The purity of 4,4′-dimethoxy-5,6,5′,6′-bis (methylenedioxy)-2′-morpholine methylenebiphenyl-2-methyl formate methanesulfonate (IMH), a new drug for fatty liver treatment, was determined through differential scanning calorimetry (DSC). Analysis of two-factor non repeatability method was performed in the investigation the effects of two factors (heating rate and sample weight) on purity determination. The DSC experimental parameters were optimized as follows: heating rate was 10 ℃·min^-1, temperature range was 150-300 ℃, sample weight was 2.0-4.1 mg, and N₂ flow rate was 80 mL·min^-1. The linear correlation coefficient (r) of this DSC method was 0.999 8. The RSD value (n = 6) of precision was 0.03%. The standard value and uncertainty of the purity results of the multiple batches of IMH drugs were (99.74 ± 0.29)%, (99.91 ± 0.28)%, (99.90 ± 0.28)%, and (99.81 ± 0.28)% with inclusion factor (K) of 2 and confidence probability (P) of 0.95. The results were basically consistent with the results of the mass balance method. The DSC mehod is a simple, rapid and accurate method, and provides a new reference method for determining the purity of IMH drugs, improves the accuracy and reliability of purity determination.

OBJECTIVE To overcome shortcomings in use of bed sheet,and to improve it for examining bed.METHODS Based on the working principle of the reel toilet paper and industrial drive belt,a reel device for(disposable) whole bed sheet was designed,and used on the bed examining more than 300 times.(RESULTS) The new designed reel aevice with disposable whole bed sheet was operated easy and safely,with decreased cost and(contamination) in use.It could alleviate infection opportunity in favor of control againt hospital infection and(environmental) protection.(CONCLUSIONS) The device can mount on any size of examining bed and widely accept for use.

Information management system of nuclear medicine (IMSNM) is an important part of modem medical information system.It is used for the scientific management of clinical works,and classification and storage of patient data and examination data (words and images).With the help of IMSNM,standardization,automation and digitization of clinical operation protocols,the scientific and normalized management,the unification of image storage and viewing could be achieved.The IMSNM plays an important role in the health care,education and scientific research.This study mainly describes the design and application of IMSNM.

Objective To observe the expression of cardiotrophin-1(CT-1) in ischemia-reinfusion cardiac muscle of rats and the effect of neuregulin-1(NRG-1).Methods The model of ischemia-reinfusion cardiac muscle of rats were prepared,35 rats were randomly divided into 4 groups:model group(n=8),NRG-1 pretreatment group(n=9),pseudo-surgery group(n=8) and normal control group(n=10).The CT-1 mRNA in the observed cardiac muscle of all groups was measured by RT-PCR and the relative amount of CT-1 mRNA were calculated,and for statistical treatment.Results The CT-1 mRNA of model group was(63.96?9.34),and it was higher than that of pseudo-surgery group(36.16?5.43)and normal control group(36.84?4.64).The significant differences were found in 3 groups(F=47.37 P

Objective:To explore the influence of ischemia/reperfusion (anoxia/reoxygenation)[FK(W16*2。142mmZQ1mm]on immunofunction of endothelial cells(ECs) and effect of intervention with 2-hydroxymethyl-3,5,6-trimethylpyrazine on it.Methods:Model of ECs induced by anoxia/reoxygenation was established to mimic ECs ischemia/reperfusion injury in vivo with human umbilical vein endothelial cell line ECV304.Then 2-hydroxymethyl-3,5,6-trimethylpyraxine was used to intervene the anoxia/reoxygenation process.Nuclear transcriptional factor-?B(NF-?B) was exhibited by fluorescent staining,HLA-ABC,HLA-DR,CD86 and CD54 were detected by flow cytometry.Mixed endothelial cell-lymphocyte reaction(MELR) was conducted to examine the proliferation of lymphocyte,production of IL-2 and percentage of apoptotic lymphocyte.Results:Anoxia/reoxygenation made the ECV304 cell became round,shrunk and abscised,with increased plasma NF-?B,and changed from positive cytoplasm to positive nucleus.HLA-ABC,HLA-DR and CD86 on surface of cells increased but CD54 showed unchanged.MELR showed the incorporation of ~3H-TdR and production of IL-2 increased significantly and the percentage of apoptotic lymphocyte decreased.After 2-hydroxymethyl-3,5,6-trimethylpyrazine intervention,the ECV304 cell shapes recovered,NF-?B expression didn’t down-regulated,but the percentage of positive cells decreased,changes to positve dominant.Besides,reversal changes were shown in other parameters.Conclusion:Anoxia/reoxygenation influences some important immune related molecules in ECV304 cells.2-hydroxymethyl-3,5,6-trimethylpyrazine could antagonize these influences to maintain the immune function of endothelial cells in a relative normal manner.

Though all the marketed drugs of dipeptidyl peptidase IV inhibitors are structurally different, their inherent correlation is worthy of further investigation. Herein we rapidly discovered a novel DPP-IV inhibitor 8g (IC50 = 4.9 nmol.L-1) which exhibits as good activity and selectivity as the market drugs through scaffold hopping and drug splicing strategies based on alogliptin and linagliptin. This study demonstrated that the employment of classic medicinal chemistry strategy to the marketed drugs with specific target is an efficient approach to discover novel bioactive molecules.
Dipeptidyl-Peptidase IV Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Drug Discovery ; methods ; Humans ; Hypoglycemic Agents ; chemical synthesis ; chemistry ; Linagliptin ; chemical synthesis ; chemistry ; Molecular Structure ; Piperidines ; chemical synthesis ; chemistry ; Structure-Activity Relationship ; Uracil ; analogs & derivatives ; chemical synthesis ; chemistry

AIMTo Investigate the effect of glutamate (Glu) and gamma-aminobutyric acid(GABA) in orbitofrontal cortex (OFC) on regulation of gastric motility.

METHODSUsing microinjection in OFC,together with lesion of related nucleus,and recording the intragastric pressure(IGP).

RESULTS(1) Microinjection of Glu in OFC caused a significant reduce of the amplitude of gastric motility, this effect could be reverse by lesion of amygdala, while lesion of LC had no influence on the effect of Glu. (2) microinjection of GABA in OFC could increase the amplitude of gastric motility significantly,and lesion of LC could abolish this effect,while lesion of amygdala could enhance the effect of GABA more.

CONCLUSIONMicroinjection of Glu in OFC may enhance the normal inhibitory effect of amygdale on gastric motility, and the effect of microinjection of GABA in OFC on gastric motility is closely related with LC.

Amygdala ; physiology ; Animals ; Female ; Frontal Lobe ; metabolism ; physiology ; Gastrointestinal Motility ; drug effects ; Glutamic Acid ; pharmacology ; Locus Coeruleus ; physiology ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; gamma-Aminobutyric Acid ; pharmacology

Objective To investigate the uptake of 99Tcm-hydrazinonicotinamide-D-alanine-D-alanine-alanine-proline-arginine-proline-glycine (HYNIC-A(D) A(D) APRPG) in rabbit models of inflammation and VX2 tumor xenografted, so as to evaluate its use as a new tracer for tumor angiogenesis. Methods Ten rabbit models of xenoplanted VX2 tumor and inflammation were randomly divided into two groups which were injected with different injected tracers, 99Tcm-HYNIC-A(D) A (D)APRPG 99Tcm-RGD, followed by serial Gamma images at various time points. The first group underwent 18F-FDG PET ahead of 99Tcm-HYNICA(D)A (D) APRPG SPECT. Analysis of variance and t-test were performed with SPSS 10.0. Results 99TcmHYNIC-A(D) A (D)APRPG scan showed negative uptake at inflammation focus but positive uptake at tumor. Pathological examination confirmed high 99Tcm-HYNIC-A(D)A(D) APRPG accumulation in tumor cells, with the highest tumor/inflammation ratio (3.25 ±0. 171) at 2 h post-injection, which was significantly higher than that of 99Tcm-RGD (2.37 ± 0.076) (F = 15. 63, P<0. 01). The tumor/inflammation ratios of 99Tcm-HYNIC-A(D)A(D)APRPG, 99Tcm-RGD, 18F-FDG were significantly different at 0.5, 1,2,3, 6 h (F = 13. 83～26. 41; t = 23.84, 12.75; all P<0. 01). Conclusion 99Tcm-HYNIC-A (D) A (D)APRPG can be used as a potential tracer for tumor angiogenesis.

Amino Acid Sequence ; Blood Donors ; Gene Deletion ; Gene Products, nef ; chemistry ; genetics ; Humans ; Molecular Sequence Data ; nef Gene Products, Human Immunodeficiency Virus

OBJECTIVETo evaluate the spiral CT and its reconstruction techniques in diagnosis and localization of gastrointestinal stromal tumor originated in the small intestine.

METHODSThe data of spiral CT scan and MPR, STS-MIP of 24 patients with gastrointestinal stromal tumor in the small intestine confirmed pathologically were analyzed retrospectrvely.

RESULTSOf 24 cases, 1 had multiple tumor, while the other 23 had single one. Seventeen of these tumors were benign and 7 malignant, with 2 in the duodenum, 12 in the jejunum and 10 in the ileum. The range of tumor diameters was from 2.5 to 12 cm. The main clinical characters of the tumors on the CT image: (1) The tumor of 15 cases located outside of the enteric cavity, 7 inside of the enteric cavity or presented as thicken bowel wall and 2 showed as niche sign. (2) The tumor shape of 19 cases were round-like, and 5 lobulated or irregular. (3) The tumor density of 12 cases was homegeneous, 7 heterogeneous and 5 map-like in the center. (4) The tumor enhancement style in 19 cases were homegeneous in dynamic enhanced scan, and 16 were slightly or mildly heterogeneous in the artery phase but apparently enhanced in the venous and equilibrium phase, with 5 showed as fast-in fast-out enhanced mode. Of those, one showed obvious enhancement in artery phase, while 2 did not. (5) The tumor of 2 cases had no clear margin and had invaded the surrounding tissue. (6) The arteries supplying tumors in 20 cases were demonstrated by multiple planar reconstruction (MPR), sliding thin slab-maximum intensity projection (STS-MIP). The accuracy of diagnosis and localization of gastrointestinal stromal tumor in the small intestine by spiral CT scan combined with MPR, STS-MIP were 91.7% (22/24) and 95.8% (23/24), respectively.

CONCLUSIONSpiral CT and its reconstruction techniques (MPR, STS-MIP) can play an important role in the differential diagnosis and localization of gastrointestinal stromal tumor originated in the small intestine.

Adult ; Aged ; Duodenal Neoplasms ; diagnosis ; diagnostic imaging ; Duodenum ; diagnostic imaging ; Female ; Gastrointestinal Stromal Tumors ; diagnosis ; diagnostic imaging ; Humans ; Ileal Neoplasms ; diagnosis ; diagnostic imaging ; Ileum ; diagnostic imaging ; Image Processing, Computer-Assisted ; methods ; Jejunal Neoplasms ; diagnosis ; diagnostic imaging ; Jejunum ; diagnostic imaging ; Male ; Middle Aged ; Tomography, Spiral Computed ; methods