0 +/- 3.69 min, 354.82 +/- 33.33 mL x min(-1) x kg(-1), 8.04 +/- 3.23 mL x min(-1) x kg(-1), 35.38 +/- 7.65 micromol x L(-1) and 8.39 +/- 4.91 micromol x L(-1) min(-1), respectively. There were nine metabolites detected from all the three species, but the relative amounts of the metabolites generated were different in three species. The results indicted that the major phase I metabolic pathway of estradiol was similar in the liver microsomes from all the three species. However, the inter-species differences were found in the view of relative amounts of the metabolites as well as the metabolic characteristics of estradiol in liver microsomal incubation.

AIM To study the chemical constituents from Buthus martensii Karsch.METHODS The dichloromethane and 70％ methanol fractions of B.martensii extract were isolated and purified by silica,ODS,Sephadex LH-20 and mid-pressure preparative column,then the structures of obtained compounds were identified by physiochemical properties and spectral data.RESULTS Nine compounds were isolated and identified as cholest4-en-3-one (1),cholesterol (2),uracil (3),1-stearyl-2-lyso-sn-glycero-3-phosphatidylcholine (4),glycerol (5),oleic acid (6),proline (7),alanine (8),leucine (9).CONCLUSION Compounds 1,4,5 are isolated from B.martensii for the first time.

Objective To observe the effect of circadian rhythm on hypnotic median effective dose( ED50) of ketamine. Methods Sixty mice were randomly divided into 4 groups which had 15 mice in each group. They were intraperitoneally injected with ketamine at different times of 2 Am,8 Am,2 Pm and 8 Pm, respectively. Righting reflex was recorded and the value of ED50 was measured with sequential experimental method. Results The hypnotic ED50 of ketamine at 2 Am was(54.57?0.82) mg/kg, with 95% confidence limit of ED50 38.06-78.22 mg/kg;ED50 was(49. 27?0. 12) mg/kg at 8 Am, with 95% confidence limit of ED50 40. 21-60. 37 mg/kg;ED50 at 2 Pm was (42.28?0.21) mg/kg, with 95% confidence limit 37.35 - 47 83 mg/kg;and ED50 at 8 Pm was(57.42?0.14) mg/kg, with 95% confidence limit 37.51-73 72 mg/kg,respectively. The ED50 were significant different at 2 Pm and 8 Pm. However, there were no significant difference in ED50 value among other groups. Conclusion The hypnotic effect of ketamine has circadian rhythm - dependent.

Objective To explore the immunophenotype of children with acute myeloid leukemia(AML) and its clinical significance.Methods Statistics was used to analyze the relationship between the immunophenotype of AML and their French-American-Britain(FAB) classification,complete remission (CR) in one month and 3-years event-free survival(EFS).Results CR rate was 71.6% and 3-years EFS rate was 50.8%. HLA-DR and CD34 absent mainly in M3, associated with higher CR and EFS rate. So did CD33 negative cases, especially in M2. CD13 positive was significantly predictive factor for achieving CR.Co-expression of lymphoid antigens and NK cell antigens(CD56) with M2 which correlated with lower CR and EFS rate.Conclusions The negative of HLA-DR, CD34, CD33,as well as CD13 positive, have relationship with good prognosis. Lymphoid antigens and CD56 are poor prognostic factors.

Adolescent ; Bile Reflux ; etiology ; Child ; Child, Preschool ; Female ; Gastritis ; etiology ; Gastroscopy ; Helicobacter Infections ; complications ; diagnosis ; Helicobacter pylori ; Humans ; Male

BACKGROUND: Metabotropic glutamate receptor(mGluR) is G-protein coupled membrane receptors, which participate in various physiology or pathology process in brain, but how it induce brain ischemic tolerance(BIT)is unclear.OBJECTIVE: To study roles of mGluR2/3 and mGluR1/5 in the BIT induction.DESIGN: Randomized controlled study based on experimental animals.SETTING: Neurological department of provincial hospital and pathophysiological department of basic institute in a university.MATERIALS: The study was conducted at the Pathophysiological Department, Institute of Basic Medicine, Hebei Medical University from May 2002 to May 2003. Totally 64 healthy male SD rats were selected from the Experimental Animal Center of Hebei Medical University. Glial fibrillary acidic protein (GFAP) antibody, MTPG and(s)-4C3HPG were got from Sigma Company.INTERVENTIONS: 4 vessel occlusion(4VO) brain ischemic models in rats stained with thionine staining and GFAP immunohistochemistry staining. were used. Sixty-four rats, of which bilateral vertebral arteries were occluded permanently by electrocautery, were divided into the following 8groups: sham operation group, cerebral ischemic preconditioning(CIP)group, ischemic insult group; BIT group; MTPG + sham operation group;MTPG+BIT group; MTPG+ischemia group and(s) -4C3HPG+BIT coup. All the rats were killed 7 days after the operation or the final ischemic treatment. Cerebral sections were selected and stained with thionine staining and GFAP immunohistochemistry staining.MAIN OUTCOME MEASURE: The changes of the morphologic hippocampal pyramidal cell and GFAP expression of astrocyte.RESULTS: ① The 8 minutes ischemic insult increased the histological grade(HG) in CA1 area, decreased the pyramidal neuronal density(ND)and increased the expression of GFAP significantly( P ＜ 0.05) . ② The above changes were not observed in the BIT group, indicating that the CIP could protect pyramidal neurons against the 8-minute ischemic insult. ③The protective effects of the CIP were blocked by MTPG or(s)-4C3HPG, as manifested by significant increases in HG and decreases in ND in the groups of MTPG + BIT, MTPG + ischemia and(s)-4C3HPG + BIT( P ＜ 0.05).CONCLUSION: MTPG or (s) -4C3HPG could block the induction of BIT induced by CIP, but mGluR2/3 or mGluR1/5 could participate in the induction of BIT by which protect effect of mGluR is further induced.

Objective To detect the expression of urinary nuclear matrix protein 22(NMP22) and cytokeratin 20(CK20) mRNA in the monitoring of bladder tumor recurrence ,and to explore the clinical value of combined detection of urinary NMP22 and CK20 mRNA in the monitoring of bladder tumor recurrence .Methods Enzyme‐linked immunosorbent assay(ELISA) and nested reverse transcriptase polymerase chain reaction(Nested RT‐PCR) were used to detect the expression of NMP22 and CK20 mRNA in the u‐rine of 46 patients with recurrent bladder cancer tumor (recurrent group) ,66 patients without recurrent tumor (no‐recurrent group) and 40 healthy volunteers(control group) respectively .Results The expression of NMP22 and CK20 mRNA in the urine of control group were negative .There was statistically significant difference between the positive expression rate of NMP 22 and CK20 mRNA in the urines of the recurrent group[78 .3% (36/46) ,80 .4% (37/46))] and that of the no‐recurrent group[6 .1% (4/62) , 6 .1% (4/62)] and the control group respectively (P<0 .01) .There was no statistically significant difference between the no‐recur‐rent group and the control group(P>0 .05) .The expression level of NMP22 in recurrent tumor increased obviously along with the progression of the pathological grade and clinical classification of tumor (P<0 .05) .The positive rate of CK20 mRNA expression in the recurrent group increased obviously along with the increase of the tumor number (P<0 .05) .The sensitivity and specificity of NMP22 for monitoring bladder cancer recurrence were 78 .3% and 93 .9% ,of CK20 mRNA were 80 .4% and 93 .9% .Combined de‐tection of both sensitivity and specificity were 95 .7% and 92 .4% .Statistical significance was observed between combined sensitivi‐ty and that of single detection(P<0 .05) .No significant difference was observed between combined specificity and that of single de‐tection(P>0 .05) .Conclusion The positive expression of CK20 mRNA may also indicate tumor multiplicity .Combined detection of NM P22 and CK20 mRNA significantly increases the sensitivity and specificity in clinical detection .

AIM: To explore the role of NO in the induction of brain ischemic tolerance (BIT) by observing changes of NOS activity and NO_2-/NO_3- content following a transient cerebral ischemia. METHODS: The rat 4-vessel occluding brain ischemic model was used. 140 male Wistar rats were divided into sham, cerebral ischemic preconditioning (CIP), ischemic insult and CIP+ischemic insult groups. An occlusion of the 4 vessels for 3 min was normally used as CIP, and a relative long one for 10 min was used as ischemic insult. When CIP was followed by ischemic insult, the interval between them was 3 d. The CA1 region of the hippocampus of rats was dissected out at 0 h, 2 h, 16 h, 24 h, 36 h, 72 h and 7 d after the last time of ischemia to assay its NOS activity and NO_2-/NO_3- content. RESULTS: The NOS activity and NO_2-/NO_3- content began to increase at 16 h, peaked at 24 h and decreased to basal level at 36 h of reperfusion after CIP. The duration of the up-regulation of NOS activity and NO_2-/NO_3- content was much shorter than that of BIT, which usually takes place 1-7 d after CIP. The pattern of upregulation of the NOS activity and NO_2-/NO_3- content was similar to the CIP group, but the maximum (24 h) was much more than that in CIP group (P

Objective To explore the clinical characteristics and treatment of Caroli′s disease in children.Methods The clinical data,laboratory examination and radiological feature of 8 children with Caroli′s disease between Feb.1998 and Dec.2007 were analyzed retrospectively.All children underwent CT and abdominal ultrasonogram.Results Five cases of the 8 children were male and 3 cases were female.The mean age was 6.3 years old.The cases′ history were from 5 days to 4 months.The clinical symptoms showed that 3 cases had hematemesis,5 cases had hepatosplenomegaly,and 1 case had fever and turbid urine.Of the total 8 cases,5 cases were hepatic fibrosis and liver cirrhosis and hepatosplenomegaly,3 cases were portal hypertension,and 1 case had cholangitis.The other 3 cases were simple types.One case had infantile polycystic kidney disease.Laboratory analysis revealed 2 cases had dysfunction of liver and 1 dysfunction of renal.The imaging characteristics showed multiplied irregular dilatation of the intrahepatic bile ducts in enlarged liver,with central dot sign on CT scan.One case presented enlarged gastroesophageal vein.The 8 cases undertook conservative treatment,with no surgery.Conclusions The symptoms of Caroli′s disease are highly variable.Caroli′s disease should be focused especially on children with abdominal pain and hepatomegaly.CT is important for diagnosis of Caroli′s disease at earlier stage.The disease can be conservatively treated,and(or) surgically operated.

· AIM: To search an easy and simple way for intraocular implantation after the eye evisceration.· METHODS: Fifteen healthy New Zealand rabbits were divided into 5 groups according to the sacrifice time, and each group included 3 rabbits; the left eye received the injection of polymethyl methacrylate (PMMA) bone cement (2g per mL), while the right eye served as control. Under general anesthetia, a 3mm incision was made on the sclera,and the eye contents and pigment tissues were extruded out with fingers. Then, PMMA bone cement (2g per ml) was injected through the scleral incision. Both the operated eye and control eye of the rabbits were enucleated and weighed,The reaction of the operated eye (macroscopically and histopathologically) was noted at frequent interval. The obtained data were then analyzed with ANOVA (SPSS11.5).· RESULTS: There was swelling of eyelids and conjunctiva at the early time after the injection, but no significant difference between the weight of the left and right eyes was noted,Histopathologic examination showed scleral and other tissues necrosis at early period, and then the tissues reaction turned into a great deal of cell proliferation and finally into extensive fibro-connective tissues. Three months after the operation,neovascularization was observed in the cornea of the operated eyes. Histopathologic examination showed formation of fibro-membrane around the intraocular implant,and disappearance of the inflammation.· CONCLUSION: The method of injecting PMMA bone cement (2g per ml) to form an intraocular implant is quite simple and economical; this method is also easy to use clinically.