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 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.

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.

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.

Adenocarcinoma ; pathology ; Adenocarcinoma, Papillary ; pathology ; Aged, 80 and over ; Carcinoma, Renal Cell ; pathology ; Duodenal Neoplasms ; pathology ; Humans ; Kidney Neoplasms ; pathology ; Lung Neoplasms ; pathology ; Male ; Neoplasms, Multiple Primary ; pathology ; Sarcoma ; pathology ; Stomach Neoplasms ; pathology

OBJECTIVETo explore the correlation of the gene polymorphisms of Toll-like receptor 2 ( TLR2) and TLR4 with the susceptibility and recurrence of condyloma acuminatum (CA).

METHODSUsing Snapshot, we detected the gene polymorphisms of TLR2 597(T/C), 1350(T/C), 15607(A/G), and 2258(G/A) and TLR4 896(A/G) and 1196(C/T) in the peripheral blood of 140 CA patients and 105 HPV-negative controls. We made comparisons between the CA patients and controls as well as between the cases of recurrent CA and those of non-recurrence at 6 months after treatment.

RESULTSThere were 72, 48, and 20 cases of genotype TT, TC, and CC of TLR2 597 (T/C), respectively, in the CA patients, as compared with 71, 31, and 3 cases in the controls. The gene frequency of mutant C was 31. 43% in the patients, significantly higher than 17.62% in the controls (χ2 = 12.04, P < 0.01), and it was 38.68% in the recurrent cases, remarkably higher than 27.01% in the non-recurrent cases (χ2 = 4.16, P < 0.05). There were 74, 49, and 17 cases of genotype TT, TC, and CC of TLR2 1350( T/C), respectively, in the CA patients, as compared with 73, 29, and 3 cases in the controls. The gene frequency of mutant C was 29. 64% in the patients, significantly higher than 16. 67% in the controls (χ2 =11.05, P < 0.01), and it was 36.79% in the recurrent cases, markedly higher than 25. 29% in the non-recurrent cases (χ2 = 4.18, P < 0.05). There were 44, 66, and 30 cases of genotype AA, AG, and GG of TLR2 15607(A/G), respectively, in the CA patients, as compared with 26, 58, and 21 cases in the controls. There was no significant difference in the gene frequencies of mutant G between the two groups (χ2 = 0.33, P > 0.05). No mutant genes of TLR2 2508 (G/A) or TLR4 896(A/G) and 1196(C/ T) were detected in either the CA patients or the controls. Linkage disequilibrium analysis showed a tight linkage between TLR2 597 (T/C) and 1350(T/C) (D' = 1, r2 = 0.93).

CONCLUSIONTLR2 597(T/C) is tightly linked to 1350(T/C), which is correlated with both the susceptibility and the recurrence of condyloma acuminatum.

Aged ; Case-Control Studies ; Condylomata Acuminata ; genetics ; Gene Frequency ; Genetic Linkage ; Genetic Predisposition to Disease ; Genotype ; Humans ; Polymorphism, Genetic ; Recurrence ; Toll-Like Receptor 2 ; genetics ; Toll-Like Receptor 4 ; genetics

Objective:To explore the use of internet-based continuous visual recognition task (MemTrax test, MTX) as a rapid screening tool for amnestic mild cognitive impairment (aMCI).Methods:Sixty-four patients with aMCI and 64 individuals with normal cognition as healthy controls were enrolled respectively from Department of Neurology and Health Examination Center of the First Affiliated Hospital of Kunming Medical University from August 2018 to December 2019. Montreal Cognitive Assessment (MoCA) scale and MTX were adopted to assess the cognitive function of all subjects. The total adjusted MoCA scale score, correct rate of MTX, reaction time of MTX and MTX score were obtained and statistically analyzed.Results:The adjusted MoCA scale scores of aMCI patients and healthy controls were 19 (14, 24) and 26 (24, 27; Z=6.795), the correct rate of MTX of aMCI patients and healthy controls were 74% (60%, 80%) and 88% (84%, 94%; Z=8.359), and the MTX score of aMCI patients and healthy controls were 51.11±14.07 and 70.56±14.91 ( t=7.590), respectively, all with statistically significant difference ( P<0.001). Reaction time of MTX of aMCI patients and healthy controls was 1.401 (1.253, 1.590) s and 1.277 (1.163, 1.410) s, respectively ( Z=3.083, P<0.01). After adjustment for age, physical or mental occupation, exercise, hypertension, hyperlipidemia, stroke, sleep time, as well as smoke, the linear regression showed that the aMCI patients had a significant decrease of adjusted MoCA score, correct rate of MTX and MTX score ( P<0.001), and an extension of reaction time of MTX ( P=0.071), compared with the controls. By MTX and MoCA scale assessment, the best cutoff value was 81% for correct rate of MTX and 23 for adjusted MoCA scale score respectively for the prediction of aMCI (with sensitivity of 79.7%, 93.8% respectively, and specificity of 68.8%, 82.8% respectively). The area under the curve (AUC) of correct rate of MTX was 0.93 (95% CI 0.89-0.97, P<0.001), and the AUC of adjusted MoCA score was 0.85 (95% CI 0.78-0.91, P<0.001). There was a statistically significant difference in paired comparison of the two AUCs (χ2=4.620, P<0.05). Conclusion:MTX acts better for the detection of aMCI than MoCA scale, and correct rate of MTX<81% can be considered as the existence of MCI.

Objective To compare the computed orthopantomography(COPT)with Sh?ller radiography(SR),film orthopantomography(FOPT)and other traditional radiographic techniques in the radiography of temporomandibular joint(TMJ).Methods Ninty-eight cases were randomly divided into 3 groups,and the open and close positions of TMJs of both sides were examined with SR,FOPT,and COPT, respectively.The satisfactory rates of the X-ray pictures were statistically analyzed with Pearson chi-square in SPSS10.0,and the satisfactory rates were analyzed with q test between the groups.Results One hundred and forty-four of the open and close positions of 144 TMJ pictures of the COPT group,128 of 128 of the FOPT group,and 6 of 120 of the SR group were satisfactory in the mandible ramus of the TMJ,with satisfactory rate being 100%,100%,and 5%,respectively(P0.01),respectively between FOPT and COPT groups.The difference was not statistically significant.The exposure was as follows:COPT,99—113 mAs;FOPT,210—225 mAs;and SR,48—75 mAs.Therefore,COPT and FOPT were superior to SR in the pictures of the mandible ramus,coronoid process,and incisure,but inferior in the joint space pictures.The satisfactory rates of the condylar process and articular tubercle were same in the 3 groups.The exposure of the FOPT group was greater than that of the COPT and SR groups.Conclusion COPT is superior to SR and FOPT in TMJ radiography,and should be applied widely in the clinic.