A rapid, sensitive and simple liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed for the simultaneous determination of yogliptin and its metabolite in Wistar rat plasma. Linagliptin and dexamethasone were chosen as the internal standards of yogliptin and its metabolite, (R)-8-(3-hydroxypiperidine- -yl)-7-(but-2-yn-1-yl)-1-((5-fluorobenzo[d]thiazol-2-yl)methyl)-3-methyl- H-purine-2, 6 (3H, 7H)-dione, respectively. After a simple protein precipitation using acetonitrile as the precipitating solvent, both analytes and ISs were separated on a Grace Altima HP C18 column (2.1 mm x 50 mm, 5 microm) with gradient elution using methanol (containing 0.1% formic acid, 4 mmol x L(-1) ammonium acetate)-0.1% formic acid (containing 4 mmol x L(-1) ammonium acetate) as the mobile phase. A chromatographic total run time of 4.4 min was achieved. Mass spectrometric detection was conducted with electrospray ionization under positive-ion and multiple-reaction monitoring modes. Linear calibration curves for yogliptin and its metabolite were over the concentration range of 0.5 to 500 ng x mL(-1) with a lower limit of quantification of 0.5 ng x mL(-1). The intra- and inter- assay precisions were all below 14%, the accuracies were all in standard ranges. The method was used to determine the concentration of yogliptin and M1 in Wistar rat plasma after a single oral administration of yogliptin (27 mg x kg(-1)). The method was proved to be selective, sensitive and suitable for pharmacokinetic study of yogliptin and M1 in Wistar rat plasma.

Healthy Beagle dogs were administrated with batroxobin by intravenous infusion at high, medium and low doses. The study of pharmacodynamics and pharmacokinetics was intended to clarify the relevance of them and provided strong evidence for clinical use of batroxobin. The blood samples were collected after injection based on the time schedule and samples were tested by ELISA method to get the concentration of batroxobin. At the same time, changes of prothrombin time (PT), thrombin time (TT), activated partial thromboplastin time (APTT), fibrinogen (Fib) and D-dimmer were tested. The results showed that the concentration of D-D increased significantly after administration compared with that of before administration. The main pharmacokinetic parameters were as follows: t1/2 were (2.27 +/- 0.42) h, (10.65 +/- 2.19) h and (11.01 +/- 3.51) h; C(max) were (11.9 +/- 1.72) ng x mL(-1), (154.53 +/- 12.38) ng x mL(-1) and (172.14 +/- 47.33) ng x mL(-1); AUC(last) were (29.38 +/- 3.69) ng xh x mL(-1), (148.43 +/- 72.85) ng x h x mL(-1) and (599.22 +/- 359.61) ng x h x mL(-1). The elimination of batroxobin was found to be in accord with linear kinetics characteristics. The results of pharmacodynamics showed that D-dimmer level increased significantly after the administration of batroxobin, which was similar with the changes of batroxobin plasma concentration. Simultaneously, Fib concentrations in Beagle dog blood decreased significantly after the iv administration of batroxobin, while recovered to base level after 48 hours. PT, TT and APTT significantly became longer after administration, which returned to normal level after 48 hours. Especially, the D-dimmer levels and the batroxobin concentration in plasma after intravenous infusion of the drug were synchronized in Beagle dogs. Changes between PD/PK results had obvious correlation, and the D-dimmer levels in plasma can be one of the important monitoring indicators of batroxobin in thrombolytic medication.

Objective To compare the efficacy of bowel-cleansing,patients′compliance, tolerability and side effects of different doses of polyethylene glycol(PEG)electrolyte solution for colonoscopy preparation.Methods Single-blind prospective randomized trial was performed.A total of 100 inpatients undergoing elective colonoscopy were randomized into three groups to receive 4 L PEG(n =35),2 L PEG (n =31)or 2 +1 L PEG(n =34),respectively,on the day of colonoscopy from May to July 2014.Bowel-cleansing efficacy was separately assessed with the Ottawa Scale for the right,middle,and left colon.Total score was obtained by adding the scores for individual evaluation of the three colon segments with the score of overall fluid in the entire colon.All patients filled in a questionnaire and were interviewed about their com-pliance to the assigned bowel preparation,tolerability,and side effects.Results Patients who did not complete the colonoscopy were excluded.A total of 91 patients were included in the last analysis:31 cases of 4 L group,30 cases of 2 L group and 30 cases of 2 +1 L group.The efficacy of bowel-cleansing of the three groups of patients according to the Ottawa Scale were similar(P >0.05),but the excellent and good rate of cleansing quality of the right colon was higher in 4 L group than in 2 L group(P <0.05).Compared with 4 L group and 2 +1 L group,patients in the 2 L group had higher compliance and tolerability,as well as lower rate of side effects(P <0.05 ).Conclusion The efficacy and safety of taking 2 L polyethylene glycol electrolyte solution in bowel-cleansing on the day of colonoscopy is good and suitable for use.Taking 4 L polyethylene glycol electrolyte solution for bowel preparation on the day of colonoscopy is more suitable for patients who are suspected highly with lesions of the right colon.

Objective To develop a sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method for the determination of forsklin in rat plasma.Methods After extraction with methyl tert-butyl ether,chromatographic separation was performed on a C18 column with the mobile phase consisting of water ( 0.1％ formic acid)-acetonitrile in a gradient elution mode.A tandem mass spectrometer equipped with electrospray ionization (ESI) source was used as detector in the positive ion mode.Quantification was performed using multiple reaction monitoring (MRM) with the precursor product combination ions of m/z 411→375.3 and 285→193 for forsklin and diazepam.Results Good linearity was obtained in the 0.5-1000 ng/ml range for the analyte and the analytical method was validated in terms of specificity,precision,accuracy,recovery,stability and matrix effect.These assays gave RSD values always lower than 14.4％ and RE values between -3.5 ％ and 3.8％.In addition,the specificity,extraction recovery,stability and matrix effect were satisfactory.Conclusion Due to its high sensitivity,specificity and simplicity,the method could be used for pharmacokinetic studies of forsklin.

Mother-to-child transmission (MTCT) of hepatitis B virus (HBV) represents the most common mode by which children acquire HBV infection. For pregnant women with high viral load and positive hepatitis B e antigen (HBeAg), antiviral therapy during late pregnancy combined with timely and standardized inoculation of neonatal hepatitis B immunoglobulin and hepatitis B vaccine can minimize the possibility of MTCT of HBV. This review focuses on using and withdrawing antiviral drugs during pregnancy, managing postpartum hepatitis, and breastfeeding issues to further optimize the combined immunization and antiviral treatment strategies and seek the optimal solution to preventing MTCT of HBV.

BACKGROUND: With social development, the average life span is prolonged. The issue of aging has increasingly attracted people's attention. It is necessary to promote the health status and the guality of life of the elderly..OBJECTIVE: To understand the status and distribution features of several common diseases which influence the quality of life of elderly.DESIGN: Random cluster sampling methods and a cross-section survey.SETTING: Beijing Institute of Geriatrics of Beijing Hospital.PARTICIPANTS:Totally 1 558 old people aged ≥60 years living in 10 communities affiliated to Jianguomen district office of the Eastern District of Beijing City,and 8 villages affiliated to Xiangyang and Henan Villagers'Commissions of Shunyi County of Beijing from May 1997 and October 1997 were recruited.In fact,1 434 persons responded,with a response rate being 92％,319 males and 498 females came from the city;242 males and 375 females came from the villages.METHODS:Questionnaires were filled up,and physical examinations were conducted in all the elderly. MAIN OUTCOME MEASURES: The 6 common diseases were observed among the elderly: Hyperplasia of prostate, abnormal audition, cartaract ,osteoarthritis, fracture and constipation.RESULTS:Totally 1434 elderly entered the stage of result analysis.①The incidence of hyperplasia of prostate in the males from the urban areas was lower than that in the rural areas (61.4％,65.7％, P ＜ 0.01 ). ② The incidence of abnormal audition among the elderly from the urban areas was lower than that in the rural areas (53.9％,64.7％,P ＜ 0.01).③ The incidence of cataract of the two eyes in the elderly from the urban areas was higher than that in the rural areas(46.4％,44.4％, P ＜ 0.01). ④ The incidence of osteoarthropathy in the elderly from the urban areas was higher than that in the rural areas (24.4％,14.9, P ＜ 0.01). ⑤ The incidence of fracture in the elderly from the urban areas was higher than that in the rural areas (14.2％,9.1％, P ＜ 0.05). ⑥ The incidence of constipation of the elderly in urban areas was lower than that in the rural areas(18.2％,23.0％,P ＜ 0.05).CONCLUSION:There is a difference between the elderly from the urban areas and the rural areas in hyperplasis of prostate,abnormal audition, cataract, osteoarthropathy, fracture and constipation, and this is related with the economy, nutrition, medical conditions and cultural traits.Therefore, attention should be attached to nutrition and health knowledge of the elderly and prevention and treatment of common diseases among the elderly people.

PEP06 is a novel endostatin-Arg-Gly-Asp-Arg-Gly-Asp(RGDRGD)30-amino-acid polypeptide featuring a terminally fused RGDRGD hexapeptide at the N terminus.The active endostatin fragment of PEPO6 directly targets tumor cells and exerts an antitumoral effect.However,little is known about the kinetics and degradation products of PEP06 in vitro or in vivo.In this study,we investigated the in vitro metabolic stability of PEP06 after it was incubated with living cells obtained from animals of different species;we further identified the degradation characteristics of its cleavage products.PEP06 underwent rapid enzymatic degradation in multiple types of living cells,and the liver,kidney,and blood play important roles in the metabolism and clearance of the peptides resulting from the molecular degradation of PEP06.We identified metabolites of PEP06 using full-scan mass spectrometry(MS)and tandem MS(MS2),wherein 43 metabolites were characterized and identified as the degradation metabolites from the parent peptide,formed by successive losses of amino acids.The metabolites were C and N terminal truncated products of PEP06.The structures of 11 metabolites(M6,M7,M16,M17,M21,M25,M33,M34,M39,M40,and M42)were further confirmed by comparing the retention times of similar full MS spectrum and MS2 spectrum information with reference standards for the synthesized metabolites.We have demonstrated the metabolic stability of PEP06 in vitro and identified a series of potentially bioactive downstream metabolites of PEP06,which can support further drug research.

Objective:To explore the disturbance of metal element balance in mice after exposure to radon.Methods:Mice were randomly divided into control group, radon exposure of 30 WLM group, 60 WLM group and 120 WLM groups, with 10 mice in each group. After radon exposure with the cumulative dose, the lung function of mice was detected by a non-invasive pulmonary function testing instrument. Mice blood was taken from eyeballs. The lungs, heart, liver, kidney and spleen were also collected. HE staining was used to observe the pathological changes of lung tissue. Inductively coupled plasma mass spectrometry (ICP-MS) was used to detect the content of metal elements, including essential trace elements in the body: chromium (Cr), molybdenum (Mo), cobalt (Co), selenium (Se), copper (Cu), zinc (Zn), manganese (Mn), nickel (Ni), and potentially toxic elements: arsenic (As), tin (Sn), lead (Pb), aluminum (Al), mercury (Hg), cadmium (Cd), and silver (Ag).Results:Compared with the control group, lung ventilation function of the radon-exposed mice was decreased, alveolar structure was destroyed, and the contents of pulmonary metal elements Cr, Al, Pb, Sn( F=0.34, 0.66, 3.14, 1.16, P<0.05) and essential trace elements Mn, Cr, Zn, and Mo in the blood were decreased( F=0.65, 1.44, 0.97, 2.08, P<0.05), while the elements of Cu, Mo, Se and As in the lungs were increased( F=1.31, 1.26, 0.81, 2.04, P<0.05), and the element contents in other tissues also fluctuated. Conclusions:Inhalation of a certain cumulative dose of radon can reduce the lung ventilation function of mice and induce lung inflammation, as well reduce the content of essential trace elements in the lung and blood so that the content of metal elements in the body fluctuates.

OBJECTIVE: Cassiae Semen (CS, Juemingzi in Chinese) has been used for thousands of years in ancient Chinese history for relieving constipation, improving liver function as well as preventing myopia. Here we aimed to elucidate the anti-steatosis effect and underlying mechanism of CS against non-alcoholic fatty liver disease (NAFLD). METHODS: High-performance liquid chromatography (HPLC) was used to identify the major components of CS water extract. Mice were fed with a high-fat and sugar-water (HFSW) diet to induce hepatic steatosis and then treated with CS. The anti-NAFLD effect was determined by measuring serum biomarkers and histopathology staining. Additionally, the effects of CS on cell viability and lipid metabolism in oleic acid and palmitic acid (OAPA)-treated HepG2 cells were measured. The expression of essential genes and proteins involved in lipid metabolism and autophagy signalings were measured to uncover the underlying mechanism. RESULTS: Five compounds, including aurantio-obtusin, rubrofusarin gentiobioside, cassiaside C, emodin and rhein were simultaneously identified in CS extract. CS not only improved the diet-induced hepatic steatosis in vivo, as indicated by decreased number and size of lipid droplets, hepatic and serum triglycerides (TG) levels, but also markedly attenuated the OAPA-induced lipid accumulation in hepatocytes. These lipid-lowering effects induced by CS were largely dependent on the inhibition of fatty acid synthase (FASN) and the activation of autophagy-related signaling, including AMP-activated protein kinase (AMPK), light chain 3-II (LC3-II)/ LC3-1 and autophagy-related gene5 (ATG5). CONCLUSION Our study suggested that CS effectively protected liver steatosis via decreasing FASN-related fatty acid synthesis and activating AMPK-mediated autophagy, which might become a promising therapeutic strategy for relieving NAFLD.

A combined radiation-wound injury refers to a radiation injury combined with a traumatic wound, with the characteristics of repeated ulceration and a long and difficult healing process, which is a focus in the field of research on difficult-to-heal wounds. To research combined radiation-wound injuries, the establishment of animal models is a key part, and appropriate animal models are a guarantee of reliable experimental results. This review summarizes the current research progress on various animal models of combined radiation-wound injuries in terms of radiation types, animal species, and injury types and location, aiming to provide a scientific basis for establishing standardized animal models, studying injury mechanisms, and evaluating prevention and treatment efficacy for combined radiation-wound injuries.