Objective To investigate the effects of advanced glycosylation end-products (AGEs) on the expression of acyl coenzyme A: cholesterol acyltransferase-1 (ACAT-1) in cultured THP-1 macrophages. Methods THP-1 cells were differentiated into macrophages after cultured in RPMI1640 media containing 0.1 ?mol/L PMA for 72 h. THP-1 macrophages were then exposed to AGE-modified bovine serum albumin (AGE-BSA, at concentration of 50, 100, 200 mg/L) for 24 h or to 200 mg/L AGE-BSA for 0, 12, 24, 36 h. Expression of ACAT-1 mRNA and protein in THP-1 macrophages was measured by RT-PCR and Western blot, respectively. Results After induced by 0.1 ?mol/L PMA, THP-1 cells stopped proliferation and differentiated into macrophages. Treatment of THP-1 macrophages with AGE-BSA resulted in an increase in the mRNA and protein levels for ACAT-1 in a dose-and time-dependent manner. Conclusion AGEs upregulate the expression levels of mRNA and protein for ACAT-1 in cultured THP-1 macrophages, which might be partly involved in the atherogenesis in diabetic patients.

OBJECTIVETo explore the effects of arecoline on hepatic insulin resistance in type 2 diabetes rats and to elucidate its possible mechanism.

METHODSForty five Wistar rats were fed with high fructose diet for 12 weeks to induce type 2 diabetic rat model. rats were randomly divided into 5 groups (n = 8): control group, model group and model group were treated with different dose (0, 0.5, 1, 5 mg/kg) of arecoline. After 4 weeks, the fasting blood glucose, blood lipid and insulin level measured , mRNA expression of liver constitutive androstane receptor (CAR), pregnane X receptor (PXR), glucose-6-phosphatase (G6Pase), phosphoenolpyruvate carboxykinase (PEPCK), interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-alpha) were detected by reverse transcription polymerase chain reaction (RT-PCR), the protein expression of p-AKT and glucose transporter4 (GLUT4) were detected by Western blot.

RESULTS1.5 mg/kg arecoline could significantly decrease the level of fasting blood glucose, blood lipid, blood insulin level and liver G6Pase, PEPCK, IL-6, TNF-alpha mRNA level in type 2 diabetes rats. 1.5 mg/kg arecoline also could significantly increase CAR, PXR mRNA level and p-AKT and GLUT4 protein expression.

CONCLUSIONArecoline improved hepatic insulin resistance in type 2 diabetes rats by increasing the mRNA levels of CAR and PXR leading to the creased glucose metabolism and inflammation related genes expression.

Animals ; Arecoline ; pharmacology ; Diabetes Mellitus, Experimental ; metabolism ; Diabetes Mellitus, Type 2 ; metabolism ; Glucose Transporter Type 4 ; metabolism ; Glucose-6-Phosphatase ; metabolism ; Insulin Resistance ; Interleukin-6 ; metabolism ; Intracellular Signaling Peptides and Proteins ; metabolism ; Liver ; drug effects ; metabolism ; Male ; Phosphoenolpyruvate Carboxykinase (GTP) ; metabolism ; Proto-Oncogene Proteins c-akt ; metabolism ; Rats ; Rats, Wistar ; Receptors, Cytoplasmic and Nuclear ; metabolism ; Receptors, Steroid ; metabolism ; Tumor Necrosis Factor-alpha ; metabolism

This study is to observe the effect of gross saponins of Tribulus terrestris (GSTT) on protein kinase Cepsilon (PKCepsilon) and apoptosis-associated protein in the apoptosis of cultured cardiocyte apoptosis induced by hydrogen peroxide (H2O2), and to explore the mechanisms of GSTT against myocardial apoptosis. Primary cardiocytes were isolated and cultured. Myocardial apoptosis was induced by H2O2 and analyzed with flow cytometry. Protein content of phospho-PKCepsilon, Bcl-2, and Bax were detected with Western blotting analysis. Cleaved caspase-3 protein content was determined with immunocytochemical technique. After the pretreatment of 100 mg x L(-1) GSTT, compared with H2O2 group, GSTT could not only decrease the apoptotic percentage in cardiocytes damaged by H2O2 (P < 0.01), but also reduce protein contents of Bax and cleaved caspase-3 (P < 0.01), and increase protein content of phospho-PKCepsilon and Bcl-2 significantly (P < 0.01). PKC inhibitor chelerythrine (Che) could prevent partly the effect of GSTT against myocardial apoptosis (P < 0.05 and P < 0.01). Mechanisms of GSTT against myocardial apoptosis might be associated with inhibition of mitochondrial apoptosis pathway after PKCepsilon activation.
Animals ; Apoptosis ; drug effects ; Benzophenanthridines ; pharmacology ; Caspase 3 ; metabolism ; Cells, Cultured ; Dose-Response Relationship, Drug ; Enzyme Activation ; Female ; Hydrogen Peroxide ; toxicity ; Male ; Myocytes, Cardiac ; cytology ; drug effects ; metabolism ; Oxidative Stress ; Phosphorylation ; Plants, Medicinal ; chemistry ; Protein Kinase C ; antagonists & inhibitors ; Protein Kinase C-epsilon ; metabolism ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; Rats ; Rats, Wistar ; Saponins ; administration & dosage ; isolation & purification ; pharmacology ; Tribulus ; chemistry ; bcl-2-Associated X Protein ; metabolism

Objective To study the effects of rehabilitation(RT)on cardiac function in cerebral infarct (CIF)patients with cardiac insufficiency(CIS).Methods Fifty-nine CIF patients with CIS were randomly divid- ed into a treatment group(T group,n=29)and a control group(n=30),and all patients were treated with routine pharmacotherapy for 2 months.In addition,RT was administrated in the T group at the same time.The grading of the New York Heart Association(NYHA)and the changes in cardiac function associated index were observed in both groups before and after treatment.Results Compared with the control group,NYHA grades,left ventricle ejection fraction(LVEF),the levels of brain natriuretic peptide(BNP)in the blood plasma,and the 6min walking range of the T group patients were all significantly improved after treatment(P＜0.05).Conclusion RT can improve car- diac function in CIF patients with CIS.

OBJECTIVETo study the thin layer chromatographic (TLC) fingerprint of flavonoid constituents from Polygonatum odoratum, to set up the identification protocol of the herbal and provide scientific information for its quality control.

METHODThe ethanol extracts were separated on silica gel G precoated plate with a mixture of toluene-ethylacetate-formic acid (5:4:1) as the mobile phase. The spots were visualized with ammonia vapor, then were examined under ultraviolet light (365 nm). The plate was scanned at wavelengths of lambdaR = 500 nm, lambdaS = 280 nm.

RESULTA fingerprint of flavonoids of P. odoratum, with 10 specific fluorescent spots while examined under ultraviolet light, was set up.

CONCLUSIONThe method can be used for quality control of P. odoratum.

Chromatography, Thin Layer ; methods ; Flavonoids ; analysis ; chemistry ; Plants, Medicinal ; chemistry ; Polygonatum ; chemistry ; Quality Control ; Rhizome ; chemistry

No abstract available.
Ectropion* ; Eyelids* ; Skin*

Cinobufacino injection is a significant anti-tumor medicine for the treatment of various tumors in clinic, which was made from water extraction of the skin of Bufo bufo gargarizans. In present paper, HPLC-DAD-FT-ICR-MS method was used to identify the major bufadienolides in cinobufacino for the first time. Solid-phase extraction with dichloromethane and silica was used to enrich the total bufadienolides in cinobufacino. Based on the UV and high resolution MS/MS data, 33 bufadienolides were analyzed and characterized. Among them, eight compounds were identified by comparing with standard references unambiguously. This study elucidated the major bufadienolides in cinobufacino, which provided material foundation of cinobufacino and will be benefit for the further pharmacological research.
Amphibian Venoms ; chemistry ; Animals ; Bufanolides ; analysis ; chemistry ; Bufo bufo ; Chromatography, High Pressure Liquid ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

To obtain chemical constituent information of rat plasma after oral administration of Huang-Lian-Jie-Du Decoction (HLJDD), a LC-FT-ICR-MS method has been established, and both positive and negative ions scan modes were include in the analysis. By comparing their retention time, high resolution mass data of HLJDD extracts, blank plasma and dosed plasma, 38 constituents, including 22 prototype compounds and 16 metabolites, were detected in rat plasma after oral administration of HLJDD. In the 22 prototype compounds, 16 constituents were determined unambiguously by comparing with references. In the analysis of metabolites, phase II reactions like glucuronidation and sulfation were the major biotransformation pathways of HLJDD. M11 was observed as the only phase I metabolite in present experiment. The results will be beneficial for the further pharmacokinetics and pharmacological evaluations of HLJDD.
Administration, Oral ; Alkaloids ; blood ; Animals ; Biotransformation ; Chromatography, High Pressure Liquid ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; metabolism ; Flavonoids ; blood ; Iridoids ; blood ; Male ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

Cutaneous Fistula ; Digestive System Abnormalities ; therapy ; Endoscopy, Gastrointestinal ; methods ; Female ; Humans ; Infant ; Treatment Outcome

Objective To investigate the effects of repeated neonatal administration of dizocipline maleate (MK-801), the N-methyl-D-aspartate (NMDA) receptor antagonist, on the expression of NMDA receptor subunits NMDAR 1 (NR1), NMDAR2A (NR2A), NMDAR2B (NR2B) and the protein levels of nerve growth factor (NGF) in neonatal rats. Methods Neonatal Sprague-Dawley (SD) rats were randomly divided into research group and control group, with 15 ani-mals in each group. Rats were administrated subcutaneously with MK-801 or normal saline from postnatal day (PND) 5 to PND14 (0.25 mg/kg, twice a day). The expression levels of NR1, NR2A, NR2B and NGF were examined on PND15, PND42 and PND70 in the prefrontal cortex and hippocampus. Results At PND15 (neonatal period), there were no signifi-cant differences in the expression levels of NR1, NR2A, NR2B and NGF in the prefrontal cortex and hippocampus be- tween the two groups (P>0.05). At PND42 (adolescence), NGF protein levels in the prefrontal cortex was significantly low-er in research group than in control group [(56.19±37.87) vs. (152.54±53.92), P<0.01]. At PND70 (adulthood), the expres-sion of NR1, NR2A in the hippocampus was significantly higher in research group than in control group [NR1:(149.55%± 27.00%) vs. (100.00%±32.08%);NR2A:(171.54%±19.85%) vs. (100.00%±51.04%). P<0.05]. Conclusion Neonatal re-peated treatment of MK-801 increases the expression of NMDA receptor subunits NR1, NR2A in the hippocampus in adulthood while decreases the expression of NGF in the prefrontal cortex in adolescence, suggesting that neonatal block-ade of the NMDA receptor may influence the growth and development of the nervous system.