OBJECTIVE:To establish a method for determining the plasma concentration of paeoniflorin and phillyrin and phar-macokinetic study before and after intragastric administration of Qianliean granules. METHODS:LC-MS/MS method was adopted. The column was Waters C18 with mobile phase consisted of acetonitrile(A)-2 mmol/L ammonium acetate(containing 0.05% formic acid)(B)(0-9 min:15%A→50%A;9-11 min:50%A→90%A;11-17 min:90%A;17-19 min:90%A→15%A;19-20 min:15%A),at the flow rate of 0.6 ml/min;column temperature was 35 ℃ and the volume was 20 μl;quantitative ions were paeoniflorin m/z 525.2 → m/z 449.0,phillyrin m/z 552.3 → m/z 355.3. 7 SD male rats were docked to collect blood 0.5 ml from angular vein 0.25,0.5,0.75,1,1.5,2,3,4,6,8,10,12,24 h after administration Qianliean granule solution 1 g(medicinal materials)/kg to determine the blood concentration of drugs. DAS 2.1.1 software was employed to calculate pharmacokinetic parameters. RE-SULTS:The linear range of paeoniflorin and phillyri were 5.0-2500.0 μg/L(r=0.9979)and 2.0-2000.0 μg/L(r=0.9982),re-spectively;RSD of precision test was less than 5.5%(n=5);the method recovery were 96.0%-104.0% and 92.0%-107.0%,the extration recovery were 71.4%-83.5% and 81.5%-92.3% and RSD of stability test was less than 5.0%(n=3). The pharmacokinet-ic parameters of paeoniflorin and phillyrin were as follows as t1/2 of (2.206 ± 0.631) and (1.355 ± 0.317) h;cmax of (1504.069 ± 620.885) and (79.043 ± 15.568)μg/L;tmax of (1.000 ± 0.250) and (1.214 ± 0.267) h;AUC0-24 h of (4897.645 ± 2207.577) and (263.475±54.795)μg·h/L;CL of(5.025±2.773)and(76.253±13.986)L/(h·kg). CONCLUSIONS:The method is highly sensi-tive,exclusive,simple,accurate and reliable,and can be applied to study the pharmacokinetic characteristics of paeoniflorin and phillyrin in rats in vivo.

Objective To investigate the clinical efficacy of fluoroscopy-guided intestinal adhesion lysis, as a new non-surgical method, in treating incomplete adhesive small intestinal obstruction in order to improve the therapeutic results of adhesive intestinal obstruction. Methods A total of 93 patients with incomplete adhesive small intestinal obstruction were enrolled in this study. The patients were divided into study group (n=49) and control group (n=44). Fluoroscopy-guided intestinal adhesion lysis together with restoration of inter-intestinal loop enterocele was carried out for the patients of the study group , while traditional conservative surgical therapy was employed for the patients of the control group. The study group was comparable with the control group in patients’ age, gender, medical history, disease course, X-ray findings, etc. Results Of the 49 cases in the study group, complete cure was obtained in 40 with a cure rate of 81.6%. The mean hospitalization day was 0.3 day, and the average operation time was 3.25 hours. Among the 44 patients in the control group, complete cure was obtained in 37 with a cure rate of 84.1%. The mean hospitalization day was 7.6 days, and the average therapeutic time was 183.26 hours. Conclusion For the treatment of incomplete adhesive small intestinal obstruction , the therapeutic efficacy of fluoroscopy-guided intestinal adhesion lysis together with restoration of inter-intestinal loop enterocele is better than that of traditional conservative surgical therapy.

Matrine is one of the main active components extracted from Sophora flavescens, S. subprostrata and S. alopecuroides. In recent years, its anti-tumor activity has attracted wide attention. According to studies, matrine shows the anti-tumor effect through multiple channels such as inducing apoptosis and autophagy of cancer cells, arresting cell cycle, inhibiting tumor cell migration, angiogenesis and NF-kappaB, as well as the synergistic effect with chemotherapeutics. Along with the further studies on matrine's anti-tumor mechanism, it has a broad prospect for development and application in tumor clinical treatment.
Alkaloids ; pharmacology ; Animals ; Antineoplastic Agents, Phytogenic ; pharmacology ; Cell Cycle ; drug effects ; Cell Proliferation ; drug effects ; Gene Expression Regulation, Neoplastic ; drug effects ; Humans ; Neoplasms ; drug therapy ; genetics ; metabolism ; Quinolizines ; pharmacology

The study aims to investigate the effect of the compatibility of paeonol and paeoniflorin(hereinafter referred to as the compatibility) on the expression of myocardial proteins in rats with myocardial ischemia injury and explore the underlying mechanism of the compatibility against myocardial ischemia injury. First, the acute myocardial infarction rat model was established by ligation of the anterior descending branch of the left coronary artery. The model rats were given(ig) paeonol and paeoniflorin. Then protein samples were collected from rat cardiac tissue and quantified by tandem mass tags(TMT) to explore the differential proteins after drug intervention. The experimental results showed that differential proteins mainly involved phagocytosis engulfment, extracellular space, and antigen binding, as well as Kyoto encyclopedia of genes and genomes(KEGG) pathways of complement and coagulation cascades, syste-mic lupus erythematosus, and ribosome. In this study, the target proteins and related signaling pathways identified by differential proteomics may be the biological basis of the compatibility against myocardial ischemia injury in rats.
Acetophenones ; Animals ; Glucosides ; Monoterpenes ; Myocardial Ischemia/genetics* ; Myocardial Reperfusion Injury ; Proteomics ; Rats ; Rats, Sprague-Dawley

BACKGROUND:According to the thrust of document issued by State Drug Administration, the clinical experiment was carried onfufang duzhongjiangu keli (compound) (Bo Si Zhuang) in treatment of knee joint osteoarthritis.OBJECTIVE: To evaluate the improvement of the compound in treatment of knee joint osteoarthritis and its safety.DESIGN: Zhuanggu guanjie wan (bolus) was taken as controlled drug and double blind, double-simulation randomized method was designed.SETTING: Fujian Institute of Chinese Medicine, Guananmen Hospital of China Academy of Traditional Chinese Medicine, Institute of Orthopedics and Traumatology of China Academy of Traditional Chinese Medicine and Beijing Hospital of Chinese Medicine.PARTICIPANTS: Clinical experiment Ⅱ was performed since December 19, 1999, in which, 200 cases of knee joint osteoarthritis were observed and divided into compound group (100 cases) and bolus group (100 cases).From December 1999 to March 2000, clinical experiment Ⅲ was performed to observe 400 cases of knee joint osteoarthritis, in which, 300cases were divided in compound group and 100 cases in bolus group. All of cases were diagnosed by X-ray test and differentiated in Chinese medicine as insufficiency of liver and kidney and stasis of tendons and vessels. All of patients were in the known of experiment.METHODS: In compound group, fufang duzhong zhuanggu keli (1bag/time, 3 times/day) + simulated dosage of zhuanggu guanjie wan were administrated. In bolus group, fufang duzhong zhuanggu keli simulated dosage + zhuanggu guanjie wan (1bag/time, twice/day) were administrated.Double blind and double-simulation randomized control experiment was given in one-month treatment to observe clinical therapeutic effects.MAIN OUTCOME MEASURES: Evaluation on clinical indexes of joint function ,clinical therapeutic effect, syndrome score in Chinese medicine and adverse reaction.RESULTS: Totally 600 cases employed had all accomplished datum collections, no dropped-off case. ① The total effective rate of compound group was superior remarkably to bolus group (92.%, 82%). ② The result of joint function in compound group was superior remarkably to that of bolus group. ③ Concerning to improvement of syndromes in Chinese medicine, the result in compound group was superior to that of bolus group (the decreased integrals were 7.03±3.38 and 5.43±3.16 respectively). ④No obvious harmful effect presented during experiment.CONCLUSION: Fufang duzhong jiangu keli improves the symptoms of osteoarthritis of knee safely and effectively.

BACKGROUND:Discectomy and pedicle fixation fusion are golden standard to repair lumbar degenerative disease, but the treatment would induce other complications such as degeneration of adjacent segments or severer pre-existing spinal degeneration. For the problem of lumbar fusion and fixation, lumbar elastic fixation has recently been a hot focus. ＜br> OBJECTIVE:To evaluate the short-term effectiveness of dynamic lumbar pedicle fixation in repair of lumbar spinal stenosis and lumbar disc herniation. ＜br> METHODS:From December 2010 to December 2012, 62 cases of lumbar spinal stenosis and lumbar disc herniation treated with lumbar dynamic system were included. The involved segments included:5 cases at L 3/4 , 20 cases at L 4/5 , 20 cases at L 5 S 1 , 6 cases at double segment L 3/4 and L 4/5, 8 cases at double segment L 4/5 , L 5 S 1 , 3 cases at L 3/4 and L 5 S 1 . There were 34 males and 28 females with an average age of 50.8 years (range 32 to 72 years). According to different fixation systems, they were assigned to three groups:general dynamic lumbar fixation system in 17 cases, K-Rod posterior dynamic stabilization system in 28 cases, and Dynesys system in 17 cases. The fol ow-up time was from 24 to 48 months. Evaluation indexes included visual analogue scale, Oswestry disability index, imaging analysis and excellent and good rate of curative effects. ＜br> RESULTS AND CONCLUSION:Compared with before treatment, visual analogue scale score and Oswestry disability index were significantly improved at 6 months after treatment and final fol ow-up (P＜0.01). No apparent changes were detected in the length of inserted segments and adjacent segments before treatment and during final fol ow-up. There were no significant differences in the excellent and good rate in each group after treatment (P>0.05). These data indicated that the lumbar dynamic system was an effective option for lumbar disc herniation and spinal stenosis. Although there are some differences in the structure of three kinds of flexible fixation, no obvious difference in early therapeutic effects was detected. Long-term effects deserve further investigations.

Objective To investigate the quinolone resistance determinants in ciprofloxacin-resistant Acinetobacter bau-mannii (ABA)clinical isolates.Methods One hundred and fourteen ciprofloxacin-resistant ABA strains were collected from six Chinese hospitals .The quinolone resistance determining region ( QRDR) of 4 target genes ( gyrA, gyrB, parC and parE) was amplified , sequenced and compared with the reference genome of ATCC 17978 to identify possible resistance-related mutations.Nine plasmid-mediated quinolone resistance (PMQR) genes (qnrA, qnrB, qnrC, qnrD, qnrS, qepA, aac(6′)-Ⅰb-cr, oqxA and oqxB) were also amplified, and the amplicons were then sequenced to determine their character-istics.Results Almost all isolates (113/114, 99.1%) harbored a substitution in codon 83 of gyrA gene, leading to a Ser83Leu mutation.Meanwhile,58.8%(67/114) of the isolates possessed dual mutations of GyrA-Ser83Leu and GyrA-Ser80Leu, which were known determinants for ciprofloxacin resistance .There were also multiple non-synonymous substitu-tions in gyrB, leading to Arg393Ser, Arg393Cys, Thr401Ala, Pro406Ser, Val430Phe, Cys440Ser and Gly480Arg muta-tions with prevalence rates of 95.6%, 0.9%, 96.5%, 96.5%, 100%, 96.5%and 96.5%,respectively.For parE, all the seven mutations were synonymous and found in more than 96%of the tested isolates.For PMQR genes, although 83.3%(95/114) of the isolates were positive for aac(6′)-Ⅰb, nocrmutations were identified.None of the other eight PMDR genes were found in our strain collection .Conclusion Although multiple mutations are identified in gyrB and parE, these mutations might be the characteristic SNP markers for specific clones , unlikely linked to quinolone resistance .No PMQR is found in the tested isolates.Mutations in chromosomal QRDR (GyrA-Ser83Leu and ParC-Ser80Leu) are the main determi-nants of ciprofloxacin resistance in our ABA collection .

Objective　Acinetobacter baumannii (A. baumannii) is a commonly infective bacterium in the hospital. This study aims to analyze its molecular epidemiological characteristics, detect the carrying rate of efflux pump and regulatory protein genes, and investigate the effects of tigecycline on the efflux pump and expression of regulatory protein genes.　Methods　A total of 183 A. baumannii strains were collected from inpatients of the affiliated hospital of Jiangsu University from May 2017 to March 2019. They were divided into an antimicrobial-resistant group (one or more antimicrobial-resistant strains, 139 strains) and a sensitive group (the drugs in the drug sensitivity test were all non-resistant strains, 44 strains). Repeated sequence PCR was used for homology analysis of the strains, and pulse-field gel electrophoresis (PFGE) was used as the gold standard for homology analysis to verify and compare some strains. PCR was used to detect the occurrence of drug resistance-related genes. Based on homology analysis, efflux pump carrying rate detection and antibiotics sensitivity test results, 6 clinical strains carrying all efflux pump genes but different resistance phenotypes were selected as experimental strains, including sensitive strains (SAB), the multidrug resistance strain (MDRAB) and the extensively drug-resistant strain (XDRAB). All strains were induced in vitro with the minimum inhibitory concentration (MIC) of tigecycline. The induced strains were categorized as induction group, and the same strains cultured in LB agar without tigecycline was used as a control group. MIC was used to analyze the tigecycline susceptibility, and RT-qPCR was used to detect the gene expression of efflux pumps, such as TetB, AbaQ and regulatory proteins (AdeS and BaeS), in drug-resistant strains.　Results　Homology analysis showed that there were 45 clonal groups in the detected clinical isolates, with no obvious outbreak of epidemic clonal groups. Efflux pumps and regulatory proteins were widely distributed in the clinical isolates, and the expression of AdeB, TetB, AbeS, AdeS in MDRAB and XDRAB is significantly higher than that insensitive group SAB. Continuous in vitro induction with tigecycline could increase the antimicrobial resistance of some clinical strains and even significantly increase the expression levels of efflux pumps and regulatory proteins.　Conclusion　A. baumannii is widely distributed in the clinic, and efflux pumps and regulatory proteins might play an important role in drug resistance process. The unreasonable use of tigecycline could enhance the tolerance of A. baumannii by up-regulating the expression of some bacterial efflux pumps.

OBJECTIVEPatient with myocardial bridging (MB) usually has a benign prognosis, but some MB patients might experience myocardial ischemia, infarction and sudden cardiac death, especially during active physical activities. The purpose of the study was to study the stress-induced blood flow changes of the mural coronary artery in MB patients determined by intracoronary Doppler.

METHODSIn 8 patients with MB, the basic average peak velocity (bAPV), hyperemic average peak velocity (hAPV) of blood flow, coronary flow reverse (CFR) proximal and distal to the mural coronary artery were measured before and during intravenously dobutamine (10 microg kg-1 min-1, then add 10 microg kg-1 min-1 at 3 min interval till 40 microg kg-1 min-1) by intracoronary Doppler.

RESULTSThe baseline mural coronary diameter reduction was (51.7+/-21.4)% and significantly increased to (90.0+/-12.7)% (P<0.01) during dobutamine infusion. bAPV on the segments proximal and distal to the mural coronary artery significantly increased from (19.83+/-5.84) cm/s and (20.75+/-4.91) cm/s to (31.52+/-10.93) cm/s and (30.46+/-9.01) cm/s (all P<0.05 vs. baseline) respectively post dobutamine infusion. CFR measured at proximal and distal to myocardial bridging also significantly decreased from (2.91+/-0.62) and (2.46+/-0.82) to (2.17+/-0.66) and (1.83+/-0.51) (all P<0.01).

CONCLUSIONStress can significantly increase the compression of intramural coronary artery and reduce CFR on coronary segments both proximal and distal to the MB. Thus, active exercise might induce myocardial ischemia in patients with myocardial bridging.

Blood Flow Velocity ; Cardiotonic Agents ; pharmacology ; Coronary Circulation ; drug effects ; Coronary Vessel Anomalies ; physiopathology ; Coronary Vessels ; drug effects ; Dobutamine ; pharmacology ; Female ; Humans ; Male ; Middle Aged