The intracellular signal transduction pathway of histamine H 3 receptor was reviewed. The modulatory effect to some neurotransmitters on cardiovascular system and the therapeutic potential of histamine H 3 receptor agonist was summarized.

Objective To investigate the inhibitory effect on enhancement of contraction and relaxation functions of cardiomyocytes induced by of MN9202 TEA, Forskolin, and MB. Methods The twitch amplitude was measured with a video edge tracker method. The following indexes, including ph (peak height), peak height/baseline percent (ph/bl, %), maximal velocity of contraction (+dL/dt) and maximal velocity of diastolization (-dL/dt), were recorded by a computer. Results TEA, Forskolin and MB increased electrically-induced contraction as shown by the following indexes: ph, ph/bl%, +dL/dt and -dL/dt. Forskolin and MB markedly augmented function of cardiac myocyte contraction and diastolization. Comparing with the control group, Forskolin (10-8mol/L) increased ph from 0.12?0.03(um)to 0.24?0.06 (um), ph/bl % from 12?3% to 27?6%, +dL/dt from 1.8?0.5 (um/s) to 3.8?0.9 (um/s), -dL/dt from 1.8?0.22 (um/s) to 3.5?0.7 (um/s). These indexes increased by 91%, 123%, 110% and 89%, respectively. MB also increased significantly; ph, ph/bl %, +dL/dt and -dL/dt were 0.14?0.04um, 11?4%, 2.2?0.3um/s and 2.2?0.6um/s, respectively. MN9202 (3?10~ -6mol/L) decreased the indexes (+dL/dt and -dL/dt ) which were increased by Forskolin significantly. Conclusion TEA, Forskolin and MB increased function of cardiac myocyte contraction and diastolization. These drugs might elevate intracellular calcium content indirectly and directly. The effects of TEA, Forskolin and MB were attenuated by MN9202. MN9202 might not only block Dihydropyridine Receptor, but might also inhibit calcium influx. Further study is needed to elucidate exact mechanism of MN9202.

0.05). There was a higher prevalence of IBS in Heilongjiang province (14.02%) than that in Shanghai (11.72%, P

AIM: To study the role of p38 mitogen-activated protein kinase (p38MAPK) activation in high glucose-induced collagen Ⅲ synthesis in NRK52E cells. METHODS: Normal rat tubular epithelial cell line NRK52E was cultured in D-glucose of different concentrations, pretreated with SB203580 and collected at different time points. The levels of phospho-p38MAPK and extracellular matrix collagen Ⅲ were examined by Western blotting. RESULTS: The activation of p38MAPK was shown to be dependent upon D-glucose concentration and the time-course. Pretreatment with SB203580 blocked p38MAPK activation induced by high concentration of D-glucose in NRK52E cells. CONCLUSIONS: The activation of p38MAPK induced by high concentration of glucose may play a role in diabetic interstital renal fibrosis. SB203580 has a potential value of clinical applications in the prevention and treatment of diabetic nephropathy.

Objective To detect the location of histamine in peripheral sympathetic nerves of guinea pig. Methods Histidine decarboxylase mRNA was detected using in situ hybridization histochemistry with specific oligonucleotide probe,while histamine and tyrosine hydroxylase were detected using double labeled immunohistochemistry with anti-histamine antibody and anti-tyrosine hydroxylase antibody in the superior cervical ganglia of guinea pig. Results The histidine decarboxylase mRNA hybridization signal were detected in both of large and small cells.The TH immunoreactive substance distributed in cytoplasm steadly,but lacked in the nuclei,while the histamine immunoreactive substance distributed in cytoplasm nearby the plasmalemma.After chemical destroy of the guinea pig SCG′s neuron with 6-OHDA,the immunoreactive materials were hardly detected.Conclusion Because the histidine decarboxylase is the only enzyme which catalyzes histidine into histamine,histamine may be synthesized and coexisted with monoaminergic neurotransmitters in the superior cervical ganglia of guinea pig.

Objective To evaluate the inhibitory effects of gefitinib on the growth of colon carcinoma cells with different degree of sensitivity,and the activated status of epidermal growth factor receptor(EGFR) associated signal pathway proteins.Methods The colon carcinoma cell lines(Lovo,HCT116 and HT29) were treated with 10?mol/L of gefitinib,and flow cytometry was employed to detect the cell cycle and apoptosis.Another portion of cells were treated with 50ng/ml of epidermal growth factor(EGF) or 5?mol/L or 10 ?mol/L of EGF+gefitinib,and Western blotting was used to determine the expressions of PTEN,EGFR,AKT and MAPK,as well as their corresponding phosphorylated proteins,p-EGFR,p-AKT and p-MAPK.Results After being treated with gefitinib,the G1 phase cells and apoptosis rate increased remarkably in Lovo,slightly in HT29,while no significant change was found in HCT116.With the treatment of EGF alone,the expressions of p-EGFR,p-AKT and p-MAPK increased significantly in Lovo and HT29 cells(P0.05).Conclusions The growth of colon carcinoma cells,which are resistant to gefitinib,is not dependent on EGFR,and the activated status of signal pathway of the gefitinib-resistant cells will not be inhibited as the EGFR is blocked.The present findings suggest that sensitivity of colon carcinoma cells to gefitinib relies on EGFR as well as the activation of its downstream signal pathway.

Objective To investigate the relationship between the sensitivity of colon carcinoma cells to epidermal growth factor receptor(EGFR) inhibitor,gefitinib,and the downstream proteins of EGFR.Methods The expressions of EGFR proteins of 6 colon carcinoma cell lines(Lovo,HCT116,HT29,LS174T,SW480 and SW620) were determined with immunocytochemistry staining.The inhibitory effects of gefitinib on the growth of colon carcinoma cells were assessed by MTT,and the expression levels of Akt and MAPK as well as their phosphorylated forms(p-Akt and p-MAPK) were assessed by Western blotting.Results EGFR protein expressed in all the Lovo,HCT116,HT29,LS174T and SW480 cells,and the highest expression was found in Lovo cells,but not in SW620 cells.Lovo cells showed the highest,HT29 and SW480 cells showed moderate,sensitivity to gefitinib,while the others showed more or less resistance to gefitinib.No significant difference was found between the growth inhibition and IC50 values among the 6 cell lines despite of being treated with fetal bovine serum or EGF.Akt protein existed in all the cell lines without notable difference.Lovo and SW620 cells showed the least of p-Akt expression(P

Objective Sodium-bile acid cotransporter plays an important role in the development of Echinococcus.The present study aimed to clone sodium bile acid cotransporter gene in Echinococcus multilocularis (EmSBACT5) and to analyze the bioinformatics of its coding protein.Methods EmSBACT5 gene was amplified by reverse transcription RCR (RT-PCR) technology and its nucleotide sequence was sequenced.Bioinformatics softwares were used to predict and analyze the physical and chemical properties, hydrophilicity/hydrophobicity, transmembrane domain, post-translational modification sites, structural domain, secondary structure, tertiary structure, subcellular localization and biological functions of the coding protein.Results The complete open reading frame was amplified with 654 bp in length, encoding 217 amino acids.The homology of the nucleic acid sequence and amino acid sequence of EmSBACT5 gene were 98% and 96% with the published SBACT5 in Echinococcus granulosus (EgSBACT5) respectively.Protein analysis results showed that the molecular formula of EmSBACT5 protein was C1141H1797N273O284S11.Its relative molecular mass was 24240 and isoelectric point was 8.99.There were 9 post-translational modification sites and 4 typical domains.Alpha helical, β-sheet, β-turn and random coil accounted for 29.95%, 31.80%, 7.83% and 30.41%, respectively.This protein was a hydrophobic membrane protein and was mainly located in the cytoplasmic membrane, and it might play a role in the processes of material transport and signal transmission.Conclusion The EmSBACT5 gene was cloned successfully and the informatics characteristics of its coding protein were obtained, which provides basic information for prevention and control of echinococcosis.

BACKGROUND:Our previous study has already manifested that Chinese medicine Xiaokening can effectively prevent and treat the early diabetic nephropathy. OBJECTIVE:To compare the effect of rhein and archen on the apoptosis of mesangial cells of rats cultured with high glucose. METHODS:Mesangial cells were stimulated by different concentrations of rhein and archen (20, 40 and 80 μmol/L). Morphology of apoptotic cells was observed by hematoxylin-eosin staining. Karyon apoptosis was examined by fluorescence staining of DAPI. cellapoptosis rate was detected by flow cytometry. RESULTS AND CONCLUSION:The outcome of hematoxylin-eosin staining and DAPI staining indicated that the effect of rhein was much stronger than that of archen on the apoptosis of mesangial cells in the rats cultured with high glucose. Comparison of the apoptosis rate also indicated that the rhein had a stronger effect on the earlier and the later stage apoptotic rate of mesangial cells than archen. Both rhein and archen with different concentrations can induce apoptosis of mesangial cells, but the effect of rhein is much stronger.

SELEX is a newly developed biochemical technique,which filter out high specificity and high affinity ligand for the target molecules through the identification of aptamer combined with the target molecules.The specific aptamer was used in a variety of clinical applications,such as diagnosis of the disease,development of new therapeutic drugs and even directly applied to disease treatment.