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

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 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.

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

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

Objective:To investigate the inhibitory effect of in vivo non-targeting transfection of recombinant fibronectin polypeptide CH50 against tumors and to study the related mechanisms.Methods:After inoculated with tumor cells, BALB/c mice were injected with CH50 plasmids,control plasmids,and normal saline separately.The growth of the tumor was observed;the expression of genes (such as B7-1,B7-H1 etc.) in tumor tissues was detected by RT-PCR;and the count of T lymphocytes in local tumor tissues was analyzed by flow cytometry.Results:The tumor growth was obviously suppressed by in vivo CH50 expression.The expression of genes (B7-1 and B7-H1) was up-regulated along with the growth of tumor.CH50 increased the ratios of B7-1/B7-H1 and B7-1/B7-DC and suppressed the up-regulation of IL-10 and TGF-?genes.The direct action of CH50 on H22 cells resulted in the down-regulatoin of TGF-?gene.The count of T lymphoeytes in tumor tissues of CH50 treatment group was significantly higher than that in other groups.Conclusion:Ex- pression of CH50 by non-targeting transfection can effectively inhibit the growth of tumor;the regulation of the immuno- regulatory genes in tumor mieroenvironment is an important part of the treatment mechanism of CH50.

Objective To investigate the effect of 131I on apoptosis of thyrocytes in patients with Graves disease. Methods Forty-seven patients with Graves disease were divided into two groups, two week group (G2w) and four week group (G4w). All patients underwent thyoid needle biopsy before 131I treatment and the repeated biopsy at two weeks (G2w) or four weeks (G4w) after 131I treatment. The positive units of pro-apoptotic proteins (Fas, FasL) and anti-apoptotic protein (Bcl-2) were studied with immunohistochemistry staining. The differences of the two groups were compared with t-test. Liner correlation analysis was applied to study the correlation between 131I dose and apoptosis-related proteins and that between serum sTSH after 131I treatment and apoptosis-related proteins. Results Fas, FasL and Bcl-2 expression (positive units) were significantly increased in both groups after 131I treatment, G2w :22.84 ± 9.31 vs 16.20 ± 6.75,21.13±6.29vs 14.56±4.06, 21.69±7.83 vs 15.22 ±5.94, t= -3.08, -3.73, -4.05 (allP<0.05); G4w:21.69 ±4.52 vs 15.83 ±5.03, 19. 11 ±3.75 vs 14.02 ±4.98, 19.06 ±3.44 vs 16.63 ±4. 73, t = - 5.26, - 5.00, - 2.41 (all P<0.05). However, no statistical differences were found between G2w and G4w (t = 0. 53, 0. 82, 1.46, all P > 0.05). Significant correlation was found between 131I 0. 727, rFasL = 0. 763 (both P<0.05)), but not between the dose and Bcl-2, rBcl-2 = - 0. 094, 0. 102(both P > 0.05). There were significant correlation between serum sTSH three months after 131I treatment and apoptosis-related proteins, rFas = 0.433, rFasL = 0. 601, rBcln2 = - 0. 397, (all P<0. 05). Conclusions 131I can induce thyrocytes to express the pro-apoptotic proteins in patients with Graves disease.