1. Macrophage colony-stimulating factor receptor and its inhibitors: Research advances
Journal of International Pharmaceutical Research 2010;37(5):340-345
Macrophage colony-stimulating factor receptor(c-Fms),encoded by the c-fms proto-oncogene,is a member of type III receptor tyrosine kinase family. c-Fms activation by binding with its ligand plays important roles in the survival, proliferation and differentiation of the monocyte-macrophage lineage and the development of embryo. Over expression of c-Fms and its ligand result in abnormalities of intracellular signaling pathways mediated by c-Fms, which is associated with tumorigenesis and inflammation. The inhibitors targeting c-Fms block intracellular signaling pathways by inhibiting c-Fms receptor tyrosine kinase are potential drugs for tumor and arthritis therapeutics.
2.The role of synaptic plasticity on rats with visceral hypersensitivity induced by transient intestinal infection
Xiaojun YANG ; Yang GUAN ; Wei QIAN ; Lei SHENG ; Xiaohua HOU
Chinese Journal of Digestion 2008;28(10):660-665
Objective To investigate the role of synaptic plasticity on the formation of visceral hypersensitivity induced by transient intestinal infection in rats. Methods Thirty male Sprague-Dawley rats were divided into normal control, acute infection and chronic infection groups with 10 each. The area under curve (AUC) of electromyography (EMG) in 10 s was used to evaluate the visceral sensitivity induced by different eolorectal distention (20,40,60 and 80 mmHg). Histological change of the colon was evaluated by H-E staining. Synaptic uhrastrueture such as synaptic cleft and synaptic vesicles was observed using transmission electron mieroseope. The mRNA and protein expressions of synaptophysin and postsynaptic density protein-95 (PSD-95) were examined by RT-PCR and Western blot, respectively. significantly higher than those of normal controls(P=0. 012, 0. 005, respectively ). In contrast, AUC of acute infection were significantly lower than those of normal controls ( P = 0. 018,0. 012, respectively ). Under the distention of 20 and 80 mmHg, no significant difference was observed among three groups (P= rats compared to normal controls(23.45±4.10 vs. 9.10±2.42, P=0. 027),but there was no statistical difference between chronic infection rats and normal controls (13. 95±7.96 vs. 9.15±2.42, P=0.78). increased. In acute infection rats, mitochondria cristae disappeared, synaptic vesicles and the length of controls, mRNA and protein of synaptophysin in ileocecum, proximal colon and distal colon were significantly increased in chronic infection rats (P<0. 05 ), but decreased in acute infection rats with no significant difference. Compared with controls, no significant downregulation was noted in the expression protein expressions of PSD-95 were both increased in chronic infection rats (P<0.05), and decreased in acute infection rats (P<0.05). Conclusion Synaptic plasticity plays an important role in the formation of visceral hypersensitivity induced by transient intestinal infection in rats.
4.Effect of glibenclamide on viability and acid-base equilibrium of glioblastoma cells
Ling GUO ; Huajun SHENG ; Qian LIU ; Qinghua YANG ; Shujuan ZHU
Chinese Journal of Pathophysiology 2017;33(8):1405-1410
AIM: To investigate the effect of glibenclamide (Glib) on the viability and acid-base equilibrium of glioblastoma cells.METHODS: U251 cells and U87 cells were treated with Glib at different concentrations.The inhibitory rates were detected by CCK-8 assay.The effective dose was screened and the experiment was divided into control group and drug treatment groups.The migration ability was monitored by wound healing assay, and intracellular pH was detected by pH indicator fluorescent probe.The protein expression levels of inwardly-rectifying potassium channel 4.1 (Kir4.1) and monocarboxylate transport protein 1 (MCT1) were determined by Western blot.RESULTS: The half maximal inhibitory concentrations (IC50) of Glib for 48 h exposure of U251 cells and U87 cells were 400.20 μmol/L and 553.70 μmol/L, respectively.The effective inhibition doses of Glib for U251 cells were from the ranges of 100 μmol/L to 1 600 μmol/L, and those for U87 cells were from 50 μmol/L to 1 600 μmol/L in a concentration-dependent manner (P<0.05).Glib not only inhibited the migration (P<0.05) of U251 cells and U87 cells, which was negatively correlated with drug concentration (P<0.05), but also reduced the intracellular fluorescence intensity in experimental group (P<0.05), suggesting that with the increase in drug concentration, the intracellular pH decreased gradually (P<0.05).The protein expression of Kir4.1 and MCT1 was down-regulated by treatment with Glib, and was negatively correlated with concentration of Glib.CONCLUSION: Glib, a kind of potassium channel blocker, induces intracellular acidification via down-regulating the expression of Kir4.1 and MCT1, thus inhibiting the growth of glioblastoma in a certain dose range.
5.Endocytosis of Ca Alginate Nanocapsules by Dendritic Cells and Function Induction
Wei CUI ; Bing-Qian SHEN ; Sheng-Li YANG ;
China Biotechnology 2006;0(07):-
The endocytosis/phagocytosis of calcium alginate nanocapsules by peripheral blood derived dendritic cells was confirmed with the use of Quantum dots labeling.Results further demonstrated these nanoparticles could cause the upregulation of HLA-DR expression to induce the maturation of dendritic cells in vitro.Dendritic cells stimulated by nanocapsules covalently loaded with BSA were shown to stimulate the proliferation of self T cells with blank capsules and free BSA as controls,suggesting their potential applications in cancer cell therapy as a new antigen delivery vehicle with a strong adjuvant effect.
6.Clinical observation on warm needling moxibustion plus acupoint sticking therapy for cervical radiculopathy
Xi-Bing YANG ; Li-Feng QIAN ; Lai-Hua SHEN ; Ji-Sheng LI
Journal of Acupuncture and Tuina Science 2019;17(2):137-140
Objective:To observe the clinical effect of warm needling moxibustion plus acupoint sticking therapy for cervical radiculopathy.Methods:A total of 120 cases were allocated into an observation group,a warm needling group and an acupoint sticking group according to the random number table,with 40 cases in each group.Cases in the observation group received warm needling moxibustion plus acupoint sticking therapy;cases in the warm needling group received the same warm needling moxibustion in the observation group;cases in the acupoint sticking group received the same acupoint sticking therapy in the observation group.The scores of Japanese Orthopaedic Association (JOA) and visual analog scale (VAS) were recorded before and after treatment.Results:The total effective rate was 95.0% in the observation group,versus 77.5% in the warm needling group and 75.0% in the acupoint sticking group (both P<0.05).Inter-group differences in JOA and VAS between the observation group and the other two groups were statistically significant (all P<0.05).Conclusion:Warm needling moxibustion plus acupoint sticking therapy is effective in treating cervical radiculopathy,and it can significantly alleviate pain and enhance clinical efficacy,and thus is worth clinical popularization.
7.Alteration of electrophysiology in pilocarpine mice model of epilepsy with impairment of contextual fear memory
yue, ZHANG ; guo-en, CAI ; qian, YANG ; sheng-tian, LI ; qin-chi, LU
Journal of Shanghai Jiaotong University(Medical Science) 2006;0(02):-
0.05).However,there was no significant difference in the AMPAR-mediated basal synaptic transmission on hippocampal CA1 between those at the later period(6 weeks) of epilepsy induced by pilocarpine and controls,while LTP was inhibited(P
8.Preparation of Calcium Alginate Nanocapsules with Adjuvant Effect
Ke-Xiao ZHENG ; Wei CUI ; Bing-Qian SHEN ; Sheng-Li YANG ;
China Biotechnology 2006;0(01):-
A novel reverse emulsification-phase transition process was designed to prepare alginate-based nanocapsules in the present study. Ca alginate nanocapsules with an average hydrodynamic diameter below 300 nm were obtained by adjusting surfactant and alginate concentration. Instrumental analysis observations revealed a morphologically spherical shape with a relatively uniform size distribution without aggregation.?-potential measurements indicated an topically electrostatically negative nature of capsules in neutral aqueous solution. These nanocapsules were proven to have an equivalent potency to stimulate the maturation of dendritic cells originated from CD14 positive cells isolated from human peripheral blood. Protein loading via covalent conjugation was demonstrated feasible with EDC/NHS facilitated reaction between carboxyl and amino groups. These nanocapsules are considered to have important applications as a new adjuvant in cancer cell therapy, vaccine design and targeted drug delivery for active components of protein nature.
9.A novel azo-type compound from Dendrolobium triangulare.
Qian-Jun ZHANG ; Xiao-Sheng YANG ; Hai-Yan ZHU ; Qian-Yun SUN ; Xiao-Jiang HAO
Acta Pharmaceutica Sinica 2009;44(9):1009-1013
Thirteen compounds from Dendrolobium triangulare (Retz.) Schindl. were isolated and purified by chromatography on silica gel, macroporous resin column and recrystallization method, and their structures were elucidated by chemical and spectral analyses as azo-2, 2'-bis [Z-(2, 3-dihydroxy-4-methyl-5-methoxy) phenyl ethylene] (1), beta-sitosterol (2), N-(2'-hydroxy-tetracosanoyl)-2-amino-1, 3, 4-trihydroxyoctadec-8E-ene (3), lupeol (4), cycloeucalenol (5), daucosterol (6), betulinc acid (7), betulin (8), glyceryl hexacosanoate (9), glyceryl 26-hydroxy hexacosanoate (10), methyl pheophorbide-a (11), acacetin-7-O-alpha-L-rhamnopyranosyl (1-6)-beta-D-glucopyranoside (12) and robinin (13). To our knowledge, all compounds are obtained from Dendrolobium genus for the first time and compound 1 is a novel compound. Moreover, it is understood that compound 1 has better protection against PC12 cell damnification deduced by glutamate, than that of Vitamin E in 2 microg x mL(-1) concentration.
Animals
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Azo Compounds
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isolation & purification
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pharmacology
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Fabaceae
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chemistry
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PC12 Cells
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Rats
10.Construction of efficient conjugal plasmids between Escherichia coli and Streptomycetes.
Hong-Bo MO ; Lin-Quan BAI ; Sheng-Lan WANG ; Ke-Qian YANG
Chinese Journal of Biotechnology 2004;20(5):662-666
Conjugal plasmid pGH112 has been developed based on the replicons of Streptomyces coelicolor plasmid SCP2 and E. coli ColE. The plasmid contains ampicilin resistance gene(amp) for selection in E. coli and thiostrepton resistance gene (tsr) for selection in Streptomycetes, and a 0.76 kb oriT fragment of (IncP) RK2. Conjugal transfer of pGH112 was performed from E. coli to S. coelicolor A3(2), S. avermitilis, S. lividans TK54, S. toxytricini NNRL15443, S. venezuelae ISP5230 and Sacc. erythraea by conjugation, results show that the plasmid was able to transfer efficenctly from E. coli to Streptomycetes, was stably inherited in the recipients. pGH113 was constructed from pGH112 by combining the constitutive ermE promoter with green fluorescent protein gene(gfp).
Ampicillin Resistance
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genetics
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Conjugation, Genetic
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Escherichia coli
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genetics
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Green Fluorescent Proteins
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genetics
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Plasmids
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Streptomycetaceae
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genetics
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Thiostrepton
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pharmacology