A transgenic maize event ZD12-6 expressing a Bacillus thuringiensis (Bt) fusion protein Cry1Ab/Cry2Aj and a modified 5-enolpyruvylshikimate-3-phosphate synthase (EPSPS) protein G10 was characterized and evaluated. Southern blot analysis indicated that ZD12-6 is a single copy integration event. The insert site was determined to be at chromosome 1 by border sequence analysis. Expression analyses of Bt fusion protein Cry1Ab/Cry2Aj and the EPSPS protein G10 suggested that they are both expressed stably in different generations. Insect bioassays demonstrated that the transgenic plants are highly resistant to Asian corn borer (Ostrinia furnacalis), cotton boll worm (Helicoverpa armigera), and armyworm (Mythimna separata). This study suggested that ZD12-6 has the potential to be developed into a commercial transgenic line.
3-Phosphoshikimate 1-Carboxyvinyltransferase/metabolism* ; Animals ; Bacillus thuringiensis Toxins ; Bacterial Proteins/metabolism* ; China ; Disease Resistance/genetics* ; Drug Resistance/genetics* ; Endotoxins/metabolism* ; Gene Expression Profiling ; Glycine/chemistry* ; Hemolysin Proteins/metabolism* ; Insecta ; Plant Diseases/prevention & control* ; Plants, Genetically Modified/genetics* ; Zea mays/genetics* ; Glyphosate

Peptide nucleic acid (PNA) is a DNA surrogate in which the phosphate deoxyribose backbone of DNA is replaced by repeating N-(2-aminoethyl)glycine units. PNA can hybridize to the complementary DNA and RNA with higher affinity than their oligonucleotide counterparts. This character of PNA not only makes it a new tool for the studies of molecular biology but also the potential candidate for gene-targeting drugs. The non-ionic backbone of PNA leads to stable hybrids with the nucleic acids, but at the same time, the neutral backbone results in poor cellular uptake. To address this problem, studies on modified PNA progress rapidly in recent years. We reviewed literature reports combined with our study about the delivery methods, including backbone modified PNA and PNA-ligand conjugates, and the cellular uptake of modified PNA. In addition, we summarized the problems and future prospect of the cellular delivery of modified PNA.
DNA, Complementary ; Drug Delivery Systems ; Glycine ; analogs & derivatives ; Humans ; Nucleic Acid Hybridization ; Oligonucleotides ; Peptide Nucleic Acids ; chemistry ; RNA

The purpose of this study is to explore depression metabolic markers in rat hippocampus and to investigate the anti-depressant effect of genipin and its mechanisms using nuclear magnetic resonance (NMR) metabonomics. Chronic unpredictable mild stress (CUMS) procedure was conducted to establish the depressive rat model. At the beginning of the third week, genipin low dose (25 mg x kg(-1)), middle dose (50 mg x kg(-1)), high dose (100 mg x kg(-1)), and venlafaxine (50 mg x kg(-1)) were given to the CUMS rats separately once daily for two weeks except control and model groups. Rat hippocampus was analyzed by 1H NMR based metabonomics after drug administration for 2 weeks. Significant differences in the metabolic profile of rat hippocampus of the CUMS treated group and the control group were observed with metabolic effects of CUMS including decreasing in glycine and N-acetylaspartate, increasing in inositol, glutamate, lactate, glutamine, taurine and alanine. Genipin showed ideal antidepressive effects at a dose of 50 mg x kg(-1) in rats, decrease of inositol, glutamate, lactate, alanine were observed, while glycine and N-acetylaspartate were increased. Important influence has been found on normal nervous system function of these significant changed metabolites, which suggests that the antidepressant effect of genipin may be played by enhancing the activity of neurons in hippocampus, repairing and improving the function of the neuron. The metabonomics approach is an effective tool for the investigation of the anti-depressant effect and pharmacologic mechanisms of genipin.
Alanine ; metabolism ; Animals ; Antidepressive Agents ; isolation & purification ; pharmacology ; Aspartic Acid ; analogs & derivatives ; metabolism ; Behavior, Animal ; drug effects ; Chronic Disease ; Depression ; drug therapy ; metabolism ; physiopathology ; Gardenia ; chemistry ; Glutamic Acid ; metabolism ; Glycine ; metabolism ; Hippocampus ; drug effects ; metabolism ; Inositol ; metabolism ; Iridoids ; isolation & purification ; pharmacology ; Lactic Acid ; metabolism ; Magnetic Resonance Spectroscopy ; Male ; Metabolomics ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley

We investigated whether glyphosate influences the cellular toxicity of the surfactants TN-20 and LN-10 on the mouse fibroblast-like cells, alveolar epithelial cells, and a heart cell line. The cytotoxicity of TN-20 and LN-10 (0.4-100 microM), in the presence or absence of glyphosate was determined by assessing membrane integrity. TN-20 toxicity was significantly lower in the presence of 50 microM glyphosate for the fibroblast-like cell (6.25 microM; 3.9% +/- 3.4% vs -4.8% +/- 0.7%), for the alveolar cells (0.78 microM; 5.7% +/- 0.9% vs 0.1% +/- 0.6%), and for the heart cell line (25.0 microM; 7.9% +/- 3.0% vs 19.4% +/- 0.7%) compared to that of TN-20 alone. The cellular toxicity of LN-10 towards the fibroblast-like cells was found to be increased in the presence of 50 microM glyphosate when LN-10 concentrations of 50 microM (31.3% +/- 3.9% vs 19.2% +/- 0.9%) and 100 microM (62.1% +/- 3.4% vs 39.0% +/- 0.7%) were compared to that of LN-10 alone. These results suggest that the mixture toxicity may be a factor in glyphosate-surfactant toxicity in patients with acute glyphosate herbicide intoxication.
Animals ; Cell Line ; Cell Survival/drug effects ; Glycine/*analogs & derivatives/chemistry/toxicity ; Herbicides/chemistry/*toxicity ; Mice ; Polyethylene Glycols/*chemistry ; Surface-Active Agents/*chemistry

OBJECTIVETo evaluate the effect of decoction of turtle shell for anti-fibrosis combined with stronger neo-minophagen C on the indices of hepatic fibrosis in chronic hepatitis B.

METHODThe 94 cases of chronic viral hepatitis B patients were randomly divided into two groups. The treatment group was treated with stronger neo-minophagen C 100 mL dissolved in 10% dextrose 250 ml once a day intravenously, combined with decoction of turtle shell for anti-fibrosis one powder daily. And the control group was treated with stronger neo-minophagen C alone, 3 months as a course. Liver fibrosis indexes and liver function index were tested for two groups of patients before and after the treatment.

RESULTBoth the difference of liver fibrosis indexes between the treatment group and the control group and before and after the treatment in the treatment group had statistical significance (P < 0.01). Both the difference of liver function index between the treatment group and the control group and before and after the treatment in the treatment group had statistical significance (P < 0.01). The basic cure rate and total effective rate were 40% and 84.0% in the treatment group and 27.27% and 86.18% in the control group respectively with significant difference. The treatment group was superior to control group in the mean size of diameter of portal vein and the thickness of spleen (P < 0.01).

CONCLUSIONDecoction of turtle shell for anti-fibrosis combined with stronger neo-minophagen C could significantly improve the clinical efficacy and the liver fibrosis indexes and liver function index in chronic hepatitis B.

Adult ; Aged ; Alanine Transaminase ; blood ; Animal Shells ; chemistry ; Animals ; Aspartate Aminotransferases ; blood ; Cysteine ; administration & dosage ; therapeutic use ; Drug Combinations ; Drug Therapy, Combination ; Female ; Glycine ; administration & dosage ; therapeutic use ; Glycyrrhetinic Acid ; administration & dosage ; analogs & derivatives ; therapeutic use ; Hepatitis B, Chronic ; complications ; Humans ; Liver Cirrhosis ; blood ; drug therapy ; etiology ; Male ; Medicine, Chinese Traditional ; methods ; Middle Aged ; Tissue Extracts ; therapeutic use ; Treatment Outcome ; Turtles ; gamma-Glutamyltransferase ; blood

OBJECTIVETo research the content changes of excitatory neurotransmitter and inhibitory neurotransmitter in corpus striatum of rats after single-used borneol and combining it with diazepam in hope of comprehending the activity of borneol on central nervous system and to observe whether borneol could increase the penetration of other drugs into the brain.

METHODThe content of four amino acids neurotransmitters in corpus striatum of rats were sampled by brain microdialysis technology at different time after administration and were determined by RP-HPLC which involved pre-column derivation with orthophthaladehyde (OPA), using phosphate gradient elution and fluorescence detection to detect the content of excitatory neurotransmitter aspartate (Asp), glutamate (Glu) and inhibitory neurotransmitter glycine (Gly), gamma-aminobutyric acid (GABA) in standards and samples and carry on statistical analysis.

RESULTThe content of both Gly and GABA in corpus striatum of rats with borneol increased significantly, compared with diazepam group (P < 0.05), while Asp and Glu showed no significant difference.

CONCLUSIONBorneol can improve permeability of diazepam through BBB.

Animals ; Aspartic Acid ; analysis ; Blood-Brain Barrier ; Bornanes ; administration & dosage ; pharmacology ; Corpus Striatum ; chemistry ; drug effects ; Diazepam ; administration & dosage ; pharmacology ; Glutamic Acid ; analysis ; Glycine ; analysis ; Male ; Neurotransmitter Agents ; analysis ; Rats ; Rats, Sprague-Dawley ; gamma-Aminobutyric Acid ; analysis

OBJECTIVETo establish a method to determine the underivatized glycine (Gly) and proline (Pro) in vinegar turtle shell.

METHODAn HPLC-ELSD method was conducted on a Prevail C18 column (4.6 mm x 250 mm, 5 microm) with the mobile phase of acetonitrile and 0.7% trifluoroacetic acid solution (containing 5.0 mmol x L(-1) heptafluorobutyric acid), and elution time was 15 min.

RESULTThe calibration curves were showed good linearity within the concentration range of 0.14-0.6 g x L(-1). The average recoveries were 101.2% and 102.5%, and RSD were 1.9% and 2.5%, respectively.

CONCLUSIONSince this method needs neither the special amino acid analyzer nor derivation of amino acid., it is efficient, simple and accurate., which could be used for quality control of vinegar turtle shell.

Animal Shells ; chemistry ; Animals ; Chromatography, High Pressure Liquid ; Glycine ; analysis ; Proline ; analysis ; Quality Control ; Reference Standards ; Reproducibility of Results ; Turtles

To research the structure-activity relationship (SAR) of glycinamide-bearing compounds that used as inhibitors of dipeptidyl peptidase IV (DPP-IV), P32/98 and compound A were chosen as the leading compounds, heterocycles containing nitrogen atom were introduced to form amide, and different residues on a-position of carbonyl were designed. The nineteen designed compounds were synthesized by a simple route and were evaluated as inhibitors of DPP-IV. All of the structures were characterized by 1H NMR and HRMS. The preliminary SAR result was obtained.
Dipeptidyl Peptidase 4 ; metabolism ; Dipeptidyl-Peptidase IV Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Glycine ; analogs & derivatives ; chemistry ; Magnetic Resonance Spectroscopy ; methods ; Molecular Structure ; Piperazines ; chemistry ; pharmacology ; Structure-Activity Relationship

OBJECTIVETo investigate the correlation effects between single or combined administration of Calculus Bovis or zolpidem and changes of inhibitive neurotransmitter in rat striatum corpora.

METHODSampling from rat striatum corpora was carried out through microdialysis. The content of two inhibitive neurotransmitters in rat corpus striatum- glycine (Gly) and gama aminobutyric acid (GABA), was determined by HPLC, which involved pre-column derivation with orthophthaladehyde, reversed-phase gradient elution and fluorescence detection.

RESULTGABA content of rat striatum corpora in Calculus Bovis group was significantly increased compared with saline group (P < 0.01). GABA content of zolpidem group and Calculus Boris plus zolpidem group were increased largely compared with saline group as well (P < 0.05). GABA content of Calculus Bovis group was higher than combination group (P < 0.05). GABA content of zolpidem group was not significantly different from combination group. Gly content of Calculus Bovis or zolpidem group was markedly increased compared with saline group or combination group (P < 0.05).

CONCLUSIONContents of two inhibitive neurotransmitters in rat striatum corpora were all significantly increased in Calculus Bovis group, zolpidem group and combination group. The magnitude of increase was lower in combination group than in Calculus Bovis group and Zolpidem group, suggesting that Calculus Bovis promoted encephalon inhibition is more powerful than zolpidem. The increase in two inhibitive neurotransmitters did not show reinforcing effect in combination group, suggesting that Calculus Bovis and zolpidem may compete the same receptors. Therefore, combination of Calculus Bovis containing drugs and zolpidem has no clinical significance. Calculus Bovis shouldn't as an aperture-opening drugs be used for resuscitation therapy.

Animals ; Calculi ; chemistry ; Cattle ; Chromatography, High Pressure Liquid ; Corpus Striatum ; drug effects ; metabolism ; Glycine ; metabolism ; Male ; Medicine, Chinese Traditional ; Neurotransmitter Agents ; metabolism ; Pyridines ; administration & dosage ; pharmacology ; Rats ; Rats, Wistar ; gamma-Aminobutyric Acid ; metabolism

This study was undertaken to explore and compare the radiochemical behavior and biological property of antisense oligonucleotide (ASON) labeled with Technetium-99m using two methods: N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline (NHS-MAG3) versus hydrazino nicotinamide derivative (SHNH). After SHNH and NHS-MAG3 were synthesized, ASON was labeled with Technetium-99m using SHNH and NHS-MAG3 as a bifunctional chelator, separately. The stability in vivo and in vitro, the combination with plasma albumen of rabbit, the biodistribution in BALB/ C mice and the HT29 cellular uptake were compared between labeled compound 99mTc-SHNH-ASON, using SHNH as a bifunctional complex reagent, and 99mTc-MAG3-ASON, using NHS-MAG3 as a bifunctional chelator. The results revealed that the labeling rate and the stability of 99mTc-MAG3-ASON were evidently higher than that of 99mTc-SHNH-ASON (P < 0.05), the combination rate of 99mTc-MAG3-ASON with plasma albumen was markedly lower than that of 99mTc-SHNH-ASON (P < 0.05); the biodistribution of 99mTc-MAG3-ASON was markedly lower than that of 99mTc-SHNH-ASON in blood, heart, stomach and intestines (P < 0.05), slightly lower than that of 99mTc-SHNH-ASON in liver and spleen (P > 0.05), and markedly higher than that of 99mTc-SHNH-ASON in kidney (P < 0.05); the HT29 cellular uptake rates of 99mTc-MAG3-ASON was markedly higher than that of 99mTc-SHNH-ASON (P < 0.05). Therefore, the radiochemical behavior and biological property of 99mTc-MAG3-ASON labeled using NHS-MAG3 is better than that of 99mTc-SHNH-ASON labeled using SHNH.
Animals ; Colonic Neoplasms ; metabolism ; pathology ; Glycine ; analogs & derivatives ; chemistry ; pharmacokinetics ; Humans ; Isotope Labeling ; methods ; Mice ; Mice, Inbred BALB C ; Niacinamide ; analogs & derivatives ; chemistry ; pharmacokinetics ; Oligonucleotides, Antisense ; chemistry ; pharmacokinetics ; Radiopharmaceuticals ; chemical synthesis ; pharmacokinetics ; Succinimides ; chemistry ; pharmacokinetics ; Technetium Tc 99m Mertiatide ; chemistry ; pharmacokinetics ; Tumor Cells, Cultured