2.Effect of Pirfenidone on Activity of Hepatic Cytochrome P450 in Rats
Ji WU ; Hui CHEN ; Jianhong WU ; Shunchang ZHOU ; Fandian ZENG
Herald of Medicine 2014;(6):723-726
Objective To study the effects of pirfenidone on total enzyme and isoenzyme of liver microsomal cytochrome P450 in rats. Methods The activites of liver microsomal dimethyl nitrosamine N-demethylase( NDMA )and erythromycin demethylase( ERD ) were determined. Fifty-six SD rats were randomly divided into six groups,in which they received CMC,dexamethasone 100 mg·kg-1 ,ketoconazole 40 mg·kg-1 ,pirfenidone 25,50,100 mg·kg-1 ,respectively. After administration for 6 and 12 days,livers were prepared liver microsome,the concentration of proteinum in microsome and shade selection to plasma samples were determined by spectrophotometer. Results After administration of pirfenidone for 6 days, cytochrome P450 was significantly increased in 50 and 100 mg·kg-1 pirfenidone groups,as compared with solvent control group (1%sodium carboxymethylcellulose)(P﹤0. 01). After administration of pirfenidone for 6 and 12 days,NDMA of liver microsome was not changed significantly(P﹥0. 05). ERD of liver microsome was significantly increased in 100 mg·kg-1 pirfenidone group after administration for 12 days(P﹤0. 01). Conclusion Pirfenidone can induce P450 and ERD activities in a dose-and time-dependent manner.
3.Synthesis and antitumor effect of novel andrographolide derivatives
Qianqian FAN ; Qiujuan WANG ; Bubing ZENG ; Yulin WU ; Hui JI
Journal of China Pharmaceutical University 2010;41(4):326-332
A series of andrographolide derivatives with the structure of 12-N-substituted-14-deoxyandrographolide were synthesized from the parent compound andrographolide.Their antitumor activities were preliminarily evaluated on various cancer cell lines and compound 4d stood out due to its potent growth inhibitory effect in comparison with andrographolide.Compound 4d also demonstrated significant antitumor effect on human hepatoma HepG2cells in vitro and on sarcoma 180 (S180) and hepatoma 22(H22)-bearing mice in vivo.Then,the apoptosis induced by compound 4d in HepG2cells was detected by Annexin V/PI double staining assay.Further mechanic study showed that the expression of p53 and Bax was significantly elevated and that of Bcl-2was downregulated in 4d-treated HepG2cells.Collectively,these data suggested that compound 4d had remarkable antitumor effect both in vitro and in vivo and could effectively induce apoptosis via a p53-dependent pathway in HepG2 cells,thus deserving further investigation.
4.Report of 16 cases of eosinophilic fasciitis with literature review
Hui WANG ; Aiyu WU ; Xinwang DUAN ; Xiaofeng ZENG ; Qian WANG
Chinese Journal of Rheumatology 2013;(3):179-181
Objective We reported 16 eosinophilic fasciitis (EF) patients with eosinophilic fasciitis and performed a systematic review of the literature to improve the disease awareness.Methods The clinical course of 16 patients with eosinophilic fasciitis at the Peking Union Medical College Hospital were described,inclu-ding demographic data,clinical manifest-ations,laboratory tests,pathology and treatment.Results The mean age at diagnosis was (47±8) years,with 13 female and 3 male patients.Three cases had exertion or strenuous sports before the onset of EF.Positive ANA was noted in 6 of 12,positive RF was noted in 3 of 10,hyper-gammaglobulinemia was noted in 6 of 7,elevated IgG was noted in 8 of 13,peripheral blood eosinophilia was noted in 10 of 16,while thrombocytopenia was found in one patient.Conclusion Based on this and other reported cases in the literature,EF may be a kind of autoimmune disease.Genetic influence and environ-mental factors are involved in the development of this disease.Systemic involvement is rare.In general,corticosteroids and immunosuppressive are effective in EF.
5.Analysis of primary metabolites of tramadol in rat urine by LC-MS(n.
Hui LU ; Di WU ; Jing YAN ; Qin ZENG ; Yanping WU ; Lu SUN
Acta Pharmaceutica Sinica 2011;46(8):968-75
Tramadol and its metabolites in rat urine were identified by LC-MS(n). Rat urine samples of 0-36 h were collected after ip 9.0 mg x kg(-1) tramadol, then the samples were enriched and purified through solid-phase extraction cartridge. Purified samples were analyzed by LC-MS(n). Possible metabolites were discovered by comparing the full scan and SIM chromatograms of the test samples with the corresponding blanks and analyzing the retention time, quasi-molecular ion and fragment ion of all chromatograms. Nine phase I metabolites and four phase II metabolites were identified in rat urine. One of the metabolites was found first time in living body. The metabolites were formed via the following metabolic pathways: O-demethylation, N-demethylation, hydroxylation, N-oxidation and conjugation. The method can be used to identify tramadol and its metabolites in other animals and human.
6.Solitary infantile choriocarcinoma of liver: report of a case.
Wenping YANG ; Yan WU ; Shouhua ZHANG ; Jinshi HUANG ; Songtao ZENG ; Hua ZENG ; Hui HUANG
Chinese Journal of Pathology 2015;44(9):673-674
7.Prediction and identification of B-cell epitopes of Treponema pallidum repeat protein F
Longgu CAO ; Hui LING ; Hengling CAI ; Feijun ZHAO ; Danming OUYANG ; Sufang CHEN ; Yimou WU ; Tiebing ZENG
Chinese Journal of Zoonoses 2015;(10):919-922
To predict and identify the dominant B‐cell epitopes of conserved region of Treponema pallidum repeat protein F (TprFN ) and provide the basis for development of polyvalent epitope‐based syphilis vaccine ,the amino acid sequence of TprFN was obtained from GenBank and analyzed with comprehensive meta‐analysis Mobyle ,ABCpred and IEDB online software .The peptides containing predicted epitopes were artificially synthesized . To obtain and measure the titers of antibodies against TprFN ,New Zealand rabbits were immunized with recombinant protein TprFN expressed in E .coli and identified by Western blot (WB) .Sera from TprFN‐immunized rabbits ,syphilis patients ,and normal human and normal rabbits were used to deter‐mine the immunoreactivity and specificity of 7 predicted peptides of TpFN by indirect ELISA .Comprehensive meta‐analysis of online software showed that P1 (43‐62AA) ,P2(57‐71AA) ,P3(81‐88AA) ,P4(89‐103AA) ,P5(125‐138AA) ,P6(231‐251AA) and P7(268‐279AA) might be the B‐cell epitopes .A protein was expressed in a soluble form and identified as TpFN by WB .The ELISA indicated that P1 and P3 were active with TprFN‐immunized rabbit sera and syphilis patient sera but not with negative control sera .These results indicate that P1 and P3 are the potential dominant B‐cell epitopes .
8.MRI combined with PET in diagnosis of primary lymphoma of bone
Jinglei LI ; Hui ZENG ; Changhong LIANG ; Haijun WU ; Meiping HUANG ; Dan SHAO
Chinese Journal of Medical Imaging Technology 2010;26(2):319-322
Objective To observe the imaging features of primary lymphoma of bone (PLB) on MRI and PET, and to assess the value of MRI combined with PET for PLB. Methods Sixteen patients with pathologically confirmed PLB were collected, and the MRI and PET appearances were analyzed retrospectively. Results Single bone infiltration was detected in 15 patients (5 in femurs, 3 in vertebro, 3 in right iliums, 2 in tibias, 1 in radius and 1 in maxillae), while multiple bones infiltration were noticed in 1 patient (lesion located in manubrium sterni and the 7th right rib). MRI demonstrated heterogeneous focal-lamellar or diffuse signal intensity within marrow, isointense or hypointense on T1WI and slightly hyperintense on T2WI with homogeneous or heterogeneous enhancement. Severe soft tissue mass was seen in all 16 patients, the range of soft tissue mass was larger than osseous lesion in 15 patients and equal to osseous lesion in 1. Most PLB were homogeneous isointense or slightly hypointense on T1WI and homogeneous or heterogeneous slight-hyperintense on T2WI with slightly or moderately homogeneous or heterogeneous enhancement, while in 3 patients showed single vertebral compression fracture with local epidural- and/or paravertebral-soft tissue, and the range of soft tissue larger than the pathologic vertebrae. PET was performed before operation in 13 patients, showing local increasement of glycometabolism and uptake of radioactive nuclide without abnormality for other sites. For three patients of primary lymphoma of vertebrae underwent PET after operation, and recurrence was detected in 1 patient after 2 months. Conclusion Large soft mass with small osseous destruction and relatively hypointensity on T2WI is somehow characteristic for PLB. PET features of PLB are not specific, but has some advantages in determining the nature of lesion, differentiating lesions and follow-up after operation. MRI combined with PET is an appropriate imaging method for PLB.
9.DADS induces G2/M arrest through Chk1/Cdc25C/CyclinB1/CDK1 pathway in human leukemia HL-60 cells
Xiaoxia JI ; Ying ZENG ; Jie HE ; Hui TAN ; Lan YI ; Weiguo HUANG ; Youhua WU ; Qi SU
Chinese Pharmacological Bulletin 2015;(2):221-226
Aim To study the effects of cycle arrest and molecular mechanism in human leukemia HL-60 cells induced by diallyl disulfide ( DADS ) . Methods Cell count, colony formation in soft agar experiments and flow cytometry analysis were employed to observe the DADS-induced cell growth inhibition and the effect of cycle arrest in HL-60 cells. The expressions of Chk1/2 and its downstream element in HL-60 cells were detected by Western blot. Results Cell count revealed that population doubling time increased to 35. 03 h and 71. 82 h, respectively, from 19. 14 h in HL-60 cells treated with 60 and 120 μmol·L-1 DADS ( P<0. 05 ) . Colony formation in soft agar experiments showed that colony formation inhibition rate of HL-60 cells exposed to 30, 60, 90 and 120μmol·L-1 DADS increased to 35. 06%, 62. 10%, 93. 79% and 99. 35%, respectively ( P<0. 05 ) . Flow cytometry a-nalysis exhibited that HL-60 cells treated with 60 and 120 μmol · L-1 DADS for 24 h and 48 h arrested in G2/M phase in a concentration-and time-dependent manner ( P <0. 05 ) . Western blot disclosed that the expression of p-Chk1 increased in a time-dependent manner ( P <0. 05 ); however, Chk1, Chk2 and p-Chk2 were not changed in HL-60 cells treated with 60μmol·L-1 DADS (P >0. 05). The expression of Cdc25C, CyclinB1 and CDK1 decreased after treated with 60 μmol·L-1 DADS in a time-dependent manner ( P<0. 05 ) , but the expression of 14-3-3 protein did not change ( P>0. 05 ) . Conclusion DADS can in-hibit the proliferation of HL-60 cells, and induce G2/M arrest through Chk1/Cdc25 C/CyclinB1/CDK1 path-way.
10.Research on the clinical value between gene polymorphism of HPA 1-6,9,15 and platelet transfusion refractoriness
Yuan LI ; Hui ZENG ; Haibin WU ; Xiaoyan ZHAO ; Minchao YAN ; Xiaojun GUO
Chinese Journal of Biochemical Pharmaceutics 2016;36(4):173-175
Objective To research the clinical value between gene polymorphism of human platelet alloantigens (HPA) 1-6, 9, 15 and platelet transfusion refractoriness ( PTR) .Methods Totally 40 patients with platelet transfusion refractoriness( PTR) were randomly selected, and patients and donors’ peripheral blood specimens were collected and tested these samples with platelet GP specific antibodies, and judged the results of platelet transfusion, and with the help of the combination of PCR and direct sequencing for classification of HPA 1-6,9,15 antigens and observe the percent platelet recovery ( PPR ) after the same type of platelet transfusion, and explore the relationship between HPA gene polymorphism and PTR. Results There was no HPA-b gene was found neither on patients and donors’ HPA 1,4,9, showed the distribution of aa homozygous form; HPA 5,6 were mainly aa homozygous form, little bb homozygous form was discorvered.And HPA 2,3,15 were distributed of polymorphism, the frequency of HPA 2,3,5,6,15 were found with polymorphism.Conclusion For these patients who were happened with PRT many times, in addition to taking HLA into account, HPA gene polymorphism are also need to be considered.Most people only need to test patients and donors’ HPA2,3,15 gene to decrease the occurrence of PTR significantly when making HPA matching.