Psychotic symptoms presented in familial Creutzfeldt-Jakob disease, subtype E200K.
Explore the source record for details and available documents.
Antipsychotic Agents↗
Biomedical subjects
S Zeng
Publications and source records attributed to S Zeng.
Stereoselective metabolism of propafenone by human liver CYP3A4 expressed in transgenic Chinese hamster CHL cells lines.
AIM: To investigate the stereoselective metabolism of propafenone (PPF) by human liver CYP3A4. METHODS: A chiral and an achiral HPLC were combined to determine the enantiomer of PPF in S9 incubates prepared from transgenic Chinese hamster CHL cells lines expressing CYP3A4. The time-dependent study was performed using individual enantiomer or racemate at low or high substrate concentration. Kinetic parameters were determined employing individual enantiomers as substrates. Enantiomeric inhibition experiments were performed by using R(-)-PPF as an inhibitor and S(+)-PPF as a substrate. RESULTS: Stereoselectivity was found in metabolism of racemic PPF at low substrate concentration (10 mg/L) (S < R), and lost at high substrate concentration (400 mg/L) When an individual enantiomer of high concentration (200 mg/L) was used as a substrate, S(+)-PPF was eliminated faster than its isomer (S < R). However, the opposite situation was observed at low concentration (5 mg/L) (S < R). The Vmax of S(+)-PPF was significantly greater than that of R(-)-PPF [(2.66 +/- 0.32) vs (1.71 +/- 0.19) micromol . mg-1 . min-1]. The Km of R(-)-PPF was significantly lower than that of S(+)-PPF [(73 +/- 11) vs (185 +/- 17) micromol/L]. R(-)-PPF inhibited S(+)-isomer with an IC50 value of 125 micromol . L-1. CONCLUSION: It is concluded that stereoselectivity in metabolism of propafenone via CYP3A4 depend on substrate concentration. Enantiomer/enantiomer interaction of PPF occurred at high concentration of substrate, and resulted in the loss of stereoselectivity. There maybe no enantiomer/enantiomer interaction at low concentration thus keeping the superiority of R(-)-PPF in metabolism.
Animals↗
[Muscarinic receptor subtype-3 expression in trabecular meshwork of normal human eye and primary open-angle glaucoma].
OBJECTIVE: To identify the muscarinic receptor subtype-3 (M3-receptor) expression in trabecular meshworks (TM) of normal human eyes and eyes with primary open-angle glaucoma (POAG) and discuss the pathological changes of TM in POAG. METHOD: TM specimens were taken from 5 normal persons and 10 patients with POAG at late stage. Then LSAB immunohistochemical technique was used to identify M3-receptors. The results were observed under microscope and compared with computer-image-analysis system. RESULTS: (1) The trabecular meshwork cells in all the 5 normal persons expressed M3-receptors. The positive cells mainly existed in the uveal part of TM, from Schwalbe's line to scleral spur. (2) In TM from eyes with POAG, the amount of both TM cells and M3-receptor positive cells were reduced obviously, even some specimens had no such positive expression. The positive cells were correspondingly decreased in number and scattered in distribution. CONCLUSION: The TM cells in normal human eyes express M3-receptors. The TM cells and M3-positive cells in eyes with late POAG are reduced in number and their distribution is irregular.
Adolescent↗
[Study on anticancer activity of Syngnathus in vitro].
OBJECTIVE: To study the anticancer activity of Syngnathus in vitro. METHOD: Observing the influence of different extracts from Syngnathus on growth of different cancer cell strains by MTT method. RESULT: It has been found out that the fat-soluble nonsaponified extract from Temminck et Schlegel and the alcoholic extract from Syngnathus acus have cytotoxic activities. The nonsaponified extract from Temminck et Schlegel can inhibit the growth of cancer cell strains KB, Hela, PAA, K562, and Bcap37, and the alcoholic extract from Syngnathus acus can inhibit the growth of cancer cell strin KB, But Bloch shows no apparent anticancer activity. CONCLUSION: Syngnathus has promising prospects as an anticancer Chinese medicine.
Animals↗
Stable and unstable transgene integration sites in the human genome: extinction of the Green Fluorescent Protein transgene in K562 cells.
In gene transfer experiments including gene therapy studies, expression of the integrated transgenes in host cells often declines with time. The molecular basis of this phenomenon is not clearly understood. We have used the Green Fluorescent Protein (GFP) gene as both a selectable marker and a reporter to study long-term transgene integration and expression in K562 cells. Cells transfected with plasmids containing the GFP gene coupled to the HS2 or HS3 enhancer of the human beta-globin Locus Control Region (LCR) or the cytomegalovirus (CMV) enhancer were sorted by either fluorescence-activated-cell-sorting (FACS) alone or FACS combined with drug selection based on a co-integrated drug resistance gene. The two groups of selected cells were subsequently cultured for long periods up to 250 cell generations. Comparison of long-term GFP transgene integration and expression in these two groups of cells revealed that the K562 genome contains two types of transgene integration sites: i) abundant unstable sites that permit transcription but not long-term integration of the transgenes and thus eliminate the transgenes in 60-250 cell generations and ii) rare stable sites that permit both efficient transcription and long-term stable integration of the transgenes for at least 200 cell generations. Our results indicate that extinction of GFP expression with time is due at least in part to elimination of the gene from the host genome and not entirely to transcriptional silencing of the gene. However, long-term, stable expression of the transgene can be achieved in cells containing the transgene integrated into the rare, stable host sites.
Binding Sites↗
Inhibition of the amygdala and hippocampal calcium/calmodulin-dependent protein kinase II attenuates the dependence and relapse to morphine differently in rats.
Learning and memory have been suggested to play an important role in the development of opiate addiction. Based on the recent finding that calcium/calmodulin protein kinase II (CaMKII) is essential in learning and memory processes, the present study was performed to examine whether inhibition of hippocampal and amygdala CaMKII prevents the dependence and relapse to morphine. The results showed that inhibition of CaMKII by microinjection of specific inhibitors KN-62 into hippocampus decreased the morphine withdrawal syndromes induced by opiate antagonist naloxone. In contrast, inhibition of CaMKII in amygdala failed to do so. Microinjection of KN-62 into both hippocampus and amygdala suppressed the development of formation and reactivation of morphine conditioned place preference (CPP). However, inhibition of CaMKII in amygdala, but not in hippocampus, could attenuate the maintenance of morphine CPP. These results suggest that hippocampal CaMKII is critically involved in the development of morphine physical and psychological dependence, and amygdala CaMKII is some different from hippocampal CaMKII in regulating the dependence and relapse to opiates. Inhibition of this kinase may have some therapeutic benefit in the treatment of opiate dependence and relapse.
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine↗
Reversed-phase high-performance liquid chromatographic analysis of atenolol enantiomers in rat hepatic microsome after chiral derivatizaton with 2,3,4,6,-tetra-O-acetyl-beta-D-glycopyranosyl isothiocyanate.
A reversed-phase high-performance liquid chromatographic method for the determination of the enantiomers of atenolol in rat hepatic microsome has been developed. Racemic atenolol was extracted from alkalinized rat hepatic microsome by ethyl acetate. The organic layer was dried with anhydrous sodium sulfate and evaporated using a gentle stream of air. Atenolol racemic compound was derivatized with 2,3,4,6-tetra-O-acetyl-beta-D-glycopyranosyl isothiocyanate at 35 degrees C for 30 min to form diastereomers. After removal of excess solvent, the diastereomers were dissolved in phosphate buffer (pH 4.6)-acetonitrile (50:30). The diastereomers were separated on a Shimadzu CLC-C18 column (10 microm particle size, 10 cm x 0.46 cm I.D.) with a mobile phase of phosphate buffer-methanol-acetonitrile (50:20:30, v/v) at a flow-rate of 0.5 ml/min. A UV-VIS detector was operated at 254 nm. For each enantiomer, the limit of detection was 0.055 microg/ml (signal-to-noise ratio 3) and the limit of quantification (signal-to-noise ratio 10) was 0.145 microg/ml (RSD <10%). In the range 0.145-20 microg/ml, intra-day coefficients of variation were 1.0-7.0% and inter-day coefficients of variation were 0.4-16.5% for each enantiomer. The assay was applied to determine the concentrations of atenolol enantiomers in rat hepatic microsome as a function of time after incubation of racemic atenolol.
Adrenergic beta-Antagonists↗
Expression of functional soluble forms of human beta-1, 4-galactosyltransferase I, alpha-2,6-sialyltransferase, and alpha-1, 3-fucosyltransferase VI in the methylotrophic yeast Pichia pastoris.
The cDNAs encoding soluble forms of human beta-1, 4-galactosyltransferase I (EC 2.4.1.22), alpha-2,6-sialyltransferase (EC 2.4.99.1), and alpha-1,3-fucosyltransferase VI (EC 2.4.1.65), respectively, have been expressed in the methylotrophic yeast Pichia pastoris. The vector pPIC9 was used, which contains the N-terminal signal sequence of Saccharomyces cerevisiae alpha-factor to allow entry into the secretory pathway. The recombinant enzymes had similar kinetic properties as their native counterparts. Their identity was confirmed by Western blotting. Recombinant enzymes may be used for in vitro synthesis of oligosaccharides.
Cloning, Molecular↗
Stereoselective determination of propafenone enantiomers in transgenic Chinese hamster CHL cells expressing human cytochrome P450.
An enantioselective assay for S(+)- and R(-)-propafenone in transgenic Chinese hamster CHL cells expressing human cytochrome P450 was developed. The method involved extraction of propafenone from the S9s incubates, and formation of propafenone diastereomeric derivatives with the chiral reagent 2,3,4, 6-tetra-O-beta-D-glucopranosyl isothiocyanate. Separation and quantitation of diastereomeric propafenone derivatives were carried out in a reverse-phase-HPLC system with UV detection. The assay was linear from 2 to 200 microg/mL for each enantiomer. The analytical method gave average recoveries of 97.5% and 97.0% for S(+)- and R(-)-propafenone, respectively. The limits of detection and quantitation for the method are 0.1 and 2.0 microg/mL for both S(+)- and R(-)-propafenone, respectively. The reproducibility of the assay was good (RSD <10%). The method allowed study of the depletion of S(+)- and R(-)-propafenone in transgenic Chinese hamster CHL cells expressing human cytochrome P450. The stereoselectivity of propafenone phase I metabolism via cDNA-expressed CYP3A4 was observed.
Animals↗
A new video-synchronized multichannel biomedical data acquisition system.
This data acquisition system records video frames onto a video tape, and simultaneously acquires biomedical data along with video time codes onto a computer hard disk to achieve a 30-min video-synchronized data recording with a summed data rate of 2.16 Mbit/s. A time-code-bridge-file created during acquisition matches each video frame-start with the corresponding index number of the acquired data. The mean synchronization accuracy of the system is 0.22 ms.
Computer Graphics↗
In vitro evaluation of schedule-dependent interactions between docetaxel and doxorubicin against human breast and ovarian cancer cells.
Docetaxel, a novel member of the taxoid family, has shown greater potency than paclitaxel in the treatment of advanced breast cancer and certain other solid tumors. The promising clinical activity of docetaxel has also promoted considerable interest in combining this drug with other antitumor agents. In this study, we assessed the cytotoxic interaction between docetaxel and doxorubicin administered at various schedules to human breast and ovarian cancer cells. Through a series of in vitro assays including DNA fragmentation analyses, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays, and flow cytometric analyses, we found that the antagonistic interaction occurred when tumor cells were exposed to the two drugs simultaneously or exposed to doxorubicin before docetaxel. However, no antagonism was observed when docetaxel was added before doxorubicin. Further analyses demonstrated that doxorubicin could interfere with the cytotoxic effect of docetaxel on both mitotic arrest and apoptotic cell death. In addition, biochemical examinations revealed that docetaxel could induce phosphorylation of both bcl-2 and c-raf-1, but these changes were inhibited when tumor cells were pretreated or simultaneously treated with doxorubicin. These results indicate that the interaction between docetaxel and doxorubicin is highly schedule dependent. Exposure of tumor cells to doxorubicin before docetaxel could result in pronounced antagonism. The optimal schedule for this combination might be sequential exposure to docetaxel followed by doxorubicin.
Antineoplastic Combined Chemotherapy Protocols↗
[Inhibitory effects of ligustrazine on the expression of intercellular cell adhesion molecule-1, vascular cell adhesion molecule-1 in human umbilical vein endothelial cells induced by preeclamptic plasma].
OBJECTIVE: To determine whether plasma from preeclamptic women induces expression of intercellular cell adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) on cultured endothelial cells, and the effects of ligustrazine (LTZ) on the expression of ICAM-1, VCAM-1. METHODS: Human umbilical vein endothelial cells (HUVEC) were isolated by collagenase mixed with trypsin. LTZ was added to HUVEC monolayers grown to confluency on 96-well microplates for 30 minutes. Then HUVEC were incubated with medium containing 20% plasma (volume/volume) either from women with preeclampsia or normotensive pregnancy or nonpregnant women. ICAM-1, VCAM-1 expression was determined after 16 hours of exposure by an enzyme-linked immunosorbent assay (ELISA) technique performed on the cell monolayer. RESULTS: There was a statistically significant increase in ICAM-1, VCAM-1 expression in the endothelial cells exposed to preeclamptic and nonpregnant plasma compared with those exposed to normotensive plasma. Pretreatment with LTZ could reduce the expression of ICAM-1 exposed to preeclamptic plasma, and reduce the expression of VCAM-1 exposed to any of the three sources of plasma. CONCLUSIONS: Preeclamptic plasma induces ICAM-1 and VCAM-1 expression in HUVEC in vitro. Ligustrazine may inhibit the upregulation effects of ICAM-1 and VCAM-1 expression induced by preeclamptic plasma.
Adult↗
[Study on smoking pattern and related factors among residents aged over 15 years in Guangdong province].
OBJECTIVE: To investigate the prevalence of smoking and related factors among residents aged over 15 years in Guangdong province. METHODS: Sampling survey, descriptive analysis and nonconditional logistic regression. RESULTS: Rates on general smoking, current smoking, regular smoking and heavy smoking among male residents aged over 15 years were 70.03%, 66.57%, 65.16% and 35.47% respectively and those among females were 3.04%, 2.67%, 2.54% and 1.12% respectively. There was significant difference between sex distribution. 86.71% of the male smokers started smoking at 15 to 29 years old, while the age distribution of noset of smoking among females was more scattered. Main reasons of starting smoking were to experience with social pressure and getting rid of feelings of fatigue. Tobacco products they often smoked included filter tip cigarette, handmade cigarette or dry cigarette. 52.42% of the smokers claimed that they often smoked in public places. 66.7% of the residents believed that smoking was either no harm or just minor while, 35.5% of them believed that smoking could get rid of fatigue and enhance the efficiency of work. Sex, age, occupation, marriage status and knowledge about the harm of smoking to health were factors related to smoking. CONCLUSION: Smoking has laid great harm to the health of residents in Guangdong province. Health education, stopping smoking in public places and no advertisement of cigarette under the management of laws are the best way to control the harm of smoking.
Adolescent↗
[Tissue culture and rapid propagation of Aloe arborescens].
Tissue culture and rapid propagation of Aloe arborescens have been studied. The main results are as follows: the optimum medium for cluster shoots induction is MS + 6-BA 3.0 mg/L + NAA 0.2 mg/L; for cluster shoots propagation is MS + 6-BA 2.0 mg/L + NAA 0.2 mg/L; for roots induction is 1/2 MS + NAA 0.5 mg/L. The survival rate of the tube plantlets is 100% in the transplanting. Cutting down the cost of medium in large scale of production have been studied also.
Aloe↗
[The muscarinic receptor subtype study of the action on lowering IOP of cholinomimetic drugs].
PURPOSE: Clarify the relationship between lowering intraocular pressure (IOP) action of cholinomimetic drugs and muscarinic receptor subtypes. METHODS: Measuring rabbit IOP with gas driving ophthalmotonometer, measuring size of pupil with pupil rule and measuring contraction of rabbit iris by iris experiment in vitro. Figuring out pD2 of cholinomimetic drugs and pA2 of the antagonists of muscarinic receptor subtypes. RESULTS: The order of effect on lowering IOP and miosis of cholinomimetic drugs is Erycibele Alkaloid > Aceclidine > Pilocarpine and the order of effect on constracting iris is Erycibele Alkaloid > Pilocarpine > Aceclidine. The sequence of antagonistic effect of subtype antagonists is 4-DAMP(M3) > Pirenzepine(M1) > Gallamine(M2). CONCLUSION: Effect cholinomimetics on lowing IOP and miosis is primary mediated by M3 receptor, next by M1 receptor and has little relation with M2 receptor.
Animals↗
Migration of Polystyrene Latex Particle Bands in Density-Gradient Electrophoresis.
Electrophoretic migration of sulfated polystyrene latex particle bands was investigated in a density-gradient electrophoresis apparatus. The bands spread with time, and their velocity was found to depend on particle concentration and to decrease during the initial stages of electrophoresis. A change in pH during electrophoresis occurred, and this change may have caused variations in band velocity. Copyright 1999 Academic Press.
Journal Article↗
High-performance liquid chromatography separation and quantitation of ofloxacin enantiomers in rat microsomes.
A sensitive, simple and accurate method for determination of enantiomers of ofloxacin in microsomal incubates was developed by chiral ligand-exchange RP-HPLC with fluorescence detection to examine stereoselective metabolism of ofloxacin in the glucuronidation process. The C18 stationary phase was used as analytical column. The solution of chiral mobile phase additive was made up of 6 mM L-phenylalamine mixed with 3 mM CuSO4 in water. Mobile phase consisted of the solution of chiral mobile phase additive-methanol (86:14). The fluorescence detector was operated at lambda(ex) 330 nm and lambda(em) 505 nm. The flow-rate of mobile phase was set at 1.0 ml/min. The achiral ODS column offers good separation of the two enantiomers in less than 25 min. The recovery of the assay was 97.9+/-6.1% (n=10) for S-ofloxacin and 99.6+/-6.0% (n = 10) for R-ofloxacin. The method provides a high sensitivity and good precision (RSD<10%). The LOD was 0.6 microM for both enantiomers and the LOQ was 5.70+/-0.45 microM (n=8) for S-ofloxacin and 5.66+/-0.47 microM (n=8) for R-ofloxacin. The standard curves showed excellent linearity over the concentration range 5.5-2078 microM for S-(-)-ofloxacin and R-(+)-ofloxacin. The enantioselective method developed has been applied to determine the stereoselectivity of glucuronidation metabolism of ofloxacin optical isomers in rat liver microsomes.
Animals↗
Stereoselective determination of fenfluramine enantiomers in rat liver microsomal incubates.
An enantioselective assay for l- and d-fenfluramine in rat liver microsomal incubates was developed. The method involves extraction of fenfluramine from the microsomal incubates, and formation of fenfluramine diastereomeric derivatives with the chiral reagent S-(-)-N-trifluoroacetyl prolyl chloride. Separation and quantitation of the diastereomeric fenfluramine derivatives are carried out by a capillary gas chromatographic system with flame ionization detection. The assay is linear from 1 to 50 microg/ml for each enantiomer. The analytical method affords average recoveries of 92.28 and 96.44% for l- and d-fenfluramine, respectively. The limits of detection and quantitation for the method are 0.1 and 1.0 microg/ml for the l- and d-fenfluramine isomers, respectively. The reproducibility of the assay was <10% (RSD). The method allowed study of the depletion of l- and d-fenfluramine in rat liver microsomal incubates. The stereoselectivity of fenfluramine phase I metabolism was observed.
Animals↗