2.Expression of recombinant human acetylcholinesterase and its application in screening its inhibitors.
Xiang-Jun WANG ; Huai-Xiu WU ; Shan-Shan YE ; Lan-Ying PAN ; Yong-Chang QIAN
Acta Pharmaceutica Sinica 2014;49(1):50-54
This study is designed to obtain recombinant human acetylcholinesterase (rhAChE) and apply it in screening acetylcholinesterase inhibitors. The rhAChE was overexpressed in HEK293 cells transfected by plasmid of pCMV-AChE with the cationic liposome and rhAChE was found to be secreted into cell culture medium. AChE activity was assayed according to modified Ellman method to obtain kinetic parameters. IC so50 values for donepezil compounds of rhAChE were calculated to determine their activities of inhibition. The results showed that Km value was 151.9 micromol.L-1 donepezil inhibited rhAChE in a mixed competitive-noncompetitive way (Ki= 16.03 nmol.L-1, Ki = 18.36 nmol.L-1) and that most new compounds tested exhibited high activities of inhibition on rhAChE. The study suggests that rhAChE is available to be applied in screening AChE inhibitors in vitro.
Acetylcholinesterase
;
genetics
;
metabolism
;
Cholinesterase Inhibitors
;
analysis
;
pharmacology
;
HEK293 Cells
;
Humans
;
Indans
;
analysis
;
pharmacology
;
Inhibitory Concentration 50
;
Kinetics
;
Piperidines
;
analysis
;
pharmacology
;
Plasmids
;
Recombinant Proteins
;
genetics
;
metabolism
;
Transfection
3.The safety and efficacy of radiofrequency ablation for treating large hepatic hemangiomas
Shaohong WANG ; Jun GAO ; Shan KE ; Xuemei DING ; Yiming ZHOU ; Xiaojun QIAN ; Wenbing SUN
Chinese Journal of General Surgery 2014;29(3):172-176
Objective To assess the safety and efficacy of radiofrequency ablation (RFA) for the treatment of large (≥5 cm in diameter) hepatic hemangiomas.Methods Clinical data of 50 patients with large hepatic hemangiomas (≥5 cm in diameter) treated with RFA between October 2007 and December 2012 were analyzed.Patients were divided into two groups (5-10 cm and ≥ 10 cm) according to tumor size.Results Thirty-two patients had 36 hemangiomas of 5-10 cm in diameter and 18 patients had 19 hemangiomas of ≥ 10 cm in diameter.Technical success,complications related to RFA,completed ablation,symptom relief,change in size of ablation zone and recurrence of the residual tumor were analyzed.The average diameters of the two groups were 7.1 ± 1.2 cm and 13.2-± 2.4 cm separately (t =-12.57,P < 0.01) ; the technical achievement ratios of the two groups were both 100% ; Seven of 32 patients with hemangiomas 5-10 cm and all the 18 patients with hemangiomas ≥ 10 cm had 13 and 61 complications related to RFA,the incidence of complications were 21.88% and 100% respectively (x2 =28.13,P < 0.01); 94.55% hemangiomas (52/55) acquired complete ablation,the complete ablation rates of 5-10 cm hemangiomas and ≥10 cm hemangiomas were 100% (36/36) and 84.21% (16/19) respectively (P =0.014).The mean diameters of ablation zone were respectively decreased to 5.3 ± 1.0 cm and 10.62±1.8 cm (t =-14.30,P <0.01).Conclusions RFA for hepatic hemangiomas 5-10 cm in diameter is safe and effective; while its complication for ablation of hemangiomas ≥ 10 cm is high.
4.Focal Nodular Hyperplasia of the Liver: MR and CT Appearances (An Analysis of 6 Cases
Su LI ; Jianmin XU ; Jun SHAN ; Li QIAN ; Huiling HE ; Weiwen QIU
Journal of Practical Radiology 2001;17(4):281-283
Objective To evaluate the MR imaging and CT appearances of focal nodular hyperplasia (FNH) of the liver and improve the accuracy of diagnosis in FNH. Methods 6 patients with solitary FNH underwent MR exiamnation. Dynamic Gd-DTPA enhancement were performed in all the lesions. Of the 6 patients, three underwent CT plain and dynamic contrast scan; one underwent CT plain scan. More attention was payed to the atypical appearances. Results Atypical lesion appearances ineludod:apparent hypointensity on T1 WI and hyperintensity on T2WI,diffusly heterogeneous enhancement in arterial phase, pseudocapsule enhancement in delayed phase;the dynamic contrast MR and CT appearance in each phase were not all similar. Conclusion MR and CT especially dynamic contrast enhancemenl is of great value to the diagnosis of FNH. The atypical appearances of FNH shoud keep in mind to avoid misdiagnosis.
5.Study of the antiulcer effect of pantoprazole
Ying-Xin WANG ; Xiao-Qiang LI ; Guang-Wu WU ; Shan-Jun QIAN ; Hong LEI ; Chang CAO ;
Chinese Journal of Clinical Pharmacology and Therapeutics 1999;0(04):-
Aim To evaluate the effects of pantoprazole on various experimental acute ulcer inrats and mice. Methods The model of a gastric ulcer of rats or mice was caused bystree- induced ulcer and ligatel pylurus-induced ulcer. Results & Conclusions At adose of 5, 10, 20 mg? kg-1 of Pantoprazole can markedly decrease the ulcer index ofstree-induced ulcer. Pantoprazole(4, 8, 16 mg? kg -1 ) significantly decrease the areaof ligated pylorus-induced gastric ulcer. It was also found that pantoprazole caninhibit the output of basic gastric acid.
7.Pregnancy outcome among patients with chronic myelogenous leukemia treated with tyrosine kinase inhibitors.
Qian JIANG ; Bin JIANG ; Shan-shan CHEN ; Hao JIANG ; Ya-zhen QIN ; Yue-yun LAI ; Hong-xia SHI ; Xiao-jun HUANG
Chinese Journal of Hematology 2012;33(1):6-9
OBJECTIVETo observe the pregnancy outcome among patients with chronic myelogenous leukemia (CML) treated with tyrosine kinase inhibitors (TKIs).
METHODSData associated with pregnancy, delivery and neonate from the patients or patient's spouse who conceived while receiving TKIs were collected retrospectively.
RESULTSTwo young female patients (who had been on imatinib therapy for 90 and 91 months, respectively) and spouses of 10 male patients (involving 7 patients who had received imatinib for a median of 60 months and 3 who had received dasatinib for 2.5 months to 7 months, respectively) with median age of 33.5 years (range 26 - 46 years) conceived and gave birth to 12 babies. One woman took imatinib throughout her pregnancy except one month. The other one took imatinib throughout her pregnancy and had breast-fed while on imatinib therapy for nearly half a year postpartum. Among the 12 babies, one was born prematurely with low birth weight and hypospadias (surgical repair after birth), the others were all healthy with no congenital defects. The median age of the children at the date of this report is 17.5 months (range 3 to 101 months), and they all have a normal pattern of growth and development.
CONCLUSIONSConception among patients with CML while receiving TKIs may result in normal pregnancies. The possible effects of TKIs on birth abnormalities cannot be ruled out. It is recommended that childbearing female patients should be advised to practice adequate methods of contraception and should not breast-feed while on TKIs therapy. In cases of accidental pregnancy, risk/benefit evaluations must be carried out carefully on an individual basis. No special precautions apply for male patients being treated with imatinib.
Adult ; Antineoplastic Agents ; therapeutic use ; Benzamides ; Dasatinib ; Female ; Humans ; Imatinib Mesylate ; Infant ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive ; drug therapy ; Male ; Middle Aged ; Piperazines ; therapeutic use ; Pregnancy ; Pregnancy Outcome ; Protein Kinase Inhibitors ; therapeutic use ; Protein-Tyrosine Kinases ; antagonists & inhibitors ; Pyrimidines ; therapeutic use ; Retrospective Studies ; Thiazoles ; therapeutic use ; Treatment Outcome
8.Effects of ginsenoside Rb1 on the oxidative stress in the skeletal muscles of rats with postoperative fatigue syndrome.
Shan-Jun TAN ; Zhen YU ; Qian-Tong DONG
Chinese Journal of Integrated Traditional and Western Medicine 2012;32(11):1535-1538
OBJECTIVETo observe the effects of ginsenoside Rb1 (GRb1) on the oxidative stress in the skeletal muscles of rats with postoperative fatigue syndrome (POFS) and to study its anti-fatigue mechanisms.
METHODSThe POFS model was established using resection of 70% of mid-small intestine. Ninety-six Sprague-Dawley (SD) rats were screened using grasping test. The rats were randomly divided into the control group, the model group, and the GRb1 treated group (at 10 mg/kg) by the body weight. The maximum grip strength of rats was detected on the 1st, 3rd, 7th, and 10th day after operation, respectively. The contents of malondialdehyde (MDA), the activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-PX) were detected.
RESULTSCompared with the model group, the maximum grip strength was obviously enhanced on the postoperative day 7 and 10 (P < 0. 05), the MDA content obviously decreased on the postoperative day 3 and 7 (P < 0.05), the SOD activity obviously increased in the GRb1 treated group (P < 0.05). There was no obvious change in the activities of CAT and GSH-PX among the three groups at each time point (P > 0.05).
CONCLUSIONGRb1 could reduce the oxidative stress injury in the skeletal muscles, improve the activities of antioxidant enzymes, and enhance the functions of the skeletal muscles in POFS rats, which may be important reasons for fighting against POFS.
Animals ; Catalase ; metabolism ; Fatigue ; etiology ; metabolism ; Ginsenosides ; pharmacology ; Glutathione Peroxidase ; metabolism ; Male ; Malondialdehyde ; analysis ; Muscle, Skeletal ; drug effects ; metabolism ; Oxidative Stress ; drug effects ; Postoperative Period ; Rats ; Rats, Sprague-Dawley ; Superoxide Dismutase ; metabolism
9.In vitro and in vivo MR imaging of SHU 555A-labelled swine bone marrow mesenchymal stem cells
Zhe-Yong HUANG ; Jun-Bo GE ; Shan YANG ; Shao-Heng ZHANG ; Rong-Chong HUANG ; Meng-Su ZENG ; Hang JIN ; Ai-Jun SUN ; Ju-Ying QIAN ; Yunzeng ZOU ;
Journal of Interventional Radiology 1994;0(02):-
Objective To detect the feasibility of magnetically labeled swine bone marrow mesenehymal stem cells(MSCs)with SHU 555A combined with poly-L-arginine(PLL),under MR imaging in vitro and in vivo.Methods Swine mesenehymal stem cells were isolated and culture-expanded 3 passages in vitro,then magnetically labeled by incubation with SHU 555A(25?g Fe/ml,Resovist,Schering)for 24 hours with 750 ng/mL poly-L-lysine(PLL;average MW_275 kDa)added 1 hour before incubation.Cellular iron incorporation and detention at 0 d,4 d,8 d,12 d,16 d,20 d after labeling was qualitatively assessed using Prussian blue and quantified at atomic absorption spectrometry.Cell viability was assessed by trypan-blue exclusion test.Cell suspensions underwent MR imaging with T_1-and T_2-weighted spin-echo and fast field-echo sequences on a clinical 1.5 T MR system.At last,1?10~6 SHU 555A labeled and unlabeled MSCs were transextracardially implanted into the infracted and normal myocardium approximately 2 week following the ligation of left anterior descending coronary artery in 1 swine respectively,and finally performed 1.5-T MRI within 1 week after infarction.Results①Intracytoplasmic particles stained with Prussian blue stain were detected for all cells with mean cellular iron content of(13.13?2.30)pg per cell.With division of stem cells, the stained particles decreased gradually with iron content(0.68?0.20)pg per cell.at 16 days after labeling, approximately to the prelabeled baseline values.(0.21?0.06)pg per cell(P>0.05).The viability of the labeled cells at various time points were not significantly different with that of nonlabeled cells(P>0.05).②MR images showed signal intensity changed most obviouly in T2*WI in vitro.The percentage change of signal intensity increased with increasing cell numbers,and decreased with the time.As few as 5?10~4-1?10~5 cells could be detected by using this approach.③Two injected sites containing MR-MSCs were detected in vivo,presentingas low signal intensity areas with the T_2*WI scanning sequence.Conclusion Swine bone marrow MSCs can be labeled with SHU555A-PLL and depicted with a standard 1.5-T MR imager in vitro and in vivo.(J lntervent Radiol,2007,16:115-121)
10.Repair of hard cleft palate with absorbable membranes made by poly-DL-lactic acid: a feasibility study.
Wan-shan LI ; Shi-cheng WEI ; Qian ZHENG ; Xiao-jun ZHANG ; Qiu NING ; Cheng-dong XIONG
West China Journal of Stomatology 2004;22(2):132-134
OBJECTIVETo investigate the feasibility and clinical results of applying poly-DL-lactic acid (PDLLA) biomembranes in cleft palate repair.
METHODS68 cleft palate patients were divided into study group and control group. The traditional surgical method was used to control group to close the soft cleft palate, and the PDLLA biomembrane was used to study group and implanted into the surgical gap between the periosteum and bone at the hard palate, and fixed with suture. The duration, blood loss at operation, post-operative complication, wound healing and recovery were recorded and compared to conventional cleft palate repair.
RESULTSOperations were successfully completed on all 34 patients. Wound healing of soft palate and uvula was uneventful with no incidence of fistula or dehiscence. The primary healing on tissue defect of hard palate occurred in 29 patients, secondary healing occurred in 3 patients, permanent fistula between the oral cavity and the nasal cavity occurred in only one patients, and 3 patients left over fistula on alveolar process. Compared to traditional cleft palate repair, blood loss and incidence of fistula on alveolar process were decreased; the average surgical time was 89.25 minutes and was not prolonged; and there was no significant increase in post-operative complication.
CONCLUSIONHard cleft palate repair with PDLLA biomembranes is safe, simple and practical with good clinical results and is beneficial to minimize the bad influences towards the development and growth for maxilla of cleft palate patients.
Absorbable Implants ; Adolescent ; Adult ; Child ; Child, Preschool ; Cleft Palate ; surgery ; Feasibility Studies ; Female ; Guided Tissue Regeneration ; methods ; Humans ; Lactic Acid ; therapeutic use ; Male ; Maxillofacial Development ; Palate, Hard ; surgery ; Polyesters ; Polymers ; therapeutic use ; Reconstructive Surgical Procedures