Animals ; Carbon Disulfide ; adverse effects ; Light ; Male ; Neurons ; drug effects ; radiation effects ; Noise ; adverse effects ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo investigate the therapeutic effect of Yiqi Huaju Recipe (YHR) combined with routine therapy on the blood pressure, the blood pressure variability and other cardiovascular risk factors in hypertension patients complicated with metabolic syndrome (MetS).

METHODSTotally 43 hypertension patients complicated with MetS were recruited in this study and randomly assigned to the treatment group (22 cases, treated with basic routine treatment +YHR) and the control group (21 cases, treated with basic routine treatment + placebo). The treatment course was 12 weeks. Detected were parameters such as 24-h ambulatory blood pressure monitoring (ABPM), body mass index (BMI), waist circumference (WC), waist to hip ratio (WHR), homeostatic model assessment for insulin resistance (HOMA-IR), fasting glycosylated hemoglobin A1c (HbA1c), fasting plasma glucose (FPG), 2 h postprandial plasma glucose (2 h PPG), fasting plasma insulin (FPI), serum lipid, etc.

RESULTSThe anthropometric parameters and plasma glucose levels (except HbAlc) were obviously lowered after treatment than before treatment in the treatment group (P < 0.01, P < 0.05). Besides, better effects were obtained in the WC, WHR, 2 h PPG, FPI and HOMA-IR (P < 0.05). The average blood pressure amplitude, the blood pressure variability, and blood pressure load at any time point were more obviously improved in the two groups after treatment than before treatment (P < 0.01, P < 0.05). Besides, partial indices were better in the treatment group than in the control group (P < 0.01, P < 0.05).

CONCLUSIONSYHR combined with routine therapy exhibited better effect on reducing the blood pressure amplitude, the blood pressure variability, and the blood pressure load in hypertension patients complicated with MetS. It could also effectively decrease the risk of other vascular disease.

Adult ; Blood Pressure ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Hypertension ; complications ; drug therapy ; Male ; Metabolic Syndrome ; complications ; Middle Aged

AIMTo investigate the in vitro recovery and influencing factors of ketoprofen in microdialysis probe, and study the pharmacokinetic of unbound ketoprofen in rat after iv administration.

METHODSThe recovery of ketoprofen was detected by a concentration difference method. After microdialysis probe was inserted into the jugular vein of male Wistar rats, the probe was infused with various concentrations perfusate. The in vivo recovery and the pharmacokinetics of unbound ketoprofen in rat were investigated. Dialysate samples were determined by HPLC.

RESULTSThe recovery detected by gain was as the same as that by loss; the recovery was independent of the drug concentration surrounding the probe. The in vitro recovery was 28.75% by concentration difference method and the in vivo recovery was (40.3 +/- 2.7) % by retrodialysis method. After i.v. administration of ketoprofen in rat, T 1/2, AUC and CL of unbound ketoprofen were (181 +/- 16) min, (112 +/- 27) microg x min x mL(-1) and (0.22 +/- 0.05) L x min(-1), respectively.

CONCLUSIONMicrodialysis sampling can be used for the pharmacokinetic study of unbound ketoprofen in rat.

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; pharmacokinetics ; Area Under Curve ; Chromatography, High Pressure Liquid ; Injections, Intravenous ; Ketoprofen ; administration & dosage ; pharmacokinetics ; Male ; Microdialysis ; methods ; Rats ; Rats, Wistar

Experiments were performed on Sprague Dawley rats with multibarrel microelectrode technique. The effects of acoustic response of A I cortex neurons produced by electrical stimulation of lateral amygdaloid nucleus (LA) and the influence of GABA were observed. Experimental results showed that iontophoretic administration of GABA caused a pronounced inhibition of the electrical activity of A-I neurons. Blockade of GABA(A) with bicuculline (BIC) facilitated the acoustic response. The acoustic response of A-I neurons was inhibited when the LA was stimulated. Iontophoretic application of GABA resulted in a similar inhibitory effect as that of LA stimulation. Blockade of GABA(A) with bicuculline reversed the inhibitory effect of LA stimulation on the acoustic response of A-I neurons. In contrast, application of strychnine, a glycine receptor antagonist, could not reverse the inhibitory effect of LA. Baclofen, a GABA(B) agonist, did not affect the acoustic response of the auditory neurons. These results indicate that GABA is the ultimate transmitter which mediates the LA stimulation-induced inhibition of the acoustic response of A-I neurons in rats, possibly via the GABA(A) receptor.
Acoustic Stimulation ; Amygdala ; physiology ; Animals ; Baclofen ; pharmacology ; Bicuculline ; pharmacology ; Cerebral Cortex ; physiology ; Electric Stimulation ; Evoked Potentials, Auditory ; physiology ; GABA Agonists ; pharmacology ; GABA Antagonists ; pharmacology ; Iontophoresis ; methods ; Male ; Microelectrodes ; Neurons ; physiology ; Rats ; Rats, Sprague-Dawley ; Receptors, GABA-A ; physiology ; gamma-Aminobutyric Acid ; physiology

AIMTo prepare the sustained-release nitrendipine microspheres with a solid dispersed structure in liquid system.

METHODSThe sustained-release nitrendipine microspheres with a solid dispersed structure was prepared in liquid system by combining spherical crystallization technique and solvent deposition method in one step. The resultant microspheres were evaluated for the recovery, micromeritc properties, incorporation efficiency. The factors of effect on the formation and the release rate of microspheres were also investigated.

RESULTSThe recovery of microspheres (280-900 microns) was more than 70% and the bulk density was around 0.7 kg.L-1. The incorporation efficiency always exceeded 95%. The formation of microspheres was mainly affected by the amount of bridging liquid and the emulsifying agents in poor solvent. The release rate of nitrendipine from the microspheres could be controlled as desired by adjusting the ratio of talc to Eudragit RS PO in the formulation.

CONCLUSIONThe presented method was suitable for preparing sustained-release microspheres of a water insoluble drug.

Delayed-Action Preparations ; Drug Carriers ; Microspheres ; Nitrendipine ; administration & dosage ; Particle Size ; Technology, Pharmaceutical ; methods

OBJECTIVETo observe changes of soluble CD40 ligand (sCD40L) in patients with hyperlipidemia of blood stasis syndrome and its correlation with blood stasis syndrome integral, P-selectin, and high sensitive creatine reactive protein (hs-CRP), to investigate the roles of platelet activation and inflammation in the physiopathologic process of blood-stasis type hyperlipidemia, and to explore the pathogenetic mechanism of blood-stasis syndrome (BSS).

METHODSSeventy hyperlipidemia patients were assigned to two groups, 39 in the BSS group and 31 in the non-BSS group. Meanwhile, thirty healthy subjects were grouped as the control. Main physiochemical indices, blood levels of sCD40L, P-selectin, hs-CRP were detected in all. The correlations of the aforesaid indices were analyzed.

RESULTSBSS score in the BSS group was higher than that in the non-BSS group and in the control group. Higher blood levels of P-selectin and sCD40L were shown in the BSS group than in the non-BSS group [(25.13 +/- 5.49) ng/L vs. (21.37 +/- 3.56) ng/L and (2.45 +/- 0.48) ng/L vs. (2.07 +/- 0. 41) ng/L] respectively, and the two indices were higher in hyperlipidemia patients than in healthy persons [(14.91 +/- 2.48) ng/L and (1.63 +/- 0.25) ng/L, P < 0.01]. Correlation analysis showed that in patients with hyperlipidemia, blood level of sCD40L was positively correlated with low-density lipoprotein cholesterol (LDL-C) level (r = 0.503, P < 0.01), P-selectin (r = 0.897, P < 0.01), and the BSS score (r = 0.603, P < 0.01).

CONCLUSIONSThe over-expressed sCD40L indicated persistent inflammatory state in patients with hyperlipidemia of BSS. BSS would further accelerate the chronic inflammation process of hyperlipidemia.

Adult ; Aged ; C-Reactive Protein ; metabolism ; CD40 Ligand ; blood ; Case-Control Studies ; Female ; Humans ; Hyperlipidemias ; blood ; diagnosis ; pathology ; Inflammation ; blood ; Male ; Medicine, Chinese Traditional ; Middle Aged ; P-Selectin ; blood

OBJECTIVETo study the immunohistochemical expression of OCT4, CD117 and CD30 in germ cell tumors and to assess their diagnostic value.

METHODSImmunohistochemical study for OCT4 was performed on formalin-fixed, paraffin-embedded tissues of 63 cases of germ cell tumors, including seminoma (21), dysgerminoma (7), germinoma (8), embryonal carcinoma (8), yolk sac tumor (6), mature teratoma (10) and immature teratoma (3), as well as 25 cases of non-germ cell tumors, including granulosa cell tumor (8), clear cell adenocarcinoma (4), Leydig's cell tumor (5), diffuse large B-cell lymphoma (4) and malignant melanoma (4). Besides, the expression of CD117 and CD30 in all germ cell tumors was studied.

RESULTSAll cases of seminoma and germinoma, 6/7 cases of dysgerminoma and 7/8 cases of embryonal carcinoma were positive for OCT4, with strong nuclear staining. All other germ cell tumors and non-germ cell tumors were negative for OCT4, except for 1 case of yolk sac tumor and 1 case of clear cell adenocarcinoma which showed weak staining. Positive membranous expression of CD117 was demonstrated in 19/21(90.5%) seminoma, 5/7 dysgerminoma and 7/8 germinoma. Focal weak membranous staining was also noted in 1 case of yolk sac tumor. The melanocytes in teratoma were also positive for CD117. All cases of embryonal carcinoma were negative. On the other hand, positive membranous expression of CD30 were demonstrated in 6/8 embryonal carcinoma. One case of germinoma and 1 case of yolk sac tumor showed weak cytoplasmic positivity. All cases of seminoma and dysgerminoma, 7/8 germinoma and all cases of teratoma were negative for CD30.

CONCLUSIONSOCT4 is a sensitive and relatively specific marker for diagnosing seminoma, dysgerminoma, germinoma and embryonal carcinoma. CD117 and CD30 immunostains, when used in combination, represent valuable tools for distinguishing embryonal carcinoma and seminoma, dysgerminoma, germinoma.

Carcinoma, Embryonal ; metabolism ; pathology ; Diagnosis, Differential ; Dysgerminoma ; metabolism ; pathology ; Endodermal Sinus Tumor ; metabolism ; pathology ; Female ; Germinoma ; metabolism ; pathology ; Humans ; Ki-1 Antigen ; metabolism ; Male ; Neoplasms, Germ Cell and Embryonal ; metabolism ; pathology ; Octamer Transcription Factor-3 ; metabolism ; Ovarian Neoplasms ; metabolism ; pathology ; Proto-Oncogene Proteins c-kit ; metabolism ; Seminoma ; metabolism ; pathology ; Teratoma ; metabolism ; pathology ; Testicular Neoplasms ; metabolism ; pathology

OBJECTIVETo define the differences in gene expression patterns between glycidyl methacrylate (GMA)-transformed human lung fibroblast cells (2BS cells) and controls.

METHODSThe mRNA differential display polymerase chain reaction (DD-PCR) technique was used. cDNAs were synthesized by reverse transcription and amplified by PCR using 30 primer combinations. After being screened by dot blot analysis, differentially expressed cDNAs were cloned, sequenced and confirmed by Northern blot analysis.

RESULTSEighteen differentially expressed cDNAs were cloned and sequenced, of which 17 were highly homologous to known genes (homology = 89%-100%) and one was an unknown gene. Northern blot analysis confirmed that eight genes encoding human zinc finger protein 217 (ZNF217), mixed-lineage kinase 3 (MLK-3), ribosomal protein (RP) L15, RPL41, RPS 16, TBX3, stanniocalcin 2 (STC2) and mouse ubiquitin conjugating enzyme (UBC), respectively, were up-regulated, and three genes including human transforming growth factor beta inducible gene (Betaig-h3), alpha-1,2-mannosidase 1A2 (MAN 1A2) gene and an unknown gene were down-regulated in the GMA-transformed cells.

CONCLUSIONAnalysis of the potential function of these genes suggest that they may be possibly linked to a variety of cellular processes such as transcription, signal transduction, protein synthesis and growth, and that their differential expression could contribute to the GMA-induced neoplastic transformation.

Air Pollutants, Occupational ; toxicity ; Carcinoma, Squamous Cell ; genetics ; pathology ; Cell Line, Transformed ; Epoxy Compounds ; toxicity ; Fibroblasts ; cytology ; drug effects ; Gene Expression Profiling ; Glycoproteins ; metabolism ; Humans ; Lung ; cytology ; Male ; Mannosidases ; drug effects ; metabolism ; Methacrylates ; toxicity ; Mitogen-Activated Protein Kinase 3 ; drug effects ; metabolism ; Oligonucleotide Array Sequence Analysis ; Ribosomal Proteins ; metabolism ; Signal Transduction ; genetics ; Transforming Growth Factor beta ; drug effects ; metabolism ; Ubiquitins ; metabolism ; Zinc Fingers ; drug effects ; physiology

OBJECTIVETo evaluate the genotoxic and nongenotoxic effects of short-term exposure to glycidyl mathacrylate (GMA) on human lung fibroblast cells (2BS cells) in vitro.

METHODSDNA strand breakage was determined by single cell gel electrophoresis, and DNA ladder formation assay and flow cytometric analysis were carried out to detect apoptic responses of cells to GMA exposure. The HPRT gene mutation assay was used to evaluate the mutagenicity, and the effect of GMA on gap junctional intercellular communication (GJIC) in the exposed cells was examined with the scrape loading/dye transfer technique. The ability of GMA to transform 2BS cells was also tested by an in vitro cell transformation assay.

RESULTSExposure to GMA resulted in a dose-dependent increase in DNA strand breaks but not apoptic responses. GMA was also shown to significantly induce HPRT gene mutations and morphological transformation in 2BS cells in vitro. In contrast, GMA produced a concentration-dependent inhibition of GJIC.

CONCLUSIONSGMA elicits both genotoxic and nongenotoxic effects on 2BS cells in vitro. The induction of DNA damage and gene mutations and inhibition of GJIC by GMA may casually contribute to GMA-induced cell transformation.

Cell Communication ; Cell Differentiation ; Comet Assay ; DNA Damage ; DNA Mutational Analysis ; Epoxy Compounds ; toxicity ; Fibroblasts ; Gap Junctions ; Humans ; Hypoxanthine Phosphoribosyltransferase ; genetics ; Lung ; cytology ; Methacrylates ; toxicity

OBJECTIVETo explore the effect of Changji'an Capsule (CA) on mRNA expressions of neuropeptide Y (NPY) in the hypothalamus and colon and serum levels of adreno-cortico-tropic hormone (ACTH) in rats of diarrhea predominant irritable bowel syndrome (IBS-D) model rats.

METHODSTotally 48 SD rats were randomly divided into six groups, i.e., the normal control group, the model group, the Pinaverium Bromide group (PB, 0.018 g/kg), the high dose CA group (2.812 g/kg), the medium dose CA group (1.406 g/kg), and the low dose CA group (0.703 g/kg), 8 in each group. The IBS-D rat model was established by using separation of breast milk + stimulation of acetic acid + constraint of four limbs. Normal saline was given to rats in the normal control group and the model group. All medication lasted for 14 successive days by gastrogavage. The serum content of ACTH was detected by enzyme linked immunosorbent assay (ELISA). The expressions of NPY mRNA in the colon and the hypothalamus were detected using real-time fluorescence quantitative PCR.

RESULTSCompared with the normal control group, the serum ACTH content significantly increased (P < 0.01), the NPY mRNA expression in the colon and the hypothalamus obviously decreased (P < 0.01) in the model control group. Compared with the model group, the serum ACTH obviously decreased in the high dose CA group, the medium dose CA group, and the PB group (P < 0.01, P < 0.05). The NPY mRNA expression in the colon and the hypothalamus were obviously up-regulated in the high dose CA group, the medium dose CA group, the low dose CA group, and the PB group (P < 0.05).

CONCLUSIONSCA could modulate the abnormity of brain-gut axis of IBS-D rats possibly by up-regulating NPY mRNA expressions in the hypothalamus and the colon and down-regulating the ACTH content in the hypothalamic-pituitary-adrenal axis.

Adrenocorticotropic Hormone ; blood ; Animals ; Colon ; metabolism ; Disease Models, Animal ; Drugs, Chinese Herbal ; pharmacology ; Female ; Hypothalamus ; metabolism ; Irritable Bowel Syndrome ; metabolism ; Male ; Neuropeptide Y ; metabolism ; RNA, Messenger ; genetics ; Rats ; Rats, Sprague-Dawley