1.Study on Radicamine A as a ?-glucosidase inhibitor
Chunyan LIU ; Aiguo MENG ; Huan ZHAN
Journal of Third Military Medical University 1983;0(04):-
Objective To study the inhibitory effect of radicamine A on ?-glucosidase and the glucose's absorption by small intestine.Methods Inhibitory effect of radicamine A was studied both in ?-glucosidase inhibition experiments and by a valgus cyst model of small in testine in vitro.Results Radicamine A inhibited ?-glucosidase and glucose's absorption in a dose-dependent manner(P
2.Crystal structure of SMU.2055 protein from Streptococcus mutans and its small molecule inhibitors design and selection.
Xiaodan CHEN ; Xiurong ZHAN ; Xinyu WU ; Chunyan ZHAO ; Wanghong ZHAO
West China Journal of Stomatology 2015;33(2):182-186
OBJECTIVEThe aim of this study is to analyze the three-dimensional crystal structure of SMU.2055 protein, a putative acetyltransferase from the major caries pathogen Streptococcus mutans (S. mutans). The design and selection of the structure-based small molecule inhibitors are also studied.
METHODSThe three-dimensional crystal structure of SMU.2055 protein was obtained by structural genomics research methods of gene cloning and expression, protein purification with Ni²⁺-chelating affinity chromatography, crystal screening, and X-ray diffraction data collection. An inhibitor virtual model matching with its target protein structure was set up using computer-aided drug design methods, virtual screening and fine docking, and Libdock and Autodock procedures.
RESULTSThe crystal of SMU.2055 protein was obtained, and its three-dimensional crystal structure was analyzed. This crystal was diffracted to a resolution of 0.23 nm. It belongs to orthorhombic space group C222(1), with unit cell parameters of a = 9.20 nm, b = 9.46 nm, and c = 19.39 nm. The asymmetric unit contained four molecules, with a solvent content of 56.7%. Moreover, five small molecule compounds, whose structure matched with that of the target protein in high degree, were designed and selected.
CONCLUSIONProtein crystallography research of S. mutans SMU.2055 helps to understand the structures and functions of proteins from S. mutans at the atomic level. These five compounds may be considered as effective inhibitors to SMU.2055. The virtual model of small molecule inhibitors we built will lay a foundation to the anticaries research based on the crystal structure of proteins.
Bacterial Proteins ; chemistry ; Cloning, Molecular ; Crystallization ; Crystallography, X-Ray ; Dental Caries ; Humans ; Streptococcus mutans ; chemistry ; X-Ray Diffraction
3.Literature Analysis of 66 Cases of Drug-induced Hyperkalemia
Xiaolei REN ; Yiqiu ZHAN ; Chunyan ZHANG ; Haiying ZHANG ; Wanyu FENG
China Pharmacy 2015;(20):2790-2792
OBJECTIVE:To investigate the characteristics and related factors of drug-induced hyperkalemia,present preven-tive measures and provide reference for the rational drug use. METHODS:46 literatures of individual cases and group cases of drug-induced hyperkalemia publicly reported in domestic medical journals from 1979 to 2014 were collected and analyzed statistical-ly,including 66 cases. RESULTS:66 cases with drug-induced hyperkalemia were mainly involved in cardiovascular drugs and im-munosuppressants. Most of them were improved after drug withdrawal and symptomatic treatment,and 2 cases died. CONCLU-SIONS:Drug-induced hyperkalemia are potentially dangerous. It is necessary to be vigilant,prevent and control timely and reduce the incidence of severe adverse reactions.
4.Effect of berberine on D-dimer, fibrinogen and interleukin-6 in peripheral blood of ovarian cancer patients
Lingye FAN ; Lei SHI ; Chunyan WANG ; Ping ZHAN ; Qianchuan REN
Chinese Journal of Biochemical Pharmaceutics 2015;(6):114-117
Objective To analyse the effect of berberine on D-dimer, fibrinogen (FIB) and interleukin-6(IL-6) in peripheral blood of ovarian cancer patients.Methods 130 cases selected from the hospital were diagnosed as unilateral ovarian cancer, treated by surgery and chemotherapy.The patients were divided into control group (25 cases) and experimental group (105 cases), and the experimental group were randomly divided into A, B, C three groups, 35 cases in each group.The experimental group received berberine hydrochloride tablets, orally, three times a day, on the basis of conventional chemotherapy.The experimental groups were divided into three subgroups according to the dosage: A group: 0.3 g, B group: 0.2 g, C group:0.1 g, 35 cases in each group, continuously treated for 2 weeks.The levels of D-dimer, FIB and IL-6 and quality of life score were detected before and after treatment.Results After treatment, D-dimer level in each subgroup of experimental group was lower than that in control group, respectively, and A group
5.Efficacy and Safety of Alprostadil Injection in Treatment of Viral Hepatitis:A Meta-analysis
Xiaolei REN ; Yiqiu ZHAN ; Zhen HE ; Haiying ZHANG ; Chunyan ZHANG ; Wanyu FENG
Herald of Medicine 2017;36(6):687-691
Objective To systematically evaluate the efficacy and safety of alprostadil injection in patients with viral hepatitis.Methods Medline,Embase,The Cochrane Library,CBMdisc,CNKI,Wanfang Database and VIP were searched.The quality of included studies such as randomization,blinding,allocation concealment and loss of follow-up were evaluated and meta-analysis was performed by RevMan5.1 software.Results In total,14 RCTs and 1 232 patients were included.Meta-analysis showed that in patients with viral hepatitis,the total effective rate of alprostadil injection treatment was significantly superior to that of conventional therapy (P<0.000 01).Serious adverse drug reactions (ADRs) induced by alprostadil injection were not reported.Conclusion Alprostadil injection is effective and safe for treating viral hepatitis.However,the evidence is not strong due to the generally low methodological quality of RCTs.Further high quality and large sample-sized randomized controlled trials and more pharmacoeconomics studies should be carried out.
6.Early evaluation of left ventricular global systolic function in patients with metabolic syndrome by three dimensional speckle tracking echocardiography
Lu CHEN ; Yue CHEN ; Jia ZHAN ; Lin CHEN ; Yinjia ZHANG ; Chunyan ZHONG ; Haier WANG
Chinese Journal of Ultrasonography 2013;22(10):843-846
Objective To assess the value of early evaluation of left ventricular global systolic function in patients with metabolic syndrome(MS) by three-dimensional speckle tracking echocardiography (3D-STI).Methods 33 healthy subjects and 41 MS subjects who didn't have the left ventricular remodeling were recruited in this study,and the myocardial motions were tracking by 3D-STI.The parameters of left ventricular global longitudinal peak systolic strain(LS),circular peak systolic strain(CS),radial peak systolic strain(RS) and area peak systolic strain (AS) and the values of body mass index (BMI),waist circumference,waist-to-hip ratio and biochemical indicators were compared between the two groups.Results Compared with controls,LS of MS group was significantly decreased (P < 0.01),while no significantly differences were found in CS,RS,and AS(P >0.05).The BMI,waist circumference and waist-to-hip ratio were positive correlated with LS (r =0.559,0.617,0.681,P <0.01).Conclusions 3D-STI could early evaluate the changes of left ventricular global systolic function for metabolic syndrome patients,and longitudinal peak systolic strain could be the most sensitive index.
7.Expression of LRP16 in human endometrial carcinoma tissues and its role on cell proliferation
Yujiao ZHANG ; Ling LIU ; Chunyan WANG ; Ping ZHAN ; Zonghui WU ; Wen HE ; Dingyu WANG
Chongqing Medicine 2013;(25):2983-2985
Objective To investigate the expression change of LRP16 in endometrial cancer tissues and its influence on the pro-liferation of human endometrial carcinoma HEC-1-B cells .Methods HEC-1-B cells were transfected with LRP16 .RT-PCR was used to examine the expression of LRP16 in 26 normal endometrium specimens ,10 endometrial cancer specimens .RT-PCR was used for verifying the transfection success .WES-T was used to observe the proliferation change of HEC-1-B cells .Results The positive expression rate and level of LRP16 mRNA in the endometrial cancer tissues were 83 .33% and 0 .82 ± 0 .21 ,which were significantly higher than 30 .00% ,0 .47 ± 0 .18 in the normal endometrium tissues(P<0 .05) .The RT-PCR detection results revealed that the expression of LRP16 mRNA after transfection was significantly increased .HEC-1-B cells in the transfection group could continued to proliferate in vitro ,but the proliferation capacity was not increased .Conclusion The expression abnormality of LRP16 may be closely related to the occurrence and progress of endometrial cancer ,LRP16 gene may have potential value for the endometrial canc-er gene therapy .
8.Expression of interleukin-18 and interleuldn-18 receptor a chain of the peripheral white blood cells in immune thrombocytopeula
Qian WANG ; Fengxia ZHAN ; Ningning SHAN ; Ming HOU ; Xiaojing YANG ; Nan LU ; Hongchun WANG ; Xiaolin ZHANG ; Xuebin JI ; Chunyan JI
Chinese Journal of Internal Medicine 2010;49(4):316-319
Objective To detect the expression of interleukin (IL)-18 of the peripheral blood cells and IL-18 receptor α chain(IL-18Rα) on the surface of CD_3~+ cells in patients newly diagnosed as immune thrombocytopenia (ITP) before medication and to explore the roles of IL-18 and IL-18Rα in the development of ITP. Methods Eighteen out-patients or inpatients with acute ITP accepting treatment in Qilu Hospital were enrolled in this study and 15 matching healthy subjects were taken as control. Plasma IL-18 level was detected with enzyme linked immunosorbent assay (ELISA), the expression of IL-18Rα on CD_3~+ lymphocytes and total lymphoeytes were measured with flow cytometry; T-bet and GATA-3 mRNA were measured with reverse transcriptase polymcrase chain reaction (RT-PCR). Results The expression of IL-18 in acute ITP plasma was (468. 57 ± 141.62) ng/L and IL-18Rα on the surface of CD_3~+ cells and lymphocytes were (8.50 ±3. 16)% and (9. 16±2.98)% respectively. The levels of IL-18 and IL-18Rα were increased in active ITP patients as compared with those in the controls (P <0. 05). The levels of IL-18 mRNA (0. 12 ±0. 02) and T-bet mRNA (0. 07 ±0. 02) were significantly increased in patients with active ITP as compared with those in the controls (P <0.05), while GATA-3 mRNA (0.0039±0.0014) were significantly decreased in patients with active ITP (P < 0. 05). The balance between T-bet and GATA-3 was significantly disturbed in ITP. Conclusions Through the variation of the levels of gene and protein, our study showed that IL-18 and IL-18Rα might upregulate the expression of Th1-cytokines in ITP patients. It is also suggested that IL-18 has potential association with the development of ITP. Especially, it may provide a new treatment method for ITP by regulating the ratio of T-bet and GATA-3 and resuming the balance of Th1/ Th2.
9.The construction and expression of phage display library of anti human lung adenocarcinoma monoclonal antibody 5F-11.
Wentao YUE ; Baitang LAI ; Hui WANG ; Xiuping ZHAN ; Chunyan ZHANG ; Xuehui YANG
Chinese Journal of Lung Cancer 2002;5(2):119-122
BACKGROUNDTo construct and express a phage display library of anti human lung cancer monoclonal antibody 5F-11.
METHODSImmunoglobulin variable regions (VH,VL) were amplified from 5F-11 hybridrom by RT-PCR. ScFv genes consisting of VH DNA and VL DNA joined together by a linker DNA were cloned into a phage vector pCANTAB5E. After 4 rounds of screening with lung adenocarcinoma cell line A2 as antigen, an enriched secondary phage display library was obtained.
RESULTSA recombinant phage display library with total of 8×10⁷ pfu/ml was established. Randomized clones from unselected library digested with BstNⅠ showed different patterns, however, those from selected library showed that phages with special pattern were enriched. Twenty-three out of 30 clones were found to respond strongly to A2 cell lines.
CONCLUSIONSThe ScFv of anti-lung adenocarcinoma monoclonal antibody 5F-11 can be successfully produced, which may be useful to widen the application of the antibody.
10.Effects of p53 antisense RNA on malignant phenotype and sensitivity to cisplatin of human lung cancer cell line.
Hui WANG ; Baitang LAI ; Jinzhao LI ; Xuehui YANG ; Chunyan ZHANG ; Xiuping ZHAN ; Yue WANG
Chinese Journal of Lung Cancer 2002;5(1):1-5
BACKGROUNDTo study the effects of extraneous p53 antisense RNA on malignant growth and sensitivity to cisplatin of human lung cancer cell line.
METHODS801D cell line with p53 deletion and mutation at 248 codon was selected as a parent cell line. An 1.8 kb human p53 full length cDNA was inserted into a mammalian expression vector PEGFP to construct a p53 antisense RNA recombined plasmid PEGFP-p53(AS) and GFP gene at plasmid was a report gene to monitor extraneous gene expression. The extraneous gene was detected by PCR. The p53 mutation protein was examined by immunohitochemical stain of p53 monoclonal antibody. The inhibition growth efficacy of extraneous p53 in vitro was determined by clonogenic survival assay. Sensitivity of cells to cisplatin was examined with MTT assay. FCM analysis was performed to measure the effect of p53 antisense RNA on cell cycle.
RESULTSTwo cell lines, PEGFP-p53(AS)-801D and PEGFP-801D, were established after transfection of 801-D cells by lipofection and selection. Presence of extraneous p53 gene in PEGFP-p53(AS)-801D was proved by PCR and expression of extraneous p53 was estimated when green fluorescence in those cells was found out under the fluorescent microscopy. Mutated p53 protein in parent cell line 801D was positive and in PEGFP-p53(AS)-801D was negative with immunochemical stain. The inhibition rate of colony formation was 61% for PEGFP-p53(AS)-801D (P < 0.001). The sensitivity of PEGFP-p53(AS)-801D cells to cisplatin was increased. FCM analysis showed that the cell line was arrested at G1 phase.
CONCLUSIONSp53 mutation at 248 code plays an important role on malignant growth and resistance to cisplatin of human lung cancer cell line 801D. Malignant growth of cells with p53 deletion and mutation at 248 codon can be inhibited by extraneous p53 antisense RNA, and simultaneously the sensitivity to cisplatin is also increased.