Objective To measure the levels of serum transferrin receptors (sTfR) and serum ferritin (SF) in children with hemoglobin H disease for investigation the iron metabolism(sideropenic or iron overload) and to guide the proper intervention.To get a best index of judging the iron overload in HbH children by analysis of the values of sTfR and sTfR/lgSF.Methods Peripheral blood specimens were obtained from 50 cases of HbH children and 30 cases of healthy normal controls,the levels of sTfR and SF were examined by enzyme linked immunosorbent assays(ELISA).The diagnosis efficiency of sTfR and sTfR/lgSF in HbH children′s iron metabolism was judged by receiver operator cha-racteristic (ROC) curve analysis.Results The level of sTfR in HbH group was (6.74?1.02) mg?L-1,which was significantly lower than that in healthy control group[(8.09?0.67) mg?L-1](P

Objective To study the effect of balloon dilatation therapy on dysphagia caused by cricopharyn- geal achalasia.Methods Ten cases of dysphagia were diagnosed as cricopharyngeal achalasia by videofluoroscopic swallowing study(VFSS).A 14~* urethral catheter was inserted into the esophagus and an amount of water was injec- ted into the balloon of the urethral catheter to make it turgid.Then the catheter was pulled upwards and passed through the stricture of esophagus to dilatate the cricopbarygeus muscle.Meanwhile,low frequency electrical stimula- tion was used and combined with functional training of the organs related to deglutition and ingestion.The results be- fore and after the treatment were evaluated.Results After 19.7 times of dilatation therapy,the content of water in- jected into the balloon was increased from 2.65?0.91 ml to 8.20?0.92 ml.Cricopharyngeal achalasia was alle- viated significantly(P

Objective To undemtand the rhythm of urinary iodine level of children aged 8-10 in Chongqing city.Methods In April 2008,using the stratified random sampling method,we sampled 60 children aged 8-10 in a lodging primary school in Chongqing(20 per age group,half male and half female),the urine samples were collected in the morning and at 10:00,12:30,16:00,iodine in urine was detected by method of Ce and arsenic catalytic speetrophotometry(WS/T 107-2006).The difference of the urinary iodine level was compared by age,sex and time of day.Results The median urinary iodine of 60 children was 265.07μg/L on the overall.Irrespective of the stratification factors,excluding morning urinary iodine(366.75μg/L)and urinary iodine at 10:00(338.30 μg/L),the urinary iodine between 12:30(235.15μg/L)and 16:00(251.50μg/L)was not significant(all P>0.05),statistically significant differences(all P<0.05)were found between any two.The urinary iodine of 8-year-old group at different times of the day was significantly different(all P<0.05),except between morning urinary iodine (298.90 μg/L)and at 10:00,16:00(279.00,286.59 μg/L),between urinary iodine at 10:00 and 16:00(all P>0.05).The 9-year-old group's urinary iodine were not significantly different between morning urine(366.15μg/L)and 10:00(368.10 μg/L),and between 12:30(244.00 μg/L)and 16:00(186.30 μg/L,all P>0.05),significant differences were faund at other times of the day(all P<0.05).The 10-year-old group of urinary iodine changed very little before 12:30 (382.85,449.60,337.00 μg/L, all P > 0.05 ), followed by rapid decline to 16: 00 (269.35 μg/L), and compared with the morning urine and 10:00, there was significant difference(all P < 0.05).Regardless boys or girls, the urinary iodine at different times qf the day was significantly different (all P < 0.05),except between morning urinary iodine(337.32,309.28 μg/L) and at 10:00(316.15,288.27 μg/L), between urinary iodine at 12:30(251.18,211.45 μg/L) and 16:00(235.02,211.45 μg/L, all P > 0.05). Conclusions The change of urinary iodine level in children aged 8 - 10 was not obvious before noon, changes can be seen in the afternoon.Urinary iodine level before 10:00 is indicative.

This paper is to report the study of the metabolism of forscolin in plasma and liver microsomes for guiding clinical therapy. Forscolin was quantified by HPLC-MS/MS. The metabolic stability of forscolin in rat, Beagle dog, monkey and human plasma and liver microsomes, mediated enzymes of forscolin and its inhibition on cytochrome P450 isoforms in human liver microsomes were studied. Results showed that forscolin was not metabolized in plasma of the four species but metabolized in liver microsomes of the four species. The t1/2 of forscolin in rat, Beagle dog, monkey and human liver microsomes were (52.0 +/- 15.0), (51.2 +/- 5.9), (6.0 +/- 0.2) and (11.9 +/- 1.8) min; CL(int) were (75.6 +/- 18.7), (60.9 +/- 6.8), (513.8 +/- 14.3) and (176.2 +/- 25.6) mL x min(-1) x kg(-1); CL were (34.8 +/- 4.5), (23.3 +/- 1.0), (40.3 +/- 0.5) and (17.9 +/- 0.3) mL x min(-1) x kg(-1), respectively. Forscolin was metabolized by CYP3A4 in human liver microsomes. There was definite inhibition on CYP3A4 at the concentrations of forscolin between 0.1 ng x mL(-1) and 5 microg x mL(-1). Therefore, forscolin is rapidly excreted from liver microsomes. Attention should be paid to the drug interaction when forscolin was used along with other drugs metabolized by CYP3A4 in clinics.
Animals ; Chromatography, High Pressure Liquid ; Coleus ; chemistry ; Colforsin ; blood ; isolation & purification ; metabolism ; Cytochrome P-450 CYP3A ; metabolism ; Dogs ; Humans ; Macaca ; Metabolic Clearance Rate ; Microsomes, Liver ; metabolism ; Plants, Medicinal ; chemistry ; Rats ; Tandem Mass Spectrometry

Granulocyte colony-stimulating factor (G-CSF) is a kind of hematopoietic growth factor which is produced by monocytes, fibroblasts and endothelial cells. G-CSF acts on neutrophilic progenitor cells by binding to specific cell surface receptors, thereby stimulates proliferation, differentiation, commitment, and selected end-cell functional activation including enhanced phagocytic ability, priming of the cellular metabolism associated with respiratory burst, antibody dependent killing and the increased expression of some functions associated with cell surface antigens. G-CSF is effective and safe for treatment of neutropenia. In this paper, structure of G-CSF and its mechanism, recent status of research on G-CSF, pharmacokinetics, clinical application, adverse effects and prospect of G-CSF are mainly reviewed.
Granulocyte Colony-Stimulating Factor ; pharmacokinetics ; pharmacology ; therapeutic use ; Hematopoiesis ; drug effects ; Humans

Objective To investigate the expression of transforming growth factor β1,transforming growth factor beta receptor(TBR)Ⅰ,TβR Ⅱ,Smad4 and C-Jun in rats with nonalcoholic fatty liver disease(NAFLD)and to find out the mechanisms of liver fibrosis in patients with NAFLD.Methods A total of 18 male SD rats were randomly divided into normal control group(n=9)and model group(n=9).The rats in control group were fed with normal diet,and those in model group were fed with fat-rich diet(consisted of 10%lard oil+2%cholesterol).An rats were sacrificed at the 20th week.The levels of TGFβ1,TβR Ⅰ and TβR Ⅱ mRNA were examined by RT-PCR.The expressions of TGFβ1 and Smad4 in liver tissue were detected by immunohistochemistry.The expression of C-Jun protein was detected by Western blotting.Results The NAFLD model was successfully established.The immunohistochemistry examination revealed that TGFβ1 and Smad4 were expressed weekly in control group,but strongly expressed in model group.RT-PCR showed that A values of TGFβ1,TβR Ⅰ and TβR Ⅱ mRNA were 0.46±0.12,5.z4±2.70 and 3.35±1.95,respectively,in model group,which were higher than those in control group(0.21±0.09,1.36±0.77 and 0.52±0.19,all P values＜0.01).The Western blotting results demonstrated that the expression of C-Jun protein in model group(0.93±0.41)was higher than that in control group (0.32±0.25,P=0.001).Conclusion TGFβ1/Smad4 signal pathway might be involved in the development of hepatic fibrosis in NAFLD.Blocking TGFβ1/Smad4 signal pathway will be helpful in treatment of NAFLD.

This paper is to report the study of the metabolism of lidamycin in vitro including in plasma and microsomes to guide clinical therapy. Lidamycin was quantified by detecting its active ingredient using HPLC-MS/MS. The metabolic stability of lidamycin in rat, Beagle dog, monkey and human plasma and liver microsomes, and its inhibition to cytochrome P450 isoforms in human liver microsomes were studied. Results showed that lidamycin was metabolized in the four species of plasma, and the sequence of metabolic rates in plasma were in rat > in dog > in human > in monkey. But among the four species of liver microsomes, lidamycin was metabolized only in monkey liver microsomes. There was almost no inhibition to cytochrome P450 isoforms at the concentrations of between 0.0005 and 10 ng x mL(-1). Therefore, the property of lidamycin metabolism in human is similar with that in dog, and metabolism of other drugs would not be decreased by cytochrome P450 as used along with lidamycin in clinic.
Aminoglycosides ; blood ; metabolism ; Animals ; Antibiotics, Antineoplastic ; blood ; metabolism ; Chromatography, High Pressure Liquid ; Cytochrome P-450 CYP1A2 ; metabolism ; Cytochrome P-450 Enzyme System ; metabolism ; Dogs ; Enediynes ; blood ; metabolism ; Enzyme Activation ; Humans ; Macaca ; Microsomes, Liver ; metabolism ; Rats ; Tandem Mass Spectrometry

CD22 is a transmembrane sialoglycoprotein and a member of the immunoglobulin superfamily. Its expression is restricted to the B cell lineage and a vast majority of B cell NHLs. CD22 plays a key role in B cell development, survival, and function. Humanized anti-CD22 antibodies were developed to minimize the immunogenicity and to enhance effector interactions during their developments of diagnostic and immunotherapeutic agent. Preclinical test with anti-CD22 antibodies indicates that a single, conjugated or radiolabeled agent has shown preliminary antitumor activity in patients with recurrent and heavily pretreated NHL. Anti-CD22 antibodies were well tolerated, without dose-dependant toxicity. Anti-CD22 antibodies are currently being evaluated in combination with rituximab, and the early results suggest that the combination of the two antibodies are well tolerated and may result in better clinical activity than the single agent alone. Thus, anti-CD22 antibodies are theoretically good candidates alone and in combination with other drugs in the treatment of B cell malignancies. In this review, the physiologic function and characteristics of CD22 antigen as target molecule of guide therapy for NHL, the types of anti-CD22 antibodies in therapy of NHL and the combination use with other antibodies were summarized.
Animals ; Antibodies, Monoclonal ; immunology ; therapeutic use ; Antibodies, Monoclonal, Humanized ; Humans ; Immunotherapy ; Lymphoma, Non-Hodgkin ; therapy ; Sialic Acid Binding Ig-like Lectin 2 ; immunology

A rapid, sensitive and simple liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed for the simultaneous determination of yogliptin and its metabolite in Wistar rat plasma. Linagliptin and dexamethasone were chosen as the internal standards of yogliptin and its metabolite, (R)-8-(3-hydroxypiperidine- -yl)-7-(but-2-yn-1-yl)-1-((5-fluorobenzo[d]thiazol-2-yl)methyl)-3-methyl- H-purine-2, 6 (3H, 7H)-dione, respectively. After a simple protein precipitation using acetonitrile as the precipitating solvent, both analytes and ISs were separated on a Grace Altima HP C18 column (2.1 mm x 50 mm, 5 microm) with gradient elution using methanol (containing 0.1% formic acid, 4 mmol x L(-1) ammonium acetate)-0.1% formic acid (containing 4 mmol x L(-1) ammonium acetate) as the mobile phase. A chromatographic total run time of 4.4 min was achieved. Mass spectrometric detection was conducted with electrospray ionization under positive-ion and multiple-reaction monitoring modes. Linear calibration curves for yogliptin and its metabolite were over the concentration range of 0.5 to 500 ng x mL(-1) with a lower limit of quantification of 0.5 ng x mL(-1). The intra- and inter- assay precisions were all below 14%, the accuracies were all in standard ranges. The method was used to determine the concentration of yogliptin and M1 in Wistar rat plasma after a single oral administration of yogliptin (27 mg x kg(-1)). The method was proved to be selective, sensitive and suitable for pharmacokinetic study of yogliptin and M1 in Wistar rat plasma.
Animals ; Chromatography, Liquid ; Dexamethasone ; blood ; Dipeptidyl-Peptidase IV Inhibitors ; blood ; pharmacokinetics ; Linagliptin ; blood ; Rats ; Rats, Wistar ; Tandem Mass Spectrometry

The metabolism, distribution and excretion profiles of recombinant human thrombopoietin (rhTPO) in mice were studied by means of (125)I-labeled rhTPO ((125)I-rhTPO) combined with size exclusive high performance liquid chromatography (SHPLC) or trichloroacetic acid (TCA) precipitation analysis. (125)I-rhTPO was prepared by iodogen method. Purification was performed on Sephacryl S-200 HR gel. Radioactive-purity of (125)I-rhTPO identified by SHPLC was (96.9 +/- 1.5)% (n = 3). The proliferation effect of TPO dependent cell line (TD-3) and the increase of peripheral platelet counts in mouse by (125)I-rhTPO demonstrated that (125)I-labeled protein maintained the biological activities of TPO both in vitro and in vivo. SHPLC analysis of serum and urine samples taken after sc 1 micro g/mouse (345 kBq/mouse) of (125)I-rhTPO revealed that there were two lower molecular weight (125)I-degradation metabolites ((125)I-MI and (125)I-MII) other than parent molecule. (125)I-MI was mainly found in urine, and (125)I-MII was detected both in serum and in urine. The maximal concentration of (125)I-rhTPO was reached at 2 hours after injection. The terminal half-life was 10.8 hours, which was much longer than those of other peptides. TCA precipitable radioactivity in tissue showed that the radioactivity in bone marrow was rather high. The highest level was found in urinary system. Levels in adrenals, lymph nodes, and fat were near to that in serum. Lowest was found in brain. The main excretion route was urinary system and (98 +/- 5.6)% of (125)I-rhTPO was excreted within 72 hours after dosing.