Aim To study the effect of novel AChE inhibitors, 2-phenoxy-indan-1-one derivatives (YKY-1~7), against glutamatic acid-induced neurotoxicity in PC12 cells and on learning & memory impairment in dementia model mice induced by A?25~35 icv Methods The PC12 cells were preincubated with different concentrations of YKY-1~7 for 24 h and subsequently treated by glutamatic acid, at the high concentration of 2 mmol?L-1 for 15 min to induce cytotoxicity. The cell viability was assessed with MTT method.. Dementia model mice were made by intracerebroventricular injection (icv) of aggregated A?25~35. From the next day, the model mice were administered YKY-7 (2.5, 5, 10 mg?kg-1, ig) for 10 consecutive days and sham control mice or A? model control mice received daily ig saline. After the final treatment, the passive avoidance learning was tested, regional cerebral blood flow at cerebral cortex was assessed, and the activity of AChE in the cerebral cortex, hippocampus and blood serum were determined. Results Six out of the seven YKY compounds appeared to be effective against glutamatic acid-induced neurotoxicity in PC12 cells, with YKY-7 demonstrating the most activity. YKY-7 significantly ameliorated the learning and memory ability in dementia model mice induced by A?25-35 icv, slightly and selectively inhibited the cortical and hippocampal AChE, and gently increased the blood flow at cerebral cortex. Conclusion Some of 2-phenoxy-indan-1-one derivatives reported here have protective effects against glutamatic acid induced neurotoxicity in PC12 cells, and improve the learning and memory impairment induced by A?25-35, which may be partly attributable to its selective inhibition of AChE activity in the cerebral cortex and hippocampus.

Adolescent ; Child ; Humans ; Male ; Manipulation, Orthopedic ; methods ; Radius Fractures ; therapy

Volatile oil components and the contents and types of amino acid in spica of Prunella vulgaris were analysed by GC-MS and amino acid analyzer. Esters, fatty acids, aromatic hydrocarbon, ketone and several alcohol compounds were identified by mass spectrum comparison. In these ingredients, beta-ionone smelled aroma of cedar, raspberry, nerolidol showed weak sweet soft orange blossom flavor, neroli tasted sweet and fresh, nerolidol tasted sweet with light aroma of wood, hexadecanal showed a weak aroma of flowers and wax, alpha-sinensal had rich and fresh sweet orange flavor. To some extent, these types of aromatic substances can affect the taste of herbal tea or decoction made of Spica Prunellae. Among amino acids detected, natural amino acids accounted for a larger proportion, and those natural amino acids showed bitterness, slight bitterness, sourness (freshness), sweetness, slight sweetness, sourness (slight freshness). The results indicated that bitter and slightly bitter amino acids have the greatest impacts on the sense of Spica Prunellae.
Amino Acids ; analysis ; Gas Chromatography-Mass Spectrometry ; Oils, Volatile ; analysis ; Prunella ; chemistry ; Taste

Objective To investigate the correlation ofClaudin-1, Ki-67 and CD34 expressionsin the tumor tissue to the invasiveness, grading and proliferation of astrocytic tumors. Methods In 50cases of astrocytic tumor, the expressions of Claudin-1, IO-67 and CD34 were detectedimmunohistochemically in the tumor tissue, normal brain tissues and in the junctional area between thetumor and normal tissues. The expressions of Claudin-1, Ki-67, and CD34 were analyzed in relation tothe clinicopathoiogical characteristics of the patients. Results The expression rate of Claudin-1 was70.59% in the astrocytic tumors of histological grades Ⅰ and Ⅱ, significantly higher than that in grade Ⅲand Ⅳ tumors (9.09%, χ2=20.206, P=0.000). In grade Ⅲ and Ⅳ tumors, the positivity rates of Ki-67 inthe normal tissues, junctional area and the tumor tissue were all significantly higher those in grade Ⅲ andⅣ tumors (t=9.144, 5.958, and 6.297; P=0.000, 0.000, and 0.000, respectively). Grade Ⅲ and Ⅳ tumorsdisplayed significantly greater mierovessel density (MVD) than grade Ⅰ and Ⅱ tumors in the tumor tissue(t=3.101, P=0.003) and the junctional area (t=4.139, P=0.000). In all the tumors, significantly higherKi-67 expression was seen in the tumor tissue (12.74±6.93) than in the junctional area (7.42±3.93) andthe normal tissue (3.22±1.57) (F=51.726, P=0.000), and the MVD was also greater in the tumor tissue(27.48±8.26) than in the junctional area (10.72±3.93) and normal tissue (6.48±1.45) (F=215.538, P=0.000).Conclusion Expressions of Claudin-1, Ki-67, and CD34 are closely correlated to the proliferation andinvasion of astrocytic tumors, and these cytokines may serve as important indicators for evaluating themalignancy of astrocytic tumors..

OBJECTIVE: To develop a method to measure trihexyphenidyl, chlorpromazine and clozapine in human blood with GC-MS. METHODS: The specimens were alkalized (pH > 10) and extracted with V (benzene):V(ethyl acetate) = 1:1, and qualitatively analyzed using GC-MS-Full Scan with internal standard SKF525A. The specimens were alkalized (pH > 10) and extracted with V(benzene):V(ethyl acetate) = 1:1, and quantitatively analyzed using GC-MS-SIM with internal standard diazepam-d5. RESULTS: The lowest detection limits of trihexyphenidyl, chlorpromazine and clozapine were 0.3, 0.3 and 0.7 ng/mL (S/N > or = 3) respectively. The calibration curve in 20-10 000 ng/mL showed a good linear distribution. The recovery rate was 79.9% to 85.5%. The RSDs of intraday and interday were less than 5.1%. CONCLUSION The established method was simple, sensitive and accurate for simultaneous determination of trihexyphenidyl, chlorpromazine and clozapine in human blood, and can be applied in forensic toxicological cases.
Adult ; Antipsychotic Agents/poisoning* ; Chlorpromazine/blood* ; Clozapine/blood* ; Female ; Forensic Toxicology ; Gas Chromatography-Mass Spectrometry/methods* ; Humans ; Hydrogen-Ion Concentration ; Male ; Middle Aged ; Reproducibility of Results ; Sensitivity and Specificity ; Solvents/chemistry* ; Trihexyphenidyl/blood*

OBJECTIVETo investigate the impact of early rapid virological response on the outcomes of hepatitis B associated acute on chronic liver failure during antiviral treatment.

METHODS106 acute on chronic liver failure patients in our hospital from January 2008 to July 2010 were enrolled in present study retrospectively. Besides internal medicine therapy, all patients received lamivudine (100 mg/d) or entecavir (0.5 mg/d) treatment. The profile of liver biochemistry, prothrombin time activity and viral load were detected at baseline and week 4, respectively. The patients were divided into HBV DNA negative group and HBV DNA positive group according to the viral load at week 4. The clinical features and treatment outcomes were compared between groups. Frequency variables were compared by x2 test or Fisher's exact test. Continuous variables were compared using independent samples T-test. The factors that impact on the treatment outcomes were determined using stepwise multivariate logistic regression analysis.

RESULTSAt the week 4, the TBil and PTA in HBV DNA positive group [(261.6+/-205.6)mumol/L and 44.7%+/-19.7%, respectively] were significantly different from those in HBV DNA negative group [(160.1+/-173.4) mumol/L and 56.8%+/-23.1%, respectively] ( t = 2.190 and -2.077, respectively, P less than 0.05). The non-effective rate of HBVDNA positive group (50%, 9/18) was significantly higher than that of HBV DNA negative group (14.8%, 13/88) (x2 = 9.235, P less than 0.01). By using stepwise multivariate logistic regression analysis, the disease stage and HBV DNA undetectable at week 4 were the independent factor. The OR values of disease stage and HBV DNA undetectable were 6.559 and 0.209, respectively, and 95% CI was 2.316~18.576 and 0.058~0.747, respectively.

CONCLUSIONThe rapid suppression of viral load by nucleotide analogue may improve the efficacy of hepatitis B associated acute on chronic liver failure treatment. The early rapid virological response within first 4 weeks may contribute to the prediction of the treatment outcomes.

Adult ; Antiviral Agents ; therapeutic use ; DNA, Viral ; blood ; End Stage Liver Disease ; drug therapy ; virology ; Female ; Hepatitis B ; drug therapy ; Humans ; Liver Failure, Acute ; drug therapy ; virology ; Male ; Middle Aged ; Prognosis ; Retrospective Studies ; Treatment Outcome ; Viral Load

OBJECTIVETo study the clinical effectiveness of applying comprehensive medical model in treating stroke in Chinese medicine (CM) hospitals.

METHODSTotally 236 stroke inpatients were randomly assigned to the comprehensive treatment group (as the experimental group, 121 cases) and the conventional treatment group (as the control group, 115 cases). A standard comprehensive treatment mode was applied in the experimental group. The Chinese materia medica (CMM) or acupuncture was combined during the rehabilitation treatment. Traditional basic drug treatment method was applied in the conventional treatment group. The health education for patients and their families was launched non-systematically. The mortality, the occurrence rate of complications, short-term clinical effectiveness, as well as NIHSS, Barthel index (BI), and Oxford Handicap Scale (OHS) were compared between the two groups.

RESULTSBefore treatment there was no statistical difference in NIHSS score, BI, or OHS score between the two groups (P > 0.05). On day 21 and 90 of the treatment, there was statistical difference in NIHSS score, BI, and OHS score (P < 0.01). Better results were obtained in the experimental group. On day 21 and 90 of the treatment, the total effectiveness rate was 80.99% and 88.43% in the experimental group, higher than that of the control group (61.74% and 72.17% respectively), showing statistical difference (P < 0.05, P < 0.01). The occurrence rate of common complications in the experimental group was obviously lower than that in the control group (30.58% vs 69.56%, P < 0.01). There was no statistical difference in the mortality between the two groups (P > 0.05).

CONCLUSIONSThe application of the comprehensive medical model in treating stroke in CM showed better effects than using traditional basic drug treatment method. Treatment of stroke by CM showed superiorities.

Acupuncture Therapy ; Aged ; Combined Modality Therapy ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Integrative Medicine ; Male ; Middle Aged ; Stroke ; therapy ; Treatment Outcome

OBJECTIVETo investigate effect of tramadol on c-fos expression in spinal cord dorsal horn and serum IL-6 levels induced by plantar incision in rats.

METHODSThe Brennan pain model was induced by incision on the planter surface of left hind paw in rats. Forty-eight rats were randomly divided into six groups: Sham group (Group C), control group (Group I,pretreatment with saline 5 ml), three tramadol pretreatment groups (Group T1, T10 and T20,pretreated with 1 mg/kg, 10 mg/kg and 20 mg/kg tramadol, respectively) and one tramadol treatment group (Group PT10, treated with tramadol 10 mg/kg immediately after operation). Pain behavior was assessed by withdrawal threshold to von Frey filament stimulation intensity, response latency of the hind paw to radiant thermal and a cumulative pain score 2 h after incision. Fos-positive neurons in spinal cord were identified by the immunohistochemical technique. Serum IL-6 levels were measured by enzyme-linked immunosorbent assay (ELISA).

RESULTSWithdrawIal threshold to von Frey filament stimulation intensity and response latency of the hind paw to radiant thermal in Group I were significantly lower than those in Group C (P<0.01). Cumulative pain score in Group I was significantly higher than that in Group C (P<0.01). In Groups of T10 and T20, withdrawal threshold to von Frey filament stimulation intensity and response latency of the hind paw to radiant thermal were significantly higher than those in Group I (P<0.01), cumulative pain score was significantly lower than that in Group I in a dose-dependent manner (P<0.01), and were also those in Group PT10. The greatest density of Fos-positive neurons was located in lamine I-II in Group I. Serum IL-6 levels were significantly elevated in Group I. Pretreatment with tramadol showed a dose-depended inhibitory effect on c-fos expression and serum IL-6 production,but not in Group T1. Administration of tramadol postoperatively also suppressed the c-fos expression and serum IL-6 production as showed in PT10 but were weaker than those in Group T10.

CONCLUSIONPretreatment with tramadol can produce dose-dependent inhibitory effect on c-fos expression in spinal cord dorsal horn and then suppress the inflammatory response to the trauma.

Analgesics, Opioid ; pharmacology ; therapeutic use ; Animals ; Interleukin-6 ; blood ; Male ; Pain Threshold ; drug effects ; Pain, Postoperative ; drug therapy ; metabolism ; Posterior Horn Cells ; drug effects ; metabolism ; Proto-Oncogene Proteins c-fos ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tramadol ; pharmacology ; therapeutic use

OBJECTIVEHepatic stellate cells (HSC) in hepatocellular carcinoma (HCC) transdifferentiate into extracellular matrix-producing myofibroblasts. Activated HSC can promote invasion and metastasis of HCC. To understand the differences of HSC in normal liver and HCC, we compared the gene expression patterns in HCC cell induction-activated and culture-activated rat HSC.

METHODSHSC were isolated by density centrifugation and exposed to conditioned medium from rat HCC cell line C5F. Expression of 22 012 genes in quiescent HSC, culture-activated HSC and HCC induction-activated HSC was analyzed by cDNA microarray and confirmed by real-time RT-PCR and Western blot.

RESULTS1672 genes were differentially expressed in culture-activated HSC, including proinflammatory factors, cell adhesion molecules, cell surface receptors, signaling transduction molecules and immune factors. 711 genes were differentially expressed in HCC induction-activated HSC. Some of them were identical to those in culture-activated HSC. HCC Induction-activated HSC showed specific gene expression patterns, including Raf1, Rac2, Adam17, Wnt6, MMP-9 and TNF, suggesting that HCC cells can specifically induce HSC activation.

CONCLUSIONThe gene expression patterns in HCC induction-activated HSC are different from those in culture-activated HSC. HCC induction-activated HSC may play a major role in the invasion and metastasis of HCC. In vivo activation should be considered as the standard for the study of HSC biology. HCC induction-activated HSC should be considered as the standard for HSC biology studies.

Animals ; Carcinoma, Hepatocellular ; metabolism ; pathology ; Cell Line, Tumor ; Cells, Cultured ; Gene Expression Profiling ; Gene Expression Regulation, Neoplastic ; Hepatic Stellate Cells ; metabolism ; pathology ; Liver Neoplasms ; metabolism ; pathology ; Male ; Oligonucleotide Array Sequence Analysis ; Rats ; Rats, Inbred F344

OBJECTIVETo investigate and compare the clinical significance of (18)F-FDG single-photon emission computed tomography and computed tomography (SPECT-CT) in the diagnosis and staging of lung cancer.

METHODSFrom July 2005 to July 2007, 71 patients with suspected lung cancer received conventional CT and SPECT-CT examination. Fifty-seven of the 71 patients had definite pathological or cytological diagnosis, consisting of 52 malignant lung tumors and 5 benign pulmonary nodules. Forty-three patients underwent surgical resection with different modes. Thirty-seven of the 43 surgically treated patients had available complete data of CT, SPECT-CT and pathological results.

RESULTSTaking the pathological diagnosis as gold standard, the sensitivity, specificity and accuracy of diagnosing pulmonary lesions suspected as lung cancer were 84.6% (44/52), 80.0% (4/5), 84.2% (48/57) for conventional CT and 92.3% (48/52), 80.0% (4/5), 91.2% (52/57) for SPECT-CT, respectively. If taking the pathological TNM staging results as gold standard, the concordance rates of TNM staging with pathological TNM staging results was 59.5% (22/37) for CT and 67.6% (25/37) for SPECT-CT. The sensitivity, specificity, accuracy, positive predictive value and negative predictive value of staging hilar and mediastinal lymph nodes were 76.9%, 79.2%, 78.4%, 66.6%, 86.4% for conventional CT versus 61.5%, 75.0%, 70.3%, 57.1%, 78.3% for SPECT-CT (P > 0.05), respectively. There was no statistically significant difference between conventional CT and SPECT-CT in the accuracy of diagnosing and staging for the suspected pulmonary lesions (P > 0.05).

CONCLUSIONSPECT-CT is likely superior to conventional CT in the diagnosing and staging for lung cancer. It can be used as a non-invasive supplementary tool for differential diagnosis between malignant and benign pulmonary lesions and in diagnosis of lymph node > 1 cm in diameter.

Adenocarcinoma ; diagnosis ; diagnostic imaging ; pathology ; Adult ; Aged ; Aged, 80 and over ; Carcinoma, Squamous Cell ; diagnosis ; diagnostic imaging ; pathology ; Female ; Fluorodeoxyglucose F18 ; Humans ; Lung Neoplasms ; diagnosis ; diagnostic imaging ; pathology ; Lymphatic Metastasis ; Male ; Middle Aged ; Neoplasm Staging ; Radiopharmaceuticals ; Small Cell Lung Carcinoma ; diagnosis ; diagnostic imaging ; pathology ; Tomography, Emission-Computed, Single-Photon ; methods ; Tomography, X-Ray Computed