Humans ; Membrane Proteins ; metabolism ; Myelodysplastic Syndromes ; metabolism ; Receptors, Colony-Stimulating Factor ; metabolism ; Signal Transduction

Using bioactive compounds 7-hydroxy flavone, salicylaldehyde, cinnamic acid and 4-amino-5- mercapto-1,2,4-triazoles as starting materials, three new types of flavone derivatives containing 1,2,4-triazole structure were synthesized via different step reactions. These new compounds were characterized by 1IHNMR, ESI-MS, IR and elemental analysis. Their scavenging effects on the superoxide radical (O2·-), hydroxyl radical (·OH), DPPH · radical and their total reduction activities were tested. The results showed that all of the compounds possessed some antioxidative activity at the concentration of 0.5 mg · mL(-1), but the scavenging ability of the target compounds was lower than that of the standard compound Vc.
Cinnamates ; chemistry ; Flavones ; chemical synthesis ; chemistry ; Flavonoids ; chemistry ; Free Radical Scavengers ; chemical synthesis ; chemistry ; Triazoles ; chemistry

Objective: To study the effects of soybean phospholipids on fatty acids and phospholipids content in erythrocyte membranes of mice. Methods:The mice were fed with soybean phospholipids of 2 . 5, 5 . 0 , 10.0 g/kg bw respectively while control group with distilled water for 30 days. Then the mice were killed and contents of fatty acids and phospholipids in erythrocyte membranes were detected by HPLC. Results: (1)The contents of linoleic acid (C18 ∶2) and linolenic acid ( C18 ∶3), the composition of polyunsaturated fatty acid (PUFA) were increased obviously (P

Objective To detect the size distribution and Zeta potential of LHRH-MPG△NLS/CDK-siRNA nanoparticles,to observe the effect of different solvents on the nanoparticle size,and to investigate the inhibitory effect of nanoparticles on HepG2 cell growth.Methods LHRH-MPG △NLS and CDK2-siRNA were mixed by continuous stirring to form nanoparticles at different N/P ratios (10/1,20/1 and 40/1).The size distribution and Zeta potential of LHRH-MPG△NLS/CDK2-siRNA nanoparticles were detected by dynamic light scattering,and the stability of the nanoparticles in normal saline,10％ glucose and pure water was discussed.Finally,the inhibitory effect of the nanoparticles on HepG2 cells was determined by CCK8 kit.Results The mean size of the nanoparticles was within 200 nm,and the Zeta potentials were (70±5) mV (N/P=10/1),(120±5) mV (N/P=20/1) and (130±5) mV (N/P=40/1),respectively.The size of the nanoparticles in normal saline was significantly increased,which demonstrated that strong electrolytes had a great impact on the nanoparticles size.When nanoparticle concentration was 200 nmol/L,LHRH-MPG△NLS/CDK2-siRNA nanoparticles (N/P=10/1) showed significantly inhibitory effect on HepG2 cell growth.Conclusions The mean size of the LHRH-MPG△NLS/CDK2-siRNA nanoparticles was within 200 nm,which was ideal for cellular uptake.The Zeta potential of nanoparticles revealed that nanoparticles could be stable in aqueous solution,while strong electrolytes would affect nanoparticle size.When nanoparticle concentration was 200 nmol/L,LHRH-MPG△NLS/CDK2-siRNA nanoparticles (N/P=10/1) showed significantly inhibitory effect on HepG2 cell growth.

Objective To study the value of serum galectin-3 detected by nanomagnetic beads sorting time resolved fluoroimmunoassay (TRFIA) tandem analysis in the diagnosis of pancreatic cancer.Methods The serum of 88 cases of pancreatic cancer,50 cases of acute pancreatitis,10 cases of pancreatic cysts,and 20 cases of healthy volunteers as control were collected.First,galectin-3 antibody coupled nanomagnetic-beads was used to sort the semm,then TRFIA was applied to detect the level of galectin 3,and the result was compared with that of routine TRFIA.ROC curve was constructed to determine the cutoff value and sensitivity for pancreatic cancer diagnosis.Results The method of nanomagnetic beads sorting TRFIA detected the level of galectin 3 between O.78 and 100 ng/ml in a linear manner,the intra-CV was ≤6.38％,and inter-CV was ≤7.22％,and average recovery rate was 105.3％.The serum level of galectin-3 in control group by nanomagnetic beads sorting TRFIA was 0.38 (0.02 ～ 3.06) ng/ml,which was significantly higher than that detected by routine TRFIA [0.18 (0.00 ～ 2.64) ng/ml,P =0.000).The serum levels of galectin-3 by nanomagnetic beads sorting TRFIA in pancreatic cancer,acute pancreatitis,pancreatic cysts and healthy volunteers were 4.85(0.00 ～42.67),0.69(0.00～ 13.62),0.70(0.00 ～ 14.54),0.38(0.02 ～ 3.06) ng/ml,and the level of galectin-3 in pancreatic cancer was significantly higher than that in acute pancreatitis,pancreatic cysts and healthy volunteers group (P ＜0.01),while the difference among the other three group was not significantly different.The AUC of galectin-3 for pancreatic cancer was 0.851 ± 0.040,95％ CI:0.772 ～ 0.929.While using 1.07 ng/ml as the cut-off value,the positive rates for the diagnosis of pancreatic cancer,acute pancreatitis,pancreatic cysts and healthy volunteers were 84.1％ (74/88),34.0％ (17/50),20.0％ (2/10),10.0％ (2/20),and the sensitivity for diagnosis of pancreatic cancer was significantly higher than those in other 3 groups (P ＜ 0.01).Conclusions Nanomagnetic beads sorting TRFIA tandem analysis method can enrich serum galectin-3,and increase the sensitivity of detection for pancreatic cancer and enhance the diagnostic value of galectin-3 for pancreatic cancer.

OBJECTIVETo study the effect of Mudan Granule (MD) on the glucose metabolism and beta cell function in monosodium glutamate (MSG) induced obese mice with insulin resistance (IR).

METHODSMSG obese mice were induced by subcutaneous injecting MSG (4 g/kg for 7 successive days in neonatal ICR mice). Forty MSG mice with IR features were recruited and divided into four groups according to body weight, fasting blood glucose, triglyceride (TG), total cholesterol (TC), and the percentage of blood glucose decreased within 40 min in the IR test, i.e., the model group (Con), the low dose MD group, the high dose MD group, and the Metformin group (Met). Besides, another 10 ICR mice were recruited as the normal control group (Nor). The water solvent of 2.5 g/kg MD or 5 g/kg MD was respectively administered to mice in the low dose MD group and the high dose MD group. Metformin hydrochloride was given to mice in the Met group at 0.2 g/kg body weight. Equal dose solvent distilled water was administered to mice in the Nor group and the Con group by gastrogavage, once per day. All medication was lasted for 15 weeks. Insulin tolerance test (ITT) and oral glucose tolerance test (OGTT) were performed after 6 weeks of treatment. Beta cell function was assessed by hyperglycemic clamp technique. The morphological changes in the pancreas were evaluated by hematoxylin-eosin (HE) staining. Changes of iNOS, NF-kappaB p65, and p-NF-kappaB p65 in the pancreas were tested.

RESULTSCompared with the Nor group, the blood glucose level, AUC, and fasting blood insulin, ONOO-contents, iNOS activities, and the expression of iNOS, NF-kappaB p65 subunit, pNF-kappaB p65 subunit obviously increased; decreased percentage of blood glucose within 40 min in ITT, glucose infusion rate (GIR), Clamp 1 min insulin, and Max-Insulin obviously decreased in the Con group (P < 0.05, P < 0.01). Compared with the Con group, the aforesaid indices could be improved in the Met group (P < 0.05, P < 0.01). In the low dose MD group, AUC, iNOS activities, and the expression of iNOS and p-NF-kappaB p65 subunit obviously decreased; percentage of blood glucose within 40 min in ITT and GIR obviously increased (P < 0.05, P < 0.01). In the high dose MD group, AUC, ONOO-contents, iNOS activities, and the expression of iNOS, NF-kappaB p65 subunit, and p-NF-KB p65 subunit obviously decreased; percentage of blood glucose within 40 min in ITT, Max-Insulin, and GIR obviously increased (P < 0.05, P < 0.01).

CONCLUSIONMD could significantly improve IR and functional disorder of 3 cells in MSG obese mice, which might be associated with lowering inflammatory reaction in the pancreas.

Animals ; Disease Models, Animal ; Drugs, Chinese Herbal ; pharmacology ; Female ; Insulin Resistance ; Insulin-Secreting Cells ; drug effects ; metabolism ; Male ; Metformin ; pharmacology ; Mice ; Mice, Inbred ICR ; Mice, Obese ; Obesity ; chemically induced ; metabolism ; Pancreas ; cytology ; drug effects ; Sodium Glutamate

This study is to evaluate the effects of the metformin (Met) on β cell function of diabetic KKAy mice. Female diabetic KKAy mice selected by insulin tolerance test (ITT) were divided randomly into two groups. Con group was orally administered by gavage with water, Met group with metformin hydrochloride at a dose of 0.2 g x kg(-1) for about 12 weeks. ITT and glucose tolerance tests (OGTT) were determined. Beta cell function was assessed by hyperglycemic clamp. Pancreatic biochemical indicators were tested. The changes of gene and protein expression in the pancreas and islets were also analyzed by Real-Time-PCR and immunostaining. Met significantly improved glucose intolerance and insulin resistance in KKAy mice. Fasting plasma glucose and insulin levels were also decreased. In addition, Met markedly increased glucose infusion rate (GIR) and elevated the Ist phase and maximum insulin secretion during clamp. It showed that Met decreased TG content and iNOS activities and increased Ca(2+) -Mg(2+)-ATPase activity in pancreas. Islets periphery was improved, and down-regulation of glucagon and up-regulated insulin protein expressions were found after Met treatment. Pancreatic mRNA expressions of inflammation factors including TLR4, NF-κB, JNK, IL-6 and TNF-α were down-regulated, p-NF-κB p65 protein levels also down-regulated by Met. And mRNA expressions of ion homeostasis involved in insulin secretion including SERCA2 and Kir6.2 were up-regulated by Met. Met increased SIRT5 expression level in pancreas of KKAy mice under the hyperglycemic clamp. These results indicated that chronic administration of Met regulated pancreatic inflammation generation, ion and hormone homeostasis and improved β cell function of diabetic KKAy mice.
Animals ; Blood Glucose ; Diabetes Mellitus, Experimental ; drug therapy ; Down-Regulation ; Female ; Glucose Tolerance Test ; Homeostasis ; Inflammation ; drug therapy ; Insulin ; secretion ; Insulin Resistance ; Insulin-Secreting Cells ; drug effects ; Interleukin-6 ; metabolism ; Metformin ; pharmacology ; Mice ; NF-kappa B ; metabolism ; Pancreas ; drug effects ; Tumor Necrosis Factor-alpha ; metabolism

Based on the infrared spectra of Lophatheri Herba and Commelinae Herba, one-dimensional infrared spectra, second derivative spectra and two-dimensional correlated spectra were used to find out the differences between Lophatheri Herba and its imitations, respectively. The common peak ratio and variant peak ratio dual-indexes sequential were calculated and established according to infrared spectra of eleven batches of herbs. Infrared spectral data of Lophatheri Herba cluster analysis was applied to explore the similarity between each sample. The grouping results trend of sequential analysis of dual-indexes and cluster analysis was accordant. The results showed that the differences could be found by multi-level identification, and the source and the quality of the herbs could be effectively distinguished by the two analysis methods. Infrared spectroscopy, used in the present work exhibited some advantages on quick procedures, less sample required, and reliable results, which could provide a new method for the identification of traditional Chinese medicine with the imitations and adulterants, and the control of quality and origin.
Drugs, Chinese Herbal ; analysis ; chemistry ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Reproducibility of Results ; Spectrophotometry, Infrared ; methods ; Spectroscopy, Fourier Transform Infrared ; methods

Objective To evaluate the reliability of mannitol for fluid responsiveness test in the patients undergoing intracranial surgery.Methods Sixty-two ASA physical status Ⅰ or Ⅱ patients,aged 18-64 yr,with body mass index of 18-25 kg/m2,scheduled for elective intracranial surgery,were enrolled in the study.The patients were mechanically ventilated after induction of anesthesia.The radial artery and central vein were cannulated,and FloTracTM/VigileoTM system was connected for stroke volume variation monitoring.Before infusion of mannitol,effective circulating blood volume was confirmed according to stroke volume variation.20％ mannitol 250 ml was infused over 20 min starting from onset of craniotomy.The fluid responsiveness test was recorded at the end of mannitol infusion.Results The sensitivity of fluid responsiveness test was 43％,and the specificity of fluid responsiveness test was 44％.Conclusion Mannitol can not be used for fluid responsiveness test in the patients undergoing intracranial surgery.

Objective To explore the expression of pituitary tumor transforming gene (PTTG) and c-myc gene in patients with non-Hodgkin lymphoma (NHL),its relationship with NHL and its clinical significance.Methods PTTG mRNA and c-myc mRNA levels in bone marrow mononuclear cell (BMMNC) isolated from 38 NHL patients and 10 chronic lymphadenitis patients were quantified by reverse transcriptionpolymerase chain reaction (RT-PCR).Results mRNA expression of PTTG and c-myc gene in BMMNC was significantly higher in NHL patients than those in normal controls (PTTG:0.567 7±0.270 7 vs 0.071 2± 0.020 1,t =4.706,P ＜ 0.05; c-myc:0.352 6±0.185 4 vs 0.107 3±0.043 5,t =3.303,P =0.002).The expression of PTTG and c-myc gene in peripheral T cell lymphoma and diffuse large B cell lymphoma showed no significant difference (PTTG:0.556 8±0.211 3 vs 0.602 8±0.244 6,t =0.640,P =0.527; c-myc:0.350 1± 0.177 6 vs 0.361 0±0.190 2,t =0.302,P =0.765).Both expression of PTTG and c-myc were positively related to NHL clinical stage and IPI.Expression of PTTG mRNA was positively related to the expression of c-myc mRNA.Conclusion There was overexpression of PTTG and c-myc in NHL,which indicates that PTTG might be involved in tumorigenesis of NHL through direct or indirect activation of c-myc oncogene.