1.Discussion of the application of three-point interaction principle to the phenylglycine racemic compound in IR spectrometry and its enantiomers separation in HPLC.
Yi SHEN ; Da-nian YI ; Ji-ning LIU
Acta Pharmaceutica Sinica 2002;37(8):636-638
AIMTo discuss the relationship between the three-point interaction principle in the stereoselective separation of chromatography and applying this principle to survey the infrared spectrometry of racemate.
METHODSIn proving the applicability of the three-point interaction principal in IR spectrometry, a special case was found that phenylglycine did not obtain enantioselective separation on the chiral column but its IR spectrometry still obey this principle and explained such special case by experiment.
RESULTSAfter an equal quantity of solid crystal of d-phenylglycine and l-phenylglycine were mixed and ground for several minutes, they transformed to racemic compound. X-powder diffraction also confirmed this fact.
CONCLUSIONThe three-point principle was relatively reliable when it was used in the enantioselective chromatography separation and the IR spectrometric analysis. The reason of the fact that phenylglycine was not separated by chiral column can be explained by the fact that the acting force between the three polarity groups in the enantiomers is so strong that they can not form the instantaneous diastereoisomer with the chiral column, it was agreeable with the phenomenon that racemic mixture easily became racemic compound only by simply grinding the mixture in IR spectrometric experiment.
Chromatography, High Pressure Liquid ; Glycine ; analogs & derivatives ; analysis ; chemistry ; Orosomucoid ; chemistry ; Spectrophotometry, Infrared ; Stereoisomerism
2.In Vitro Cytotoxic Effect of Glyphosate Mixture Containing Surfactants.
Ho Yeon SONG ; Young Hee KIM ; Su Jin SEOK ; Hyo Wook GIL ; Sae Yong HONG
Journal of Korean Medical Science 2012;27(7):711-715
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
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Cell Line
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Cell Survival/drug effects
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Glycine/*analogs & derivatives/chemistry/toxicity
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Herbicides/chemistry/*toxicity
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Mice
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Polyethylene Glycols/*chemistry
;
Surface-Active Agents/*chemistry
3.Evaluation of correlation between gelatin crosslinking indicators and influence factors.
Jian-ping LIU ; Xu MA ; Jia-bi ZHU
Acta Pharmaceutica Sinica 2005;40(3):279-284
AIMTo evaluate the correlation between the swelling equilibrium quantity (Seq), dissolution rate and amino group content which were used to estimate the degree of gelatin crosslinking, and the factors which influence the crosslinking, and to investigate the crosslinking mechanism of delayed dissolution of soft capsules.
METHODSThe swelling equilibrium quantity, dissolution rate and amino group content of formaldehyde-crosslinked capsule shells were determined. Gelatin structure was analyzed by means of DSC.
RESULTSA good lineal relativity was found between the swelling equilibrium quantity, dissolution rate and amino group content (r = 0.9953-0.9985). The Seq of capsule shells was influenced by high temperature, lighting and some additives. Glycine and sodium pyrosulfite might retard the decrease of Seq of capsule shells.
CONCLUSIONThe swelling equilibrium quantity, dissolution rate and amino group content exhibited the same rule in gelatin crosslinking extent. High temperature, lighting and some additives might induce gelatin crosslinking. Antioxidant such as glycine and sodium pyrosulfite might retard the crosslinking.
Amino Acids ; analysis ; Capsules ; Cross-Linking Reagents ; chemistry ; Drug Compounding ; methods ; Drug Stability ; Formaldehyde ; chemistry ; Gelatin ; chemistry ; Glycine ; Humidity ; Lighting ; Pharmaceutic Aids ; chemistry ; Solubility ; Temperature
4.Cellular delivery of modified peptide nucleic acids: a review.
Chundong LIU ; Jianhua WANG ; Fang ZENG
Chinese Journal of Biotechnology 2016;32(3):292-305
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
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Drug Delivery Systems
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Glycine
;
analogs & derivatives
;
Humans
;
Nucleic Acid Hybridization
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Oligonucleotides
;
Peptide Nucleic Acids
;
chemistry
;
RNA
5.Determination of underivatized glycine and proline in vinegar turtle shell by HPLC-ELSD.
Xinyu WANG ; Xiaomei TAN ; Mingze GAO ; Jinlong PENG
China Journal of Chinese Materia Medica 2011;36(15):2107-2109
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
6.Effect of hypocapnia on extracellular glutamate and glycine concentrations during peri-ischemic period in the rabbit hippocampus.
Kyu Taek CHOI ; Jung Kil CHUNG ; Chun Sik KWAK ; Hae Kyu KIM
Journal of Korean Medical Science 1994;9(5):394-401
Glutamate (GLU) is a neurotransmitter. Massive release of GLU and glycine (GLY) into the brain's extracellular space may be triggered by ischemia, and may result in acute neuronal lysis or delayed neuronal death. The aim of this study was to evaluate the possible relationship between hyperventilation and the level of GLU and GLY during brain ischemia. Rabbits were anesthetized with halothane and oxygen. Group 1 was allowed to hyperventilate (PaCO2 25-35 mmHg). PaCO2 was maintained throughout the study. Group 2 was a normal control group that maintained normocapnia. Two global cerebral ischemic episodes were produced. Microdialysate was collected during the peri-ischemic and reperfusion periods from the dorsal hippocampus. GLU and GLY concentrations were determined using high-performance liquid chromatography. In the control group, GLU and GLY were significantly elevated during each episode of ischemia; these levels returned to baseline within 10 minutes after reperfusion. In contrast, in the hyperventilation group GLU and GLY concentrations increased during ischemia, but they were not statistically significant. We were able to demonstrate that hypocapnia during periischemic period lowered extracellular GLU and GLY concentrations. These results can explain a part of the protective action of hypocapnia during cerebral ischemia.
Animal
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Brain Ischemia/*metabolism
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Glutamic Acid/*analysis
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Glycine/*analysis
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Hippocampus/*chemistry
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Hyperventilation/metabolism
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Hypocapnia/*metabolism
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Potassium/metabolism
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Potassium Channels/physiology
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Rabbits
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Support, Non-U.S. Gov't
7.A Korean Family of Hypokalemic Periodic Paralysis with Mutation in a Voltage-gated Calcium Channel (R1239G).
June Bum KIM ; Kyung Yil LEE ; Jae Kyun HUR
Journal of Korean Medical Science 2005;20(1):162-165
Hypokalemic periodic paralysis (HOPP) is a rare disease characterized by reversible attacks of muscle weakness accompanied by episodic hypokalemia. Recent molecular work has revealed that the majority of familial HOPP is due to mutations in a skeletal muscle voltage-dependent calcium-channel: the dihydropyridine receptor. We report a 13-yr old boy with HOPP from a family in which 6 members are affected in three generations. Genetic examination identified a nucleotide 3705 C to G mutation in exon 30 of the calcium channel gene, CACNA1S. This mutation predicts a codon change from arginine to glycine at the amino acid position #1239 (R1239G). Among the three known mutations of the CACNA1S gene, the R1239G mutation was rarely reported. This boy and the other family members who did not respond to acetazolamide, showed a marked improvement of the paralytic symptoms after spironolactone treatment.
Acetazolamide/pharmacology
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Adolescent
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Arginine/chemistry
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Calcium Channels/chemistry/*genetics
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Codon
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Exons
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Family Health
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Female
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Glycine/chemistry
;
Humans
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Hypokalemia/metabolism
;
Hypokalemic Periodic Paralysis/*diagnosis/*genetics
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Korea
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Male
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Muscle, Skeletal/metabolism
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Mutation
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Pedigree
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Protein Structure, Tertiary
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Sequence Analysis, DNA
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Spironolactone/pharmacology
8.Design, synthesis and in vitro activity of glycinamide-bearing compounds as DPP-IV inhibitors.
Bei HAN ; Yi HUAN ; Zi-Yun LIN ; Peng LI ; Zhu-Fang SHEN ; Da-Li YIN ; Hai-Hong HUANG
Acta Pharmaceutica Sinica 2010;45(11):1379-1384
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
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metabolism
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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
9.A comparison on radiochemical behavior and biological property of antisense oligonucleotide labeled with technetium-99m by two methods: NHS-MAG3 versus SHNHP.
Yunchun LI ; Tianzhi TAN ; Jianguo ZHENG ; Chun ZHANG
Journal of Biomedical Engineering 2008;25(4):889-902
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
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Colonic Neoplasms
;
metabolism
;
pathology
;
Glycine
;
analogs & derivatives
;
chemistry
;
pharmacokinetics
;
Humans
;
Isotope Labeling
;
methods
;
Mice
;
Mice, Inbred BALB C
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Niacinamide
;
analogs & derivatives
;
chemistry
;
pharmacokinetics
;
Oligonucleotides, Antisense
;
chemistry
;
pharmacokinetics
;
Radiopharmaceuticals
;
chemical synthesis
;
pharmacokinetics
;
Succinimides
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chemistry
;
pharmacokinetics
;
Technetium Tc 99m Mertiatide
;
chemistry
;
pharmacokinetics
;
Tumor Cells, Cultured
10.Co-existence of calcium-binding proteins and gamma-aminobutyric acid or glycine in neurons of the rat medullary dorsal horn.
Wen WANG ; Sheng-xi WU ; Yun-qing LI
Chinese Medical Journal 2004;117(3):430-433
BACKGROUNDWe investigated the co-expression of calbindin-D28k (CB), calretinin (CR) and parvalbumin (PV, a combination of the three is referred to as CaBPs) with gamma-aminobutyric acid (GABA) or glycine in neurons of the rat medullary dorsal horn (MDH).
METHODSImmunofluorescence histochemical double-staining for CaBPs and GABA or glycine was performed on the sections from rat MDH.
RESULTSCB-, CR-, PV-, GABA- and glycine-like immunoreactive (LI) neurons were differentially observed in all layers of the MDH, but particularly in lamina II. Neurons that exhibited immunoreactivity for both CaBPs and GABA or glycine were also observed mainly in lamina II. A few of them were found in laminae I and III. The percentages of neurons which co-expressed CB/GABA or CB/glycine out of the total numbers of CB- and GABA-LI neurons or CB- and glycine-LI neurons were 5.3% and 12.1% or 4.1% and 10.0%, respectively. The ratios of CR/GABA or CR/glycine co-existing neurons out of the total numbers of CR- and GABA-LI neurons or CR- and glycine-LI neurons were 5.8% and 7.6% or 4.4% and 7.1%, respectively. The rates of PV/GABA or PV/glycine co-localized neurons out of the total numbers of PV- and GABA-LI neurons or PV- and glycine-LI neurons were 11.1% and 5.1% or 9.9% and 5.1%, respectively.
CONCLUSIONThe results indicate that some neurons in the MDH contain both CaBPs and GABA or glycine.
Animals ; Calbindin 1 ; Calbindin 2 ; Calbindins ; Calcium-Binding Proteins ; analysis ; Fluorescent Antibody Technique ; Glycine ; analysis ; Immunohistochemistry ; Medulla Oblongata ; cytology ; Parvalbumins ; analysis ; Posterior Horn Cells ; chemistry ; Rats ; S100 Calcium Binding Protein G ; analysis ; gamma-Aminobutyric Acid ; analysis