Objective To study the effect of ketamine on inward rectifier potassium currents(I_k1)in isolated rat ventricular myocytes using whole-cell patch clamp technique.Methods Adult Wistar rats of both sexes were anesthetized with pentobarbital.The hearts were removed and ventricular myocytes were prepared by the technique described by Liu et al.Whole-cell patch clamp technique was used to study I_(k1) in isolated rat ventricular myocytes The changes in I_(KI) produced by 100 ?mol?L~(-1) with different holding potentials or by different concentrations of ketamine with holding potential of-120 mV were analyzed.Results Ketamine 100 ?mol?L~(-1) inhibited the Ira without any significant effects on reverse potential (-50--60 mV)and the shape of the Ⅰ-Ⅴ curve.Ketamine inhibited I_(k1) evoked by a holding potential of-120 mV in a dose-dependent manner with a mean IC_(50) value of (162.3?8.4)?mol?L~(-1).Conclusion Ketamine significantly inhibits I_(k1) in ventricular myocytes. This may explain the prolonged duration of action potential of ventricular myocyte produced by ketamine.

In the present study, the efficacy of Naoxintong capsule (NXT), a compound Chinese herbal medicine, combined with dual antiplatelet therapy (DA) in a rat model of coronary microembolization (CME) was evaluated.

AIMTo investigate the inhibitory effects of artesunate on angiogenesis.

METHODSThe in vitro anti-angiogenic effect of artesunate was tested on models of angiogenesis: proliferation, migration and tube formation of human umbilical vein endothelial (HUVE) cells; The anti-angiogenic effect in vivo was evaluated in nude mice by means of human ovarian cancer HO-8910 implantation and immunohistochemical stainings for microvessel (CD31), vascular endothelial growth factor (VEGF) and VEGF receptor KDR/flk-1.

RESULTSArtesunate significantly inhibited angiogenesis in a concentration-dependent form in range of 0.5-50 mumol.L-1. The IC50 of artesunate for HUVE cells was (21 +/- 3) mumol.L-1. Growth of xenograft tumor was decreased and microvessel density was reduced following drug-treatment with no apparent toxicity to the animals. Artesunate also remarkably lowered VEGF expression on tumor cells and KDR/flk-1 expression on endothelial cells as well as tumor cells.

CONCLUSIONArtesunate was shown to inhibit angiogenesis in vitro and in vivo. These findings together with the known low toxicity of artesunate are clues that artesunate may be a promising angiogenesis inhibitor.

Angiogenesis Inhibitors ; pharmacology ; Animals ; Artemisia ; chemistry ; Artemisinins ; isolation & purification ; pharmacology ; Endothelial Cells ; cytology ; Female ; Humans ; Male ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Neoplasm Transplantation ; Ovarian Neoplasms ; metabolism ; pathology ; Receptors, Vascular Endothelial Growth Factor ; biosynthesis ; Sesquiterpenes ; isolation & purification ; pharmacology ; Tumor Cells, Cultured ; Umbilical Veins ; cytology ; Vascular Endothelial Growth Factor Receptor-2 ; biosynthesis

Objective To investigate the pathogenesis of peripheral blood mononuclear cells(PBMC) nuclear factor kappa-?B(NF-?B) in children with primary nephritic syndrome(PNS) and the effect of astragalus on the activity of NF-?B.Methods Twenty-five children with PNS and 20 normal children were studied.Isolated PBMC were separated from 5 mL venous blood in asepsis condition.NF-?B stimulator,NF-?B inhabitor and astragalus were added into the different tubes of PBMC,respectively.The nuclear protein was extracted from the pellets and the optical density(A) values of nuclear protein was measured by enzyme-linked immunosorbent assay(ELISA).Results The activity of PBMC NF-?B in PNS group was higher than that in normal group(P0.05).Astragalus could decrease the activity of PBMC NF-?B which had been stimulated by interleukin-1?(IL-1?)(P

Objective To explore the effect and mechanism of metastasis associated gene 1 (MTA1) on epithelial-mesenchymal transition(EMT) of esophageal squamous cell carcinoma(ESCC).Methods Lentivirus infection method was used to establish the MTA1 knocking out cell line (LV3-shMTA1-KYSE410) and the MTA1 overexpressing cell line (LVS-MTA1-KYSE450).Western Blot was used to measure the expression of MTA1 and the proteins associated with EMT process.Furthermore,the expression and localization of E-cadherin and Vimentin were observed by immunofluorescence assay under confocal microscope.Finally,the wound healing method was performed to confirm the changes of migration ability of the established cell lines.Results When KYSE-450 cells were overexpressed MTA1,the expression level of E-cadherin was down-regulated while Vimentin was up-regulated,and the migration ability was enhanced (0.91 ± 0.00 vs.0.23 ± 0.04,P ＜0.05).When MTA1 was knocked out in KYSE-410 cells,the results were the opposite (0.19±0.01 vs 0.53±0.01,P ＜0.05).Conclusion Overexpression of MTA1 may promote the process of epithelial-mesenchymal transition and enhance the migration ability of ESCC.

Polyethylene glycol (PEG) lipid derivatives could increase the stability of liposomes in vivo and in vitro and prolong the circulation time of liposomes in vivo. However, the chemical bond between PEG and lipid was so stable that liposomes modified with traditional PEG-lipid derivatives could not release their contents at targeted tissue immediately and the pharmacodynamic effect was reduced. The concept of cleavable PEG-lipid was raised in recent years and these PEG-lipid derivatives could break under physiological or pathological condition. The cleavable PEG-lipid derivatives could prolong the circulation time of liposomes, and after arriving at targeted location, PEG fragment had cleaved from the surface of liposomes, so liposomes could bind with pathological cells and release contents into cells. Removal of the protective polymer layer is necessary once the liposome close to the tumour to allow to fuse and release drug. Attempts have been made to increase the circulation time and reconstitute the cellular affinity of liposomes by incorporating PEG-lipid derivatives. This review focused on the kinds of cleavable PEG-lipid derivatives, types of cleavage, the application feature to liposomes and the advantages and localizations.
Cholesterol ; analogs & derivatives ; chemistry ; Drug Delivery Systems ; methods ; Humans ; Liposomes ; chemistry ; Phosphatidylethanolamines ; chemistry ; Polyethylene Glycols ; chemistry

OBJECTIVETo observe the effect of Shenshuaining Granule (SG) combined telmisartan on serum creatinine (SCr) levels and urinary albumin contents in diabetic nephropathy (DN) patients, and to explore its efficacy.

METHODSTotally 204 DN patients were recruited, and further assigned to 3 groups, i.e., the early DN group, the clinical stage of DN with normal renal function group, the clinical stage of DN with insufficient renal function group. Patients in the same group were randomly allocated to the telmisartan treatment group, the SG treatment group, and the combination of SG and telmisartan treatment group, 68 in each group. Patients in the telmisartan treatment group took telmisartan tablet, 80 mg per day, once daily. Those in the SG treatment group took SG, 5 g each time, 3 times per day. Those in the combination of SG and telmisartan treatment group took telmisartan tablet (80 mg per day, once daily) and SG (5 g each time, 3 times per day). The therapeutic course for all was 3 successive months. SCr levels, serum urea nitrogen (BUN),24 h urine microalbumin (24 h U-MA) were detected before and after treatment. Results In three different treatment groups, 24 h U-MA decreased after treatment in the telmisartan treatment group; SCr and BUN decreased after treatment in the SG treatment group; and 24 h U-MA, SCr and BUN decreased after treatment in the combination of SG and telmisartan treatment group (P<0.05). In the clinical stage of DN with insufficient renal function group, SCr obviously increased after treatment in the telmisartan treatment group (P <0. 05). In the 3 DN stages, SCr and 24 h U-MA obviously decreased in the combination of SG and telmisartan treatment group, when compared with the telmisartan treatment group and the SG treatment group (P<0.05). Compared with the telmisartan treatment group, SCr and BUN obviously decreased in the SG treatment group, but 24 h U-MA quantitation obviously increased (P<0.05). BUN obviously decreased in the combination of SG and telmisartan treatment group (P<0. 05).

CONCLUSIONThe combination of SG and telmisartan could decrease urinary albumin, and stabilize SCr levels.

Adult ; Albumins ; metabolism ; Antihypertensive Agents ; therapeutic use ; Benzimidazoles ; therapeutic use ; Benzoates ; therapeutic use ; Diabetic Nephropathies ; drug therapy ; Drugs, Chinese Herbal ; administration & dosage ; therapeutic use ; Female ; Humans ; Male ; Middle Aged ; Phytotherapy ; Tablets

6-11 years old were 9.67%, 6.81%, 3.49% and 0.80%, respectively.Furthermore, the infection rates between each two age stages were significantly different(Pa0.05).4.Infection rates in 2005,2006 and 2007 were 4.0%, 8.92%, 8.85%,respectively.Infection rates between 2005 and 2006,2007 were significantly different(Pa

Objective: To observe the effect of acupoint massage plus Vitalstim electrical stimulation on deglutition function and surface electromyography (SEMG) of deglutition muscle groups. Methods: A total of 60 patients with deglutition disorder after stroke were selected and divided into an electrical stimulation group, a massage group and an integrated group according to the random number table method, with 20 cases in each group. Patients in these three groups were given the same routine rehabilitation training for deglutition. In addition, patients in the electrical stimulation group were given extra Vitalstim electrical stimulation, patients in the massage group were given extra acupoint massage on the head, face and neck, and patients in the integrated group were given extra acupoint massage plus Vitalstim electrical stimulation. Fujishima Ichiro food intake level scale (FILS) was scored before and after treatment. The swallowing duration and maximal amplitude of masseter muscle in SEMG were evaluated before and after treatment. Results: After treatment, the FILS score and the maximal amplitude of recruitment potential generated by muscular contraction of masseter muscle group in the three groups were higher than those before treatment (all P<0.05), and the swallowing duration of masseter muscle group was shortened compared with that in the same group before treatment (all P<0.05). After treatment, the FILS score in the integrated group was higher than that in the electrical stimulation group and the massage group (both P<0.05). The swallowing duration of masseter muscle group measured by SEMG was lower than that in the electrical stimulation group and the massage group (both P<0.05), while the maximal amplitude was higher than that of the electrical stimulation group and the massage group (P<0.05). After treatment, there were no significant differences in the FILS score, swallowing duration and maximal amplitude of masseter muscle group between the electrical stimulation group and the massage group (all P>0.05). Conclusion: Both acupoint massage and electrical stimulation can improve the deglutition function in patients with deglutition disorder after stroke, and improve the coordination and flexibility of masseter muscle. The integration of the two is more effective.

OBJECTIVETo investigate the correlation between pro-B-type natriuretic peptide (NT-proBNP) and heart rate variability (HRV) in patients with diabetes.

METHODSHRV and NT-proBNP levels were assessed in 58 patients with diabetes.The time domain and frequency domain indices and the level of NT-proBNP were compared between patients with normal and abnormal HRV, and the correlation of HRV index and NT-proBNP was analyzed.

RESULTSThe NT-proBNP level was significantly higher in patients with abnormal HRV than in those with normal HRV (320.2±88.3 vs 80.4±25.2 pg/ml, P<0.01).The level of NT-proBNP was negatively correlated with SDNN (r=-0.55, P<0.05), triangle index (r=-0.52, P<0.05), LF (r=-0.62, P<0.01), and VLF (r=-0.56, P<0.05).

CONCLUSIONNT-proBNP level is correlated with HRV, and an increased NT-proBNP indicates cardiac autonomic neuropathy in diabetic patients.

Diabetes Mellitus ; metabolism ; physiopathology ; Heart Rate ; Humans ; Natriuretic Peptide, Brain ; metabolism ; Peptide Fragments ; metabolism