OBJECTIVE　To determine the pharmacokinetic parameters of perlolyrine in rats.METHODS　The plasma concentration and pharmacokinetic parameters of perlolyrine were determined by means of GC-MS with selected ion (m/z 247 and m/z 248) and ［2-15N］perlolyrine(m/z 248) as the internal standard.RESULTS　The concentration-time profile of perlolyrine after oral administration of perlolyrine fitted a two-compartment open model.The pharmacokinetic parameters were t1/2α=0.31 h, t1/2β=4.62 h, t1/2ka=0.10 h, tmax=0.34 h, cmax=18.74 ng.mL-1,K12=0.82 h-1, K21=0.38h-1,K10=0.29 h-1,Vb=108.16 L.kg-1,AUC=98.54 ng.h.mL-1,respectively.CONCLUSION　The method is constant,sensitive and accurate.It provided a scientific basis for the clinical use of perlolyrine.

Glycine ; analogs & derivatives ; toxicity ; Herbicides ; toxicity

Objective This study aimed to investigate the expression of Cyclin E protein in the progress of occurrence and development of gastric cancer and lymphonode metastatic cancer.Methods The expression of Cyclin E protein analyzed by immunohistochemistry in gastric tissue array included of normal gastric mucosa,cancer side tissues,atypical hyperplasia tissues,primary cancer tissues and lymphonode metastatic cancer tissues.Results The positive expression rate of Cyclin E protein was 14.3％,20.0％,34.7％,85.1％ and 82.9％ in normal gastric mucosa,atypical hyperplasia tissue,carcinoma side tissue,primary cancer and lymphonode metastatic cancer,respectively.Compared with normal gastric mucosa and carcinoma side tissues and atypical hyperplasia tissues,the Cyclin E protein in primary cancer and lymphonode metastatic carcinoma tissues was over-expression ( P ＜ 0.01 ).Conclusions The Cyclin E protein was a possible molecular marker that can be used to diagnosis gastric cancer and lymphaden metastasis cancer.

Objective To investigate the value of spiral CT in therapy observation during and after radiofrequency ablation (RFA) for lung or liver tumors. Methods Spiral CT-guided RFA were performed in 35 patients (38 lesions) with lung or liver tumors. CT value of lesions during operation and the changes of lesions after operation were observed. Results Thirty-eight lesions were accurately located under spiral CT. The position of the electrode and the expension of claw-like thin needle electrode could be observed directly. CT value of lesions decreased and some gasification foci in some lesions were observed after RAF therapy. One month after RFA, tumor volume decreased, and the tumors present as slightly low-density mass on contrast-enhanced CT. The total effective rate of RFA was 85.71% (30/35). Conclusion Spiral CT is able to accurately guide RFA treatment for lung or liver tumors and evaluate the efficacy of therapy.

AIM: To explore the influence of different concentration midazolam on the macroscopic voltage gated potassium currents and to discuss the relationship between potassium currents and inhibitory effect of clinical relevant concentration midazolam on sympathetic nervous system. METHODS: Superior sympathetic ganglion neurons were dissociated enzymatically from 7 to10 day old rat. Experiments were performed about 5 h after plating at room temperature (20- 24 ℃ ). Appropriate solution was chosen to separate the K + current from the other transmembrane currents. 1 ?mol?L -1 TTX was applied to the extracelluar solution to block the Na + current. Midazolam was also resolved in extracelluar solution to get various concentration ( 0.1 , 0.3 ,3,10,50,100 ?mol?L -1 ). Currents were recorded with the patch clamp technique in whole cell configuration using glass electrodes with a tip resistance of 2- 4 M . Potassium currents were evoked by test pulse from -100 mV to +30 mV with holding potential -80mV. Data were analyzed using Clampfit 6.0 and Oringih 5.0 software. Whole cell current records were corrected for leakage and capacitance by using the P/5 protocol. RESULTS: Midazolam dose dependently inhibited the whole cell potassium currents. Clinical relevant concentration midazolam ( 0.3 ?mol?L -1 ) only reduced the peak currents by 3.89 %(P= 0.88 ). The concentration required to produce 50% current inhibition(IC 50 ) was 76.065 ?mol?L -1 . CONCLUSION: Midazolam inhibits the whole cell potassium current significantly and dose dependently, but clinical relevant concentration midazolam has minor effect on the potassium currents, indicating that the inhibitory effect of midazolam on potassium current is not related to the suppression of activity of sympathetic system.

To improve the expression of heterologous genes using baculovirus expression system, we constructed a novel shuttle vector based on the Bm-Bacmid. In the Bm-Bacmid, partial sequences of Chitinase and Cystein Protease were replaced with a tandem cassette of Cm and egfp through homologous recombination. Bombyx mori bidensovirus (BmBDV) ns1 under the control of polyhedrin promoter was inserted into the modified Bm-bacmid by transposition. For comparison, BmBDV ns1 under the control of polyhedrin promoter was also cloned in the wild type Bm-bacmid. The resulting Bm-bacmids were transfected into the cultured BmN cells to prepare recombinant virus to infect silkworms for expression of BmBDV ns1. Total proteins of hemocyte from infected silkworms were subjected to Western blotting and ELISA analysis. The yield of BmBDV NS1 1 with the modified vector was three times as much as that with the unmodified vector. The method to improve the yield of BmBDV NS1 in silkworms will facilitate the function and three-dimensional structure study of BmBDV NS1.
Animals ; Baculoviridae ; Bombyx ; virology ; Cell Line ; Chitinases ; Cysteine Proteases ; Genetic Vectors ; Insect Viruses ; Promoter Regions, Genetic ; Transfection

Objective To compare the effects of telmisartan and (or) amlodipine on the reversal left ventricular re-modeling in two-kidney one clip hypertensive rats. Methods A total of 50 healthy male SD rats were randomly divided into 5 groups (n=10):two-kidney one clip renal hypertensive (2KIC) model group, sham group, telmisartan (10 mg/kg) group, am-lodipine (2.5 mg/kg) group and telmisartan (10 mg/kg)+amlodipine(2.5 mg/kg) group. The model of two-kidney one clip re-nal hypertensive rats was established. The tail arterial blood pressure was detected once a week. After 20 weeks, rats were sacrificed and specimens were collected. The left ventricular mass index (LVMI) was assessed. The myocardial ultrastructur-al changes were observed by electron microscope. Values of plasma renin activity (PRA), angiotensionⅡ(AngⅡ) and atrial natriuretic peptide (ANP) were measured by enzyme linked immunosorbent assay (ELISA).Results Compared with sham group, the levels of systolic blood pressure (SBP), LVMI, PRA, AngⅡand ANP were significantly higher in 2KIC group (P＜0.01). Compared with 2KIC group, values of SBP, LVMI, PRA and ANP were significantly lower in telmisartan group and am-lodipine group (P＜0.01), but the value of AngⅡwas significantly higher (P＜0.01). The levels of SBP, LVMI, AngⅡand ANP were significantly lower in combined medication group than those of single drug medication group (P＜0.01). There was no significant difference in the plasma PRA level between those groups (P>0.05). Results of myocardial electron microsco-py showed that the left ventricular remodeling was significantly improved in combined treatment group. Conclusion Telmisartan and amlodipine can effectively improve the left ventricular remodeling induced by hypertension. There was more effective therapy using both medications together.

Objective To analyze the effect of compound Minwei on serum interleukin-4(IL-4),interferon-γ(IFN-γ)value in children with acute urticaria.Methods in our hospital from March 2015 to October 2016 received 148 cases of children with acute urticaria eczema,were randomly divided into study group and control group,74 cases in each group,study the application of compound chlorphenamine maleate and vitamin syrup for treatment,the control group were applied paeonol ointment treatment,curative effect,evaluation of children with symptoms before and after treatment respectively,and detection serum IL-4 and IFN-levels.Results before treatment,the two groups had no statistical significance with symptom score,serum IL-4,IFN-levels difference(P>0.05);after treatment,the clinical efficacy of the study group,serum IFN-γ levels higher than the control group,the serum level of IL-4 score,symptoms than the control group,the difference has statistical significance(P<0.05).Conclusion acute eczema urticaria children with compound Minwei syrup treatment,can significantly relieve the symptoms of children,improve the body immunity,promote children rehabilitation,has good treatment effect.

Objective To evaluate the individualized 3D) printed drilling guide we developed and used for placement of C1/2 pedicle screws in the clinical treatment of fracture and dislocation of the atlantoaxial joint.Methods From January 2014 to June 2016,we treated a total of 17 patients with fracture and dislocation of the atlantoaxial joint.All the cervical CT data of the patients were imported into the digital orthopaedic workstation for 3D reconstruction,data modeling and 3D printing to design and manufacture individualized atlantoaxial vertebral guide templates.Intraoperatively,C1 and C2 pedicle screws were placed under the guide of individualized 3D printed drilling template.Cervical short-segment fixation and fusion were conducted for the patients.Postoperatively,regular clinical and radiographic follow-ups were carried out.Results No serious complications like injury to spinal cord and vertebral artery happened due to failed placement of C1/2 pedicle screws.The operation time ranged from 136 to 222 min (average,168.0 rmin);the intraoperative blood loss ranged from 260 to 556 mL (average,356.0 mL).The 17 patients were followed up for 6 to 36 months (average,13.5 months).The patients obtained bony union after 4 to 6 months (average,4.8 months).At the final follow-up,according to ASIA92 scoring system,the average sensory score was improved significantly from preoperative 7.4 + 3.2 to postoperative 13.1 + 5.9,and the average motor score was improved significantly from preoperative 5.3 + 3.1 to postoperative 11.7 + 5.1 (P ＜ 0.05).No such complications as infection or implant failure occurred after operation.Conclusion Individualized 3D printed drilling guide for implantation of atlantoaxial pedicle screws can make the complicate and risky placement become accurate,safe and simple.