Rotundine (1 micromol L(-1)) was incubated with a panel of rCYP enzymes (1A2, 2C9, 2C19, 2D6 and 3A4) in vitro. The remained parent drug in incubates was quantitatively analyzed by an Agilent LC-MS. CYP2C19, 3A4 and 2D6 were identified to be the isoenzymes involved in the metabolism of rotundine. The individual contributions of CYP2C19, 3A4 and 2D6 to the rotundine metabolism were assessed using the method of total normalized rate to be 31.46%, 60.37% and 8.17%, respectively. The metabolites of rotundine in incubates were screened with ESI-MS at selected ion mode, and were further identified using MS2 spectra and precise molecular mass obtained from an Agilent LC/Q-TOF-MSMS, as well as MS(n) spectra of LC-iTrap-MS(n). The predominant metabolic pathway of rotundine in rCYP incubates was O-demethylation. A total 5 metabolites were identified including 4 isomerides of mono demethylated rotundine and one di-demethylated metabolite. The results also showed that CYP2C19, 2D6 and 3A4 mediated O-demethylation of methoxyl groups at different positions of rotundine. Furthermore, the ESI-MS cleavage patterns of rotundine and its metabolites were explored by using LC/Q-TOF-MSMS and LC/iTrap-MS(n) techniques.

Chronic infection of hepatitis B virus(HBV)presents one of the serious public health challenges worldwide.Current treatment of chronic hepatitis B(CHB)is limited,and is composed of interferon and nucleoside/nucleotide reverse transcriptase inhibitors(NRTI).Interferon is poorly tolerated and is only responsive in a small fraction of CHB patients and NRTIs often face the problem of emergence of drug resistance during long-term treatment.The current treatment of CHB earl be improved in several ways including genotyping mutations associated with drug resistance before treatment to guide the choice of NRTIs and suitable combinations among NRTIs and interferon.It is important to continue research in the identification of novel therapeutic targets in the life cycle of HBV or in the host immune system to stimulate the development of new antiviral agents and immunotherapies.Several antivirai agents targeting HBV entry,cecDNA,capsid formation,viral morphogenesis and virion secretion,as well as two therapeutic vaccines are currently being evaluated in preclinical studies or in clinical trials to assess their anti-HBV efficacy.

responses of glycemia.

OBJECTIVE:To study the chemical constituents of Sedum lineare. METHODS:Silica gel column chromatogra-phy,TLC and crystallization were adopted to isolate the chemical constituents of S. lineare. And chemical structures were analyzed and identified based on physicochemical properties and spectral data of compounds. RESULTS:A total of 6 sterols and 2 triterpe-noids were isolated from petroleum ether fraction of S. lineare,which were identified as stigmaster-5-ene-3β-ol-7-one(1),stigmas-ter-5-ene-3β,7α-diol(2),daucosterol(3),daucosterol palmitate(4),β-sitosterol(5),stigmaster-7-ene-3β-ol(6),δ-amyrin(7),andδ-amyrone(8)respectively. CONCLUSIONS:Compounds 3,4 and 7 are isolated from S. lineare for the first time,and compound 4 is isolated from genus S.lineare for the first time. The study has laid certain foundation for the quality evaluation of S. lineare.

From both doctors and patients′different perspectives , this paper analyses the causes of conflict of doctor-patient communication , and from the subjective and the objective , the history and reality , individual and social aspects of light on the restricting factors for good doctor -patient communication , and puts forward strengthe-ning the consciousness of active , rule execution , achieving full coverage , explore ways to standard mode , rich di-verse ways and other countermeasures .

BACKGROUND:Stimulation of the pudendal nerve as a target can improve neurogenic bladder dysfunction after spinal cord injury, by adjusting the frequency, intensity, pulse width, as wel as regulating synergistic effect of detrusor and urethral sphincter. OBJECTIVE: To assess the research status of electrical stimulation of the pudendal nerve in the treatment of neurogenic bladder dysfunction after spinal cord injury. METHODS: We searched the folowing databases for articles addressing electrical stimulation of the pudendal nerve for neurogenic bladder dysfunction after spinal cord injury: PubMed, Cochrane Central Register of Controled Trials (CENTRAL), China National Knowledge Infrastructure, Wanfang Database, and VIP Database. The search was updated to July 2014, and the reference lists of the identified studies were manualy screened for additional studies. The study selection and data extraction were independently conducted by two reviewers. RESULTS AND CONCLUSION:Fourteen studies were included in this review. We derived the folowing points by analyzing the included studies: Electrical stimulation of the pudendal nerve has positive effects on rehabilitation of neurogenic bladder dysfunction after spinal cord injury; pudendal nerve electrical stimulation can modulate the coordination of the detrusor and the external urethral sphincter, improve the bladder compliance and restore bladder function by regulating pudendal-to-bladder reflex and spinal reflexes to the bladder. Electrical stimulation of the pudendal nerve may be potentialy implemented as a feasible treatment of neurogenic bladder dysfunction after spinal cord injury. More high quality researches should be conducted to clarify the efficacy and the potential active mechanisms of pudendal nerve electrical stimulation for neurogenic bladder dysfunction after spinal cord injury because the number of clinical reports published in this study area is limited, neurophysiological mechanisms underlying biphasic regulation of frequency on bladder function are not wel known, and which intensity of pudendal nerve electrical stimulation is more effective than others for the treatment of neurogenic bladder dysfunction after spinal cord injury remains unknown.

An on-site method for the determination of sulfur mustard ( SM) was developed based on pinhole shell-isolated nanoparticle-enhanced Raman spectroscopy. By using 0. 1 mol/L MgSO4 as effective agglomeration reagent, more Raman “hot spots” were induced, and thus a limit of detection for SM at 10 μg/L was achieved with a linearity of 10-1000 μg/L and an analytical enhanced factor of 1. 1×106. This method can be directly applied in the measurement of SM in environmental water samples with good sensitivity and reproducibility, and the standard addition recovery was between 88%-114%. Good differentiation of four SM related compounds, 2-chloroethyl ethylsulfide, thiodiglycol, bis-β-chloroethyl sulphoxide and bis-β-chloroethyl sulphone, was also obtained.

Objective To find the efficient modification groups of anti-proteinase hydrolyzation in polypeptide by investigat-ing and comparing the relation between the functional groups and their ability to inhibit proteinase hydrolyzation. Methods Reverse phase-high performance liquid chromatography(RP-HPLC)method was developed to investigate in vitro metabolisms of new drug LXT101 and its structural modified analogs LZN series and LMP series in pancreatin system. All the separations of peptide drugs and their digested fragments were monitored at 225 nm. Results The good linear range was 4.0-400 μg/ml(r>0.9990)for new drug LXT101 and its structural modified analogs,i.e.,LZN series and LMP series. The recoveries of all peptide drugs ranged from 95.0%to 98.7%in pancreatin systems. The relative standard derivations(RSD)of intra-day and inter-day were less than 1.5%and 2.5%,re-spectively. The revealed order of digested half-life of the peptide drugs was LZN series>LMP series>LXT101. Conclusion The study of different sites and different functional groups on the lifetime indicates that the half-lives of peptides are prolonged by introducing the functional groups in the suitable sites of peptide,which feature as proteinase inhibitors,such as carbamoyl(Cbm),acetyl(Ac),para-amino-phenylalanine(Aph)or para-uramido-phenylalanine(Uph),which work as either proton donor or acceptor. Our results can pro-vide some useful and valuable information on structural design of peptide drug with long lifetime and high activity.

OBJECTIVE: To explore the effects of piracetam on superoxide dismutase(SOD) activity and malonaldehyde(MDA) content in brain tissues of D-galactose-induced ageing rats.METHODS: 30 SD rats were randomized to one of the 3 groups: blank control group(NS),model group(D-galactose+NS) and piracetam group(D-galactose+piracetam 432 mg?kg-1?d-1).All the rats were put to death at 90 days after medication,and the SOD activity and MDA content in brain tissues were determined.RESULTS: As compared with the blank control,the SOD activity decreased(P

Objective To investigate ~1H-MRS findings of brain tumor and the clinical application of ~1H-MRS.Methods 80patients with brain tumors clinically or pathologically-proved underwent ~1H-MRS.Normal opposite hemispheres in 30 cases were used as control group.Single voxel spectroscopy(SVS) or 2D-MRS imaging was performed with excited echo sequence.The mean ratio of metabolisms with difference was compared.Results Compared with control group,NAA of tumor decreased in certain degree(P