Advances in ApoA- I mimic peptides against atherosclerosis / 中国药理学通报

Apolipoprotein A-I (ApoA-I), the main protein component of high density lipoprotein (HDL) , which plays a key role in the process of reverse cholesterol transport (RCT) , is considered as an important anti-atherosclerosis (As) drug target. ApoA- I mimic peptides developed based on its a-helix, and HDL mimic peptides that developed by recombinant ApoA- I have entered clinical trials, exhibiting favorable RCT promotion and anli-As activity. The paper reviewed the advances in the structure and function of ApoA- I , the molecular interaction mechanism between ApoA-1 and ABCA1 ( ATP-binding cassette transporter Al) , LCAT (lecithin cholesterol acyl transferase) and SR-B1 (scavenger receptor class B type 1) , and anti- As activity of ApoA- I mimic peptides, which would provide references for anli-As new drug development based on ApoA- I mimic peptides.

Preparation of 99Tcm-TP1623 targeting at HER-2 receptor and its distribution in animals / 中华放射医学与防护杂志

Objective To prepare 99Tcm-B2-S22-AFA (99Tcm-TP1623)and investigate its biodistribution and kinetic imaging in healthy animals.Methods TP-1623 was synthesized and labeled indirectly by 99Tcm using stannous chloride as the reductive agent.The labeling rate was determined with chromatography using Whatman 3MM filter paper and by calculating the specific activity.The biodistribution of 99Tcm-TP1623 was tested at 1,5,10,30,60,120 min after intravenous injection into mice.According to the SPECT images and the time response of the radioactivity in the region of interest (ROI),the dynamic distribution of 99Tcm-TP1623 was assayed.Results The radiolabeling rate of 99Tcm-TP1623 was (96.4-± 0.1) ％ and the specific activity was (24.35 ± 0.06) TBq/mmol.After being conserved at room temperature for 4 h,the radiochemical purity of 99Tcm-TP1623 was (95.03 ± 0.97) ％.The oil-water distribution coefficient was-(2.51 ± 0.15).The bio-distribution test showed that the radioactivity in mice blood disappeared very fast over time by a quick excretion through renal.Meanwhile,the radioactivities in the heart,lung,liver,muscle and bone of mice decreased gradually along time and after 60 min they approached to the lowest levels.The radioactivity in brain always kept at a low level,but the radioactivity in intestinal increased slowly.For rabbits,the SPECT images showed that the radioactivity in blood disappeared quickly and the radioactivities were eliminated through kidneys.Meanwhile there were excretion images in gallbladder and intestinal,but no obvious nuclide accumulation in thyroids and stomach,and low radioactivity in brain as well.Conclusions 99Tcm-TP1623 is easy to prepare and has a high radiolabeling efficiency and good stability in vivo and in vitro,and it has excellent dynamic characteristics in normal animals.

Screening and identification of peptide mimics to lipoteichoic acid by phage displayed random peptide library / 中国免疫学杂志

Objective:To screen epitope mimics to lipoteichoic acid from a random 12-mer phage display peptide library and i-dentify the specificity of the mimotopes of LTA.Methods:The monoclonal antibody against LTA was used as a target to screen the 12-mer phage display peptide library and the specificity of phage clones were identified by sandwich ELISA.The amino acid sequences of positive phage clones were deduced from DNA sequencing.The specificity of synthetic peptide were identified by sandwich ELISA.Results:4 clones were obtained after 3 rounds of screening.Amino acid sequence analysis revealed four different types of mimotope sequence.A linear peptide (GHxDFRQxxQPS),named L2,which derived from positive sequence was synthesized.ELISA result indicates that L2 can bind to anti-LTA mAb specifically in a dose-dependent manner.Conclusion:The mimotopes of LTA were obtained by using the phage display technology.

Screening and identification of the mimic peptide of Mycobacterium tuberculosis antigen / 中华微生物学和免疫学杂志

ObjectiveTo immunoscreen the mimic peptides of Mycobacterium tuberculosis antigen from phage displayed 12-mer peptide library.MethodsSpecific IgG was purified from sera of patients with TB and used as the target to immunoscreen a phage random peptide library of 12 amino acids.Positive clones which were obtained after three rounds of biopanning were detected by ELISA and sequenced.The diagnostic value of the high frequent positive clones were observed by ELISA.Results After 3 rounds of immunoscreening,the eluted phages were enriched effectively.Six kinds of animo acid sequence were obtained from twelve positive phage clones.Sensitivity of the two high frequent positive clones were 71.4％ (A2)and 55.4％ (A7) respectively.ConclusionThe antigen-mimic peptide was successfully screened from 12 random phage peptide library and the peptides can be recognized by tuberculosis patients' polyclonal antibodies.

Effective Penetration of Cell-permeable Peptide Mimic of Tyrosine Residue 654 Domain of β-catenin into Human Renal Tubular Epithelial Cells / 华中科技大学学报（医学）（英德文版）

Phosphorylation of β-catenin tyrosine residue 654 plays an important role in the epithelial to myofibroblast transition (EMT). Introducing mimic peptide of tyrosine residue 654 domain of β-catenin into cells may influence phosphorylation of β-catenin tyrosine residue 654. To deliver this mimic peptide into renal epithelial cells, we used penetratin as a vector, which is a novel cell perme-able peptide, to deliver hydrophilic molecules into cells. A tyrosine 654 residue domain mimic pep-tide of β-catenin (PM) with fused penetratin was constructed, purified and then detected for the pene-tration of the mimic peptide into human renal tubular epithelial cells (HK-2). The results showed that purified fusion mimic peptide could efficiently and rapidly translocate into human renal tubular epithelial cells. It is concluded that a cell-permeable peptides mimic of tyrosine residue 654 domain of β-catenin was successfully obtained, which may provide a useful reagent for interfering the human renal tubular epithelial-mesenchymal transition.

Contraceptive effect of fusogenic trophoblast surface epitopes / 第三军医大学学报

Objective To synthesize a multiple antigenic peptide(MAP),observe its humoral immune response and evaluate its antifertility potential.Methods Based on fusogenic epitope mimic peptide and synthetic nonnatural Pan DR T Helper Epitope(PADRE),MAP antigenic peptides were designed and synthesized.After suspending with the equivalent Freund's adjuvant,the antigens were used to immunize the female C57BL/6 mice to evalutate their humoral immune response in animals and efficiency of specific antisera on inhibiting syncytial trophoblast fusion.Results The MAP peptide was successfully synthesized.After purified with HPLC,its purity reached 95%.After immunization,the highest level of specific IgG in mice serum was 1:1 024,and the corresponding antigen of human trophoblastic cell could be identified in the antisera.In presence of mice antiserum by 1:10 dilution,forskolin-induced intercellular fusion of BeWo choriocarcinoma cells decreased remarkably(P

The study on different acting mechanisms of three types of TACE inhibitors in converting of pro-TNF? into sTNF? / 中国免疫学杂志

Objective:To study the effects of TNF? converting enzyme(TACE)inhibitors on TNF? secretion and develop an approach to interfere inflammation processes.Methods:(1)Stimulate the HL-60 cell lines in vitro with LPS for different time to establish the cellular model of inflammation and simultaneously induce in vivo inflammatoin animal model by LPS.(2)Check the cytotoxic effects of TNF? secretion using MTT colorimetric method for cell proliferaton.(3)Detect the level of expression of TACE carrying out RT-PCR,FCM techniques and immuno-histochemical dying technique.Results:(1)PDQ had the inhibitive effect on TNF?mRNA expression induced by LPS stimulation( P

Immunity against Schistosoma japonicum Induced by Phage Display Peptides Mimicking Antigenic Epitopes of Trichinella spiralis / 中国寄生虫学与寄生虫病杂志

Objective To obtain the short peptides mimicking antigenic epitopes of Trichinella spiralis ( T/^ ), and explore their cross protective immunity against Schistosoma japonicum ( S^j. ) in mice. Methods IgG antibodies were purified from sera of mice infected with T/^ . The purified IgG was used to immunoscreen a phage random peptide library of 7 amino\|acid residues displayed as a fusion to protein of filamentous phage. Positive clones were obtained by affinity selection, the reactivity of each clone binding to specific IgG was detected by ELISA. Kunming mice were immunized subcutaneously three times with mixed phage clones. The mice were sacrificed 45 days after challenge. The worms and the liver eggs were counted. Results After three rounds of panning, the relevant phages had been enriched approximately 150 times in production as compared to those from the first round. Of 24 phage clones randomly selected from the third round biopanning, 21 clones were shown to actually bind to the specific IgG. As compared with the control group, the worm and the liver egg reduction rates in vaccination group were 42^8% and 66^3% ( P

Research for IL-2R? mimic peptide on skin allograft rejection in mice / 中国免疫学杂志

Objective:To study the effects of IL-2R? mimic peptide(CP) on skin allograft rejection in mice.Methods:Mouse skin allograft model was employed in all groups.The bioactivities were determined by lymphocyte proliferation,one-way MLR,assay of T lymphocyte subset and the level of cytokine in splenic cell culture supernatant.Results:CP inhibited lymphocyte proliferation;decreased the number of CD4+T lymphocytes in spleen and the value of CD4+/CD8+;down-regulated the level of IL-2 and IFN in splenic cell culture supernatant,as well as prolonged the mean survival times(MST) of skin allografts.The combination of CP and CsA showed cooperativities.Conclusion:CP,as the IL-2R? mimic peptide has the suppressive activities,which can efficiently inhibit skin allograft rejection in mice.