OBJECTIVETo develop a method for determination of voglibose contents in its tablets by high-performance liquid chromatography-mass spectrometry (HPLC-MS).

METHODSThe measurements were carried out on an Agilent ZORBAX Eclipse Plus C18 column (2.1×150mm 3.2μm) with a temperature of 40 degrees Celsius. A mixture of methanol and water (2:3,v/v) was used as a mobile phase at a flow rate of 0.25 ml/min. Voglibose was detected in an electrospray ionization (ESI) mode with MRM.

RESULTSThe calibration curves of voglibose showed good linearity in a range of 1.5804-2.6340 μg/ml (r=0.9990). The average recovery was 100.2% with RSD of 1.37% (n=6) for m/z 268.2/74.2.Linearity was obtained with r=0.9976 and the average recovery was 99.3% with RSD of 1.78% (n=6) for m/z 268.2/92.2.

CONCLUSIONHPLC-MS method is accurate,reproducible and can be used for quality control of voglibose tablets.

Chromatography, High Pressure Liquid ; methods ; Inositol ; analogs & derivatives ; analysis ; Mass Spectrometry ; methods ; Tablets

BACKGROUNDIn vivo proton magnetic resonance spectroscopy (MRS) provides a noninvasive method of examining a wide variety of cerebral metabolites in both healthy subjects and patients with various brain diseases. Absolute metabolite concentrations have been determined using external and internal standards with known concentrations. When an external standard is placed beside the head, variations in signal amplitudes due to B1 field inhomogeneity and static field inhomogeneity may occur. Hence an internal standard is preferable. The purpose of this study was to quantitatively analyze the metabolite concentrations in normal adult brains and gliomas by in vivo proton MRS using the fully relaxed water signal as an internal standard.

METHODSBetween January 1998 and October 2001, 28 healthy volunteers and 16 patients with gliomas were examined by in vivo proton MRS. Single-voxel spectra were acquired using the point-resolved spectroscopic pulse sequence with a 1.5 T scanner (TR/TE/Ave = 3000 ms/30 ms/64).

RESULTSThe calculated concentrations of N-acetyl-asparatate (NAA), creatine (Cre), choline (Cho), and water (H2O) in the normal hemispheric white matter were (23.59 +/- 2.62) mmol/L, (13.06 +/- 1.8) mmol/L, (4.28 +/- 0.8) mmol/L, and (47,280.96 +/- 5414.85) mmol/L, respectively. The metabolite concentrations were not necessarily uniform in different parts of the brain. The concentrations of NAA and Cre decreased in all gliomas (P < 0.001). The ratios of NAA/Cho and NAA/H2O showed a significant difference between the normal brain and gliomas, and also between the high and low grades (P < 0.001).

CONCLUSIONSQuantitative analysis of in vivo proton MR spectra using the fully relaxed water signal as an internal standard is useful. The concentrations of NAA and the ratios of NAA/H2O and NAA/Cho conduce to discriminating between the glioma and normal brain, and also between the low-grade glioma and high-grade glioma.

Adult ; Aspartic Acid ; analogs & derivatives ; metabolism ; Brain ; metabolism ; Choline ; metabolism ; Creatine ; metabolism ; Female ; Glioma ; metabolism ; Glycine ; metabolism ; Humans ; Inositol ; metabolism ; Magnetic Resonance Spectroscopy ; Male

Three compounds were isolated from the extract of Taxus cuspidta Sibe et Zucc with the column chromatography on silica gel and preparative HPLC methods. Their structures were identified according to the physicochemical properties and spectral analysis, and they were identified as (E)-1-methoxy-2-O-(p-coumaroyl)-myo-inositol (1), 2-deacetoxy-7beta, 9a, 10beta-trideacetyltaxinine J (2) and (3aS, 4aR, 6S, 8S, 8aS, 9R, 10R, 10aS)-benz[f]azulene-6, 8, 9, 10 (3H)-terol, 3a, 4, 4a, 5, 6, 7, 8, 8a, 9, 10-decahydro-10a-(1-hydroxyl-1-methylethyl)-1, 8a-dimethyl-5-methylene (3). Among them, compound 1 was a new compound, and compounds 2, 3 were two novel natural products.
Azulenes ; chemistry ; isolation & purification ; Coumarins ; chemistry ; isolation & purification ; Inositol ; analogs & derivatives ; chemistry ; isolation & purification ; Molecular Structure ; Plants, Medicinal ; chemistry ; Taxoids ; chemistry ; isolation & purification ; Taxus ; chemistry

OBJECTIVE: To detect metabolic changes of bilateral frontal lobe in patients with multiple system atrophy (MSA) and cognitive dysfunction by 1H-proton magnetic resonance spectroscopy (1H-MRS).
 METHODS: N-acetylaspartate (NAA)/creatine(Cr), choline (Cho)/Cr, myoinositol (mI)/Cr in three sides of frontal lobe were detected by 1H-MRS in 48 healthy controls, 23 patients with MSA and cognitive dysfunction and 19 patients with MSA but without cognitive dysfunction.
 RESULTS: NAA/Cr of bilateral frontal lobes in patients with MSA and cognitive dysfunction was significantly decreased compared with MSA patients without cognitive dysfunction and healthy controls (P<0.05). mI/Cr of right frontal lobes was significantly increased in patients with MSA and cognitive dysfunction compared with healthy controls (P<0.05). There was a negative correlation between NAA/Cr of bilateral frontal lobes and duration while a positive correlation between NAA/Cr of bilateral frontal lobes and MoCA score in patients with MSA and cognitive dysfunction.
 CONCLUSION There is a decrease in NAA/Cr and an increase in mI/Cr in frontal lobes in patients with MSA and cognitive dysfunction, which may be associated with cognitive dysfunction in MSA patients.
Aspartic Acid ; analogs & derivatives ; metabolism ; Choline ; metabolism ; Cognition Disorders ; physiopathology ; Creatine ; metabolism ; Frontal Lobe ; metabolism ; Humans ; Inositol ; metabolism ; Multiple System Atrophy ; physiopathology ; Proton Magnetic Resonance Spectroscopy

An HPLC-UV method has been developed for the determination of valibose, miglitol, voglibose and acarbose, the four anti-diabetic drugs. The separation was accomplished successfully by using reversed phase chromatography (Prevail carbohydrate column, 250 mm x 4.6 mm, 5 microm) with a gradient acetonitrile-phosphate buffer solution (pH 8.0) at a wavelength of 210 nm. Furthermore, the method of a high-performance liquid chromatography coupled with ESI-MS in positive ionization mode has been established. These two methods were successfully applied to the assay and qualitative detection of four alpha-glucosidase inhibitors in the potential counterfeit anti-diabetic drugs.
1-Deoxynojirimycin ; analogs & derivatives ; analysis ; Acarbose ; analysis ; Chromatography, High Pressure Liquid ; methods ; Chromatography, Reverse-Phase ; Glycoside Hydrolase Inhibitors ; Hypoglycemic Agents ; chemistry ; Inositol ; analogs & derivatives ; analysis ; Spectrometry, Mass, Electrospray Ionization ; methods ; Spectrophotometry, Ultraviolet ; alpha-Glucosidases ; analysis

OBJECTIVETo investigate the correlation of neurochemical metabolism in hippocampus with memory function in young adult patients with first-episode depression.

METHODSTwenty patients with first-episode depression (patient group) and fifteen health subjects (control group) were enrolled in the study. The neurochemical metabolism, including the levels of N-acetylaspartate (NAA), Choline (Cho), Creatine (Cr), Myoinositol (mI) were measured by proton magnetic resonance spectroscope (1H-MRS) in bilateral hippocampus. Wechsler Memory Scale (WMS) were used to examine the memory function in both groups.

RESULTSThe memory quotient (89.15 ±6.62) of patient group was significantly lower than that of controls (P <0.01),the scores of long-term memory,short-term memory and immediate memory in patients were also lower than those of controls (P<0.05 or 0.01). In patient group, the ratio of NAA/Cr (1.34 ±0.08) in the left hippocampus was significantly lower than that of control group (P<0.01); and the ratio of mI/Cr in the bilateral hippocampus [(0.63 ±0.13) in left and (0.6 ±0.1) in right] was significantly higher than those in control group (P<0.05). In patient group,the ratio of NAA/Cr in the left hippocampus was positively correlated with WMS scores (P<0.01), and the ratio of mI/Cr in the left hippocampus was negatively correlated with WMS scores (P<0.05).

CONCLUSIONThe memory deficit and abnormal metabolism function of neuron cell in hippocampus coexist in young adult patients with first-episode depression, and the lower NAA/Cr and higher mI/Cr ratio in the left hippocampus may result in the memory deficit.

Adolescent ; Adult ; Aspartic Acid ; analogs & derivatives ; metabolism ; Case-Control Studies ; Creatine ; metabolism ; Depressive Disorder ; metabolism ; physiopathology ; Female ; Hippocampus ; metabolism ; Humans ; Inositol ; metabolism ; Magnetic Resonance Spectroscopy ; Male ; Memory ; Neuropsychological Tests ; Young Adult

We studied the efficacy and safety of acarbose in comparison with voglibose in type 2 diabetes patients whose blood glucose levels were inadequately controlled with basal insulin alone or in combination with metformin (or a sulfonylurea). This study was a 24-week prospective, open-label, randomized, active-controlled multi-center study. Participants were randomized to receive either acarbose (n=59, 300 mg/day) or voglibose (n=62, 0.9 mg/day). The mean HbA1c at week 24 was significantly decreased approximately 0.7% from baseline in both acarbose (from 8.43% +/- 0.71% to 7.71% +/- 0.93%) and voglibose groups (from 8.38% +/- 0.73% to 7.68% +/- 0.94%). The mean fasting plasma glucose level and self-monitoring of blood glucose data from 1 hr before and after each meal were significantly decreased at week 24 in comparison to baseline in both groups. The levels 1 hr after dinner at week 24 were significantly decreased in the acarbose group (from 233.54 +/- 69.38 to 176.80 +/- 46.63 mg/dL) compared with the voglibose group (from 224.18 +/- 70.07 to 193.01 +/- 55.39 mg/dL). In conclusion, both acarbose and voglibose are efficacious and safe in patients with type 2 diabetes who are inadequately controlled with basal insulin. (ClinicalTrials.gov number, NCT00970528)
Acarbose/adverse effects/*therapeutic use ; Blood Glucose ; Diabetes Mellitus, Type 2/blood/*drug therapy ; Enzyme Inhibitors/adverse effects/therapeutic use ; Female ; Hemoglobin A, Glycosylated/analysis ; Humans ; Hypoglycemic Agents/adverse effects/therapeutic use ; Inositol/adverse effects/*analogs & derivatives/therapeutic use ; Insulin/*blood/therapeutic use ; Male ; Metformin/therapeutic use ; Middle Aged ; Prospective Studies ; alpha-Glucosidases/antagonists & inhibitors

BACKGROUND/AIMS: Most pesticide formulations contain both chief and additive ingredients. But, the additives may not have been tested as thoroughly as the chief ingredients. The surfactant, nonyl phenoxypolyethoxylethanol (NP40), is an additive frequently present in pesticide formulations. We investigated the effects of NP40 and other constituents of a validamycin pesticide formulation on cell viability and on the expression of genes involved in cell damage pathways. METHODS: The effects of validamycin pesticide ingredients on cell viability and of NP40 on the mRNA expression of 80 genes involved in nine key cellular pathways were examined in the human neuroblastoma SK-N-SH cell line. RESULTS: The chemicals present in the validamycin pesticide formulation were cytotoxic to SK-N-SH cells and NP40 showed the greatest cytotoxicity. A range of gene expression changes were identified, with both up- and down-regulation of genes within the same pathway. However, all genes tested in the necrosis signaling pathway were down-regulated and all genes tested in the cell cycle checkpoint/arrest pathway were up-regulated. The median fold-change in gene expression was significantly higher in the cell cycle checkpoint/arrest pathway than in the hypoxia pathway category (p = 0.0064). The 70 kDa heat shock protein 4 gene, within the heat shock protein/unfolded protein response category, showed the highest individual increase in expression (26.1-fold). CONCLUSIONS: NP40 appeared to be particularly harmful, inducing gene expression changes that indicated genotoxicity, activation of the cell death (necrosis signaling) pathway, and induction of the 70 kDa heat shock protein 4 gene.
Aged ; Cell Cycle Checkpoints/drug effects/genetics ; Cell Line, Tumor ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Female ; Gene Expression Regulation/drug effects ; Genes, cdc ; HSP110 Heat-Shock Proteins/genetics/metabolism ; Humans ; Inositol/*analogs & derivatives/chemistry/poisoning ; Necrosis ; Neurons/*drug effects/metabolism/pathology ; Nonoxynol/chemistry/*toxicity ; Pesticides/chemistry/*poisoning ; RNA, Messenger/metabolism ; Signal Transduction/drug effects ; Surface-Active Agents/chemistry/*toxicity

For parthenogenetic activation as a model system of nuclear transfer, microinjection and electroporation as activation treatments in bovine metaphase II oocytes were administered to each of three groups as follows: control group (treatments with Ca2+, Mg2+ -free PBS+100 micro M EGTA), IP3 group (control+25 micro M IP3) and IP3+ ryanodine group (control+25 micro M IP3+10 mM ryanodine). In experiments using microinjection, no significant differences were observed between any of the developmental stages of the electroporation experiment. For electroporation, cleavage rates were significantly higher in the IP3+ryanodine group than in the IP3 or control group (85.6% vs 73.7% or 67.6%, respectively). In the subsequent stages of embryonic development, such as morula and blastocyst formation, the IP3 and ryanodine group exhibited significantly higher rates of morula fomation than the IP3 or control groups (40.6% vs 24.2% or 16.7%, respectively). Similarly, the rate of blastocyst formation in the IP3+ryanodine group was significantly higher than the control group (16.3% vs 6.9%) but did not differ significantly from the IP3 group (16.3% vs 9.5%). In nuclear transfer, activation was performed at 30 hpm by microinjection and elecroporation with 25 micro M IP3+ 10 mM ryanodine followed by 6-DMAP treatment. No significant differences were observed at any stage of embryonic development and none of the embryos activated by electroporation reached either the morula or blastocyst stage. However, 3.8% and 1.9% of embryos activated by microinjection sucessfully developed to the morula and blastocyst stages, respectively. In conclusion, activation treatments using IP3 and ryanodine are able to support the development of bovine parthenogenetic and reconstructed embryos.
Adenine/administration & dosage/*analogs & derivatives/pharmacology ; Animals ; Cattle/*embryology/physiology ; Cell Fusion ; Electroporation/veterinary ; Embryonic and Fetal Development/*drug effects ; Enzyme Inhibitors/administration & dosage/pharmacology ; Female ; Inositol 1,4,5-Trisphosphate/administration & dosage/*pharmacology ; Microinjections/veterinary ; Nuclear Transfer Techniques ; Oocytes/drug effects/growth & development ; Parthenogenesis/*drug effects ; Protein Kinase Inhibitors ; Ryanodine/administration & dosage/*pharmacology ; Skin/cytology

OBJECTIVETo investigate the protective effect and mechanism of sequoyitol (Sep) on high glucose-induced human umbilical vein endothelial cells (HUVECs) injury.

METHODSHUVECs were cultured with high glucose (30 mmol/L) in the presence or absence of sequoyitol (0.1, 1 and 10 micromol/L) for 24 h. Cell proliferation was measured by BrdU marking and cell cycle was detected by flow cytometry. 2', 7'-dichlorofluorescein diacetate was used to evaluate intracellular reactive oxygen species (ROS) levels. The NO, malonydialdehyde (MDA) and H2O2 levels were determined by colorimetric method according to the manufacturer's instructions. The expression of endothelial nitric oxide synthase (eNOS) and NADPH oxidase 4 (NOX4) were measured by real-time PCR and Western blot.

RESULTSIn the present study, we found that sequoyitol pretreatment for 1 h significantly decreased cell injury, promoted cell proliferation. Meanwhile sequoyitol significantly down-regulated NOX4 expression and decreased the level of ROS, MDA and H2O2 and obviously increased NO levels and up-regulated eNOS expression.

CONCLUSIONSequoyitol alleviates high glucose-induced cell injuries in HUVECs via inhibiting oxidative stress and up-regulating eNOS expression.

Cell Proliferation ; Cells, Cultured ; Glucose ; toxicity ; Human Umbilical Vein Endothelial Cells ; drug effects ; metabolism ; Humans ; Hydrogen Peroxide ; metabolism ; Inositol ; analogs & derivatives ; pharmacology ; Malondialdehyde ; metabolism ; NADPH Oxidase 4 ; NADPH Oxidases ; metabolism ; Nitric Oxide Synthase Type III ; metabolism ; Oxidative Stress ; Reactive Oxygen Species ; metabolism