Objective To investigate the variation of the oxidative stress status in type 2 diabetes mellitus(T2DM)patients with acute coronary syndrome (ACS)and significance.Methods Eighty -nine patients hospitalized in our department from September 2012 to April 2014 were divided into three groups: T2DM control (group DM), T2DM with coronary artery disease(group DM-CAD) and T2DM with acute coronary syndrome (group DM-ACS).Blood glucose,HbA1C,Lipids,serum Malondialdehyde (MDA) level, su-peroxide dismutase(SOD) activity, glutathione peroxidase (GSH-Px) activity and total anti-oxidation capacity(T-AOC) were deter-mined.Results Blood glucose、HbA1C and Lipids were similar in three groups ( P >0.05).Compared to group DM and group DM-CAD, serum MDA levels in group DM-ACS were significantly higher( P <0.05), while SOD、GSH-Px activities and T-AOC were sig-nificantly lower than those in group DM and group DM -CAD( P <0.05).Conclusions The oxidative stress level being significantly increased in T2DM patients with ACS.

Objective To establish a multi-drug resistant model of temporal lobe epilepsy,and to observe the changes of γ-aminobutyric acid (GABA) receptor expression in the hippocampal tissues so as to explore its effects in pharmacoresistant epileptogenesis.Methods One hundred rats were selected to prepare the amygdaloid kindled model of epilepsy by chronic stimulation of amygaloid basal lateral nucleus.After the kindled model of epilepsy was prepared successfully(n =52),pharmacoresistant epileptic rats were selected according to their response to the phenobabital and phenytoin.The selected pharmacoresistant epileptic rats (n =8)were sacrificed and the hippocampus was removed to determine the GABA receptor expression,and the same number of pharmacosensitive epileptic rats was used as control.Results The pharmacoresistant epileptic rats displayed degenerative and necrotic hippocampal neurons.The arrangement of hippocampal neurons was disordered,and the structural characteristics of the arrangement of the hippocampal neurons disappeared.The gray values of GABAA-positive neurons in the hippocampal tissues (141.15 ± 14.72) increased significantly compared with the pharmacosensitive epileptic rats (92.56 ± 5.17; t =3.380,P =0.006).Western blot method demonstrated that the band of GABAA became narrowed and thin.The relative quantity of GABAA in the hippocampal tissues (0.38 ± 0.08) decreased significantly as compared with the pharmacosensitive epileptic rats (0.88 ± 0.18).A significant difference was observed (t =5.420,P =0.002).Conclusions GABA receptor expression might be decreased in the hippocampal tissues of pharmacoresistant epileptic rats.It might play a certain role in the formation of pharnmacoresistant epilepsy.

Objective To analyze the image and histological results of the combined use of allograft/extracorporeally frozen tumor-bearing bone and vascularized fibular flap for the reconstruction of bony defects following tumor resection,guiding clinical practice.Methods From March 2007 to June 2013,we enrolled 63 patients who had combinative biological reconstruction after bone tumor resection (11 in humerus,22 in femur,21 in tibia,4 in calcaneus).There were 36 male and 27 female in this series.The average age at time of operation was 20 years,ranging from 9 to 48 years.The follow-up ranged from 16 to 102 months with average of 48 months.We investigated the X-ray and CT images for all patients and histological findings of two patients.Patients were assessed functionally with the Musculoskeletal Tumor Society 93 score.Results Three patients with local soft tissue recurrence and one patient with infection underwent amputation.The survival of construct was 93.6％.Bone union achieved in all cases with the average MSTS score of 92.8％.Bone union ranged from 11 to 28 months in allograft group and 9 to 14 months in devitalized tumor bearing bone group.Significant difference of bone union time was found between two groups (Z=-3.638,P=0.000).Viability of the fibular grafts was verified in 58 of 63 patients (92％).Three types of images were observed in complex.Osteopenia and spongy change in fibula were found in 51 patients (81％) with stable fixation of the complex.Five complexes with failed blood supply of fibula and stable fixation revealed no density change of fibula,small amount of callous formation and relative delayed union.In seven complexes (11％) with unstable complex due to patients' incompliance,fibula reacted with dense hypertrophy and microfracture.Fusion of grafts with amount of callus was obviously observed.Union at allograft-host bone junctions occurred by residual host bone-derived external callus and fibular-derived internal callus that bridged the junction and filled the gap between abutting cortices.Callus from fibular graft was mature than that from periosteum of residual host bone.Internal repair was observed at the internal surface of the allografts.Fibula showed significant spongy changes.Conclusion Recycled tumor-bearing bone in combined with fibular flap is a reliable reconstruction as an alternative to traditional Capanna technique.The survival of the fibula is a cornerstone in success of complex reconstruction.Sponginess of fibula and internal repair of allograft compromise the intensity of complex,necessitating the strong instrumentation during reconstruction.

Objective: To evaluate pharmacokinetic and pharmacodynamic of repaglinide tablets in Chinese subjects.Methods: Twenty healthy male volunteers were enrolled in the study. A single dose (4 mg) of repaglinide tablets was givenorally. Plasma concentrations of repaglinide were determined by HPLC method. Blood glucose and serum insulin leve1s weremeasured by biochemistry and radioimmunoassay methods respectively. Results: Plasma concentration-time curve conformedto one-compartment open model. The pharmacokinetic parameters were as follows: tmax (0. 75?0.43 ) h,cmax (54.44?24.97)ng/ml, t1/2 (0. 80?0. 31) h, MRT (1. 55?0. 41) h, C1/F (61. 43?20. 10) L/h and AUC (73. 34?29.95) h? ng/ml. Thelevel of serum insulin was raised and the level of blood glucose decreased after administration of repaglinide. The highest levelof serum insulin was (l26. 24?95.93) mU/L at 0.75h and blood glucose level reached its lowerest vaIue (2. 34I0.44) mmol/L 1 h after oral administration. Conclusion: Repaglinide is characterised by fast-acting and short effects on in-sulin secretion. It decreases serum glucose level by stimulating insulin secretion from the pancreatic ?-cells. It is a novel oralprandial glucose regulator for the treatment of type 2 diabetes mellitus.

Objective: To investigate the effect of combining acupuncture and auricular point sticking on heart rate variability (HRV) in patients with post-stroke depression (PSD). Methods: A total of 80 cases with PSD were randomized into a treatment group and a control group. The control group was intervened by oral administration of paroxetine hydrochloride, whereas the treatment group received acupuncture plus auricular point sticking base on the same oral administration. The Hamilton depression rating scale (HAMD) and HRV were measured before and after treatment in both groups. Results: The individual and global scores of HAMD significantly dropped after 8 weeks of treatment in both groups (all P<0.05). In the treatment group, anxiety/somatization factor, sleep disturbance, hopelessness factor, cognition factor and global score were significantly different from those in the control group (all P<0.05). The 24 h standard deviation of all normal-to-normal R-R interval (SDNN), standard deviation of 5-minute average of normal R-R intervals (SDANN), root mean square of successive differences (RMSSD), percent of differences between adjacent normal R-R intervals >50 ms (PNN50) and high frequency (HF) were increased while low frequency (LF) and LF/HF decreased significantly after 8 weeks of treatment in both groups (P<0.05). All items in the treatment group were significantly different from those in the control group (all P<0.05). Conclusion: Combining acupuncture and auricular point sticking can enhance the conventional medical treatment for HRV in patients with PSD.

To study the effect of Wansheng Huafeng Dan (WSHFD) and mercuric chloride on renal mercury (Hg) extraction transporters (Oat1, Oct2), renal mercury excretion transporters (Mrp4, Mate2K), renal mercury accumulation and kidney injury molecule-1 (Kim-1). The ancient prescription of WSHFD containing 10-fold Hg caused much lower renal mercury accumulation and renal toxicity than HgCl2 in rats, with less effect on renal transporters than HgCl2. The above indicators had no significant difference in WSHFDO, WSHFD2 and WSHFD3 groups, indicating no effect of WSHFD with reduced or no cinnabar.
Animals ; Ardisia ; chemistry ; Biological Transport ; drug effects ; Cell Adhesion Molecules ; genetics ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; adverse effects ; Gene Expression ; drug effects ; Kidney ; drug effects ; metabolism ; Male ; Mercuric Chloride ; metabolism ; Multidrug Resistance-Associated Proteins ; genetics ; metabolism ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo study the effect of Zhusha Anshen pill, cinnabar, HgS, HgCl2 and MeHg on the gene expression of renal transporters in mice.

METHODHealthy male mice were given equivalent physiological saline, Zhusha Anshen pill (1.8 g · kg(-1), containing 0.17 g · kg(-1) of mercury), cinnabar (0.2 g · kg(-1), containing 1.7 g · kg(-1) of mercury), high dose cinnabar (2 g · kg(-1), containing 1.7 g · kg(-1) of mercury), HgS (0.2 g · kg(-1), containing 0.17 g · kg(-1) of mercury), HgCl2 (0.032 g · kg(-1), containing 0. 024 g · kg(-1) of mercury), MeHg (0.026 g · kg(-1), containing 0.024 g · kg(-1) of mercury), once daily, for 30 d, measuring body mass gain. 30 days later, the mice were sacrificed. The mercury accumulation in kidneys was detected with atomic fluorescence spectrometer. Expressions of Oat1, Oat2, Oat3, Mrp2, Mrp4, Urat1 were detected with RT-PCR.

RESULTCompared with the normal control group, a significant accumulation of Hg in kidney in HgCl2 and MeHg groups was observed (P <0.05), but these changes were not found in other groups. Compared with normal control group, mRNA expressions of Oat1 and Oat2 were evidently lower in HgCl2 and MeHg groups, but mRNA expressions of Mrp2 were apparently higher in HgCl2 group (P <0.05), mRNA expression of Mrp4 was significant higher in HgCl2 and MeHg groups, and mRNA expression of Urat1 was apparently lower in MeHg group.

CONCLUSIONHgCl2 and MeHg groups show significant difference from the normal group in mercury accumulation in kidneys and gene expression of kidney transporters, but with no difference between other groups and the normal group. Compared with HgCl2 and MeHg, cinnabar and its compounds could cause lower renal toxicity to mice.

Animals ; Carrier Proteins ; genetics ; Drugs, Chinese Herbal ; toxicity ; Gene Expression ; drug effects ; Kidney ; drug effects ; metabolism ; Male ; Mercuric Chloride ; toxicity ; Mercury Compounds ; toxicity ; Methylmercury Compounds ; toxicity ; Mice ; Multidrug Resistance-Associated Proteins ; genetics ; Organic Anion Transport Protein 1 ; genetics ; Organic Anion Transporters, Sodium-Independent ; genetics

Objective：To evaluate bioequivalence and relative bioavailability of domestic and imported repaglinide tablets in healthy volunteers. Methods： Twenty two healthy male volunteers were randomized into A and B groups. A single dose (4 mg) of domestic and imported repaglinide tablets were given respectively according to an open 2-way crossover study design. The washout period was 1 week. Plasma concentrations of repaglinide were determined by HPLC method. Results：The pharmacokinetic parameters of domestic and imported drugs were as follows: t1/2 were(0.86±0.24) and (0.83±0.31) h；tmax were( 0.79±0.37) and (0.75±0.41) h；cmax were (52.43±20.92) and (53.32±24.94) μg/L. AUC0-t were (79.87±36.48) and (74.95±30.57) μg*h*L-1，respectively. The relative bioavailability of domestic formulation was (106.55±16.15)%. Conclusion： The results of variance analysis and two one-side t test show that 2 formulations are of bioequivalence.

Objective To explore the effect of the prevention and treatment of unstable bladder after suprapubic prostaectomy by capsaicin instilled into the bladder preoperatively combined with patient-controlled epidural analgesia(PCEA)for benign prostatic hyperplasia(BPH).Methods Sixty patients with BPH underwent suprapubic prostatectomy under epidural anesthesia were randomly divided into control group (30 cases)and treatment group(30 cases),100 ml of 100 μmol/L capsaicin was instilled into the bladder preoperatively for 30 minutes combined with PCEA after operation in treatment group,the control group was only given PCEA.Observed the incidence and continuous time of unstable bladder after operation in two groups.Results Unstable bladder was found in 3 cases of treatment group and they were Ⅰdegree,12 cases happened unstable bladder in control group,3 cases Ⅰdegree,5 cases Ⅱdegree,3 cases Ⅲ degree,1 case Ⅳ degree.There was obvious significance between two groups (P＜0.05).Conclusion Capsaicin instilled into the bladder combined with PCEA can cut off the reflex arc of detrusor contraction more completely and has obvious effect of decrease the incidence of unstable bladder after suprapubic prostatectomy and can be used widely.

In this study,a series of new sildenafil analogues 11-27 possessing a guanidine group were synthesized to investigate their PDE5 inhibitory activity and selectivity using[~3H]cGMP SPA kit in vitro and efficacy in the rat model of erection.Most of the compounds showed potent activity against PDE5,and more importantly,several compounds exhibited higher PDE5 selectivity over PDE6 than that of sildenafil.Structure-activity relationship of these sildenafil analogues was also discussed.Within this series of compounds,compound 15(IC_(50) =1.7 nmol/L)not only exhibited more potent PDE5 inhibitory activity than that of sildenafil (IC_(50) = 6.5 nmol/L),but also showed functional efficacy in the rat model of erection.