OBJECTIVE:To develop an HPLC method for the determination of 5-ISMNconcerntrations in human plasma and study the pharmacokinetics of 5-ISMN orally disintegrating tablets and the reference tablets.METHODS:A single oral dose test capsule(orally disintegrating tablets)or reference capsule of 5-ISMN(60 mg)were administered by randomized crossover way in 20 healthy male volunteers with plasma 5-ISMN concentrations determined by HPLC.The pharmacokinetic parameters were calculated with 3p87 pharmacokinetic program and the bioavailability of the two preparations was evaluated.RESULTS:The main pharmacokinetic parameters of the test preparation vs.the reference preparation were as follows:Cmax:(613.42?73.83)vs.(368.64?38.66)?g?mL-1;tmax:(26.52?2.00)vs.(95.73?4.16)min;AUC0～∞:(73 872.24?543.89)vs.(77 978.47?646.37)ng?min?mL-1,respectively.CONCLUSION:The assay was proved to be sensitive,accurate and suitable for pharmacokinetic study of 5-ISMN.The results of pharmacokinetic study after oral administration of test and reference preparations of 5-ISMN showed that the two preparations were bioequivalent while the test preparation had a higher peak concentration and could reach peak level in less time,and the test preparation showed a rapid drug releasing behavior.

Objective To observe the change of expression of inwardly rectifying K+(Kir)2.3 mRNA and protein of Kir in the hippocampus of rats with chronic temporal lobe epilepsy(TLE)in different time points and the effect of Tenidap a Kir2.3 channel opener on its expression,investigate the relationship between Kir2.3 and the pathogenesis of TLE and to explore the potential of Kir agonists as anti-epileptic drugs.Methods The pilocarpine TLE rat model was used.Animals were randomly assigned to the control or the status epilepticus(SE)groups,which were further divided into four time point subgroups consisting of 0.6,72 hours,and 2 weeks post-SE termination.Another subgroup was given Tenidap,a Kir2.3 channel opener,and tested 2 weeks post-SE.Hippoeampi were removed and the expression of Kir2.3 mRNA and protein at different time points was measured by reverse transcription polymerase chain reaction(RT-PCR)and western blotting.Results The ratios of Kir2.3 mRNA and β-actin in normal control and 0,6,72hours and 2 weeks after SE termination were 0.080±0.030,0.103±0.045,0.164±0.026,0.132±0.024.0.011±0.008,respectively(F=23.684,P<0.01).The ratios of Kir2.3 protein and GAPDH in propotional groups were0.305±0.030,0.263±0.028,0.767±0.167,0.498±0.077,0.176±0.026(F=44.183.P<0.05).The expression of Kir2.3 channel in the epileptic rats was bimodal,increasing immediately after SE,relative to controls,and declining in the chronically epileptic period.Tenidap administration upregulated both the mRNA(0.021±0.006)and protein expression(0.636±0.140) of Kir2.3(F=25.216 and 47.355,P<0.05 and 0.01).Condusion These findings suggest that the pathogenesis of TLE is accompanied by a decrease in Kit2.3 expression,which may be ameliorated by the administration of tenidap.

AIM: To study the isolation,purification and characterization of Ramulus Mori polysaccharide. METHODS: Ramulus Mori was extracted by boiling water. The raw extract was precipitated fractionally by alcohol deproteinized,passing through DEAE ion exchange cellulose ( DEAE-52) and SephadexG-100,obtained RMPS1 and RMPS2. The composition and characterization of Ramulus Mori polysaccharide were researched by TLC、IR、 GC、HPLC and smith degradation. RESULTS: The molecular weight of RMPS1 and RMPS2 were 5. 8 ? 105 and 6. 5 ? 105; RMPS1was made up of rhammose、arabinose、glucose and galactose with the molarity rate of 1. 08 ∶ 1 ∶ 1. 40 ∶ 1. 57; RMPS2 of rhammose、glucose and galactose with the molarity rate of 11. 38 ∶ 1 ∶ 1. 35. Smith degradation showed that the main linkage form in RMPS1 and RMPS2 was 1→2 and 1→4 glycosidic linkages,But some 1→3 glycosidic linkages also existed in the molecules; infrared spectrum showed that both had the polysaccharide characteristic absorption peaks. CONCLUSION: The structures of RMPS1 and RMPS2 are first determined from Ramulus Mori.

Post-stroke fatigue (PoSF) is an independent pathologic symptom after stroke which negatively influenced activities of daily living (ADL) and quality of life (QOL) of the stroke patients. PoSF is irrelevant to depression, age, state of the illness, etc. PoSF should be assessed appropriately and alleviated by medicine, diet, sleep, exercise, and health education, etc.

The PET tracer 5-([11C]methyloxy)-L-tryptophan (5-(11)CMTP) was prepared by nucleophilic fluorination and alkylation reaction via a two-step procedure in order to develop specific tumor probe. The biodistribution and microPET imaging of 5-(11)CMTP were executed. The results unveiled that the overall radiochemical yield with no decay correction was (14.6 ±7.2) %, the radiochemical purity was more than 95% and high uptake and long retention time of 5-(11)CMTP in liver, kidney and blood were observed but low uptake in brain and muscle were found, furthermore, high uptake of 5-(11)CMTP in tumor tissue was observed. It seems that 5-(11)CMTP will be a potential amino acid tracer for tumors imaging with PET.
Amino Acids ; Animals ; Neoplasms ; diagnostic imaging ; Positron-Emission Tomography ; Radioactive Tracers ; Tissue Distribution ; Tryptophan ; analogs & derivatives

"Tinglizi", the ripe seed of Descurainia sophia and Lepidium apetalum, is a member of Brassicaceae (Cruciferae). Traditionally, the former is called "Nantinglizi" (Descurainiae Semen) while the latter is called "Beitinglizi" (Lepidii Semen). In the theory of traditional Chinese medicine, it has the power to purge lung-fire, relieve dyspnea, promote diuresis and reduce edema, and it is mainly indicated in a case with phlegm-fluid accumulation, cough with excessive sputum, dyspnea with being unable to lie, and general swelling. In view of its wide-spread application in clinic, a comprehensive review of Lepidii Semen and Descurainiae Semen was conducted from the following aspects: herbalogical study, variety identification, historical evolution of processing, chemical constituents, pharmacological effects, quantitative determination and toxicity which could provide reference for further research and development of "Tinglizi".
Brassicaceae ; chemistry ; Diuresis ; drug effects ; Drugs, Chinese Herbal ; adverse effects ; chemistry ; isolation & purification ; pharmacology ; Dyspnea ; drug therapy ; Edema ; drug therapy ; Humans ; Lepidium ; chemistry ; Lung ; drug effects ; Medicine, Chinese Traditional ; Molecular Structure ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; Seeds ; chemistry

OBJECTIVETo discriminate Descurainiae Semen and Pantagirus Semen.

METHODA high-performance liquid chromatographic method was developed to establish the fingerprint of Descurainiae Semen, and hierarchical cluster analysis (HCA) and partial least squares discriminant analysis (PLS-DA) were applied to study HPLC fingerprinting and chemical recognition.

RESULTThere exists large difference of chromatographic peaks and its relative peak area of HPLC fingerprints between Descurainiae Semen and Pantagirus Semen, and after conducting statistical analysis, the result demonstrated that all samples were classified into three categories: Descurainiae Semen, Pantagirus Semen and their mixtures.

CONCLUSIONThe developed HPLC fingerprint combined with chemometrics can be utilized to discriminate between Descurainiae Semen and Pantagirus Semen, which was quick, simple, accurate and reliable an can provide the basis for the characterization and quality assess of Descurainiae Semen and Pantagirus Semen.

Brassicaceae ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Cluster Analysis ; Least-Squares Analysis ; Plants, Medicinal ; chemistry

Objective:To study the mechanism of moxibustion therapy on diabetic peripheral neuropathy for the peripheral neuroprotection.Methods:The DPN model was induced by intraperitoneal injection with streptozotocin (STZ).The rats were given moxibustion at the acupoint Yishu (Extra) and the acupoint Zusanli (ST 36).The treatment was carried out once a day and 15 minutes per acupoint,lasting for 56 d in total.The clinical effect of moxibustion was evaluated by detecting blood sugar,urine sugar,body weight and dietary intakes,as well as nerve conduction velocity with neuroelectrophysiological method.The structure variation of sciatic nerve was observed by HE staining and light microscopy,and the level of NGF in the sciatic nerve Was determined by ELISA.Results:Compared with the model group,the plasma glucose was significantly lower in the moxibustion group (P＜0.01),with significantly faster nerve conduction velocity (P＜0.01),more notably changes in pathological appearance (P＜0.01) and higher level of nerve growth factor (NGF)(P＜0.01).Conclusion:Moxibustion could improve the symptom and signs of peripheral neuropathy in rat models with DPN,which may relate to the increased NGF and enhanced peripheral nerve protection.

We retrospectively analyzed the clinical data of 17 patients with esophageal perforation and rupture from August 2007 to December 2011.Among them,there were spontaneous esophageal rupture (n =6),esophageal perforation caused by foreign bodies (n =8) and iatrogenic injury (n =3).Family members gave up treatment because of critical illness (n =2),conservative treatment was offered for surgical intolerance (n =1) and all others (n =14) underwent operation (thoractomy,n =13 ; neck incision,n =1).One patient with conservative treatment and another two surgical cases died.The other 12 cases recovered.Therefore individualized treatment is essential for the patients with esophageal perforation and rupture.

OBJECTIVETo investigate the effect of hypoxia on the human pulmonary artery smooth muscle cells two pore domain potassium channels TASK-1 and the regulation of non-receptor tyrosine kinase c-Src in this process.

METHODSThe cultured human pulmonary artery smooth muscle cells (hPASMCs) were divided into: normal group, hypoxia 30 minute group, hypoxia 6 hours group and hypoxia 48 hour group, and hypoxia 48 hour + PP2 group, hypoxia 48 hour + PP3 group, hypoxia 48 hour + bpV group. Flow cytometry was used to analyze the cell cycle, RT-PCR and Western blot technique were carried out to detect the expression changes of TASK-1 mRNA and protein in different groups.

RESULTS(1) Cell Cycle Show: Compared with normal control group, with prolonged hypoxia, the percentages of hPASMCs in S phases of cell cycle were increased. While compared with hypoxia 48 hour group, the percentages of hypoxia 48 hour + PP2 group hPASMCs in S phases of cell cycle were decreased. The expression of TASK-1 mRNA on hPASMCs in acute hypoxia 6 hour group was increased, while the expression of TASK-1 protein on hPASMCs in the acute and chronic hypoxia group was decreased, and the expression of TASK-1 mRNA on hPASMCs in the chronic hypoxia group was decreased; After pre-incubation of a potent and selective inhibitor of the Src family of protein tyrosine kinases PP2, the expression of TASK-1 mRNA and protein in hypoxia 48 hour group was increased, however after pre-incubation of the inhibitor of the Src family of protein tyrosine phosphatase bpV, the expression of TASK-1 protein in hypoxia 48 hour group was decreased.

CONCLUSIONHypoxia promotes human pulmonary artery smooth muscle cell proliferation, and non-receptor tyrosine kinase c-Src may participate in the expression of two pore domain potassium channels TASK-1 regulated by hypoxia. Therefore, we hypothesized that TASK-1 channels and c-Src participatein the acute and chronic hypoxic human pulmonary vasoconstriction.

Cell Hypoxia ; Cell Proliferation ; Cells, Cultured ; Humans ; Myocytes, Smooth Muscle ; cytology ; Nerve Tissue Proteins ; metabolism ; Potassium Channels, Tandem Pore Domain ; metabolism ; Pulmonary Artery ; cytology ; RNA, Messenger ; Vasoconstriction ; src-Family Kinases ; metabolism