Virginiamycin acetyltransferase D (VatD) plays a vital rule in streptogramins resistance by chemically inactivating streptogramin A. Therefore, it is desirable to discover novel small molecular weight inhibitors of VatD via state-of-the-art virtual screening techniques. This "cocktail" strategy by combining VatD inhibitor with streptogramins may provide new therapeutic opportunity for resistant bacteria infections. Structure-based virtual screening method (molecular docking) was applied to rank and score a chemical database containing 300 000 commercially available compounds against the VatD substrate binding site. Twenty six out of the 200 top scored compounds from the docking calculation were selected and submitted to the VatD enzymatic inhibition assay. The plasmid pRSET B/vatD was constructed and transformed into E.coli (trxB) host cells for over-expression, and VatD enzyme was purified and validated by showing acetyltransferase activity to Virginiamycin M1. Three out of these 26 tested compounds showed enzymatic inhibition on VatD with IC50 168.6, 91.0 and 55.2 μmol·L-1, separately. Other compounds could not be dissolved in the system and/or had little effect on the enzyme (IC50>200 μmol·L-1). To our knowledge, it is first time that small molecular weight organic compounds were identified as VatD inhibitors. It is expected that the VatD inhibitors identified at present study could serve as lead compounds for the further development of the novel therapeutic agents to overcome streptogramins resistance.

Objective To identify the correlation factors associated with cerebral intragenic ischemia after temporary parent arterial occlusion in intracranial aneurysm surgery. Methods One hundred and eighteen patients who underwent temporary arterial occlusion in the 120 aneurysms (from a group of 324 consecutive aneurysm patients treated from 1996 to 2002) were reviewed retrospectively. These variables included sex, age, presence of preoperative subarachnoid hemorrhage (SAH), neurological clinical grade, operational timing, duration of arterial occlusion, numbers of temporary occlusion, mode of arterial occlusion, intraoperative aneurysm rupture, hypertension, the location of temporary occlusion, aneurysm size, hyperglycemia, atheromatous mass. Univariate and multivariate were used to investigate the relationship between the variates and postoperative ischemic changes. Results The total times of temporary occlusion were 156, with an average of 1.30. The duration of arterial occlusion ranged from 1 to 45 min (9.75?7.75). Seventeen patients (14.4%) demonstrated evidence of new infarction in the vascular territory subjected to temporary arterial occlusion. Conclusion In the univariate analysis, age, presence of preoperative SAH, duration of arterial occlusion, atheromatous mass are all significantly correlated with postoperative ischemic injuries. Multivariate logistic regression revealed that the age, older more than 60 (P= 0.010 3 , relative risk=4.335), and the duration of arterial occlusion, lasting more than 20 min (P= 0.032 9 , relative risk=4.177), have significant correlation with the injuries. Based on these findings, temporary occlusion is safe and useful in aneurysm surgery and the postoperative cerebral ischemia is less likely to occur when the duration of clipping is shorter than 20 min.

This study is to investigate the effect of ZL-004 on normal mouse and mice with leukopenia induced by chemotherapeutic agents. 5-Fluorouracil were administered intraperitoneally to mice to develop leucopenia, and the mice were treated with ZL-004. The number of peripheral leukocytes and the percentage of granulocyte in total WBC were examined. The results are that ZL-004 markedly raise peripheral blood leukocytes in the normal mice and the mice model of leukopenia. So, ZL-004 could protect mice against 5-fluorouracil damage and raise peripheral blood leukocyte. Features of bone marrow smears is myeloproliferative hyperactivity in the mice, particularly the matured granulocytic series were observed. The mechanism of ZL-004 is to act on the mouse bone marrow causing proliferation and differentiation.

AIM:To establish the quality specification of Yinzhihuang Injection (extract of Herba Artemisiae scopariae,extract of Fructus Gardeniae,extract of Radix Scutellariae,extract of Flos Lonicerae Japonicae); METHODS:Extractum Artemisiae Scopariae、 Extractum Fructus gardeniae、 Extractum Flos lonicerae and Extractum Radix scutellariae were identified by TLC and were determined by HPLC. RESULTS:The average recoveries of chlorogenil、gardenoside、baicalin and p-hydroxyacetophenone were 99.8%,99.2%,100.1% and 99.9%,respectively.RSD were 0.81%,1.20%,1.90% and 0.55%,respectively.The TLC sports developed were fairly clear,and the blank test showed no interference. CONCLUSION:The method developed is simple and accurate with good reproducibility,and the method can be used for quality control of Yinzhihuang Injection.

Pulse waves contain rich physiological and pathological information of the human vascular system. The pulse wave diagnosis systems are very helpful for the clinical diagnosis and treatment of cardiovascular diseases. Accurate pulse waveform is necessary to evaluate the performances of the pulse wave equipment. However, it is difficult to obtain accurate pulse waveform due to several kinds of physiological and pathological conditions for testing and maintaining the pulse wave acquisition devices. A pulse wave generator was designed and implemented in the present study for this application. The blood flow in the vessel was simulated by modeling the cardiovascular system with windkessel model. Pulse waves can be generated based on the vascular systems with four kinds of resistance. Some functional models such as setting up noise types and signal noise ratio (SNR) values were also added in the designed generator. With the need of portability, high speed dynamic response, scalability and low power consumption for the system, field programmable gate array (FPGA) was chosen as hardware platform, and almost all the works, such as developing an algorithm for pulse waveform and interfacing with memory and liquid crystal display (LCD), were implemented under the flow of system on a programmable chip (SOPC) development. When users input in the key parameters through LCD and touch screen, the corresponding pulse wave will be displayed on the LCD and the desired pulse waveform can be accessed from the analog output channel as well. The structure of the designed pulse wave generator is simple and it can provide accurate solutions for studying and teaching pulse waves and the detection of the equipments for acquisition and diagnosis of pulse wave.
Algorithms ; Equipment Design ; Heart Rate ; Humans ; Liquid Crystals ; Models, Cardiovascular ; Pulse Wave Analysis ; instrumentation ; Regional Blood Flow

Objective To construct a eukaryotic expression system of IFN-λ,examine the expression of IFN-λand evaluate its bio-functions including anti-proliferation and anti-viral activity.Methods The genes of human IFN-λ1 /2 (hIFN-λ1 /2)were cloned from the mRNA of poly I∶C treated HuH-7 cells.The PCR product was examined with DNA sequencing.The genes of IFN-λ1 /2 were sub-cloned into pcDNA3 vector.The correct insertion of the gene IFN-λ1 /2 was identified with enzyme digestion.The constructed pcDNA3-IFN-λ1 /2 plasmids were transfected into COS-7 cells and IFN-λ1 /2 protein was checked in the supernatant and lysis of transfected cells using Western blotting analysis.The human esophageal carcinoma YES5 and T.Tn cells were treated with the IFN-λ1 /2 from the transfected cells and the proliferation of carcinoma cells were measured with CCK-8 kit.In the treated carcinoma cells,the apoptosis and antivirus related molecules such as caspase-3,ISG15 and MxA was analyzed with Western blotting or Quantitative real time PCR.Results The sequence of hIFN-λ1 /2 fragment matched that of the gene bank and the gene of the cytokines was inserted into pcDNA3 vector correctly.With Western blotting analysis,IFN-λ1 /2 protein was detected in the pcDNA3-IFN-λ1 /2 transfected COS-7 cells.The IFN-λ1 /2 from the transfected COS-7 cells inhibited the growth of YES5 and T.Tn cells, activated apoptosis related caspase-3,and up-regulated the anti-virus gene expression of ISG15 and MxA.Conclusion COS-7 cells can express IFN-λ1 /2 after transfection with pcDNA3-IFN-λ1 /2,suggesting that eukaryotic expression system of IFN-λis established.IFN-λ1 /2 from the system can perform bio-functions,such as proliferation inhibition,apoptosis induction and anti-viral gene up-regulation,which indicates that the system can contribute to further investigations of IFN-λbio-activity and its clinical application.

Objective To investigate the clinical value of transrectal ultrasound-guided improved 13-core prostate biopsy in the detection of prostate cancer.Methods Retrospective analysis was conducted in the clinical data of 82 clinically suspected prostate cancer patients in Shaanxi Provincial People's Hospital from October 2015 to October 2016.All patients were undergone transrectal uhrasound-guided improved 13-core prostate biopsy and surgical treatment,and the prostate biopsy results were compared with the postoperative pathological results.The accuracy of the improved 13-core prostate biopsy and the standard 6-core prostate biopsy was compared.The complications of improved 13-core prostate biopsy were also discussed.Results The diagnostic results of prostate biopsy included prostate cancer in 26 patients and benign prostatic hyperplasia (BPH) in 54 patients.The diagnostic results of 80 patients are consistent with postoperative pathological examination.Two patients were diagnosed as BPH by biopsy,but confirmed to be prostate cancer by postoperative pathological examination.The accuracy of the improved 13-core prostate biopsy and the standard 6-core prostate biopsy were 97.6％ (80/82) and 84.1％ (69/82) respectively,and the difference showed statistical significance (P =0.023).No severe complications were found in patients who underwent transrectal ultrasound improved 13-core prostate biopsy.Conclusion Transrectal ultrasound guided improved 13-core prostate biopsy can increase the detection rate significantly.It is safe and efficacious,and can be widely used in clinic.

Objective To study the bioequivalence of two kinds of levetiracetam extended‐release tables including the ref‐erence product of Keppra XR in Beagle dogs .Methods Dogs were administrated orally with single dose of levetiracetam tablets (1 000 mg) .The concentration of levetiracetam in dog plasma was detected by LC‐MS/MS .All parameters of pharmacokinetics were performed by WinNonlin 5 .2 software .Results Main pharmacokinetic parameters of test and reference tablets were as follow :tmax were 1.67 h and 3 .0 h ,Cmax were 89 .50 μg/ml and 71 .18 μg/ml ,t1/2 were 3 .68 h and 3 .50 h ,AUC(0‐48) were 826 .57 μg?h/ml and 757 .84 μg?h/ml ,AUC(0‐∞ )were 826 .68 μg?h/ml and 757 .93 μg?h/ml .The relative bioavailability of test tablets was 109 .07% to reference products of Keppra XR .Conclusion Therefore ,the two kinds of levetiracetam extended‐release tablets were bioequivalent in Beagle dogs .

Objective To study nursing of ureteral calculi patients treated by holmium laser lithotripsy by ureteral soft mirror under general anesthesia.Methods A total of 118 patients with ureteral calculi in our hospital were randomly divided into control group and observation group according to the double blind number method,all patients carried out general anesthesia by soft ureteral holmium laser lithotripsy,the control group was given routine nursing care and the observation group was given intensive care.And the nursing results of patients were statistically analyzed.Results The observation group had higher one-time success rate of clear stone than the control group (91.53％ vs.81.36％,P ＜ 0.05);The incidence rates of complications in the observation group was 3.39％,which was significantly lower than 8.47％ in the control group(P ＜0.05).The hospitalization time,SDS score,VAS score and SAS score of the observation group were significantly better than that of the control group (P ＜ 0.05).The observation group had significantly higher related knowledge and treatment compliance than that in the control group(88.14％,91.53％ vs.76.27％,74.58％,P ＜0.05).Conclusion Holmium laser lithotripsy by ureteral soft mirror under general anesthesia can strengthen treatment cooperation,the awareness of related disease knowledge,improve the rehabilitation effect of patients,and it is worth of popularizing.

Objective To study nursing of ureteral calculi patients treated by holmium laser lithotripsy by ureteral soft mirror under general anesthesia.Methods A total of 118 patients with ureteral calculi in our hospital were randomly divided into control group and observation group according to the double blind number method,all patients carried out general anesthesia by soft ureteral holmium laser lithotripsy,the control group was given routine nursing care and the observation group was given intensive care.And the nursing results of patients were statistically analyzed.Results The observation group had higher one-time success rate of clear stone than the control group (91.53％ vs.81.36％,P ＜ 0.05);The incidence rates of complications in the observation group was 3.39％,which was significantly lower than 8.47％ in the control group(P ＜0.05).The hospitalization time,SDS score,VAS score and SAS score of the observation group were significantly better than that of the control group (P ＜ 0.05).The observation group had significantly higher related knowledge and treatment compliance than that in the control group(88.14％,91.53％ vs.76.27％,74.58％,P ＜0.05).Conclusion Holmium laser lithotripsy by ureteral soft mirror under general anesthesia can strengthen treatment cooperation,the awareness of related disease knowledge,improve the rehabilitation effect of patients,and it is worth of popularizing.