OBJECTIVE: To stereospecifically synthesize disaccharide galactopyranosyl(α1 → 2) glucopyranoside with protecting groups which are easily and selectively deprotected. METHODS: With D-glucose as a raw material, a donor methyl 3, 4, 6-tri-O-benzoyl-β-D-glucopyranoside was synthesized through acetylation, bromination, methylation, deacetylation, benzylidenation, selective benzoylation, chloroacetylation, and dechloroacetylation; the glucopyranosyl acceptor and a donor isopropyl 3-O-allyl-2-O-benzoyl-4, 6-O-benzylidene-β-D-1-thiogalactopyranoside were reacted at catalysis to achieve an α-coupled product. RESULTS: At the catalysis of TMSOTf/NIS, galactopyranosyl donor and glucopyranosyl acceptor were coupled to afford stereospecifically a full protected disaccharide galactopyranosyl(α1 → 2) glucopyranoside fragment, methyl 3-O-allyl-2-O-benzoyl-4, 6-O-benzylidene-α-D-galactopyranosyl(1 → 2)-3, 4, 6-tri-O-benzoyl-β-D-glucopyranoside. All products were characterized with NMR and MS etc. CONCLUSION: A full protected 1, 2-cis disaccharide fragment was stereospecifically obtained through coupling reaction due to concerted effect of the special configurations of the galactopyranosyl donor and the glucopyranosyl acceptor. Copyright 2012 by the Chinese Pharmaceutical Association.

The pathogenesis and etiology of still remain unknown. Current evidence suggests that the occurrence of depression may be related to a reduced secretion of neurotransmitters, neuronal apoptosis, inflammation, intestinal flora and other factors. Although the commonly used antidepressants such as SSRIs, SNRIs, NaSSA, and SARIs produce some therapeutic effects, they fail to relieve the full spectrum of the symptoms of depression. In recent years, esketamine was found to produce a potent and a long-lasting antidepressant effect by acting on the NMDA receptors. Herein the authors review the progress in the study of the pathogenesis and drug therapies of depression, the efficacy of esketamine treatment and the underlying mechanism, and the prospect of esketamine treatment. Currently the mechanism of the antidepressant effect of esketamine remains indeterminate and its clinical application is limited, but its effect in rapidly alleviating the symptoms of depression suggests its bright prospect for clinical applications.
Antidepressive Agents ; pharmacology ; Depression ; drug therapy ; Humans ; Ketamine ; pharmacology ; Receptors, N-Methyl-D-Aspartate

OBJECTIVETo investigate the effects of advanced oxidation protein products (AOPP) on epithelial-to-mesenchymal transition (EMT) in cultured human proximal tubular epithelial cells (HK-2) and explore the mechanism.

METHODSHK-2 cells treated with 50, 100, 200, and 400 µg/ml AOPP or 50 µg/m bovine serum albumin (BSA) for 24 h, or with 200 µg/ml AOPP for 0.5, 1, 3, 6, 12, and 24 h were examined for the protein expression of α-SMA and E-cadherin. In cells pretreated with diphenyleneiodonium (DPI) or cytoplasmic superoxide dismutase (C-SOD), the effects of 50 µg/ml BSA and 200 µg/ml AOPP were assessed on the expressions of α-SMA and E-cadherin, malondialdehyde (MDA) level, superoxide dismutase (SOD) activity, catalase (CAT) activity, and glutathione peroxidase (GSH-px) activity.

RESULTSAOPP treatment up-regulated α-SMA expression and down-regulated E-cadherin expression in a dose- and time-dependent fashion. AOPP exposure of the cells resulted in increased MDA level and lowered activities of SOD, CAT and GSH-PX. DPI and C-SOD partially attenuated the effects of AOPP on α-SMA, E-cadherin, MDA, SOD, CAT and GSH-px.

CONCLUSIONAOPP can induce EMT in cultured HK-2 cells via oxidative stress, and this effect can be attenuated by inhibiting the activation of NADPH oxidase and using antioxidants to delay the progression of renal interstitial fibrosis.

Actins ; metabolism ; Advanced Oxidation Protein Products ; Antioxidants ; metabolism ; Cadherins ; metabolism ; Catalase ; metabolism ; Cell Line ; Cells, Cultured ; Down-Regulation ; Epithelial Cells ; cytology ; Epithelial-Mesenchymal Transition ; Glutathione Peroxidase ; metabolism ; Humans ; Malondialdehyde ; metabolism ; NADPH Oxidases ; metabolism ; Oxidative Stress ; Superoxide Dismutase ; metabolism ; Up-Regulation

OBJECTIVETo study the serum level of carbohydrate antigen 125 (CA125) in patients with acute exacerbation of chronic obstructive pulmonary disease (AECOPD) and its relation with pulmonary hypertension.

METHODSForty-six patients with AECOPD complicated by pulmonary hypertension, 46 with AECOPD and 38 healthy control subjects were examined for their clinical data, pulmonary function, echocardiographic findings, and serum levels of lung tumor markers and brain natriuretic peptide (BNP).

RESULTSCompared with the healthy control group, COPD patients with or without pulmonary hypertension showed significantly decreased pulmonary function (P<0.05), especially in those with AECOPD and concurrent pulmonary hypertension (P<0.05). Serum CA125 level was obviously higher in AECOPD group than in the healthy control group, and further increased in AECOPD patients with pulmonary hypertension (P<0.05). The levels of lung tumor markers (CEA, NSE, CYFRA and PROGRP) were similar among the 3 groups (P>0.05). The serum level of BNP in patients with AECOPD and concurrent pulmonary hypertension was significantly higher than that in patients with AECOPD (P<0.05). Pearson linear correlation analysis showed that serum CA125 was positively correlated with pulmonary artery systolic pressure and BNP in AECOPD patients with pulmonary hypertension (P<0.01).

CONCLUSIONSerum CA125 may serve as a serological index to identify AECOPD patients with pulmonary hypertension.

Acute Disease ; Biomarkers, Tumor ; CA-125 Antigen ; blood ; Case-Control Studies ; Disease Progression ; Humans ; Hypertension, Pulmonary ; physiopathology ; Lung ; Natriuretic Peptide, Brain ; blood ; Pulmonary Disease, Chronic Obstructive ; blood ; physiopathology

OBJECTIVETo prepare and characterize monoclonal antibodies (mAb) and polyclonal antibodies against nucleocapsid (N) protein of severe acute respiratory syndrome (SARS)-associated coronavirus (SARS-CoV) and to establish antibodies-based sandwich ELISA for detecting N protein of SARS-CoV, which might apply to early diagnosis of patients with SARS-CoV infection.

METHODSBALB/c mice were immunized with purified recombinant N protein of SARS-CoV for producing mAbs, and New Zealand white rabbits were immunized for producing polyclonal antibodies. The identification of antibodies was performed using indirect enzyme-linked immunosorbent assay (ELISA), indirect fluorescent-antibody assay (IFA), and Western immunoblotting. Capturing and detecting antibodies were selected by pairing the mAbs and polyclonal antibodies one by one and an antibodies-based sandwich antigen capture ELISA was used for detecting N antigen of SARS-CoV.

RESULTSNine mAbs and hyperimmune rabbit polyclonal antibodies, specifically against SARS-CoV nucleocapsid protein were obtained. Using paired ELISA assay, three mAbs N1E8, N8E1 and N10E4 were selected as capturing antibody and rabbit polyclonal antibodies as detecting antibody then triple antibodies-based sandwich ELISA was established following horseradish peroxidase (HRP)-conjugated goat anti-rabbit immunoglobulin G. The recombinant N protein was used as a standard to establish a detection sensitivity of approximated 50 pg/ml with this assay. When tested with 420 serum specimens from serologically confirmed SARS patients, the positive rates of serum N protein were 90.1%, 23% and 0%, in which sera collected from 1 to 10 days, 11 to 20 days and beyond 21 days respectively after the onset of symptoms. The specificity of the assay was 99.86% in 715 control serum specimens. There was no cross-reaction with other respiratory viruses and coronaviruses.

CONCLUSIONSpecific and high affinity mAbs and rabbit polyclonal antibodies were obtained. By paired and optimized sandwich ELISA, a sensitive and specific antigen capture ELISA was established for detecting N antigen of SARS-CoV, which might apply to early diagnosis, source tracing and epidemiological studies of SARS.

Animals ; Antibodies, Monoclonal ; biosynthesis ; Antibodies, Viral ; blood ; Enzyme-Linked Immunosorbent Assay ; Humans ; Mice ; Mice, Inbred BALB C ; Nucleocapsid ; immunology ; Rabbits ; SARS Virus ; immunology ; isolation & purification ; Sensitivity and Specificity ; Severe Acute Respiratory Syndrome ; virology

OBJECTIVETo explore the morphometric abnormalities of brain gray matter (GM) in patients with chronic low back pain (CLBP).

METHODSThirty patients with CLBP and 30 healthy individuals were enrolled and examined with a 3.0 T magnetic resonance (MR) scanner. High-resolution T1 structural MR data were acquired and data analysis was performed using voxel-based morphometry (VBM) in FMRIB Software Library. The morphological differences were compared between the two groups.

RESULTSs Compared with the healthy control subjects, patients with CLBP showed decreased GM volumes in several brain cortical areas including the bilateral superior frontal gyrus, right frontal pole, left insular cortex, left middle and left inferior temporal gyrus (P<0.05, after TFCE correction). Increased GM volumes were found in the patients in the subcortical structures including the left thalamus, bilateral putamen, bilateral nucleus accumben and right caudate nucleus (P<0.05, after TFCE correction).

CONCLUSIONPatients with CLBP have different patterns of GM abnormalities in different brain regions, characterized by reduced GM volume in cerebral cortical regions and increased GM volume in the subcortical nuclei. Such changes might be associated with the maladaptation of the brain in chronic pain state.

Cerebral Cortex ; Frontal Lobe ; Gray Matter ; diagnostic imaging ; pathology ; Humans ; Low Back Pain ; physiopathology ; Magnetic Resonance Imaging ; Temporal Lobe ; Thalamus

OBJECTIVETo investigate the clinical therapeutic results of allograft tendon for anatomical reconstruction of medial patellofemoral ligament (MPFL) for the treatment of patellar dislocations.

METHODSFrom September 2008 to June 2013, 16 patients with patellar dislocation underwent MPFL reconstructions. There were 2 males and 14 females, aged 11 to 27 years old (16 years old on average). Patellar dislocations occurred in 11 left and 5 right knees. The disease course ranged from 3 to 10 years. The frequency of dislocation ranged from 9 to 33 times (19 times on average). Affected knee joints showed patellar instability; the range of action for patella obviously increased. The X-ray films showed patellar dislocation. The preoperative Q angle was (36 ± 9)°, and the congruence angle was (63 ± 18)°. Reconstruction was performed via allograft tendon. Allograft tendon was fixed through the superomedial pole of the patella, and the other end was fixed at the natural MPFL insertion site near the medial femoral condyle with an interference screw in a bone tunnel. All the patients were evaluated postoperatively; Kujala patellofemoral scores, objective knee function, complications, and reoperations were assessed.

RESULTSPrimary healing was achieved in all cases. No infection or necrosis and absorption of grafts was observed. All the patients were followed up for an average of 16.4 months (ranged, 10 to 24 months) postoperatively. At the latest follow-up, all the patients had no pain, swelling and patellar instability; neither patella redislocation nor fracture occurred. The X-ray films showed good position of tunnel 6 months after operation, and the congruence angle was (5 ± 9)°, showing statistically significant difference when compared with preoperation (P < 0.05). The postoperative Q angle was (17 ± 8)°, the Kujala knee function score improved significantly from 45.20 ± 9.20 to 89.30 ± 6.40 at the latest follow-up, showing statistically significant difference (P < 0.05).

CONCLUSIONMPFL reconstruction improves clinical symptoms. Anatomical MPFL reconstruction is effective for patellar dislocation, and it offers good recovery of the premorbid patella mechanics. The interference screw provides firm fixation. Allograft can avoid the graft harvest site morbidity, but it increases the cost of the surgery.

Adolescent ; Adult ; Allografts ; Child ; Female ; Humans ; Ligaments, Articular ; surgery ; Male ; Patellar Dislocation ; surgery ; Patellofemoral Joint ; surgery ; Reconstructive Surgical Procedures ; methods ; Tendons ; transplantation

OBJECTIVE: To establish 10-color fluorescent antibody combination panels for the detection of minimal residual disease (MRD) of acute myeloid leukemia (AML) in our laboratory and discuss the value of clinical application. METHODS: According to the antigen expression characteristics of leukemia cells of incipient AML patients, MRD in bone marrow were detected by multiparameter flow cytometry, and the test results were compared with both bone marrow cell morphology and PCR results, then 10-color fluorescent antibody combination panels in our lab for MRD detection was determined. RESULTS: The immunophenotypic characteristics of 392 incipient patients with AML in the First Affiliated Hospital of Zhengzhou University were analyzed, among them 357 (91.07%) cases showed abnormal immunophenotypes, which mainly included cross-lineage expression, cross-stage expression, deficiency of antigen expression or abnormal antigen intensity and other abnormal expression. The 10-color fluorescent antibody combination panels established according to abnormal immunophenotypic characteristics of leukemia cells were applied for detecting MRD in 156 patients with AML, the positive rate (43.6%) was higher than 26.8% of morphology, and the results were highly consistent with PCR detection results (96.49%), moreover, the recurrence rate of MRD positive patients (86.96%) was significantly higher than 5.75% of MRD negative patients. Therefore, this method could truly reflect the load of leukemia cells and prompt change of disease condition. CONCLUSION Multiparameter flow cytometry can detect various abnormal immunophenotypes of AML. The 10-color fluorescent antibody combination panels in our lab based on the characteristics of antigens expression in leukemia cells can well detect MRD of leukemia cells, so as to predict relapse and provide basis for clinical treatment.
Bone Marrow ; Flow Cytometry/methods* ; Humans ; Immunophenotyping ; Leukemia, Myeloid, Acute/diagnosis* ; Neoplasm, Residual/diagnosis*

OBJECTIVETo explore the expression of PD-L1 in acute leukemia patients, and to analyze the relationship of PD-L1 expression with the patients' clinical characteristics and prognosis.

METHODSThe expression of PD-L1 in leukemia cells of 75 patients including 59 de novo patients and 16 relapse/refractory patients with acute leukemia was detected by the flow cytometry, the clinical information was collected, and the therapeutic efficacy of de novo patients was analyzed.

RESULTSThe PD-L1 was expressed in human acute leukemia cells with total expression rate 32% (24/75), and its expression level in AML-M5 was higher than that in other leukemias [56.3% (9/16) vs 25.4% (15/59)], there was statistical significance (P = 0.019). The PD-L1 possitive rate in relapse/refractory group was higher than that in de novo patient group [(56.3% (9/16) vs 25.4% (15/59)], and there was statistical significance (P = 0.019). In 59 de novo patients, the CR rate of PD-L1 positive group after 1 course of chemotherapy was lower than that in PD-L1 negative group (66.7% vs 71.4%), the CR rate of PD-L1 positive group after 2 courses of chemotherapy was also lower than that in PD-L1 negative group (70% vs 88.6%). The relapse rate and the proportion of refractory patients in PD-L1 possitive group were higher than those in PD-L1 negative group. The expression of PD-L1 did not correlated with the clinical parameters, such as sex, age, extramedullary infiltration, percentage of blast cells in bone marrow, counts of WBC, RBC and platelet, as well as molecular biological features and cytogenetical characteristics.

CONCLUSIONPD-L1 is expressed in human acute leukemia cells, and may be involved in the immune escape and primary resistant mechanisms, PD-L1 may be used as an indicator for evaluation of the the patients' prognosis and reocurrence.

Acute Disease ; B7-H1 Antigen ; Flow Cytometry ; Humans ; Leukemia ; Prognosis ; Recurrence

OBJECTIVE: To investigate the expression of CD123 in patients with acute myeloid leukemia (AML) and its relationship between clinical features, concomitant fusion gene or gene mutation, efficacy and prognosis. METHODS: 365 patients with newly diagnosed AML (except M3) treated in the First Affiliated Hospital of Zhengzhou University were enrolled and retrospective analysis, and multi-parameter flow cytometry was performed to detect the expression of CD123 in myeloid leukemia cell population. CD123≥20% was defined as positive. Clinical features, concomitant fusion gene or gene mutation, efficacy and prognosis of CD123 RESULTS: The positive rate of CD123 in 365 newly diagnosed AML patients was 38.9%. Compared with the CD123 CONCLUSION CD123 positive indicates that AML patients have higher tumor burden and are more difficult to reach remission. It is an independent risk factor for OS and EFS in patients with normal karyotype and intermediate risk, which is important to evaluate the prognosis of patients with AML without specific prognostic marker.
Humans ; Interleukin-3 Receptor alpha Subunit ; Karyotype ; Leukemia, Myeloid, Acute/genetics* ; Mutation ; Patients ; Prognosis ; Retrospective Studies