Objective To discuss the mechanism of rubia cordifolia extractive affecting some biochemical indicators of blood serum and sporting ability in highly endurance-trained rats,which can provide theoretical basis for using rubia cordifolia extractive as sport supplements.Methods After establishing the highly endurance-trained rats model,we tested the exhaustion time in the trained rats and the contents of serum urea(BUN),lactic dehydrogenase(LOH),blood lactate(BLa)as well as the cruarin(Hb)in the rats.Results The activity of LDH in training group was greater than that in silent group(P

OBJECTIVETo discuss the changes in Wnt pathway inhibiting factors in esophageal precancerosis lesions induced by methyl benzyl nitrosamine (MBNA) and the effect of Gexia Zhuyu decoction.

METHODWistar rats were subcutaneously injected with MBNA (3.5 mg x kg(-1) for twice per week to establish the model. Since the 1st day after the model establishment, they were orally administered with Gexia Zhuyu decoction (16, 8 mg x kg(-1)). At the 10th week, esophageal tissues were collected to observe the pathological changes of esophageal mucosa, detect SFRP1, sFRP4, Axin1, Axin2 and GSK-3β mRNA levels.by fluorescent quantitation PCR analysis and β-catenin protein level by Western blotting.

RESULTBeing induced by MBNA, rats in the model group showed slight atypical hyperplasia in the histopathological examination. Compared with the normal group, Gexia Zhuyu decoction dose high and low groups showed no significant pathomorphological and histological changes. The model group showed lower gene transcription levels of esophageal tissues sFRP1, sFRP4, Axin1 and Axin2 (P < 0.05 or P < 0.01) and higher β-catenin protein expression level (P < 0.01) than the normal control group. The Gexia Zhuyu decoction low dose group showed higher gene transcription levels of esophageal tissues sFRP1, sFRP4, Axin1 and Axin2 (P < 0.05 or P < 0.01) and lower β-catenin protein expression level (P < 0.01) than the normal control group.

CONCLUSIONUp-regulated β-catenin protein level and down-regulated Wnt pathway could enhance Wnt pathway activity of MBNA-induced esophageal precancerous lesions. Gexia Zhuyu decoction could down-regulate the β-catenin protein level and up-regulate the transcription level of Wnt pathway inhibiting factors, but could not block MBNA-induced esophageal precancerosis lesions.

Animals ; Axin Protein ; genetics ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; Esophageal Diseases ; drug therapy ; genetics ; metabolism ; pathology ; Glycogen Synthase Kinase 3 ; genetics ; metabolism ; Glycogen Synthase Kinase 3 beta ; Humans ; Male ; Necrosis ; Nitrosamines ; adverse effects ; Proteins ; genetics ; metabolism ; Rats ; Rats, Wistar ; Wnt Proteins ; genetics ; metabolism ; Wnt Signaling Pathway ; drug effects

Increasing attention has been focused on the antitumor activity of artemisinin derivatives in recent years, for artemisinin had been reported to have cytotoxic effects against HL-60, P388 and MCF-7 tumor cells. We report here the synthesis and evaluation for antitumor activity of a series of artemisinin-ether derivatives bearing tetrahydropyrrole, morpholine, piperidine, substituted piperidines and azoles with various linkers. Sixteen 10-O-substituted dihydroartemisinin derivatives were designed and synthesized, all of which have never been reported in literatures and whose antiproliferative effects on human breast cancer MCF-7, MCF-7/Adr and HL-60 cells were determined by MTT assay or direct cell counting. Each of these artemisinin derivatives possessed better effects than dihydroartemisinin evidently against HL-60 and MCF-7 cells growth, while less potent than doxorubicin. All target compounds exhibited significantly improved potency compared to DHA and doxorubicin on the doxorubicin-resistant MCF-7/Adr cells, so did they in their sensitive counterparts MCF-7 cells. Among them, compounds GF02, GH04 and ZH04 showed strong activity against these three cell lines growth. Further research is undergoing.
Antineoplastic Agents ; chemical synthesis ; chemistry ; Artemisinins ; chemical synthesis ; chemistry ; Breast Neoplasms ; pathology ; Cell Proliferation ; Doxorubicin ; Drug Design ; HL-60 Cells ; drug effects ; Humans ; MCF-7 Cells ; drug effects

Objective One typical case with stress cardiomyopathy was reported and the current knowledge of the syndrome was reviewed to improve relevant knowledge.Methods A 71-year-old female patient presented dyspnea and chest pain due to emotional stress.ECG,echocardiography,selective coronary artery angiography,left ventriculography,~(99)Tc~m-MIBI single photon emission computed tomography (SPECT),~(18)F-FDG SPECT and MRI were performed.Results Electrocardiogram at admission showed ST segment elevation and T wave inversion in leads V1—V4.Pathological Q wave occurred 1 week later,it disappeared 1 month later however and severe T wave inversion occurred.Normal or slightly elevated cardiac enzymes in the blood were found during the course.Left ventriculogram at admission showed left ventricular apical ballooning with LVEF of 30%.The ballooning volume was about 3/4 of left ventricular volume, without any corresponding coronary artery diseases found in coronary angiogram.The abnormal apical ballooning decreased significantly in the follow-up left ventriculogram performed one month later.The LVEF rose up to 63.6%.~(99)Tc~m-MIBI and ~(18)F-FDG SPECT showed mismatch of perfusion and metabolism in the corresponding region,indicating presence of viable myocardium.MRI showed left ventricular apical ballooning without perfusion defect and late enhancement,indicating viability of corresponding myocardium. Conclusions Emotional stress can cause transient left ventricular apical ballooning called"stress cardiomyopathy".Either ~(99)Tc~m-MIBI SPECT associated with ~(18)F-FDG SPECT or delayed enhancement MRI plays an important role in identification of myocardial viability,which can efficiently guide clinical treatment.

AIM: To study the effects of apolipoprotein (apo) A-Ⅰon ATP binding cassette transporter A1 (ABCA1) degradation and cholesterol efflux in THP-1 macrophage-derived foam cells. METHODS: After exposure of the cultured THP-1 macrophage-derived foam cells to apolipoprotein A-Ⅰ for different time, cholesterol efflux, ABCA1 mRNA and protein level were determined by liquid scintillation counting, reverse transcriptase-polymerase chain reaction and Western blotting, respectively. The mean ABCA1 fluorescence intensity on THP-1 macrophage-derived foam cells was detected by flow cytometry. RESULTS: ApoA-Ⅰ markedly increased ABCA1-mediated cholesterol efflux from THP-1 macrophage-derived foam cells. This was accompanied by an increase in the content of ABCA1. ApoA-Ⅰ did not alter ABCA1 mRNA abundance. Thiol protease inhibitors increased the level of ABCA1 protein and slowed its decay in THP-1 macrophage-derived foam cells, whereas none of the proteosome-specific inhibitor lactacystin, other protease inhibitors, or the lysosomal inhibitor NH_4Cl showed such effects. The apoA-Ⅰ mediated cellular cholesterol efflux was enhanced by thiol protease inhibitors. CONCLUSION: Thiol protease inhibitors might provide an alternative way to upregulate ABCA1 protein. This strategy is especially appealing since it may mimic the stabilizing effect of the natural ligands apoA-Ⅰ.

Objective To investigate the value of the Wells score and D-dimer assay in assisting pulmonary perfusion imaging (PPI) for the diagnosis of acute pulmonary embolism (APE). Methods One hundred twenty-one patients with suspected APE were studied from January, 2006 to December, 2008. All patients underwent the Wells score, the quantitative D-dimer assay, chest X-ray photography, and PPI. The diagnostic sensitivity, specificity, positive predictive value and negative predictive value of PPI with the assistance of Wells score and D-dimer assay were calculated. Results Fifty (41.3%) patients were diagnosed with APE. PPI combined with chest X-ray photography (Q/X scan) showed positive results in 49 patients. The sensitivity, specificity, positive predictive value and negative predictive value of the Q/X scan were 86.0% (43/50), 91.5% (65/71), 87.8% (43/49) and 90.3% (65/72), respectively. With assistance of Wells score >4 and D-dimer≥0. 5 mg/L, Q/X scan had a positive predictive value of 100.0% (29/29), for patients with Wells score ≤4 and D-dimer<0.5 mg/L, the negative predictive value for Q/X scan was 100.0% (41/41). Conclusion Combined with Wells score and D-dimer assay, PPI can make accurate diagnosis of APE.

OBJECTIVETo study synthesis of baicalin-copper and baicalin-aluminium complex and its antimicrobial, anti-tumor activity and anti-tumor effect against macrophages.

METHODBaicalin was reacted with metallic salt under a weak base condition to produce baicalin-copper and baicalin-aluminium complex. Baicalin and its synthesized complex were detected for antimicrobial activity against Staphylococcus aureus, Hay bacillus, Escherichia coli, Salmonella and Candida albicans by twofold broth dilution technique. Their anti-tumor activity against A549 and IC50 of HepG2 cells and anti-tumor effect against macrophages were detected by the MTT. And their phagocytic effect on macrophages was determined by the neutral red assay.

RESULTThe yields of baicalin-copper and baicalin-aluminium complex were 73.93% and 91.08%, respectively. The minimum inhibitory concentration (MIC) value against Staphylococcus aureus, Hay bacillus, Escherichia coli, Salmonella and Candida albicans was 0.0004, 0.0009, 0.0004, 0.0009, 0.000 4 mol x L(-1) for baicalin-copper complex and 0.0011, 0.0011, 0.0011, 0.0011, 0.0005 mol x L(-1) for baicalin-aluminium complex. The IC50 values against A549 and HepG2 cells were 89.6, 22.6 micromol x L(-1) for baicalin-copper complex, and 138.8, 97.2 micromol x L(-1) for baicalin-aluminium complex. The inhibitory ratio of macrophage on A549 cell was 43.52%, 80.89%, 52.66%, respectively, after the macrophages were stimulated by baicalin, baicalin-copper and baicalin-aluminium complex at a concentration of 160 micromol x L(-1).

CONCLUSIONThe acute toxicity test in mice showed that the complex was nontoxic to mice. Baicalin-copper complex showed the highest antimicrobial, anti-tumor activity, and the strongest effect on the anti-tumor activity of macrophage, while baicalin showed the lowest activities compared with baicalin-copper and baicalin-aluminium complex.

Aluminum ; Animals ; Anti-Bacterial Agents ; chemical synthesis ; chemistry ; pharmacology ; Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Copper ; Drugs, Chinese Herbal ; chemical synthesis ; chemistry ; pharmacology ; Flavonoids ; Humans ; Mice ; Microbial Sensitivity Tests

OBJECTIVETo investigate the feasibility and safety of autologous peripheral blood hematopoietic stem cell transplantation (auto-PBHSCT) and its therapeutic effect on refractory rheumatism among preschool children.

METHODSThree boys with juvenile rheumatoid arthritis (JRA), juvenile systemic lupus erythematosus (JSLE) and juvenile dermatomyositis (JDM) respectively, 3 to 6 years old with the mean age of 5 years with 3.5 to 22 months course of disease with 14 months on average, received auto-PBHSCT. Their conditions were so severe that conventional therapy failed to control the diseases. The changes of both clinical manifestations and immunologic indexes were observed before and after transplantation with long term following up at specialty clinic of rheumatism.

RESULTThe time when neutrophil count >or= 0.5 x 10(9)/L in the 3 children was days +9, +13 and +11 respectively, that of platelet count >or= 20 x 10(9)/L was days +14, +18 and +13 respectively. The cellular immune function remained abnormal with CD4 cells at a low level and CD4/CD8 being inverted. As to the JDM child, the skin rash had disappeared and his muscle tone was improved to grade 5 within one month after the transplantation. The EMG and serum creatase level returned to normal and muscle MRI findings were improved greatly within 2 months after the transplantation. As to the JSLE child, skin rash and proteinuria had disappeared, MRI of brain showed that the pathological changes had been absorbed and EEG returned to normal 3 months after the transplantation, all the autoantibodies turned to negative within 8 months after transplantation. As to the JRA child, the arthritis had been improved remarkably within 3 weeks after auto-PBHSCT. There was no swelling of joints nor movement limitation 3 months post transplantation. The steroids and immunosuppressive drugs were discontinued post transplantation. Cushing syndrome disappeared. Their body heights increased by 10 to 15 cm in the past 18 months, and they all returned to school. There was no relapse during follow-up periods of 25 - 27 months.

CONCLUSIONThe therapy with auto-PBHSCT for refractory rheumatism among preschool children was remarkably effective in a short-term, yet the safety and long-term effect still need to be further studied.

Child ; Hematopoietic Stem Cell Transplantation ; Humans ; Male ; Peripheral Blood Stem Cell Transplantation ; Rheumatic Diseases ; therapy ; Transplantation, Autologous ; Treatment Outcome

Adult ; Female ; Femoral Fractures ; diagnostic imaging ; physiopathology ; surgery ; Fibula ; transplantation ; Humans ; Male ; Middle Aged ; Time Factors ; Tomography, X-Ray Computed ; Transplantation, Autologous

Objectives: To investigate the relationships between the stability of carotid plaque and serum Lp-PLA2, A-FABP levels in hypertensive postmenopausal women. Methods: 195 postmenopausal women with hypertension were selected and divided into non-plaque group, stable plaque group and unstable plaque group according to the results of carotid intima-media thickness (IMT) and plaque types derived from color doppler ultrasonography. In addition, 40 healthy postmenopausal women were recruited as normal control group. The serum Lp-PLA2 and A-FABP levels of all subjects were measured. Lp-PLA2 and A-FABP levels were compared among four groups by One-Way ANOVA. Spearman correlation analysis and multiple logistic regression analysis were also performed. Results: Plaque group included 123 subjects (unstable plaque group: 29 cases; stable plaque group: 94 cases), and non-plaque group included 72 subjects. The average serum A-FABP level was significantly higher in unstable plaque group [(172.60±33.70) ng/L] than in non-plaque group[(133.04±29.49) ng/L], P<0.05. Serum Lp-PLA2 level was similar between the four groups, P>0.05. Serum A-FABP level was positively correlated with the carotid plaque (r=0.3446, P=0.0049);serum Lp-PLA2 level was not correlated with the carotid plaque (r=0.2058, P=0.0996). Multiple logistic regression analysis showed that high A-FABP level was associated with stable plaque in hypertensive postmenopausal women (P=0.040, OR=1.017, 95%CI: 1.001~1.033), which was also associated with unstable plaque in this population (P=0.003, OR=1.031, 95%CI: 1.010~1.052). Conclusions: The level of A-FABP is a determinant responsible for the occurrence and stability of carotid plaque among hypertensive postmenopausal women. There was no correlation between Lp-PLA2 level and the stability of carotid plaque in this patient cohort.