The work aims to study the drug metabolizing enzymes involved in the metabolism of butylphthalide and evaluate the induction and inhibition activities of butylphthalide on CYP450 isoenzymes by using in vitro (liver microsome incubation system of rats and human) and in vivo (CYP induced model of rats) method. Butylphthalide was incubated with selective inhibitors of CYP450, and its metabolic rate was determined to identify the metabolizing isoenzymes of NBP in rat (normal and induced rats) and human liver microsomes. The in vitro inhibition effect of butylphthalide on 6 main liver microsomal CYP450 isoenzymes was evaluated by using probe drugs; the induction and inhibition activities in vivo of butylphthalide on CYP450 isoenzymes were evaluated by NBP ig dosing (160 mg x kg(-1)) and iv dosing (20 mg x kg(-1)) in rats. After adding the specific inhibitors of CYP2C11, 2E1 and 3A 1/2 for rat, CYP2C19, 2E1 and 3A4/5 for human, the metabolism of NBP in rat and human liver microsomes were reduced 38.8%, 86.2%, 78.4% and 51.0%, 92.0%, 58.9% of control, respectively. The metabolic rates of NBP in CYP2E1 and 3A 1/2 induced rat liver microsomes were increased 25.5% and 68.9%. High concentration of NBP (≥ 200 μmol x L(-1), in vitro) could inhibit the activities of CYP1A2, 2C6, 2C11 and 2D2 in rats, and high concentration of NBP ( ≥ 15 μmol x L(-1), in vitro) could inhibit the activity of CYP2C19 in human. All the results indicated that NBP should be mainly metabolized by CYP2E1, 2C11 and 3A 1/2 in rats and CYP2E1, 2C19 and 3A4/5 in human. High concentration of NBP could inhibit human CYP2C19 in vitro. No significant induction/inhibition effects of NBP were observed on rat liver CYP450 isoforms after ig 160 mg x kg(-1) NBP or iv 20 mg x kg(-1) NBP.

Object In order to obtain further evidence of therapeutic efficacy of sophoramine (SA) *, its effect on transplantation rejection was studied with simultaneous exploration of its mechanism of action Methods Number of T lymphocyte and its sub sets of skin allografted rat model were determined by immunofluorescence technique, and proliferation of T lymphocyte was assessed by thiazolyl blue (MTT) assay Results SA reduced the CD 3 and C 4 cell counts, lowered CD 4/C 8 ratio, inhibited T lymphocyte proliferation and prolonged the survival time of skin allografted rat Conclusion SA could inhibit transplantation rejection by inhibiting the function of T lymphocyte with simultaneous reduction of lymphocyte count

Objective To investigate the relationship between the matrix metalloproteinase-3(MMP-3)and the stability of carotid artery plaque,and explore MMP-3's prediction role on the attack and relapse of acute ischemic cerebrovascular events.Methods 100 patients with the first ever acute cerebral infarction,100 patients with chronic cerebral circulation insufficiency(CCCI)and 40 persons without cerebrovascular diseases were enrolled in this study.According to the carotid ultrasound examination,100 cerebral infarction patients were divided into three subgroup: unstable plaque group(45 patients,mixed plaque,soft plaque),stable plaque group(35 patients,plaque Group)and endometrial coarse group(25patients).Matrix metalloproteinase-3(MMP-3)levels of all the subjects were measured by enzyme-linked immunosorbent assay(as basal level).All the subjects were followed up for one year to observe cerebral infarction events.Serum MMP-3 levels of each group,and the basic serum MMP-3 levels were compared among patients who were attacked or relapsed cerebral ischemic with those who had not been attack cerebral ischemic during this period of time.Results 5 patients in the cerebral infarction group had relapse (5%),2 patients in the CCCI group were attacked by cerebral ischemic(2%),and no one in the normal control group was attacked by cerebral ischemic.Serum MMP-3 levels in the acute cerebral infarction group were significantly higher than CCCI group,and both groups were significantly higher than normal control group (P ＜0.05).The basic serum MMP-3 levels in all patients who were attacked by cerebral ischemic were significantly higher than those who had not been attack by cerebral ischemic during this period of time(P ＜0.05).The serum MMP-3 levels of the unstable plaque group were significantly higher than stable plaque group.And both groups were significantly higher than endometrial coarse group(P ＜0.05).Conclusions Elevated levels of matrix metalloproteinase-3(MMP-3)might have something with the stability of carotid atherosclerotic plaque,and participate the attack and the relapse of acute cerebral infarction.Determination of MMP-3 might be used to predict the attack and relapse of acute cerebral infarction.

The work aims to study the drug metabolizing enzymes involved in the metabolism of butylphthalide and evaluate the induction and inhibition activities of butylphthalide on CYP450 isoenzymes by using in vitro (liver microsome incubation system of rats and human) and in vivo (CYP induced model of rats) method. Butylphthalide was incubated with selective inhibitors of CYP450, and its metabolic rate was determined to identify the metabolizing isoenzymes of NBP in rat (normal and induced rats) and human liver microsomes. The in vitro inhibition effect of butylphthalide on 6 main liver microsomal CYP450 isoenzymes was evaluated by using probe drugs; the induction and inhibition activities in vivo of butylphthalide on CYP450 isoenzymes were evaluated by NBP ig dosing (160 mg x kg(-1)) and iv dosing (20 mg x kg(-1)) in rats. After adding the specific inhibitors of CYP2C11, 2E1 and 3A 1/2 for rat, CYP2C19, 2E1 and 3A4/5 for human, the metabolism of NBP in rat and human liver microsomes were reduced 38.8%, 86.2%, 78.4% and 51.0%, 92.0%, 58.9% of control, respectively. The metabolic rates of NBP in CYP2E1 and 3A 1/2 induced rat liver microsomes were increased 25.5% and 68.9%. High concentration of NBP (≥ 200 μmol x L(-1), in vitro) could inhibit the activities of CYP1A2, 2C6, 2C11 and 2D2 in rats, and high concentration of NBP ( ≥ 15 μmol x L(-1), in vitro) could inhibit the activity of CYP2C19 in human. All the results indicated that NBP should be mainly metabolized by CYP2E1, 2C11 and 3A 1/2 in rats and CYP2E1, 2C19 and 3A4/5 in human. High concentration of NBP could inhibit human CYP2C19 in vitro. No significant induction/inhibition effects of NBP were observed on rat liver CYP450 isoforms after ig 160 mg x kg(-1) NBP or iv 20 mg x kg(-1) NBP.
Animals ; Benzofurans ; pharmacology ; Cytochrome P-450 Enzyme Inhibitors ; pharmacology ; Cytochrome P-450 Enzyme System ; metabolism ; Humans ; Isoenzymes ; metabolism ; Liver ; metabolism ; Microsomes, Liver ; metabolism ; Rats

OBJECTIVETo evaluate the therapeutic effects of percutaneous kyphoplasty (PKP) for the treatment of osteoporotic vertebral compression fracture (OVCF) with degenerative scoliosis.

METHODSFrom March 2009 to March 2014,121 patients undergoing PKP for the treatment of osteoporotic vertebral compression fracture (OVCF) with degenerative scoliosis were retrospective analyzed. There were 41 males and 80 females,ranging in age from 56 to 92 years with an average of 73.2 years. Preoperative and postoperative 3 d respectively pain visual analogue scale (visual analogue score, VAS) and Oswestry Disability Index assessed pain and functional recovery of patients and preoperative and postoperative 3 d lumbar lordosis, scoliosis Cobb angle were analyzed.

RESULTSAll the patients were followed up, and the duration ranged from 6 to 24 months, with a mean time of 11 months. All the patients achieved success in operation without serious complications. The operation time ranged from 30 to 65 min with an average of 42.2 min. Local leakage of bone cement was not found in canal. The VAS and Oswestry Disability Index at the 3rd day after operation decreased significantly compared with those of the preoperative (P < 0.05), and the lumbar lordosis and scoliosis Cobb angle also improved significantly compared with those of the preoperative (P < 0.05).

CONCLUSIONPercutaneous kyphoplasty (PKP) for the treatment of thoracolumbar scoliosis osteoporotic fracture can significantly improve patients spinal deformity, pain relief, which is worth of recommending.

Aged ; Aged, 80 and over ; Female ; Fractures, Compression ; surgery ; Humans ; Kyphoplasty ; methods ; Male ; Middle Aged ; Osteoporotic Fractures ; surgery ; Scoliosis ; surgery ; Spinal Fractures ; surgery ; Visual Analog Scale

Objective To evaluate the uncertainty of the pseudo-ginsenoside GQ (PGQ) concentration in human plasma by HPLC-MS/MS.Methods The whole process of PGQ determination by HPLC-MS/MS in human plasma was evaluated and the uncertainty caused by repeatability,weighing,standard solution preparation,biological sample preparation,extraction recovery process,recovery,instrument precision and calibration curve fitting were evaluated,respectively.The combined and expanded uncertainty values were both calculated.Results The expanded uncertainty values for low (15.16 ng·mL-1),medium (2 516.67 ng·mL-1) and high (3 902.00 ng·mL-1) levels of PGQ were 1.39,177.74 and 262.69 ng·mL-1,respectively (P =95 ％,k =2).Conclusion The uncertainty of the PGQ determination in human plasma by HPLC-MS/MS is mainly caused by recovery,repeatabihty and sample preparation at low concentration,by sample preparation and recovery at medium and high concentration.

Methods The clinical data of 4445 cases (5 530 hernias) who underwent LIHR at Ruijin Hospital from Jan 2001 to Dec 2015 were analyzed retrospectively.2 125 cases underwent 2 402 trans-abdominal preperitoneal procedure(TAPP),2 306 cases did 2 907 totally extraperitoneal (TEP),and 21 IPOMs in 20 cases.There were 3 216 indirect hernias (60.3％),1 164 direct hernias (21.8％),399 recurrent hernias (7.5％),479 complex hernias (9.0％),and 72 femoral hernias (1.4％).The median time of follow-up is 51 months with a range between 7 and 187 months.Results The average operation time was 27.1 ± 8.7 min for unilateral hernia repair,and 43.0 ± 11.0 min for bilateral hernia repair.The average hospital stay was 1.4 ± 1.1 d.There were 250 seroma (4.7％),68 urinary retention (1.3％),23 transient neuropraxia (0.4％) and 3 paralytic obstruction of intestines (0.1％).Severe complications included 1 port site hernia,1 intestinal injury,and 1 mechanical intestinal obstruction.After a medium follow-up of 51 months,there were 13 recurrent cases (0.24％),including 5 cases after TAPP,7 after TEP,1 after IPOM.Conclusion LIHR is a safe and efficient technique for hernia repair.

Objective To explore the clinical value of prospective electrocardiography-triggering high-pitch spiral acquisition by dual-source CT (HP mode ) in children with congenital heart diseases (CHD).MethodsThirty-six patients ( mean age:0.67 years,range:1 month to 2 years and 6 months; 25 males;mean weight:7.7 kg)underwent prospective ECG-triggering high-pitch spiral acquisition.The dose length product (DLP) was recorded to calculate effective dose ( ED ).Two experienced radiologists made diagnosis and assessed the overall image quality by a five-point scale independently.The consistency of their judgment was determined by Kappa statistics.Surgeries were performed in 29 patients,and conventional cardiac angiography(CCA) was performed in 7 patients.The accuracy,sensitivity and specificity of HP mode were calculated based on the surgical or CCA findings.ResultsThe DLP was (5.12 ± 1.64) mGy.cm with a range of 2.4 mGy · cm to 9.2 mGy · cm and ED was (0.125 ± 0.027 ) mSv ranging from 0.078 mSv to 0.179 mSv.The average subjective image quality score was 4.2 ± 0.7.All images were diagnosable.Two radiologists made good agreement ( K =0.774,P ＜ 0.05 ).The accuracy,sensitivity and specificity of HP mode were 98.9％,94.2％ and 99.8％,respectively.ConclusionLow radiation dose with the accurate diagnosis of anomalies makes HP mode a new choice for children with CHD.

Objective To evaluate the diagnostic value of cardiac magnetic resonance (CMR) in suspected coronary heart disease patients with electrocardiogram abnormalities but normal coronary angiography. Methods The data of 25 suspected coronary heart disease patients with electrocardiogram abnormalities but normal coronary angiography were collected from Taiyuan central hospital between October 2010 and April 2012. Comparison was done in terms of anterior interventricular septal thickness, left ventricular posterior wall thickness, left ventricular end diastolic dimension, left ventricular end systolic dimension, left atrial diameterand ejection fraction measured by CMR and by UCG. Correlation of the aboved paremeters between the 2 imaging exams. Results 40%of patients had their diagnosis changed after CMR exam, 32%of the patients with adjusted assessment. The differences in anterior interventricular septal thickness, left ventricular posterior wall thickness, left ventricular enddiastolic dimension, left ventricular end systolic dimension, left atrial diameter, ejection fraction by CMR and by UCG were similar (P>0.05) with positive correlation (P<0.01). Conclusions CMR can provide diagnosis and evaluation information to chest pain patients with ECG abnormalities but normal CAG, and it is a good supplement for routine examination.

As a renewable clean energy,biodiesel has been the subject of much research in recent years owing to its excellent environmental performance.The bio-enzymatic method possesses unparalleled advantages over conventional chemical catalysis,and it would be the direction in biodiesel industrialization process.The progress and application of three biocatalytic approaches for biodiesel production including immobilized lipase,free lipase and whole-cell catalysis were summerized.Finally,the challenges of biodiesel industrialization in China are analyzed,and some effective measures are put forward.