1. Design, synthesis, and antifungal activity of 3-substituted triazole derivatives
Academic Journal of Second Military Medical University 2010;31(10):1114-1119
Objective: To study the in vitro antifungal activity of triazole alcohols by introduction of 1, 2, 3-triazole as the side chain. Methods: Twenty-one novel triazole alcohol compounds were designed, synthesized, and characterized by 1HNMR and MS spectra. The in vitro antifungal activities of the compounds were evaluated using eight kinds of pathogenic fungi. Results: All the synthesized compounds exhibited certain antifungal activities. The MIC 80 value of compound 7 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluorophenyl)-3-[N,N-(1-substituted-benzyl-4-methylene-1H-1,2,3-triazole)] against Candida albicans was 0.25 μg/ml, with its activity being 4 times that of fluconazole. The MIC80 value of compound VI 1-(1H-1,2,4-triazole- 1-yl)-2-(2,4-difluorophenyl)-3-(N,N-dipropargyl)-2-propanols against Candida albicans was 0.0156μg/ml, with its activity being 64 times that of fluconazole and 4 times that of itraconazole. Conclusion: The 1,2,3-triazole can be efficiently introduced by intermolecular 1,3-dipolar cycloaddition. Large side chains may be a disadvantage for improving the antifungal activity of the title compounds.
2.The Effect of Combination Use of 1,25(OH)_2D_3 and Celecoxib on Growth and Apoptosis in Breast Cancer Cell Line Hs578T
Xueqi HE ; Yangyi BAO ; Xin SUN ; Gang MENG ; Qin WANG
Journal of Medical Research 2006;0(08):-
Objective To study the effect of combined 1,25-dihydroxyvitamin D31,25(OH)2D3 and celecoxib on growth, call cycle and apoptosis in breast cancer cell line Hs578T.Methods We compared cell numbers by using MTT method , analyzed cell cycle percentage and apoptosis with flow cytometric.Results Both with 1,25(OH)2D3 and celecoxib could inhibite tumov growth,induc apoptosis in a dose-time-dependent manner. comparing with 1,25(OH)2D3 alone,combination wse of the two drugs had a additive effect but was inferior to cececoxib alone. The combination use of 10-8mol/L1,25(OH)2D3 and celecoxib group is more effective than the combination use of 10-7mol/L1,25(OH)2D3 and celecoxib group. Conclusion 1,25(OH)2D3 and celecoxib could be a new drug for the prevention and treatment of breast cancer.
3.The value of pedicled fat and capsule-packed nerve root in operation of sacral canal cysts
Chuankun LI ; Baixiang HE ; Gang BAO ; Minxue LIAN ; Ning WANG
Journal of Xi'an Jiaotong University(Medical Sciences) 2016;(2):187-189
Objective To evaluate the value of pedicled fat and capsule-packed nerve root in operation of sacral canal cysts.Methods We collected the information of 14 cases of sacral canal cysts for operation in our department and analyzed the operation indications and skills as well as the prognosis.Results All the operations were performed with the help of the microscope and the electrophysiological monitor.The capsules were removed in 9 cases and wrapped in 6 cases,with the total resection rate of 64.3%.The clinical symptoms were improved markedly after the operation.Conclusion The operation with pedicled fat and the capsule-packed nerve root is valuable in treating sacral canal cysts because it can protect the nerve root and get lower recurrence rate.
4.Relationships among Cerebral Vasospasm Following Subarachnoid Hemorrhage and Atrial Natriuretic Peptide and Hyponatremia
Chen-bao HAN ; Zhou LIU ; Yi-gang WANG ; Guanzhong HUANG
Chinese Journal of Rehabilitation Theory and Practice 2006;12(4):329-331
ObjectiveTo explore the relationships among atrial natriuretic peptide (ANP) and cerebral vasospasm (CVS) following subarachnoid hemorrhage (SAH) and hyponatremia.MethodsPlasma ANP levels and serum natrium and blood flow rate of intracal major arterial were assessed at different times (1 to 3 days, 7 days and 14 days after SAH) in 42 patients with SAH. Correlation analysis was carried out among plasma ANP, blood sodium level and blood flow rate of intracal major arterial.Results28 patients had CVS. Plasma ANP levels in CVS patients significantly elevated compared with non-CVS and control subjects (P<0.05). Hyponatremia in CVS patients also significantly elevated compared with non-CVS subjects (P<0.05). Plasma ANP level had significant negative relationship with serum natrium level at the 7th day and 14th day (r2=-0.778,r3=-0.653;P<0.01,P<0.05) in SAH patients. Plasma ANP level had significant positive correlation with middle cerebral artery mean flow velocity on the 7th day (r3=0.702,P<0.05) in SAH patients. Middle cerebral artery mean flow velocity had significant negative relationship with serum natrium level on the 7th day and 14th day (r2=-0.693,r3=-0.653 , both P<0.05) in SAH patients.ConclusionANP might cause hyponatremia following SAH and play an important role in pathogenesis of earlier period CVS.
5.Experimental study of antitumor immunity of DC/C6 fusion vaccine
Donghai WANG ; Xingang LI ; Ying WANG ; Xun QU ; Gang LI ; Songfeng GONG ; Quanmeng LIU ; Xiufeng BAO
Chinese Journal of Pathophysiology 1986;0(02):-
AIM:To study the anti-tumor effect and mechanism of fusion vaccine on DCs and C6 glioma cells.METHODS: PEG was used to fuse DCs with C6 glioma cells.Immunofluorescence with GFAP-FITC was used to identify the DC/C6 fusion cells.Rat brain glioma models were made by stereotactic technique.After 5 days of inoculation of C6,107 fusion cells were injected through tail vein in group A.The same number of DCs and the same volume of PBS were used in group B and group C.The survival time of rats in these three groups was analyzed by Log-rank survival analysis.Tumor samples were checked by HE staining and immunohistochemical staining with CD8Mcab.RESULTS: Positive result of GFAP-FITC immunofluorescence was observed in DC/C6 fusion cells.The Log-rank survival analysis showed that statistically significant difference in group A was observed compared to that in group B and group C(P
8.Radiosynthesis and preliminary evaluation of 5-(11Cmethyloxy)-L-tryptophan as PET tumor imaging.
Shan-zhen HE ; Shu-xia WANG ; Kong-zhen HU ; Bao-guo YAO ; Gang-hua TANG
Acta Pharmaceutica Sinica 2015;50(5):565-568
The PET tracer 5-([11C]methyloxy)-L-tryptophan (5-(11)CMTP) was prepared by nucleophilic fluorination and alkylation reaction via a two-step procedure in order to develop specific tumor probe. The biodistribution and microPET imaging of 5-(11)CMTP were executed. The results unveiled that the overall radiochemical yield with no decay correction was (14.6 ±7.2) %, the radiochemical purity was more than 95% and high uptake and long retention time of 5-(11)CMTP in liver, kidney and blood were observed but low uptake in brain and muscle were found, furthermore, high uptake of 5-(11)CMTP in tumor tissue was observed. It seems that 5-(11)CMTP will be a potential amino acid tracer for tumors imaging with PET.
Amino Acids
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Animals
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Neoplasms
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diagnostic imaging
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Positron-Emission Tomography
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Radioactive Tracers
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Tissue Distribution
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Tryptophan
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analogs & derivatives
9.Effect of rhBMP-2 on the Osteogenesis of Osteoblast Compounded Chitosan
Ai-Jun ZUO ; Dong-Chun LIANG ; Bao-Li WANG ; Gang GUO ; Jing-Yu ZHANG ;
China Biotechnology 2006;0(05):-
Recombinant human BMP-2 was compounded with chitosan/gelatin/hydroxyapatite(HCG) scaffold and the complex was sterilized by 60Co radiating. Osteoblast isolated from cranial bones of newborn rat was primary cultured and seeded onto the complexes. 3 days after culturing, scanning electron microscope(SEM) was applied to detect the compatibility of the cell with the complex. SEM showed osteoblast attached closely with the complex and grew well in its pores. Then the complexes with osteoblast modification were implanted into athymic nude mice subcutaneously. 8 weeks after implantation, X-ray photograph and histological observation were applied to detect the bone formation of the complexes. Under X-ray a high-density areas consistent with the shape of the implanted complex could be seen. Histological observation also proved there was bone formation in the interspace of the complex. A conclusion was drawn that rhBMP-2 compounded HCG scaffold had good osteogenesis ability in vivo.
10.Effect of spindle checkpoint on Akt2-mediated paclitaxel-resistance in A2780 ovarian cancer cells.
Ting, ZHOU ; Yindi, BAO ; Shuangmei, YE ; Danhui, WENG ; Gang, CHEN ; Yunping, LU ; Ding, MA ; Shixuan, WANG
Journal of Huazhong University of Science and Technology (Medical Sciences) 2010;30(2):206-11
Recent evidence has suggested that Akt2 plays an important role in the protection of cells from paclitaxel (PTX)-induced apoptosis and control of the cell cycle. In addition, some scholars suggested that the PTX sensitivity depends on a functional spindle assembly checkpoint. In the present study, we investigated the role of the Akt2/Bub1 cross-talking in apoptosis and cell cycle after exposure of the A2780 ovarian cancer cells to paclitaxel (PTX). Recombinant expression plasmid WT-Akt2 was transfected into A2780 cells by lipofectamine2000, and then the expression level of Akt2 gene was detected by using RT-PCR and Western blotting. Cell apoptosis and cell cycle were detected by flow cytometry and Hoechst 33342 staining after treatment with PTX. Moreover, we compared the expression level of Bub1 in different groups by Western blotting. Our study showed that up-regulation of Akt2 contributed to A2780 ovarian cancer cells overriding PTX-induced G(2)/M arrest, and inhibited Bub1 expression. Our findings might shed light on the molecular mechanism of PTX-induced resistance in ovarian cancer and help develop novel anti-neoplastic strategies.